Appendix — Doolittle v. United States

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—— ee |

76-5134 Tres

“PILED

IN THE oct 1s We

Supreme Court of the United dtates sx. cer _

October Term, 1976

ea ee

INTERNATIONAL RECTIFIER CORPORATION, ef al.,

Petitioners,

VS.

PFIZER, INC.,

Respondent.

VOLUME Il

APPENDIX.

PETER R. COHEN,

9601 Wilshire Boulevard, Suite 200,

Beverly Hills, Calif. 90210,

(213) 278-4011,

Attorney for Petitioner.

Parker & Son, Inc., Law Printers, Los Angeles. Phone 724-6622

INDEX TO APPENDIX

Page

Findings of Fact, Conclusions of Law and Order... 1

Appeal From the United States District Court for

the District of Minnesota .........................22.2c0000+- 95

Paragraph 8 of Examiner Adams Affidavit (Feb-

SD Fis TE: seiisnsitsnnintendastitntindnaiiautannaicinnians 129

Blackwood, et al. Affidavit (March 27, 1975) .. 129

Blackwood—Affidavit (April 9, 1975) ........... 131

Paragraph 8 of Examiner Adams Affidavit (Feb-

en ee ee 133

Paragraph 19 of Stephens Affidavit (March 27,

TEPOMIED nisisadetinaindevennistaipudentiniinittiiettaiaiiuitlereiainies 134

Last Paragraph of Pfizer Exhibit 35 M (December

20, 1960)

IN THE

Supreme Court of the United States

October Term, 1976

ERE iron

INTERNATIONAL RECTIFIER CORPORATION, ef al.,

Petitioners,

vs.

PFIZER, INC.,

Respondent.

APPENDIX.

Findings of Fact, Conclusions of Law and Order.

UNITED STATES DISTRICT COURT

DISTRICT OF MINNESOTA

FOURTH DIVISION

4-71 Civ. 435 and the following

In Re Coordinated Pretrial Proceedings

In Antibiotic Antitrust Actions

4-73 Civ. 188

PFizeR, INC., Plaintiff,

| vs.

INTERNATIONAL RECTIFIER CORPORATION, RACHELLE

LABORATORIES ITALIA, S.p.A., RACHELLE LABORA-

TORIES, INC., RACHELLE PHARMACEUTICALS INTER-

NATIONAL, S.A., and USV PHARMACEUTICAL Cor-

PORATION, Defendants.

This matter comes before the Court upon defendants’

motion for partial summary judgment.

INTRODUCTION

This action was filed by Pfizer, Inc. (Pfizer) on

January 11, 1973 against International Rectifier Corpo-

ration and its four subsidiaries, Rachelle Laboratories ~

Italia, S.p.A., Rachelle Laboratories, Inc., Rachelle

Pharmaceuticals International, $.A., and Rachelle Lab-

oratories (Philippines), Inc. (collectively the Rectifier

Defendauts) and USV Pharmaceutical Corporation

anllien

(Defendant USV) for alleged infringement of Pfizer's

Blackwood, et al., Patent No. 3,200,149 (the Doxycy-

cline Patent). Pfizer seeks damages from the defendants

and injunctive relief.

Defendants’ answers allege, among other things, that

the Doxycycline Patent is invalid and unenforceable

because of Pfizer’s fraud upon, and inequitable conduct

before, the Patent Office.

On January 10, 1973 this action, which was com-

menced in the United States District Court for the

Central District of California (Civil Action No. 73-

58-R), was transferred by the Multidistrict Panel pur-

suant to the provisions of 28 U.S.C. $1047 to this

Court for coordinated or consolidated pretrial proceed-

ings with In Re Coordinated Pretrial Proceedings In

Antibiotic Antitrust Actions, 4-71 Civ. 435 (D. Minn.

filed August 1, 1971); six of which actions are now

in trial.

Pursuant to a September 28, 1972 order in 4-71

Civ. 435, and a further request for the production

of documents by Defendant USV, Pfizer produced many

thousands of documents to defendants commencing in

mid-1973. In December 1973 Defendant USV initiated

the deposition of numerous Pfizer employees.

On May 29, 1974 Defendant USV filed the original

motion for partial summary judgment (Original Mo-

tion). On February 11, 1975 Defendant USV and

the Rectifier Defendants filed a second motion for

partial summary judgment which incorporated the

grounds set forth in the Original Motion and added

grounds thereto (Present Motion). Pfizer has opposed,

and the parties have fully briefed, both motions.

~~

The Present Motion is based almost entirely on

documents produced by Pfizer and the deposition testi-

mony of Pfizer’s employees or agents. Pfizer has submit-

ted numerous affidavits in opposition to the motions.

Defendants have submitted one affidavit in support

of the Present Motion.

Hearings on the Original Motion, the Present Motion,

and on evidentiary matters relating thereto were held

on September 11 and 13, and October 10, 1974;

and on January 24, 25 and 31, February 1 and April

11, 17, 18 and 21, 1975, after which the matter

was submitted,

The Present Motion charges Pfizer with fraud and

inequitable conduct in the prosecution of the Doxycy-

cline patent application before the Patent Office and

with fraud on this Court. Pfizer denies these charges.

Defendants contend and Pfizer denies that there is

no genuine issue of any material fact concerning the

questions of fraud and inequitable conduct in the prose-

cution of the Doxycycline Patent application and fraud

on the Court.

The Court after having considered the documents,

depositions and affidavits of the parties and the briefs

and many oral arguments of the parties makes its

findings of facts and conclusions of law as stated

herein.

The procedure to be utilized will be as follows:

Before stating the uncontroverted facts, the Court will

set forth the basic principles of law which it will

apply. After setting forth the uncontre erted facts in

each section the Court will then apply the conclusions

of law which necessarily follow from the uncontroverted

facts. The Court feels that this format will make it

_ ea

easier for those unfamiliar with the subject matter

or any reviewing judicial body to follow the Court’s

reasoning and the long and often complicated facts.

The headings set forth in the Findings of Fact,

and in the Conclusions of Law, are for convenience

only and are not part of the Findings of Fact or

Conclusions of Law. The facts set forth in the “Facts

Respecting the Chronology of the Prosecution of the

Doxycycline Application Before the Patent Office”, and

“The Facts Respecting Technical Terms and Concepts”,

are findings of fact.

Finally, since it is often difficult to completely sepa-

rate findings of fact from conclusions of law each

is intended to include the other where appropriate.

APPLICABLE PRINCIPLES OF LAW

The grant of summary judgment is appropriate where

there is no genuine issue as to any material fact and

the moving party is entitled to a judgment as a matter

of law. Rule 56(c), F.R.Civ.P., provides in part that:

The judgment sought shall be rendered forthwith

if the pleadings, depositions, answers to interroga-

tories, and admissions on file, together with the

affidavits, if any, show that there is no genuine

issue as to any material fact and that the moving

party is entitled to a judgment as a matter of

law.

Rule 56(c) is equally applicable in patent cases.

Proler Steel Corp., Inc. v. Luria Brothers & Co., Inc.,

417 F.2d 272 (9th Cir. 1969). See also, In Re Yarn

Processing Patent Validity Litigation, 185 U.S.P.Q.

334 (S.D. Fla. 1975). Bobertz v. General Motors

Corp. 228 F.2d 94 (6th Cir. 1955) cert. denied 352

enna

U.S. 824 (1956). Technograph Printed Circuits Ltd.

v. Methode Electronics, Inc., 356 F.2d 442, (7th Cir.

1966) cert. denied 384 U.S. 950 (1966). Research

Corporation v. Nasco Industries, Inc., 501 F.2d 358

(7th Cir. 1974) cert. denied .... U.S. .... (........).

In Ballantyne Instruments & Electronics Inc. v. Wag-

ner, 345 F.2d 671 (6th Cir. 1965), the Court stated:

The public interest in every patent case requires

that suits involving the validity of patents should

be speedily determined. Thus, wherever patent liti-

gation can be expeditiously handled on motions

for summary judgment it should be done provided

the necessary safeguards to protect the rights of

the litigants are observed.

When a motion for summary judgment is made

and supported as provided in this rule, [56(c)],

an adverse party may not rest upon the mere

allegations or denials of his pleading, but his

response, by affidavits or as otherwise provided

in this rule, must set forth specific facts showing

that there is a genuine issue for trial. If he does

not so respond, summary judgment, if appropriate,

shall be entered against him. /d. at 672.

In determining whether summary judgment is proper

the Court may disregard an opposing party’s mere

formal denials or generalized averments of fact, Law-

horn v. Atlantic Refining Company, 299 F.2d 353,

357 (Sth Cir. 1962); Minnesota Mining & Mfg. Co.

v. United States Rubber Co., 279 F.2d 409 (4th Cir.

1960); Liberty Leasing Co. Inc. v. Hillsum Sales Cor-

poration, 380 F.2d 1013 (Sth Cir. 1967); U.S. v.

373.70 Carats Of Cut, Polished, Rough and Cleaved

— =

Diamonds, 148 F.Supp. 618 (E.D.N.Y. 1957), as the

opposing narty is required to bring forth specific facts

in order to raise a genuine issue of fact. F.R.Civ.P.

56(e); Bruce Construction Corp. v. United States, 242

F.2d 873 (Sth Cir. 1957); Saunders v. National Basket-

ball Association, 348 F.Supp. 649 (N.D. Ill. 1972).

The Court may disregard affidavits containing specu-

lation Kern v. Tri-State Insurance Company, 386 F.2d

754 (8th Cir., 1967), or hearsay Lyon Ford Inc.

v. Ford Motor Company, 342 F.Supp. 1339 (E.D.

N.Y., 1971); Elasky v. Pennsylvania Railroad Com-

pany, 215 F.Supp. 25 (D. Ohio 1962); Willetts v.

General Tel. Directory Co., 38 F.R.D. 466 (S.D. N.Y.

1965), or opinions G.D. Searle & Co. v. Chas. Pfizer -

& Co., 231 F.2d 316 (7th Cir. 1956), or factual

and legal conclusions (Turner v. Lundquist, 377 F.2d

44 (9th Cir. 1967); Wagoner v. Mountain Savings

& Loan Ass'n, 311 F.2d 403 (10th Cir., 1962); Riggs

v. British Commonwealth Corporation, 459 F.2d 449

(10th Cir. 1972)).

Thus, vague inferences contained in affidavits oppos-

ing a motion for summary judgment are unavailing.

Burnham Chemical Co. v. Borax Consolidated, Ltd.,

170 F.2d 569 (9th Cir. 1948); Bishop v. Shaughnessy,

119 F.Supp. 62 (N.D. N.Y. 1950). Where the moving

party creates inferences in affidavits and documents

which are not denied by the opposing party, those

inferences which are “properly drawn therefrom . .

may support a motion for summary judgment” Lundeen

v. Cordner, 356 F.2d 169 (8th Cir. 1966).

The reason for these rules is clear. Where summary

judgment is proper the opposing party should not be

permitted to defeat summary judgment and put his

a

opponent to the expense of a trial by beclouding the

absence of genuine, uncontroverted issues of material

fact with generalizations, vague inferences, opinions,

or factual or legal conclusions.

It is the policy of the law, particularly in patent

cases to discourage “dilatory court tactics” Lear Inc.

v. Adkins 395 U.S. 653 (1969). Summary judgment

is designed to do precisely that where there is no

genuine issue of material fact.

The fact that patent litigation involves technical mat-

ters does not foreclose summary judgment. Where there

is no need for expert testimony in order for the Court

to understand the uncontroverted facts, the Court is

fully capable of determining those uncontroverted facts

and applying the law thereto. Bobertz v. General Motors

Corp., supra. In Research Corporation v. Nasco Indus-

tries Inc., supra, the Court of Appeals, for the Seventh

Circuit, in affirming the grant of a motion for summary

judgment, stated:

There is nothing in Rule 56 to forbid the use

of summary judgment procedures to determine

whether a genuine issue of fact exists concerning

the factual foundation for determination of the

ultimate issue of law: obviousness. Although care

must be exercised to assure that controverted fact

issues are not ignored, see Tee-Pak, Inc. v. St.

Regis Paper Co., 491 F.2d 1193, (6th Cir. 1974),

* * * a suit concerning the validity of a patent

over the prior art is not immune from disposition

on motion for summary judgment even though,

in addition to prior art patents, deposition testi-

mony of the applicant and affidavits are involved,

if no genuine issue of material fact is present.

eitlitios

A R, Inc. v. Electro-Voice, Inc., 311 F.2d 508,

511, (7th Cir. 1962). ‘Further, it is well settled

that, in a proper case, the validity of a patent

may be determined by use of summary judgment.’

Technograph Printed Circuits, Ltd. v. Methode

Electronics, Inc., 356 F.2d 442, 446, (7th Cir.

1966), cert. denied 384 U.S. 950 (1966)....

‘Rule 56 applies to patent cases and is used in

those instances where the structure and mode of

operation of the accused devise may be readily

comprehended by the court and compared with

the invention described and claimed in the patent

without need of technical explanation by expert

witnesses.” Technograph Printed Circuits, Ltd. v.

Methode Electronics, Inc., 356 F.2d 442, 447,

(7th Cir. 1966) cert. denied 384 U.S. 950,

(1966). [Emphasis added.] Jd. at 361-2.

In the present case, there are over 150 uncontroverted

facts whch appear from depositions, affidavits and

documents. Although this case is complicated by reason

of the sheer number of uncontroverted facts; the number

of issues presented by those facts; and a change in

the substantive law concerning prior art anticipation

(35 U.S.C. §102) during the prosecution of the applica-

tion, the technology necessary for a complete under-

standing of the uncontroverted facts is not overly dif-

ficult.

For example, issues concerning stereochemistry,

which are seemingly the most difficult technically, do

not require the Court to understand the chemical reac-

tions which produce Doxycycline, and the McCormick

6-deoxy products; or why, in Doxycycline, the methyl

snl

group (CH,) at the 6-position is “down” and in the

McCormick 6-deoxy compound the methyl group (CH:)

at the 6-position is “up”. To decide these issues

the Court need only understand that the stereochemical

drawings depict “down” with a dotted line and “up”

with a solid line. None of this is in dispute. Once

these simple technical concepts are understood, the

remaining uncontroverted facts consist of no more than

Pfizer’s knowledge, beliefs and uncertainties concerning

absolute stereochemistry at the 5- and 6-positions at

different points in time during the prosecution of the

Doxycycline application and Pfizer’s representations to

and withholdings from the Patent Office at certain

points in time concerning its knowledge, beliefs and

uncertainties concerning that stereochemistry.

Thus, on the issues concerning stereochemistry the

Court’s task is simply to apply the law to the uncontro-

verted facts.

Summary judgment is proper even where fraud or

inequitable conduct is in issue. In 6 Moore’s Federal

Practice 2554 (2nd Ed. 1965), Professor Moore states:

But in whatever guise the issue of fraud may

appear in an action, the general basic principles

underlying summary judgment apply and, if they

are met, the issue of fraud may be summarily

adjudicated.

Summary judgment is also appropriate in cases involv-

ing fraud on the Patent Office. In Farmer Bros. Com-

pany v. The Coca-Cola Company, 384 F.Supp. 595

(C.D. Cal. 1974), the Court granted summary judgment

declaring a patent unenforceable because the patent

owner had practiced a fraud on the Patent Office.

eniliitiis

The Court held that

The patentees’ failure to be candid with and

to make a full and fair disclosure to the Patent

Office of all facts relating to . . . their alleged

invention constitutes a breach of their duty to

the Patent Office and thus renders the Farmer

Brothers’ patent void and unenforceable.

See also, Proler Steel Corp. v. Luria Bros. & Co.,

417 F.2d 272, 273-4 (9th Cir. 1969); Ashcroft v.

Papermate Mfg. Co., 434 F.2d 910, 911 (9th Cir.,

1970).

A patent applicant has an uncompromising duty

of absolute candor and full and complete disclosure

to the Patent Office of all facts which may be relevant

to an issue of patentability. The Courts have found

anything less to be fraudulent or inequitable conduct

in procuring patent rights. In Precision Instrument Mfg.

Co. v. Automotive Maintenance Machinery Co., 324

U.S. 806 (1945), rehearing denied. 325 U.S. 893

(1944), the Supreme Court stated

Those who have applications pending with the

Patent Office or who are parties to Patent Office

proceedings have an uncompromising duty to re-

port to it all facts concerning possible fraud or

inequitableness underlying the applications in issue.

.. . This duty is not excused by reasonable doubts

as to the sufficiency of the proof of the inequi-

table conduct nor by resort to independent legal

advice. /d. at 818.

In applying an applicant’s duty of absolute candor

and full and complete disclosure, the Court of Appeals

for the Sixth Circuit has directed that

==

The Patent Office, not having testing facilities

of its own, must rely upon information furnished

by applicants and their attorneys. Pfizer and Cy-

anamid, like all other applicants, stood before

the Patent Office in a confidential relationship

and owed the obligation of frank and truthful dis-

closure. Charles Pfizer & Co., Inc. v. FTC, 401

F.2d 574, 579 (6th Cir. 1968), cert. denied 394

U.S. 920 (1969).

Because of the public interest considerations under-

lying the doctrine of absolute candor and full and

complete disclosure before the Patent Office, it is not

necessary to establish all of the elements of strict

common law fraud. An Applicant commits “Fraud

on the Patent Office” if he violates his uncompromising

duty of absolute candor and full and complete dis-

closure.

A strict fiduciary duty is imposed on patent appli-

cants which is analogous to that of a seller of securi-

ties or any other person who alone has possession

of facts bearing on the public interest. Monsanto Com-

pany v. Rohm & Haas Company, 312 F.Supp. 778

(E.D. Pa. 1970), aff'd 456 F.2d 592 (3rd Cir. 1972),

cert. denied 407 U.S. 934 (1972).

In S.E.C. v. Capital Gains Research Bureau, 375

U.S. 180 (1964), the Supreme Court stated in an

analogous fraud case that a breach of the duty of

complete disclosure constitutes inequitable conduct and

that it is not necessary to establish a specific subjective

intent to defraud in order to obtain equitable relief.

Nor is specific subjective intent a prerequisite to

finding fraudulent or inequitable conduct before the

Patent Office. In Monolith Portland Midwest Com-

—_j2—

pany v. Kaiser Aluminum & Chemical Corporation,

407 F.2d 288 (9th Cir. 1969), the patentee argued

“that it believed in good faith” that the prior art

did not anticipate its claims. The Court stated at page

295 that:

Whatever theory Monolith may have had in

mind about the legal effect of . . . [the prior

art], it failed to disclose openly and fully the

underlying facts to the Patent Office. At the least,

Monolith knew that those facts might affect the

patentability of the invention.

Similarly, the specific subjective intent of the patentee

was considered immaterial in Monsanto Company vy.

Rohm & Haas Company, supra:

We have concluded that the decisions of the

Supreme Court require the highest degree of scien-

tific candor on the part of patent applicants in

their dealings with the patent office. We believe

this standard forbids not only the affirmative mak-

ing of false statements of material fact, but also

the suppression of facts known to the applicant

which are inconsistent with statements made by

the applicant in pursuit of a patent. Id. at 739.

. . . [We hold that even if Monsanto did

not intend to deceive the Patent Office, the fact

that it intentionally withheld facts which were

material to the decision whether it was entitled

to a patent is sufficient to bar the issuance of

a patent to it. . . . We believe that all questions

of materiality in dealings with the Patent Office

ought to be resolved in favor of disclosure. Only

such a standard can protect the public from the

ee —

—- =

deadening competitive effect of improvidently

issued patents. [Emphasis added.| Jd. at 799.

See also Robbins Company v. Lawrence Manu-

facturing Company, 482 F.2d 426 (9th Cir.

1973).

Thus, Pfizer’s assertions of good faith belief, based

on its scientists’, patent agents’ and attorneys’ subjective

state of mind, in misrepresenting to and withholding

relevant facts from the Patent Office does not create

any genuine issue of material fact. Therefore, the good

faith belief assertions set forth in the majority of the

affidavits filed by Pfizer in opposition to the motion

have been excluded from the findings of material un-

controverted facts. See also United States v. Paul Harde-

man, Inc., et al., 320 F.2d 115 (Sth Cir. 1963);

and Robbins v. Gould, 278 F.2d 116 (Sth Cir. 1960).

The requirement of absolute candor and full and

complete disclosure in prosecuting patent applications

precludes the withholding of “material” prior art, facts

and beliefs from, as well as the affirmative misrepresen-

tation of “materia!” prior art, facts and beliefs to,

the Patent Office. Beckman Instruments, Inc. v. Chem-

tronics, Inc., 428 F.2d 555 (Sth Cir. 1970); Monsanto

Company v. Rohm & Haas Company, supra.

Thus the Court held in Buzzelli v. Minnesota Min-

ing & Mfg. Co., ........ F.Supp. ........ , 182 U.S.P.Q.

307 (E.D. Mich. 1974) that an applicant’s failure

to cite to the Patent Office “the prior art most material

and relevant to the subject matter claimed” renders

the patent invalid and unenforceable.

Similarly, the Court stated in Union Carbide Corp.

v. Filtrol Corp., 357 F.Supp. 37 (C.D. Cal. 1971):

—14—

A patent applicant’s duty of disclosure to the

Patent Office extends to prior art or facts known

to him which would . . . have prevented the

patent from issuing or would have restricted the

scope of the claims.

“Materiality” under Beckman and Monsanto, supra,

does not require that the patent would not have issued

as a matter of law “but for” the misrepresentation

or concealment, but only that the misrepresesntation

or withholding be relevant to an issue of patentability.

Corning Glass Works v. Anchor Hocking Glass Corp.,

253 F.Supp. 461 (D. Del. 1966), rev’d on other

grounds, 374 F.2d 473 (3rd Cir. 1967), cert.

denied, 389 U.S. 826 (1967); Monolith Portland Mid-

west Co. v. Kaiser Aluminum & Chemical Corp., supra;

SCM Corp. v. Radio Corporation of America, 318

F.Supp. 433 (S.D. N.Y. 1970); CPC International,

Inc. v. Standard Brands Inc., ........ F.Supp. ........ ;

184 U.S.P.Q. 332 (D. Del. 1974); United States Mo-

vidyn Corp. v. Hercules Incorporated, 388 F.Supp.

1146 (D. Minn. 1975).

In most of these cases the testimony of the Examiner

was unavailable; thus, the Courts have adopted the

rule that even if the applicant misrepresents or with-

holds facts which are not material in a “but for”

sense, the Courts will refuse to enforce the patent

if the applicant has misrepresented to the Patent Office

facts which may be relevant to an issue of patentability.

In this case the parties have submitted three affidavits

of Examiner Adams but no affidavits or deposition

testimony from the other two Examiners before whom

the Doxycycline Patent was prosecuted. Thus, the rec-

ord shows what Examiner Adams would have done

MT: le cient comet

~~ eres

=

had he known certain facts misrepresented to or with-

held from him, but does not show what the other

two Examiners would have done if similarly apprised.

Consequently, in applying the rule of the cases cited,

supra, the Court will consider material, or, relevant,

the facts which Examiner Adams would have been

interested in and considered relevant to an issue of

patentability.

Otherwise stated, the Court will not substitute its

judgment for Examiner Adams’ judgment in determin-

ing relevance to an issue of patentability or in deter-

mining what action Examiner Adams would have taken,

whether or not the Court believes Examiner Adams

to be right or wrong as a matter of law.

The Court recognizes that there is only one reported

decision on the use of an Examiner's testimony, as

to what prior art or facts he would have considered

relevant to an issue of patentability had he been ap-

prised of them. Chas. Pfizer & Co. v. FTC, supra.

In that case the Court held that the Examiner’s testi-

mony as to what he would have done had certain

facts been presented to him, even if based on present

interpretation with no independent recollection, is ad-

missible evidence.

If the Examiner does not allow the claims sought,

or for that matter any claims, and if the applicant

believes that the Examiner is wrong, the applicant’s

only proper remedy is by appeal. /.7.S. Rubber Co.

v. Essex Rubber Co., 272 U.S. 429, 443 (1926).

Any other rule would subvert the patent system

and permit applicants to misrepresent or withhold facts

which might be relevant to an issue of patentability

in order to obtain a patent, and then gamble on whether

ilies,

or not a Court will at a later date agree that the

facts withheld or misrepresented were not as a matter

of law relevant to an issue of patentability.

The decision in the first instance must be that of

the Patent Office, not the applicant. Monsanto Co.

v. Rohm & Haas Co., supra, Beckman Instruments

Inc. v. Chemtronics Inc., supra.

Although Examiner Adams’ affidavits are almost

entirely based on hypothetical facts, where those hypo-

thetical facts are in accord with the actual facts misrep-

resented to or withheld from him, his recollection,

or even his speculation (where he cannot separate

his recollection of what he would have done from

his speculation as to what he would have done had

he known all of the true facts) is sufficient.

It is common knowledge that the prosecution of a

patent application may take several years, as in this

case. It is also common knowledge that patent litigation

may arise many years after the patent is granted,

as in this case. In these circumstances it is not surpris-

ing that an Examiner, who handles many applications

at the same time, may not be able to recall with

exactitude what he would have done had he known

certain facts many years prior to the taking of his

testimony. Thus, his present recollection or even his

present recollection coupled with his present speculation

as to what he would have done is often the best

independent evidence available. Any other rule which

fails to adopt the Examiner’s recollection or the combi-

nation of his recollection and speculation would hardly

discourage an applicant from misrepresenting or with-

holding relevant facts. Chas. Pfizer & Co. v. FTC,

supra.

==) Fam

As to the other two Examiners, since their testimony

is not before the Court, it cannot be determined with

any certainty what they would have done had they

known the true facts during the time. they were the

Examiners for the Doxycycline application. Therefore,

for the time period that they were so acting, the Court

will regard as relevant those concealments or misrepre-

sentations which may have been relevant to the statutory

criterion for patentability.

In summary, since the testimony of Examiners Berg

and Modance is not before the Court, the Court, based

on the uncontroverted facts, will determine materiality

during the time they were acting on the Doxycycline

application in the context of whether any withholding

or misrepresentation was relevant to an issue of whether

or not Doxycycline was patentable. However, the Court

will accept as conclusive Examiner Adams’ affidavit

testimony concerning relevance during the time he

served in the Patent Office as the Examiner on the

Doxycycline application. In this regard, were there no

testimony from Examiner Adams, the Court would

conclude as set forth in Conclusions D, H, J and

L that the withholding or misrepresentation of prior

art, facts or beliefs was relevant to an issue of whether

or not doxycycline was patentable. Thus, in this alter-

native circumstance, the Court would disagree with

Examiner Adams’ affidavit testimony only on the issue

of Pfizer’s false analogy as set forth in Conclusion

F between doxycycline and the prior art “epimers”—

and on that issue the Court would conclude from

the uncontroverted facts that Pfizer’s false analogy was

material to the issue of whether or not doxycycline

was patentable under 35 U.S.C. §103 during the prose-

cution of the Doxycycline application,

=

An applicant’s duty of absolute candor and full

and complete disclosure to the Patent Office would

be meaningless were not an applicant obligated to exer-

cise reasonable diligence in discharging that duty. The

Courts cannot, therefore, excuse the failure to exercise

reasonable diligence in disclosing prior art or facts

or beliefs which may be relevant to an issue of patent-

ability, and which are known to the applicant, on

the ground that the prior art or facts or beliefs are

at some later date rendered moot by changes in the

law or by later discovered facts.

An applicant has a duty to report to the Patent

Office all facts concerning fraud or inequitable con-

duct. Precision Instrument Mfg. Co. v. Automotive

Maintenance Machinery Co., supra.

In this regard, Patent Office Rule 56 (37 C.F.R.

§1.56) provides, in part, that:

Any application in connection with which any

fraud is practiced or attempted on the Patent

Office, may be stricken from the files.

The Patent Office Rules are to be broadly applied

in the consideration of fraud or inequitable conduct

during the prosecution of a patent application. Norton

v. Curtiss, 433 F.2d 779 (C.C.P.A. 1970).

Cumulative misrepresentation or withholding of prior

art or facts during the prosecution of a patent applica-

tion, if relevant at the time of the misrepresentation

or withholding, but which eventually: become moot

for one reason or another, may evidence a course

of calculated reckless conduct as to the disclosure of

the true and complete facts, which fails to satisfy

an applicant’s duty of absolute candor and full and

complete disclosure to the Patent Office, and may

—19—

be so inequitable as to render the patent unenforce-

able.

In Honeywell Inc. v. Sperry Rand Corp., .... F.

Supp. ...., 180 U.S.P.Q. 673 (D. Minn. 1973), the

Court said:

If the conduct of the applicant is reprehensible

it matters not that it was really unnecessary, and

the patent is unenforceable.

See also, Monolith Portland Midwest Co. v. Kaiser

Aluminum Co., supra; Intermountain Research & Engr.

Co. v. Hercules, .... F.Supp. ..... 171 U.S.P.Q. 577,

631 (C.D.Cal. 1971), aff'd .... F.2d .... (9th Cir.,

1974; appeal Nos. 71-2797, 71-2938).

Although fraud on the Patent Office must be proven

by “clear, unequivocal and convincing” evidence, Schna-

dig Corporation v. Gaines Manufacturing Co., 494

F.2d 383, 392 (6th Cir. 1974), this burden is clearly

met where the uncontroverted evidence warrants the

grant of a summary judgment as a matter of law.

Fraud or inequitable conduct in obtaining a single

claim of a patent renders the entire patent invalid

or unenforceable. Marconi Wireless Telegraph v. United

States, 320 U.S. 1, 57-58 (1943); Strong v. General

Electric Co., 305 F.Supp. 1084 (N.D. Ga., 1969),

aff'd 434 F.2d 1042 (Sth Cir. 1960), cert. denied

403 U.S. 906 (1970); Kearney & Trecker Corp. v.

Giddings & Lewis, Inc., 452 F.2d 579, 596 (7th

Cir. 1971), cert. denied 405 U.S. 1066 (1972): Chrom-

alloy American Corp. v. Alloy Surfaces Co., 339 F.

Supp. 859 (D. Del. 1972); East Chicago Machine Tool

Corp. v. Stone Container Corp., .... F.Supp. ..... 181

U.S.P.Q. 744 (ND. Ill. 1974); Kearney & Trecker

— =

Corp. v. Cincinnati Milacron, .... F.Supp. ...., 184

U.S.P.Q. 134 (S.D. Ohio 1974).

Oral disclosures to a Patent Examiner, which are

not fairly summarized in an amendment filed in the

Patent Office, may not be relied upon to satisfy a

patent applicant’s duty of absolute candor and full

and complete disclosure.

Patent Office Rule 2 (37 C.F.R. §1.2) provides

that:

2. Business to be transacted in writing. All

business with the Patent Office should be trans-

acted in writing. The personal attendance of appli-

cants or their attorneys or agents at the Patent

Office is unnecessary. The action of the Patent

Office will be based exclusively on the written

record in the Office. No attention will be paid

to any alleged oral promise, stipulation, or under-

standing in relation to which there is disagree-

ment or doubt. | Emphasis added. |

Patent Office Rule 133(b) (37 C.F.R. §1.133(b))

provides that:

In every instance where reconsideration is re-

quested in view of an interview with an examiner,

a complete written statement of the reasons pre-

sented at the interview as warranting favorable

action must be filed by the applicant... .

The Patent Office acts on written applications, and

written amendments by written rejections made in “offi-

cial actions” or written notices of allowance. The pur-

pose of Patent Office Rules 2 and 133(b) is to insure

that, if a patent is either granted or rejected, all of

the reasons are set forth in the file wrapper and con-

tents. The Rules are enacted pursuant to statutory

onlin

authority, 35 U.S.C. §6 and, therefore, if not incon-

sistent with the patent statutes, have the force of law.

Hadco Products, Inc. v. Lighting Corp. of America,

Inc., 312 F.Supp. 1173 (E.D. Pa. 1970), Buzzelli

v. Minnesota Mining & Mfg. Co., supra.

The public is entitled to know from a file wrapper

and contents each and every fact and argument pre-

sented by the applicant and each and every reason

why the Examiner rejected or allowed the application.

See, In re Rubinfield, 270 F.2d 391, (C.C.P.A. 1959);

Sperry Rand Corporation v. Bell Telephone Labora-

tories, Inc., 171 F.Supp. 343 (S.D. N.Y. 1959); Gear-

on v. United States, 121 F.Supp. 652 (Ct. Cl. 1954);

Application of Kaghan et al., 387 F.2d 398 (C.C.P.A.

1967); and Halliburton Co. v. Dow Chemical Co.,

‘onteibie F.Supp. ......... 182 U.S.P.Q. 178 (N.D. Okla.

Oral disclosure of and discussion of prior art, facts

or beliefs with a Patent Examiner in an interview

which are not made of record does not satisfy the

applicant’s absolute duty of full and complete disclosure.

LaMaur v. DeMert and Dougherty, 265 F.Supp. 961

(N.D. Ill. 1965); Buzzelli v. Minnesota Mining &

Mfg. Co., supra.

Stated differently, an applicant is estopped to assert

that he called prior art, facts or beliefs to the attention

of the Patent Examiner where he makes no written

record thereof in the formal prosecution record.

Prior art, facts and beliefs which are known to

the inventors or to the officers, patent agents or key

scientists of a corporate applicant for a patent are

imputed to the applicant and his attorneys who prose-

cute the application as a matter of law. Thus, if any

_ =

of these persons misrepresents to, or withholds from,

the Patent Office prior art, facts or beliefs which are

relevant to an issue of patentability, the patent is

invalid and unenforceable. Chas. Pfizer & Co., Inc.

v. FTC, supra; Air Shields Inc. v. Air Reduction Co.

Inc., 331 F.Supp. 673 (1971), affd 474 F.2d 1351

(7th Cir. 1973).

Where a patentee in attempting to enforce a patent

commits a fraud on the Court, the Court upon the

discovery of that fraud, in the inherent exercise of

its equitable powers, may hold the patent unenforceable,

Hazel-Atlas Co. v. Hartford Empire Co., 322 USS.

238 (1944). See also, Keystone Driller Co. v. General

Excavator Co., 290 U.S. 240 (1933); and Mas v.

Coca-Cola Co., 163 F.2d 505 (4th Cir. 1947).

In Mas, the Court stated at page 508:

Although most cases in which the clean hands

doctrine has been applied are cases in which the

cause of action itself has arisen out of or been

the fruit of unconscionable conduct, we do not

understand that it is a pre-requisite to the applica-

tion of the doctrine that the cause of action shall

have so arisen. /t is sufficient to bar relief that

plaintiff has been guilty of unconscionable conduct

directly related to the cause of action, such as

the fabrication of testimony, the subornation of

perjury or other like attempt to perpetrate a fraud

upon the court or take an unconscionable advan-

tage of his adversary. . . . [Emphasis added. |

35 U.S.C. $285 provides that the Court can award

reasonable attorneys fees to the prevailing party in an

“exceptional” case whether or not the Court finds that

the applicant committed fraud on the Patent Office.

~~

Monolith Portland Midwest Co. v. Kaiser Aluminum

& Chemical Corp., supra; C. F. Strassheim Co. v. Gold

Medal Furniture Co., 477 F.2d 818 (7th Cir. 1973).

In the Strassheim case, supra, the Court awarded

reasonable attorneys fees because of the patentee’s “se-

rious lack of diligence” in representations made in prose-

cuting the patent application and its “comparable lack

of diligence in responding to discovery requests” which

the Court characterized as “exceptional oversights”

which were “critically important”. The Court said:

We do note, hdwever, that there can be no

question about the ready availability of the true

facts to defendant’s executives and attorney when

the patent application was filed. The failure to

make an appropriate investigation at that time

. reflects an extraordinary lack of diligence

to which we consider it appropriate to attach

legal significance.

Defendant and its trial counsel also displayed

a comparable lack of diligence in responding to

discovery requests... .

. . . |P|laintff's counsel requested that certain

documents be produced for use at the deposition.

Many other documents were produced .. .

but none of the items in question was mentioned

or brought to the attention of plaintiff's counsel.

The Court may take judicial notice of the Patent

Office rules in effect during the prosecution of the

Doxycycline application and the relevant proceedings

in the coordinated and consolidated actions. Federal

Rules of Evidence, Art. II, Rule 201 subd. (b), (c)

and (f).

onlitine

FINDINGS OF FACTS AND

CONCLUSIONS OF LAW

A. The Facts Respecting the Chronology of the Prose-

cution of the Doxycycline Application Before the

Patent Office

1. The Doxycycline Patent was granted on patent

application Serial No. 106,146 filed in the names of

Robert K. Blackwood, Hans H. Rennhard, John J.

Beereboom and Charles R. Stephens as inventors on

May 5, 1961 in the United States Patent Office (Doxy-

cycline application) (DX 5).’ That application was

called a “continuation-in-part” of prior application Serial

No. 31,236 filed May 23, 1960 (parent application)

(DX 5, p. 15).

2. The uncontroverted and material chronology of

the Doxycycline application is as follows:

(a) May 5, 1961: Pfizer files the Doxycycline

application (DX 5, cover page and pp. 1-56).

(b) October 26, 1961: The First Patent Office

Action, by Examiner Adams (DX 5, pp. 58-

59).

(c) On or about March 29, 1962: Interview

between Pfizer Attorney Nicholas E. Oglesby

(Oglesby) and Examiner Adams (Oglesby Affi-

davit of March 18, 1975; p. 2, paragraphs 12-

14).

1The record reference for each uncontroverted fact as found

herein is indicated after each numbered finding. “DX” refers

to exhibits placed in evidence by Defendants and “PX” refers

to exhibits placed in evidence by Plaintiff. “.... Affidavit” refers

to the affidavits submitted by the parties. “.... deposition” refers

to the depositions which are exhibits to the Original or the

Present Motion. “Tr. ...” refers to the transcripts of hearings

held before the Court.

A

_— =

(d) April 26, 1962: Pfizer’s First Amendment

and Supporting English and McBride Affidavits

(DX 5, pp. 60-67).

(e) October 30, 1962: The Second Patent Of-

fice Action, by Examiner Berg (DX 5, pp. 68-

69).

(f) On or about March 6, 1963: Interview

between Oglesby and Examiner Berg (Oglesby

Affidavit dated March 18, 1975, p. 3, paragraph

15).

(g) April 30, 1963: Pfizer's Second Amend-

ment and Exhibits thereto (DX 5, pp. 69-88).

(h) On or about April 14, 1964: Telephone

Interview between Oglesby and Examiner Modance

(Oglesby Affidavit dated March 18, 1975, p. 4,

paragraph 19).

(1) On or about July 9, 1964: Interview be-

tween Oglesby and Examiner Modance (Oglesby

Affidavit dated March 18, 1975, p. 4, paragraph

20).

(j) July 23, 1964: Pfizer’s Third Amendment

(DX 5, pp. 89-90).

(k) November 9, 1964: Pfizer's Fourth

Amendment (DX 5, pp. 91-92).

(1) January 19, 1965: Third and Final Patent

Office Action, by Examiner Adams (DX 5, pp.

93-96).

(m) February 23, 1965: Interview between

Oglesby and Examiner Adams (Oglesby Affidavit

dated March 18, 1975, pp. 13-14, paragraph 76).

(n) March 5, 1965: Pfizer’s Fifth Amendment

(DX 5, pp. 98-108).

_— =

(o) April 9, 1965: Notice of Allowance (DX

5, p. 110).

(p) August 10, 1965: Doxycycline patent

issued (DX 67).

(q) The Doxycycline application was prosecuted

by Oglesby who was then and is now a partner

in the law firm of Connolly, Bove and Lodge,

which firm transacts business before the Patent

Office under the name of Connolly & Hutz (Ogles-

by Affidavit dated July 30, 1974, paragraph 1,

page 1; Pfizer Brief dated April 21, 1975, p.

1).

B. The Facts Respecting Technical Terms and Con-

cepts

3. Doxycycline (originally described by Pfizer in

the Doxycycline application as “6-epi-6-deoxy-5-oxyte-

tracycline” and later as “«-6-deoxy-5-oxytetracycline” )

is a member of the group of tetracycline derivatives

known as 6-deoxy-tetracyclines (DX 67). In particular,

doxycycline is identical to oxytetracycline (also known

as 5-oxytetracycline; Pfizer's trademark for oxytetra-

cycline is “Terramycin” ) its parent fermentation product

except that the hydroxyl (OH) atom group (or sub-

stituent) at the “6-position” of the oxytetracycline

molecule has been removed and replaced with a hydro-

gen (H) atom (von Wittenau Affidavit dated March

27, 1975, paragraphs 2 and 9). The stereochemical

structure of doxycycline is depicted as follows (von

Wittenau Affidavit, paragraph 9):

le

The stereochemical issues in this case involve only

the methyl (CH;) group at the 6-position and the

hydroxyl (OH) group at the 5-position which in the

above drawing is depicted as follows:

CH3 \, OH Ss.

7 ~

6 5

In the preceding drawing the four connected hexagons

are carbon rings and the dotted and solid lines connected

to the rings are atom groups (or substituents) which

are oriented in the third dimension behind and in

front of the plane of the paper. Identifying numbers

have been added to designate the 5- and 6-positions

in the carbon rings which form the basic tetracycline

nucleus. The atom groups (or substituents) connected

to the tetracycline nucleus by dotted lines are all on

the same side of the molecule. The atom groups (or

substituents) connected to the tetracycline nucleus by

solid lines are all on the opposite side of the

molecule. Thus, at the 5- and 6-positions the solid

= =

lines showing the bonds to the hydrogen (H) atoms

represent the dimension rising out of the paper, or

“up”, and the dotted lines showing the bonds to the

hydroxyl (OH) atom group and the methyl (CH;)

atom group represent the dimension descending below

the plane of the paper or “down”.

4. The identification of the positions of the atoms

or atom groups of a chemical compound in space

is called the “stereochemistry” or “stereochemical con-

figuration” of that compound. The identification of

the spatial relationship between an atom group at one

position on the nucleus and another atom group at

a different position on the nucleus of the same com-

pound or at the same position on the nucleus of a

different compound is referred to as the relative stereo-

chemical configuration of the two atom groups (Tr.

April 11, 1975, pp. 126-31). In other words, the

relative configuration of the methyl group (CH;) at

the 6-position and the hydroxyl group (OH) at the

5-position in the Doxycycline molecule is the same,

because both of these atom groups are on the same

side of the molecule. Knowledge of the relative stereo-

chemical configuration of these two atom groups at

these two positions does not teach whether both atom

groups are “up” or both are “down”, but only that

both are on the same side. Similarly, knowledge of

the relative stereochemical configuration of two atom

groups at the same position does not teach one which

atom group is “up” and which atom group is “down”,

but only that one is “up” and one is “down”. (Wood-

ward Affidavit dated June 14, 1974, paragraph 4,

page 5).

5. The absolute stereochemical configuration of

a compound is the precise spatial orientation of the

— =

atom groups at the different positions of the molecule.

Thus, knowledge of the absolute stereochemical con-

figuration of Doxycycline tells us that the methyl group

(CH;) at the 6-position is “down”, or, below the

molecule as described above, whereas the hydrogen

atom (H) at the same position is “up”, or above

the molecule as described above (Tr. April 11, 1975,

p. 127).

In “up or down” terms the absolute configuration

of the atom groups at the 5- and 6-positions in Doxy-

cycline (the hydroxyl (OH) and methyl (CH,) groups,

respectively), can be depicted in a simplified, non-

technical line drawing as follows:

6 5 |

(CH5) (OH)

If in Doxycycline the hydroxyl group (OH) was up,

the atom groups at the 5- and 6-positions would be

depicted in a simple line drawing as follows:

(OH)

\s

(CH3)

As far as the issues in this case concern stereochem-

istry there is no dispute concerning the carbon rings

or the numbered positions in those carbon rings or

the identification of, or orientation of the attached

atom groups. The stereochemical issues involve only

Pfizer's knowledge, beliefs and uncertainties concern- —

ing the spatial orientation of the methyl group at

the 6-position and the hydroxyl group at the 5-position® :

—-=

of Doxycycline, at different times during the four year

prosecution of the Doxycycline application. (Woodward

Affidavit dated June 14, 1974, paragraph 4, page

9).

6. In the tetracycline nucleus there are six different

positions (asymmetric centers), including the 5- and

6-positions, at which so-called “epimers” may be formed.

At each of these positions the two atom groups attached

to the nucleus may be oriented in one of two ways,

at the 6-position the methyl (CH;) can be “down”

and the hydrogen (H) “up”, or vice versa. One chemical

compound may have the methyl “down” and the hydro-

gen “up”, and a different chemical compound may

have the methyl “up” and the hydrogen “down”. These

two compounds which differ from one another only

in the orientation of the atom groups at the same

position are each known in the art as “epimers”, or

each is the epimer of the other. (Woodward Affidavit

dated June 14, 1974, paragraph 4, pp. 3, 4).

In the art the term “epi” has been used as a prefix

to identify the compound having the second configura-

tion, i.e., if a compound with the methyl group “down”

is first produced, and the compound with the methyl

group in the “up” position is subsequently produced,

it is given the “epi” prefix to distinguish it from the

first compound produced (Woodward Affidavit dated

June 14, 1974, paragraph 4, p. 4).

As a result the term epimer as used in the art

does not indicate the absolute stereochemistry of a

compound, i.e., the “up-down” configuration of its atom

groups. Thus, knowledge that a tetracycline bearing

methyl and hydrogen groups at the 6-position is an

epimer of another such compound indicates only that

the other compound (which may also be an epimer)

— a eee

callie

has the same groups oriented in the opposite manner—

however, from this information one does not know

on which epimer the methyl group is “up” and on

which epimer it is “down”, but merely that it is “up”

on one epimer and “down” on the other epimer.

C. The Facts Respecting Pfizer’s Concealment of the

Belgian Patent and Its Inability to Distinguish

the Belgian Patent

1. The Doxycycline application disclosed a class

of epimers of the 6-deoxytetracyclines (“Pfizer's 6-

deoxytetracyclines”) including both those having a hy-

droxyl (OH) group at the 5-position, and those having

only hydrogen (H) atoms at that position (DX 5,

p. 11). As filed, the Doxycycline application claimed

only certain of Pfizer’s 6-deoxytetracyclines, i.e., those

compounds— including doxycycline—having an hydrox-

yl (or “oxy”) group at the 5-position (DX 5, pp. 53-

54).

2. Before filing the Doxycycline application Pfizer

was aware of Belgian Patent No. 572,584 (“Belgian

Patent”), (Frost letter to Oglesby dated March 17,

1961, DX 2, Pfizer Brief dated March 17, 1975,

p. 23) which issued to McCormick et al. of American

Cyanamid on April 30, 1959 (DX 1, a certified trans-

lation is the sole exhibit to the Affidavit of von Witte-

nau dated March 27, 1975). The Belgian Patent dis-

closed the preparation of 6-deoxy-5-oxytetracycline (Mc-

Cormick 6-deoxy compound), by hydrogenation of its

parent fermentation produced tetracycline, i.e., oxytetra-

cycline (DX 1, p. 2; Oglesby Affidavit dated July

30, 1974, paragraph 3, p. 2). The Belgian Patent

further depicted a stereochemical formula (DX 1, p.

2) purporting to show the absolute stereochemical con-

figuration of the McCormick 6-deoxy compound at

—_— =

the 5- and 6-positions (Pfizer Brief dated January

3, 1975, pp. 11-12), as follows:

In a simple line drawing, the absolute stereochemical

formula for the major atom groups, the methyl (CH;)

and the hydroxyl (OH), at the 6- and 5-positions,

respectively, as described in the Belgian Patent appear

as follows:

(OH)

\°

(CH,)

3. At the time the Doxycycline application was

filed Pfizer believed that the stereochemical formula

described in the Belgian Patent did not correctly depict

the absolute stereochemical configuration of the Mc-

Cormick 6-deoxy compound at the 6-position, Pfizer

believed that in the McCormick 6-deoxy compound

the methyl group (CH;) at the 6-position was “up”

(DX 2, 3 and 20; Oglesby Affidavit dated March

18, 1975, paragraph 6, p. 2).

4. At the time the Doxycycline application was

filed Pfizer believed that Doxycycline had the opposite

absolute stereochemical configuration at the 6-position

from the McCormick 6-deoxy compound (Oglesby Affi-

davit dated March 18, 1975, paragraph 32, p. 2),

—-

Pfizer believed that in Doxycycline the methyl group

(CH;) at the 6-position was “down” (DX 3).

5. At the time the Doxycycline application was

filed Pfizer had an uncertain belief that the absolute

stereochemical formula in the Belgian Patent did not

correctly depict the absolute stereochemical configura-

tion of the McCormick 6-deoxy compound at the 5-

position, Pfizer had an uncertain belief that in the

McCormick 6-deoxy compound the hydroxyl group

(OH) at the 5-position was “down” (DX 3, p. 9

and DX 30; Woodward Affidavit dated June 14, 1974,

pp. 7-8; Oglesby Affidavit dated July 30, 1974, para-

graph 3, p. 2; Oglesby Affidavit dated March 18,

1975, paragraph 6, p. 2).

6. At the time the Doxycycline application was

filed Pfizer had an uncertain belief that Doxycycline

had the same absolute stereochemical configuration at

the 5-position as the McCormick 6-deoxy compound

(Oglesby Affidavit dated March 18, 1975, paragraph

5, p. 2), i.e., Pfizer had an uncertain belief that

in both Doxycycline and the McCormick 6-deoxy com-

pound the hydroxyl group (OH) at the 5-position

was “down” (DX 3, p. 9; Oglesby deposition of March

6, 1974, pp. 231-2; Pfizer Brief dated August 8, 1974;

Tr. September 11, 1974, pp. 131-132; Tr. April 17,

1975, p. 244; Tr. April 21, 1975, pp. 498-499).

7. Pfizer's belief as to the absolute stereochemical

configuration of Doxycycline at the 6-position and its

uncertain belief as to the absolute stereochemical con-

figuration of Doxycycline at the 5-position was as fol-

lows:

In a simple line drawing Pfizer's belief and uncertain

belief as to absolute stereochemical formula for the

major atom groups at the 5- and 6-positions of Doxycy-

cline was:

"

(OH)

8. At the time the Doxycycline application was

filed Pfizer knew that Doxycycline had a relative stereo-

chemical configuration in which at the 6-position the

methy! group (CH;) was opposite (or reverse) to

the methyl! group at the 6-position in the McCormick

6-deoxy compound, and Pfizer believed that Doxycy-

cline had a relative stereochemical configuration in

which at the 6-position the methyl group (CH;) was

in the same position as the methyl group at the 6-

position in the natural fermentation produced oxytetra-

cycline compound (Woodward Affidavit dated June

14, 1974, paragraph 4, pp. 7-8; Tr. September 11,

1974, p. 129).

9. At the time the Doxycycline application was

filed, Pfizer knew that Doxycycline had a relative stereo-

chemical configuration in which at the 5-position the

hydroxyl group (OH) was the same as the hydroxyl

group in the McCormick 6-deoxy compound and in

(CH)

a oe Enea tee Se nic,

_ wi ot ee

= =

the natural fermentation produced oxytetracycline com-

pound (Oglesby Affidavit dated March 18, 1975).

10. At the time the Doxycycline application was

filed, and based on its belief as to the absolute stereo-

chemistry of Doxycycline at the 6-position and its uncer-

tain belief as to the absolute stereochemistry of Doxy-

cycline at the 5-position, and its establishment of the

relative stereochemistry of Doxycycline at the 6-position,

Pfizer understood that the absolute stereochemical for-

mula depicted in the Belgian Patent was equally perti-

nent prior art, if not more pertinent prior art, than

the relative stereochemistry of the McCormick 6-deoxy

compound.

11. At the time the Doxycycline application was

filed Oglesby understood that it was his duty to bring

the most pertinent prior art to the attention of the

Patent Office with reasonable diligence (Tr. January

31, 1975, p. 422).

12. At the time the Doxycycline application was

filed Oglesby understood that if the absolute stereo-

chemical formula depicted in the Belgian Patent was

the most pertinent prior art and if Pfizer had uncer-

tainties as to the absolute stereochemical configura-

tion of Doxycycline at the 5-position, it was his duty

to disclose the Belgian Patent and those uncertainties

to the Patent Office with reasonable diligence. (Tr.

January 31, 1975, pp. 422-425).

13. At the time the Doxycycline application was

filed Pfizer did not disclose the Belgian Patent or

the absolute stereochemical formula depicted therein

to the Patent Office. Rather, in the original specification

Pfizer made no mention of the Belgian Patent or its

absolute stereochemical formula, but compared Doxy-

= x

cycline only to the relative stereochemistry of “known

6-deoxytetracyclines”, that is, the compounds actually

produced by the process of the Belgian Patent such

as the McCormick 6-deoxy compound, stating that

Doxycycline was the reverse of the “known 6-deoxy-

tetracyclines” at the 6-position, thereby indicating rela- -

tive stereochemistry only (DX 5, p. 1).

14. At the time the Doxycycline application was

filed Pfizer believed that the absolute stereochemical

configuration of Doxycycline was the same as the abso-

lute stereochemical formula depicted in the Belgian

Patent at the 6-position, and had an uncertain belief

that the absolute stereochemical configuration of Doxy-

cycline was the opposite of the absolute stereochemical

formula depicted in the Belgian Patent at the 5-posi-

tion.

15. At the time the Doxycycline application was

filed Pfizer had not proven its belief that Doxycycline

had an absolute stereochemical configuration in which

the methyl group (CH;) at the 6-position was “down”

or proven its uncertain belief that in Doxycycline the

hydroxyl group (OH) at the 5S-position: was “down”

(Stephens Affidavit dated March 27, 1975, paragraph

6, p. 1; Woodward Affidavit dated June 14, 1974,

paragraph 4, p. 4; Pfizer Brief dated May 1, 1974,

p. 6; Tr. September 11, 1974, p. 104).

16. At the time the Doxycycline application was

filed and until on or about April 24, 1963, Pfizer

believed that the “von Bramer Doctrine”, In re von

Bramer, 127 F.2d 149 (C.C.P.A. 1942), precluded

the grant of a patent on a chemical compound over

a prior art reference which depicted that compound

2 occa AT st cea ee SCR oe

,

= =

even though the prior art reference did not enable

those having ordinary skill in the art to produce the

compound depicted (DX 2; Pfizer Brief dated March

7, 1975, p. 25).

17. At the time the Doxycycline application was

filed Pfizer understood that if its belief concerning

the absolute stereochemical configuration of Doxycy-

cline at the 6-position was correct the Belgian Patent

depicted the absolute stereochemical configuration of

Doxycycline at the 6-position and did not depict the

McCormick 6-deoxy compound at the 6-position (Ogles-

by Affidavit dated March 18, 1975, paragraphs 6

and 7, p. 2).

18. At the time the Doxycycline application was

filed Pfizer understood that if its uncertain belief con-

cerning the absolute stereochemical configuration of

Doxycycline at the 5-position was correct the Belgian

Patent did not depict the absolute stereochemical con-

figuration of Doxycycline at the 5-position (Oglesby

Affidavit dated March 18, 1975, paragraphs 5 and

6, p. 2), and conversely at the time the Doxycycline

application was filed Pfizer understood that if its uncer-

tain belief concerning the absolute stereochemical con-

figuration of Doxycycline at the 5-position was incorrect

the Belgian Patent depicted the absolute stereochemical

configuration of Doxycycline at the 5-position (Wood-

ward Affidavit dated June 14, 1974, paragraph 4,

p. 9).

19. At the time the Doxycycline application was

filed Pfizer, in claiming Doxycycline, resolved its uncer-

tain belief concerning the absolute stereochemistry of

Doxycycline at the 5-position in its own favor (Tr.

April 17, 1975, p. 244).

— =

20. At the time the Doxycycline application was

filed, Pfizer believed that the absolute stereochemical

formula depicted in the Belgian Patent correctly de-

picted Pfizer’s 6-deoxytetracyclines which did not have

a hydroxyl (OH) group at the 5-position but had

two hydrogen (H) groups at the 5-position, one “up”

and one “down”. Since the Belgian Patent described

either a hydroxyl (OH) or a hydrogen (H) at the

5-position (DX 1) (depicted as “up” in the absolute

stereochemical formula depicted in that patent) and

since one of the two hydrogens at that position had

to be “up” in Pfizer’s 6-deoxytetracyclines having two

hydrogens at the 5-position, Pfizer knew that it could

not distinguish those compounds from the absolute

stereochemical formula depicted in the Belgian Patent.

Thus Pfizer stated in the original specification of the

Doxycycline application that Pfizer’s 6-deoxytetracy-

clines having two hydrogen groups at the 5-position

were “products of the present invention” (DX 5, p.

11), but did not claim them in the original claims

(DX 5, pp. 52-54; DX 2; Pfizer Brief dated September

9, 1974; Pfizer Brief dated March 7, 1975, p. 25).

21. At the time the Doxycycline application was

filed, Pfizer believed, based on its prosecution of the

parent Doxycycline application (DX 21), that the Pat-

ent Office might insist on the presentation of product-

by-process claims if it revealed its uncertainties about

absolute stereochemistry (DX 21, pp. 13, 38 and 47).

Pfizer still believed that the Patent Office might insist

on the presentation of product-by-process claims if it

revealed its uncertainties about absolute stereochemistry

on April 25, 1962, and still so believed on December

18, 1962. (DX 6; DX 8; Tr. January 31, 1975,

pp. 420-421).

ON I at

(en ee —tten etter

= SS

22. The last draft of the Doxycycline application

dated May 2, 1961 stated, at Pfizer's patent agent

Charles Knuth’s (Knuth) suggestion, that

These new tetracyclines possess a definite micro-

biological activity against a variety of Gram-posi-

tive and Gram-negative microorganisms and are

appropriately designated as 6-epi-6-deoxytetra-

cyclines since the steric configuration of the 6-

methyl group is opposite to that of the known

6-deoxytetracyclines. Thus, the nomenclature ‘6-

epi’ as employed herein, is completely analogous

to the accepted nomenclature for naming the

known 4-epitetracyclines. However, it should be

understood that inasmuch as the stereochemical

relationship between the 6-methyl group of the

known 6-deoxytetracyclines and the parent (6-

oxygenated) tetracyclines has not yet been estab-

lished, the same is true with respect to the re-

lationship between the new substances and the

parent tetracyclines. (Emphasis added; DX 23:

DX 24).

Pfizer deleted this italicized sentence from the last

draft prior to filing the Doxycycline application.

23. In the original specification of the Doxycycline

application Pfizer deliberately did not state whether

Doxycycline had the same or the opposite stereochemical

configuration at the 6-position from its naturally pro-

duced parent fermentation product, oxytetracycline, and

did not state whether or not the “known 6-deoxytetra-

cyclines” (e.g., the McCormick 6-deoxy compound)

had the same or the opposite stereochemical configura-

tion at the 6-position from their naturally produced

parent fermentation products, i.e., oxytetracycline (DX

2).

—

24. In the original specification of the Doxycycline

application Pfizer did not disclose any absolute stereo-

chemistry, did not disclose its belief as to the absolute

stereochemistry of the McCormick 6-deoxy compound

and doxycycline at the 6-position or its uncertain belief

as to the absolute stereochemistry of the McCormick

6-deoxy compound and Doxycycline at the 5-position,

and did not disclose that it had not proven its said

beliefs. (DX 5; Pfizer Brief dated August 8, 1974).

25. On or about March 29, 1962 Pfizer brought

the Belgian Patent to the attention of the Patent Office

during an interview by Oglesby with Examiner Adams

(the March 1962 interview) (Oglesby Affidavit dated

March 18, 1975, paragraph 12, p. 3). During the

interview Oglesby informed Examiner Adams that Pfizer

believed that the absolute stereochemical formula de-

picted in the Belgian Patent was incorrect at the 5-

position and that Pfizer further believed that the abso-

lute stereochemical formula depicted in the Belgian

Patent did not correctly depict the McCormick 6-deoxy

compound at the 6-position (Oglesby Affidavit dated

March 18, 1975, paragraphs 12, 13 and 14, p. 3).

Oglesby did not reveal to Examiner Adams during

that interview either Pfizer's belief that the stereo-

chemical formula in the Belgian Patent depicted Doxy-

cycline at the 6-position or Pfizer’s uncertain belief

that Doxycycline could be distinguished at the 5-position

from the absolute stereochemical formula depicted in

the Belgian Patent (DX 7).

26. In its first amendment to the Doxycycline appli-

cation on April 26, 1962, Pfizer did not disclose its

—

belief that the absolute stereochemical formula depicted

in the Belgian Patent depicted Doxycycline at the 6-

position or its uncertain belief that Doxycycline could

be distinguished from the absolute stereochemical for-

mula depicted in the Belgian Patent at the 5-position.

In this amendment Oglesby referred to the fact of

the March 1962 interview but did not state that he

had informed Examiner Adams of the Belgian Patent

and did not state that Pfizer believed that the stereo-

chemical formula depicted in the Belgian Patent depict-

ed Doxycycline at the 6-position or that Pfizer had

an uncertain belief that the Belgian Patent did not

depict Doxycycline at the 5-position (DX 5, pp. 65-

67). This amendment concluded with a reque.: for

reconsideration and allowance of the claims (DX 5,

p. 67).

27. On April 26, 1962 Oglesby wrote a memoran-

dum to his files expressing concern that disclosure

to the Patent Office of uncertainties regarding absolute

stereochemistry might limit Piizer to product-by-process

claims (DX 6, p. 2).

28. On October 30, 1962 the Patent Office in

the second Office Action, by Examiner Berg, cited,

inter alia, the Belgian Patent and rejected the compound

(product) claims for Doxycycline and other compounds

as anticipated under 35 U.S.C. §102 (DX 5, p. 68).

29. On December 17, 1962 Knuth informed Ogles-

by of Pfizer's continued and increased uncertainty as

to the absolute stereochemistry of Doxycycline at the

5-position, citing a publication; Muxfeldt, Angew.

a

Chem. Internat. Edit., pp. 372-381 (1962), (Muxfeldt

publication) giving two possible alternative absolute

stereochemical configurations for the natural parent

fermentation produced oxytetracycline, one in which

the hydroxyl group at the 5-position was “up” (as

depicted in the Belgian Patent) and one in which

it was “down” (DX 26).

30. In a memorandum to his files dated December

18, 1962 Oglesby noted Pfizer’s continued and increased

uncertainty as to the absolute stereochemical configura-

tion of Doxycycline at the 5-position, and outlined

his proposed further strategy not to reveal Pfizer's

increased uncertainty about the absolute stereochem-

ical configuration of Doxycycline at the 5-position to

the Patent Office unless other arguments failed to over-

come the Examiner’s rejection based on the Belgian

Patent (DX 8).

31. On or about March 6, 1963 Oglesby and Knuth

interviewed Examiner Berg (March 1963 interview)

and informed him that the Muxfeldt publication had

created some uncertainty as to the absolute stereochemi-

cal configuration of Doxycycline at the 5-position

(Oglesby Affidavit dated March 18, 1975, paragraph

15, p. 3; Knuth Memo to his files dated March

12, 1963, DX 20). Examiner Berg responded that

because of that uncertainty Pfizer could no longer

rely on its belief that the absolute stereochemical formu-

la depicted in the Belgian Patent did not depict Doxy-

cycline at the 5-position, and indicated that the product

(compound) claims would be rejected (Tr. January

31, 1975).

32. Shortly after the March 1963 interview Oglesby

learned of the decision in In re Le Grice, 301 F.2d

—_

929, 133 U.S.P.Q. 365 (C.C.P.A. 1962) and, beginning

about April 24, 1963, believed that Jn re Le Grice

overruled the von Bramer Doctrine and mooted the

possible use of the absolute stereochemical formula

depicted in the Belgian Patent as an anticipation of

Doxycycline (Oglesby Affidavit dated March 18, 1975,

paragraph 17, p. 4).

33. On April 30, 1963 Pfizer filed a second amend-

ment in the Doxycycline application (DX 5, pp. 69-

74). In the remarks accompanying this amendment,

Oglesby referred to the fact of the March 1963 inter-

view but he did not state that he had informed Exam-

iner Berg of Pfizer's uncertainty as to the absolute

stereochemical configuration of Doxycycline at the 5-

position, or that Examiner Berg had stated that those

uncertainties precluded Pfizer from relying on its belief

that the absolute stereochemical formula depicted in

the Belgian Patent at the 5-position did not depict

Doxycycline and indicated that the product (compound )

claims would be rejected.

34. The April 30, 1963 amendment stated that

the Belgian Patent “accidentally” depicted the absolute

stereochemical configuration of. Pfizer's 6-deoxytetra-

cyclines at the 6-position, and cited the Muxfeldt pub-

lication and two other prior art publications (DX

5, pp. 70-71). Oglesby then argued that since- the

Belgian Patent did not enable those skilled in the

art to make the compounds depicted in the stereo-

chemical formula under the Le Grice decision the Bel-

gian Patent could not be relied on as an anticipation.

Based on this argument Pfizer also added claims in

the amendment directed to its 6-deoxytetracyclines

which did not have an hydroxyl (OH) group at the

—

5-position (and which had two hydrogen atoms (H)

at the 5-position) and which Pfizer had not previously

claimed because it believed they were anticipated by

the Belgian Patent under the von Bramer Doctrine

(see Finding 20, supra). Pfizer did not state or indicate

in that amendment that Pfizer was uncertain as to

the absolute stereochemical configuration of Doxycy-

cline at the 5-position, either because of the disclosures

of the three cited publications or for any other reason.

The disclosures of the Muxfeldt publication are set

forth in Finding 29, supra. Of the two remaining

publications, one relates only to oxytetracycline, as

did Muxfeldt, and the other, by Pfizer’s von Wittenauw

et al. (DX 28), does not disclose any uncertainty

at the 5-position.

Pfizer did not state or indicate in the April 30,

1963 amendment, or disclose to the Patent Office

at any other time during the prosecution of the Doxy-

cycline application, that it knew that Doxycycline, the

McCormick 6-deoxy compound and the natural fer-

mentation produced oxytetracycline compound all had

the same relative stereochemical configuration.

35. In December 1963 Pfizer scientist von Wit-

tenau theorized that in Doxycycline the hydroxyl group

(OH) at the 5-position was “up” (as shown in the

Belgian Patent) and prepared a technical paper sum-

marizing the basis for his theory and submitted it

to Pfizer's Patent Department for pre-publication ap-

proval (von Wittenau Affidavit dated March 27, 1975,

paragraph 20, p. 4; DX 9). Von Wittenau’s theory

— =

created additional uncertainty at Pfizer as to the ab-

solute stereochemical configuration of Doxycycline at

the 5-position, and Pfizer deferred publication of the

proposed von Wittenau paper pending review of von

Wittenau’s theory with its consultant Dr. Woodward

(DX 12).

36. On or about April 14, 1964 Oglesby contacted

the Patent Office by telephone (the April 1964 inter-

view) and advised Examiner Modance of the prospec-

tive meeting with Woodward which was expected to

“shed more conclusive light on the structure of the

compounds under discussion” (DX 12, p. 4; Oglesby

Affidavit dated March 18, 1975, p. 4, paragraph 19).

During the April 1964 interview Oglesby was advised

by Examiner Modance that the chemical section in

the Patent Office (which section was acting on the

Doxycycline application) still followed the von Bramer

Doctrine notwithstanding the Le Grice decision (DX

12, p. 5).

37. As of April 14, 1964, because of Pfizer’s in-

creased uncertainty as to the absolute stereochemical

configuration of Doxycycline at the 5-position and the

continued application of the von Bramer Doctrine by

the chemical section of the Patent Office, Pfizer was

still in doubt as to whether the Belgian Patent would

be applied’ by the Patent Office as an anticipation

of Doxycycline under 35 U.S.C. §102. Pfizer did not

inform the Patent Office of its increased uncertainty

as to the absolute stereochemical configuration of Doxy-

cycline at the 5-position.

—

38. By June of 1964, after the meeting with Dr.

Woodward, Pfizer was still uncertain as to the absolute

stereochemical configuration of Doxycycline at the 5-

position which was, in the words of Pfizer patent agent

Knuth, “completely up in the air again” (DX 13).

39. In June of 1964 Oglesby was still uncertain

whether Examiner Modance would accept his Le Grice

argument, notwithstanding a decision, Jn re Brown,

329 F.2d 1006 (C.C.P.A. 1964), casting yet further

doubt on the von Bramer Doctrine (DX 14, p. 2).

Oglesby concluded at that time that he wouid disclose

Pfizer’s continued uncertainty as to the abolute stereo-

chemical configuration of Doxycycline at the 5-position

to Examiner Modance only if the Examiner was willing

to follow the Le Grice and Brown decisions and thus

disregard the absolute stereochemical formula depicted

in the Belgian Patent as an anticipation under 35

U.S.C. § 102 (DX 14, p. 2).

40. On or about July 9, 1964 Oglesby in an inter-

view with Examiner Modance (July 1964 interview)

advised him that Pfizer was uncertain as to the absolute

stereochemical configuration of Doxycycline at the 5-

position (DX 15; Oglesby Affidavit dated March 18,

1975, paragraph 20).

41. In the third amendment filed on July 23, 1964

Pfizer made the fact of the July 1964 interview formally

of record (DX 5, pp. 89-90) but did not state in

the amendment that Pfizer was uncertain as to the

absolute stereochemical configuration of Doxycycline

at the 5-position or that Pfizer’s uncertainties as to

the absolute stereochemical configuration of Doxycy-

cline at the 5-position had been disclosed to or discussed

with Examiner Modance.

— =

42. During the prosecution of the Doxycycline ap-

plication Examiner Adams was not interested in the

absolute stereochemical configuration of either the Mc-

Cormick 6-deoxy compound or Pfizer's 6-deoxytetra-

cyclines because Examiner Adams did not know of

Pfizer’s belief that the Belgian Patent depicted the

absolute stereochemical formula of Doxycycline at the

6-position or Pfizer’s uncertainties as to whether the

Belgian Patent depicted the absolute stereochemical

formula of Doxycycline at the 5-position (Adams

Affidavit dated October 9, 1974, paragraph 7, p. 4;

Adams Affidavit dated February 3, 1975, paragraph

4, p. 2).

43. Had Examiner Adams known at any time be-

tween the date of filing of the Doxycycline application

and April 29, 1962 (the date that Examiner Adams

left the Patent Office) that Pfizer was uncertain as

to whether or not the Belgian Patent correctly depicted

the absolute stereochemical configuration of Doxycy-

cline at the 5-position, Examiner Adams would have

rejected and product (compound) claims of the Doxy-

cycline application as anticipated by the Belgian Patent

under 35 U.S.C. §102 (Adams Affidavit dated February

3, 1975, paragraph 4, p. 2). Had Pfizer after such

rejection not been able to establish by scientific proof,

i.e., scientific evidence which quantitatively and qualita-

tively would be regarded as convincing by a prudent,

experienced chemist skilled in the art, that the absolute

stereochemical formula in the Belgian Patent did not

depict Moxycycline, Examiner Adams would at any

time prior to April 29, 1962 (the date that Examiner

Adams left the Patent Office) have issued a final

rejection, again based on 35 U.S.C. §102 (Adams

—483—

Affidavit dated February 3, 1975, paragraph 4, p.

2; PX 9, paragraph 7, p. 7).

44. Pfizer did not know and did not prove at

any time prior to on or about November 13, 1964

whether or not its uncertain belief that the Belgian

Patent did not depict the absolute stereochemical con-

figuration of Doxycycline at the 5-position was correct

or incorrect (DX 12, 13 and 14).

45. On or about November 13, 1964 Pfizer first

believed that in Doxycycline the absolute stereochemical

configuration of the hydroxyl group (OH) at the 5-

position was “down” (DX 4; Pfizer's Supplemental

Response dated February 11, 1974 to Defendant USV’s

Interrogatory dated July 13, 1973).

46. Pfizer did not at any time during the prosecu-

tion of the Doxycycline application disclose to the

Patent Office when it believed for the first time that

in Doxycycline the absolute stereochemical configura-

tion of the hydroxyl group (OH) at the 5-position

was “down”.

47. With the exception of the March 1963, April

1964 and July 1964 interviews Pfizer did not at any

time during the prosecution of the Doxycycline applica-

tion disclose to the Patent Office that from the time

of the filing of the Doxycycline application and until

on or about November 13, 1964 it had either uncer-

tainties or increased uncertainties, which it had not

proven correct or incorrect, as to whether or not the

Belgian Patent depicted the absolute stereochemical

configuration of Doxycycline at the 5-position.

—49—

D. Conclusions of Law Concerning Pfizer’s Failure

to Disclose the Belgian Patent and its Beliefs

and Uncertainties Concerning the Stereochemistry

of Doxycycline to the Patent Office

1. When Pfizer filed the Doxycycline application

it deliberately withheld informing the Patent Office

of the Belgian Patent.

2. When Pfizer filed the Doxycycline application

it deliberately withheld from the Patent Office its belief

that the Belgian Patent depicted Doxycycline at the

6-position and its uncertainty that the Belgian Patent

did not depict Doxycycline at the 5-position.

3. When Pfizer filed the Doxycycline application

it knew that the Belgian Patent was equally pertinent

if not more pertinen: to the patentability of Doxycycline

than the McCormick 6-deoxy compound, and was there-

fore equally pertinent prior art, if not the most per-

tinent prior art.

4. When Pfizer filed the Doxycycline application

it had a duty to bring the Belgian Patent to the

attention of the Patent Office with reasonable diligence.

5. When Pfizer filed the Doxycycline application

it had a duty to disclose to the Patent Office its

belief that the Belgian Patent depicted Doxycycline

at the 6-position and its uncertain belief that the Belgian

Patent did not depict Doxycycline at the 5-position

with reasonable diligence.

6. When Pfizer filed the Doxycycline application

the significance of the absolute stereochemical formula

depicted in the Belgian Patent as an anticipation under

35 U.S.C. §102 or in limiting the product (compound)

claims to produci-by-process claims under 35 U.S.C.

—_—-

§112, depended upon the disclosure of that depiction

and Pfizer’s knowledge, belief or uncertain belief con-

cerning the absolute stereochemical configuration of

Doxycycline at the 5- and 6-positions. The Patent Office

could not determine the significance of the absolute

stereochemical formula depicted in the Belgian Patent

unless Pfizer disclosed its belief that the Belgian Patent

depicted Doxycycline at the 6-position and its uncertain

belief that the Belgian Patent did not depict Doxycycline

at the 5-position. (Tr. January 24, 1975, pp. 123-

124).

7. When Pfizer filed the Doxycycline application

it deliberately disclosed only the relative stereochemistry

of Doxycycline at the 6-position and the relative stereo-

chemistry of the McCormick 6-deoxy compound at

the 6-position in order to withhold from the Patent

Office the significance of the Belgian Patent as an

anticipation under 35 U.S.C. §102 or in limiting the

product (compound) claims to product-by-process

claims under 35 U.S.C. §112 based on its belief and

uncertain belief concerning the absolute stereochemistry

of Doxycycline at the 6- and 5-positions, respectively.

8. At the time Pfizer filed the Doxycycline applica-

tion the Belgian Patent, coupled with Pfizer's belief

and uncertain belief concerning the absolute stereochem-

istry of Doxycycline at the 6- and 5-positions, respec-

tively, was material to the issue of whether or not

Doxycycline was anticipated under 35 U.S.C. §102,

and was material to the issue of whether or not only

product-by-process claims were allowable under 35

U.S.C. §112.

9. Pfizer is estopped to assert that it brought

the Belgian Patent to the Examiner’s attention in the

March 1962 interview because it failed to state in

undies

writing and of record that it brought the Belgian Patent

co the attention of the Patent Office in that interview.

Alternatively, if Pfizer is not estopped, then Pfizer

deliberately failed to bring the Belgian Patent to the

attention of the Patent Office until the March 1962

interview.

10. Pfizer is estopped to assert that it disclosed

its uncertainties concerning the absolute stereochemistry

of Doxycycline at the 5-position to the Patent Office

in the March 1963, April 1964 and July 1964 inter-

views because it failed to state in writing and of

record that it made these disclosures to the Patent

Office during those interviews. Alternatively, if Pfizer

is not estopped, then Pfizer deliberately failed to disclose

its uncertainties concerning the absolute stereochemistry

of Doxycycline at the 5-position to the Patent Office

until the March 1963 interview.

11. Pfizer is estopped to assert that it disclosed

its beliefs concerning the absolute stereochemistry of

Doxycycline at the 6-position to the Patent Office in

the March 1963 interview because it failed to state

in writing and of record that it made that disclosure

to the Patent Office in that interview. Alternatively,

if Pfizer is not estopped then Pfizer deliberately failed

to disclose its belief concerning the absolute stereochem-

istry of Doxycycline to the Patent Office until the

March 1963 interview.

12. The Belgian Patent and Pfizer’s belief and un-

certainties respecting the absolute stereochemistry of

Doxycycline at the 6-position and 5-position, respec-

tively (and, therefore, the relationship between Doxy-

cycline and the absolute stereochemical formula depicted

in the Belgian Patent) were material to the issues

of whether or not Doxycycline was anticipated under

—=— =

35 U.S.C. $102 or whether or not only product-by-

process claims were allowable under 35 U.S.C. $112

for a period of more than three years after the Doxy-

cycline application was filed and until on or after

June, 1964 when the Patent Office Examiners in charge

of the Doxycycline application accepted Pfizer’s argu-

ment that the Le Grice and Brown decisions overruled

the von Bramer Doctrine.

13. Regardless of the immateriality of the absolute

stereochemistry depicted in the Belgian Patent and Pfiz-

er’s beliefs and uncertainties concerning the absolute

stereochemistry of Doxycycline at the 6- and 5-positions

on or after June, 1964, and based on the estoppels

set forth in Conclusions 9, 10 and 11, supra, Pfizer’s

deliberate failure to bring the Belgian Patent to the

attention of the Patent Office before the October 30,

1962 Official Action (citing the Belgian Patent) and

its deliberate delay in disclosing its belief concerning

the absolute stereochemistry of Doxycycline at the 6-

position to the Patent Office until the April 30, 1965

amendment, and its intentional failure to disclose its

uncertain belief concerning the absolute stereochemistry

of Doxycycline at the 5-position to the attention of

the Patent Office during the prosecution of the Doxy-

cycline application, constitutes a breach of its duty

to bring pertinent prior art and its belief and uncertain

belief concerning the applicability of that prior art

as an anticipation to the attention of the Patent Office

with reasonable diligence. It also constitutes inequitable

conduct which fails to satisfy an applicant’s uncom-

promising duty of absolute candor and full and com-

plete disclosure to the Patent Office of all pertinent

prior art, facts and beliefs which may be relevant

to an issue of patentability.

— =

Alternatively, if there is no estoppel Pfizer’s deliberate

delay in bringing the Belgian Patent to the attention

of the Examiner until March 1962 and its deliberate

delay in disclosing its belief concerning the absolute

stereochemistry of Doxycycline at the 6-position until

March, 1963, and its deliberate delay in disclosing

its uncertainties concerning the absolute stereochemistry

of Doxycycline at the 5-position until March 1963,

constitutes a breach of its duty to bring pertinent

prior art and its belief and uncertain belief concerning

the applicability of that prior art as an anticipation

to the attention of the Patent Office with reasonable

diligence, and also constitutes inequitable conduct which

fails to satisfy an applicant’s uncompromising duty

of absolute candor and full and complete disclosure

to the Patent Office of all pertinent prior art, facts

and beliefs which may be relevant to an issue of

patentability.

E. The Facts Respecting Pfizer's False Analogy Be-

tween Doxycycline and the Prior Art “Epimers”

of the Natural Fermentation Produced Tetra-

cyclines

1. Prior to the grant of the Doxycycline patent

Examiner Adams knew from the prior art that there

were tetracycline epimers which were the opposite of

the natural fermentation produced tetracyclines and

which had lower antibacterial activities than tk» natural

fermentation produced tetracyclines (Adams Affidavit

dated February 3, 1975, p. 7, paragraph 12).

2. Prior to the grant of the Doxycycline patent

Examiner Adams did not know of any tetracycline

epimers which were the opposite of the natural fermenta-

tion produced tetracyclines and which had antibacterial

—

activities superior to the natural fermentation produced

tetracyclines (Adams Affidavit dated February 3, 1975,

paragraph 12, p. 7).

3. Prior to the issuance of the Doxycycline patent

there was no epimer which was the opposite of a

natural fermentation produced tetracycline which had

antibacterial activities superior to the natural fermenta-

tion produced tetracyclines.

4. At all times during the prosecution of the Doxy-

cycline application Pfizer believed that Doxycycline

had the same stereochemical configuration at the 6-

position as its parent natural fermentation produced

tetracycline (both “down”), i.e., oxytetracycline (DX

30, 31 and 40).

5. The Doxycycline application describes the

claimed compounds as “6-epi-6-deoxytetracyclines”, and

states that “the nomenclature ‘6-epi’ as employed herein,

is completely analogous to the accepted nomenclature

for naming the known 4-epitetracyclines” (DX 5, p.

1).

6. The known 4-epi tetracyclines were epimers

which were the opposite of natural fermentation pro-

duced tetracyclines and were so recognized by those

skilled in the art.

7. In a publication dated October 20, 1958 (80

JACS 5572) Cyanamid’s McCormick et al. disclosed

and depicted Sa-epi-tetracyclines. The 5a-epi-tetracy-

clines were epimers which were the opposite of the

natural fermentation produced tetracyclines.

8. In the first rejection of the Doxycycline applica-

tion on October 26, 1961, Examiner Adams cited

the prior art references which described the 4- and

5a-epi-tetracyclines which he believed were (and in

—_ =

fact were) the opposite of natural fermentation pro-

duced tetracyclines at other asymmetric centers of the

nucleus and rejected Pfizer's product (compound)

claims to Doxycycline and other compounds as obvious

under 35 U.S.C. $103, stating that since “epimers”

were well known at other positions in the tetracycline

nucleus, Pfizer’s “epimers” were only a routine develop-

ment (DX 5, pp. 58-59; Tr. April 17, 1975, p. 200).

9. In the first amendment filed April 26, 1962

Pfizer stated that Doxycycline was not a routine or

obvious development, because the antibacterial activity

of Doxycycline was superior to the antibacterial activity

of the McCormick 6-deoxy compound “of normal as

opposed to epimeric. configuration”, and further stated

that such superiority was unexpected. To support the

statement that the superiority of Doxycycline was un-

expected, Pfizer compared Doxycycline (which it be-

lieved to have the same configuration at the 6-position

as the natural fermentation produced tetracyclines, i.e.,

“down”) with prior art “epimers” at other asymmetric

centers on the nucleus (all of which it knew were

the opposite of the natural fermentation produced tetra-

cyclines, i.e., “up”) and stated that while the prior

art “epimers” had less antibacterial activity than their

“conventional” counterparts, Doxycycline had miore

antibacterial activity than the prior McCormick 6-deoxy

compound (DX 5, p. 66).

10. In his final rejection of the Doxycycline appli-

cation on January 19, 1965, based in part on obvious-

ness under 35 U.S.C. $103, Examiner Adams errone-

ously concluded that Doxycycline had an absolute

stereochemical configuration at the 6-position which

was the opposite of the natural fermentation produced

tetracyclines; stating that “. . . the claimed compounds

—56——

have a methy! group in the 6-position which allegedly

is oriented in a different manner than the corresponding

compounds produced by fermentation methods,” and

further stated that it was “well known . . . that

epimerization at various positions reduced the antibiotic

properties of the compound... .” (DX 5, pp. 93-

94).

11. In that rejection Examiner Adams erroneously

stated that the stereochemical configuration of oxytetra-

cycline, the McCormick 6-deoxy compound and Doxy-

cycline at the 6-position were as follows:

Oxytetracycline \ 5

(CH)

McCormick

6-Deoxy Compound 6 5

(CH,)

(CH,)

3

Doxycycline

5

On January 19, 1965 Pfizer believed that the absolute

stereochemical configuration of oxytetracycline, the Mc-

Cormick 6-deoxy compound and Doxycycline at the

6-position were as follows:

—_ =

6 5

Oxytetracycline

(CH)

McCormick (CH |

6-Deoxy Compound -

5

Doxycycline | P 5

(cH 3)

12. In its fifth amendment dated March 5, 1965

responding to the January 19, 1965 final rejection,

Pfizer stated that “the claimed compounds have a

methyl group in the 6-position which is oriented in

the opposite direction to that of the known 6-deoxytetra-

cyclines [e.g., the McCormick 6-deoxy compound] pro-

duced by hydrogenation of fermentation produced tetra-

cyclines . . .” and that “the prior art catalytic hydro-

genation of fermentation produced tetracyclines not

only replaces the 6-OH substituent with a hydrogen

substituent but also reverses the spatial orientation

of the 6-methyl substituent, the orientation of the hydro-

gen substituent being opposite thereto in the final prod-

uct... .” (DX 5, pp. 100-101).

13. The language quoted in Finding E-12, supra,

told the Patent Office that at the 6-position the relative

configuration of Doxycycline was the opposite of the

McCormick 6-deoxy compound which was the opposite

of the natural fermentation produced tetracyclines. That

= =

language, while technically correct, does not state that

Doxycycline and the natural fermentation produced

tetracyclines have the same configuration at the 6-

position, although it can be inferred that if the methyl

group (CH:) at the 6-position has one epimer which

is “up” and one epimer which is “down”, and if the

relative configuration of Doxycycline is the opposite

of the McCormick 6-deoxy compound; and the relative

configuration of the McCormick 6-deoxy compound

is the opposite of the natural fermentation produced

tetracyclines; then in Doxycycline the methyl group

at the 6-position must be “down” and the same as

the natural fermentation produced tetracyclines.

14. In a draft of the March 5, 1965 amendment

Pfizer stated that

this rejection states the claimed compounds have

a methyl group in the 6-position which allegedly

is oriented in a different manner than the corres-

ponding compounds produced by fermentation

methods. Actually . . . the claimed compounds

have a methyl group in the 6-position which is

oriented in precisely the same manner as the corres-

ponding 6-OH containing compounds produced

by fermentation methods . .. . (DX 37).

The above italicized statement was deleted from the

March 5, 1965 amendment before filing.

15. On February 11, 1965 Knuth wrote to Oglesby

and stated that in Doxycycline “. . . the 6-methyl

group has the same configuration as that of the parent

fermentation produced antibiotic” (DX 26).

16. In further response to the January 19, 1965

final rejection, Pfizer's March 5, 1965 amendment re-

peated the representations set forth in its April 26,

—

1962 amendment that the superior antibacterial activi-

ties of Doxycycline were unexpected because of the

low antibacterial activities of prior tetracycline “epi-

mers” (DX 5, p. 104), but did not relate this statement

to the language quoted in Finding E-12, supra.

17. At all times during the prosecution of the

Doxycycline application including the date of allowance

and the date of issuance, Examiner Adams believed

that Doxycycline and the other claimed compounds

had a stereochemical configuration at the 6-position

opposite that of their parent natural fermentation pro-

duced tetracyclines, e.g., oxytetracycline, and that the

superior antibacterial activity of Doxycycline was, be-

cause of this difference, unexpected (Adams Affidavit

dated February 3, 1975, paragraph 12, p. 7 and para-

graph 13, p. 8); but that the unexpected superiority

of Doxycycline was immaterial to patentability (Adams

Affidavit dated February 24, 1975 raph 13

17-18). ee

F. Conclusions of Law Concerning Pfizer's False Anal-

ogy Between Doxycycline and the Prior Art “Epi-

mers”.

1. At page | of the specification, and in the April

25, 1962 and the March 5, 1965 amendments, Pfizer

deliberately misrepresented, by falsely analogizing Doxy-

cycline to prior art tetracycline “epimers” at other

asymmetric positions on the tetracycline nucleus, that

Doxycycline had unexpected superior antibacterial ac-

tivities.

. 2. Pfizer deliberately failed to state in clear, con-

cise and readily understood language and further, delib-

erately used confusing and unclear language in the

March 5, 1965 amendment to conceal, that the absolute

— =

stereochemical configuration of Doxycyciine was the

same as the parent natural fermentation produced tetra-

cyclines at the 6-position. This language was in turn

designed to conceal Pfizer’s false analogy that Doxycy-

cline was comparable to the prior art tetracycline epi-

mers and therefore unexpectedly superior.

3. Pfizer's deliberate misrepresentations in the speci-

fication and in the April 25, 1962 and March 5,

1965 amendments falsely analogizing Doxycycline to

the prior art tetracycline “epimers”, misled the Patent

Office to erroneously conclude from the date of the

January 19, 1965 Office Action to the date of the

issuance of the Doxycycline patent that the stereo-

chemistry of Doxycycline was opposite to that of the

natural fermentation produced tetracyclines at the 6-

position.

4. Pfizer's deliberate misrepresentations in the speci-

fication and in the April 25, 1962 and March 5,

1965 amendments falsely analogizing Doxycycline to

prior art tetracycline “epimers” was not material to

the issue of whether or not Doxycycline was patentable

under 35 U.S.C. §103.

5. Pfizer deliberately falsely analogized Doxycycline

to the prior art tetracycline “epimers” in the specifica-

tion and in the April 25, 1962 and March 5, 1965

amendments, and its deliberate use of misleading and

unclear language in the March 5, 1965 amendment.

All of which was designed to conceal the fact that

Doxycycline had the same absolute stereochemical con-

figuration as its parent natural fermentation produced

tetracycline at the 6-position, amd which was in turn

designed to conceal Pfizer’s false amalogy that Doxycy-

cline was comparable to the prior art tetracycline epi-

mers at the 6-position, constitutes inequitable conduct

_- =

which fails to satisfy an applicant’s uncompromising

duty of absolute candor and full and complete disclosure

of all facts which may be relevant to an issue of

patentability.

G. The Facts Respecting Pfizer's Misrepresentations

to the Patent Office Concerning the Antibacterial

Activity of Doxycycline

1. As filed, the specification of the Doxycycline

application states that Doxycycline and the other

claimed 6-deoxytetracycline compounds “have particu-

larly good in vivo effectiveness” [in animal tests],

and that these compounds “are useful by virtue of

their high order of activity against a variety of micro-

organisms, both in vivo and in vitro” [in test tubes]

(DX 5, p. 11).

2. As filed, the specification also compares the

in vitro activities of Doxycycline and the McCormick

6-deoxy compound against a number of organisms stat-

ing that Doxycycline is markedly superior to the Mc-

Cormick 6-deoxy compound when tested against an

antibiotic resistant strain Micrococcus pyogenes var.

aureus 400 (“Staph 400”), and is equivalent to the

McCormick 6-deoxy compound when tested against

an antibiotic susceptible strain Micrococcus pyogenes

var. aureus 5 (“Staph 5”) (DX 5, p. 12).

3. On February 14, 1961 Pfizer's Dr. McBride

reported the “side by side comparison of Doxycycline

with tetracycline in mice infected with [Staph 5] and

[Staph 400]” and concluded that Doxycycline “remains

inactive against | Staph 400|” (DX 43).

4. At the time the Doxycycline application was

filed, Pfizer knew that Doxycycline was active against

— =

Staph 400 in vitro but inactive against Staph 400

in vivo (DX 42 and 43).

5. In its rejection dated October 26, 1961 the

Patent Office by Examiner Adams rejected the product

claims of the Doxycycline application as obvious under

35 U.S.C. §103 (DX 5, p. 59).

6. In its first amendment dated April 26, 1962

responding to the October 26, 1961 rejection Pfizer

stated that Doxycycline had outstanding antibacterial

activities both in vitro and in vivo (DX 5, p. 66)

and included two affidavits—one by Pfizer’s Dr. English

and one by Pfizer's Dr. McBride—in support thereof

(DX 5, pp. 60-64).

7. The English Affidavit (DX 5, pp. 61-62) set

forth the same in vitro data incorporated in the original

application with respect to the activity of Doxycycline

against Staph 5 and Staph 400. The McBride Affidavit

(DX 5, pp. 63-64) stated that Doxycycline was effective

in vivo against Staph 5 when administered orally and

by injection.

8. Pfizer did not, in its April 26, 1962 amendment,

or at any other time during the prosecution of the

Doxycycline application disclose to the Patent Office

its knowledge that Doxycycline was inactive in vivo

against Staph 400.

9. In the McBride Affidavit Pfizer indicated that

Doxycycline was about 36 times as effective as the

McCormick 6-deoxy compound against Staph 5 in vivo

when administered orally and possessed high activity

against Staph 5 when administered by injection (DX

5, pp. 63-64).

10. In the second Office Action on October 30,

1962 th: Patent Office, by Examiner Berg, stated

—EE —— -

—_— =

that “applicants have submitted two affidavits under

Rule 132 which have been carefully considered and

are deemed persuasive in overcoming the rejection. . .

and are deemed sufficient to overcome the rejection.

”

11. On June 20, 1964 Pfizer scientists English

and Blackwood, among others, knew that further in

vivo tests of Doxycycline against Staph 5 showed that

it was less than one-half as effective as reported in

the McBride affidavit when administered orally, and

only about one-fifth as effective as reported in the

McBride affidavit when administered by injection (DX

44; English Affidavit dated March 27, 1975, paragraph

2).

12. On January 19, 1965, the Patent Office by

Examiner Adams entered a final rejection of the Doxy-

cycline application on the ground that Doxycycline

was obvious under 35 U.S.C. §103 (DX 5, pp. 94-

95).

13. In its fifth amendment dated March 5, 1965,

in response to the final rejection of January i8, 1965,

Pfizer stated that Doxycycline was about 36 times

as effective as the McCormick 6-deoxy compound

against Staph 5 when administered orally, and that

such difference was evidence that Doxycycline was

not obvious (DX 5, p. 104).

14. Pfizer did not, in its March 5, 1965 amendment

or at any other time prior to the grant of the Doxy-

cycline patent in August 1965, disclose to the Patent

Office its June 20, 1964 knowledge that its most

recent in vivo tests of Doxycycline against Staph 5

showed that Doxycycline was less than one-half as

effective as reported in the McBride Affidavit when

administered orally, and only one-fifth as effective as

aiitiiin

reported in the McBride Affidavit when administered

by injection.

15. During the prosecution of the Doxycycline ap-

plication Examiner Adams would have been interested

in; and considered material, any evidence in Pfizer’s

possession inconsistent with the data presented in the

English and McBride Affidavits, incluaing evidence

of inconsistencies between the actual in vivo antibac-

terial activities of Doxycycline and the in vitro activities

of Doxycycline (Adams Affidavit dated February 3,

1975, pp. 5-6), even though he knew during the

prosecution of the Doxycycline application that an anti-

biotic displaying in vitro activity against a particular

organism is not necessarily active in vivo against the

same organism (PX 9, paragraph 10, pp. 11-12).

H. Conclusions of Law Concerning Pfizer’s Misrep-

resentations to the Patent Office Regarding the

Antibacterial Activity of Doxycycline

1. Pfizer deliberately disclosed only the favorable

in vitro and in vivo activity data and deliberately

withheld the unfavorable in vivo activity data from

the Patent Office at all times during the prosecution

of the Doxycycline application. Pfizer did this by delib-

erately concealing the fact that Doxycycline was inactive

against Staph 400 in vivo, and by deliberately with-

holding from the Patent Office from June 20, 1964

and thereafter throughout the prosecution of the Doxy-

cycline application, its June 20, 1964 knowledge that

Doxycycline was less effective against Staph 5 in vivo

than it had reported in the April 25, 1962 amendment

and by representing in the March 5, 1965 amendment

that Staph 5 was as effective in vivo as it had earlier

reported.

—_— =

2. Pfizer’s deliberate concealment of the fact that

Doxycycline was inactive against Staph 400 in vivo

and Pfizer’s deliberate withholding of, and misrepresen-

tation of its June 20, 1964 knowledge that Doxycycline

was less effective in vivo against Staph 5 than it

had earlier reported was material to the issue of whether

or not Doxycycline was obvious under 35 U.S.C. §103.

3. Pfizer’s deliberate concealment of the fact that

Doxycycline was inactive against Staph 400 in vivo,

and its deliberate withholding of and misrepresentation

of its June 20, 1964 knowledge that Doxycycline was

less effective against Staph 5 in vivo than it had

earlier reported, constitutes inequitable conduct which

fails to satisfy an applicant’s uncompromising duty

of absolute candor and full and complete disclosure

of all facts which may be relevant to an issue of

patentability.

I. The Facts Respecting Pfizer’s Misrepresentations

to the Patent Office Concerning the Prior Inherent

Coproductior of Doxycycline

1. In the late 1950's, prior to the filing of the

Doxycycline application, scientists at both Pfizer and

Cyanamid had hydrogenated oxytetracycline and pro-

duced the McCormick 6-deoxy compound. This work

was disclosed in Pfizer’s Stephens et al. paper in the

Journal of the American Chemical Society, Vol. 80,

pp. 5324-25 (1958) (JACS reference) and U.S. Patent

No. 3,019,260 and Belgian Patent No. 565,025 (cited

references), and in the Belgian Patent, all of which

were cited during the prosecution of the Doxycycline

application. None of the cited references state or

indicate that in following the processes stated, Doxy-

cycline is inherently coproduced.

ein

2. Prior to filing the Doxycycline application, Pfizer

knew that the hydrogenation of oxytetracycline to pro-

duce the McCormick 6-deoxy compound had been de-

scribed in the prior art including the cited references

and the Belgian Patent (DX 1; DX 2; Tr. March

17, 1975, p. 23).

3. In 1958 and 1959 (DX 47, 48), Pfizer filed

two patent applications in the names of Stephens and

Conover (Stephens applications), disclosing the pro-

duction of the 6-deoxytetracyclines, including the Mc-

Cormick 6-deoxy compound, by the hydrogenation of

the corresponding tetracyclines, e.g., oxytetracycline.

In the Stephens applications Pfizer disclosed that in

prior experimental work involving the hydrogenation

of oxytetracycline (Stephens’ prior work) they had

produced a “trace” of an “additional active entity”,

which Stephens believed was Doxycycline, and stated

that the “additional active entity” “may be the C-

6 epimer of 6-deoxy-5-oxytetracycline . . .” (doxycy-

cline )(DX 47, pp. 8, 11), and “. . . is thought to

be the C-6 epimer of 6-deoxy-5-oxytetracycline .. .”

(doxycycline) (DX 48, pp. 10, 14).

4. Prior to the filing of the Doxycycline application,

Pfizer contemplated relying on the disclosures in the

Stephens applications and filing a continuation-in-part

application claiming Doxycycline as the invention of

Stephens and Conover (DX 2). However, on Oglesby’s

advice Pfizer filed the Doxycycline application in the

names of Messrs. Blackwood, Beereboom, Rennhard

and Stephens (DX 20; DX 5, pp. 55-56).

5. When Stephens executed the oath for the Doxycy-

cline application with Blackwood, Beereboom and Renn-

hard as one group of inventors he swore that he

ee ee eee

_

did not know and did not believe that Doxycycline

was ever known or used by any other group of inventors,

e.g., Stephens and Conover, prior to the Blackwood,

Beereboom, Rennhard and Stephens invention (DX

5, pp. 55-56).

6. At the time of the filing of the Doxycycline

application and continuously until June, 1964 Stephens

believed that Doxycycline was inherently coproduced

in Stephens’ prior work and in following the process

of one example of the Stephens applications (Stephens

belief). Stephens further believed that if Doxycycline

was inherently coproduced in accordance with the proc-

ess described in the Stephens’ applications it was also

inherently coproduced in following the processes of

the cited references and the Belgian Patent (Stephens’

further belief) (DX 21, pp. 3, 12, 49 and 74; and

Stephens’ Affidavit dated March 27, 1975, paragraph

18, p. 3).

7. When Pfizer filed the Doxycycline application

it did not disclose to the Patent Office the evidence

(the Stephens evidence) obtained in Stephens’ prior

work and described in an example of each of the

Stephens’ applications (DX 47, pp. 10-11; DX 48,

pp. 13-14) which indicated that Doxycycline had in

fact been inherently coproduced.

8. When Pfizer filed the Doxycycline application

it did not advise the Patent Office of Stephens’ belief

or Stephens’ further belief.

9. In the October 30, 1962 Official Action, the

Patent Office by Examiner Berg rejected the pertinent

product claims for Doxycycline and other claimed com-

pounds as anticipated under 35 U.S.C. §102 by the

— =

Belgian Patent and U.S. Patent No. 3,019,260 and

Belgian Patent No. 565,025 (DX 5, p. 68).

10. In its second amendment dated April 30, 1963,

in response to the October 30, 1962 rejection, Pfizer

represented to the Patent Office that Doxycycline was

not in fact inherently coproduced by the Belgian Patent

or by U.S. Patent No. 3,019,260 or by Belgian Patent

No. 565,025, and that these references produced only

the previously known 6-deoxytetracycline compounds,

i.e., the McCormick 6-deoxy compounds (DX 5, p.

70).

11. In its April 30, 1963 amendment Pfizer did

not disclose the Stephens’ evidence or Stephens’ belief

or Stephens’ further belief.

12. On March 20, 1964 Oglesby stated in a mem-

orandum to his files that Stephens believed that the

amount of Doxycycline inherently coproduced in Steph-

ens’ prior work and in following the process of the

Stephens’ applications was “. . . of the same order

of magnitude as tetracycline is produced in Duggar

2209 aureomycin fermentations” (DX 10).

13. On March 20, 1964 Pfizer knew that, if there

was a basis for Stephens’ belief and Stephens’ further

belief then the denial of inherent coproduction in its

April 30, 1963 amendment was false (DX 10).

14. On April 14, 1964 Pfizer knew that it was

still Stephens’ belief that Doxycycline was inherently

coproduced in his prior work and in the process de-

scribed in the Stephens’ applications. Pfizer also knew

that it was still Stephens’ further belief that Doxycy-

cline was inherently coproduced in following the proc-

esses of the cited references and the Belgian Patent

(DX 12).

_—

15. During the Spring of 1964, at Oglesby’s sugges-

tion, Pfizer’s Dr. Murai repeated Stephens’ prior work

(the Murai 1964 investigation), on which Stephens’

belief and further belief were based, and obtained

chromatographic evidence tending to indicate that Steph-

ens’ “additional active entity” was Doxycycline and

ultraviolet spectral evidence indicating that the “addi-

tional active entity’ was not Doxycycline (DX 35

and DX 52). During the Spring of 1964, Pfizer’s

Beereboom believed that chromatographic data was

“much more effective” than ultraviolet spectral data

in identifying Doxycycline (Beereboom deposition, DX

54, p. 310).

16. In June 1964, at the conclusion of the Murai

1964 investigation, Stephens was satisfied that the inher-

ent coproduction of Doxycycline in his prior work

had not been demonstrated and concluded that no

detectable Doxycycline was inherently coproduced there-

in. (Stephens’ Affidavit dated March 18, 1975, para-

graph 18, p. 3).

17. In June 1964, at the conclusion of the Murai

1964 investigation, Pfizer concluded that it could not

State unequivocally that the “additional active entity”

previously produced in Stephens’ prior work was not

Doxycycline, but could state that it believed that it

was not (Oglesby Affidavit dated March 18, 1975,

paragraph 65, p. 9).

18. On July 9, 1964 Oglesby interviewed Examiner

Modance (the July 1964 interview), and disclosed

that Stephens’ prior work might possibly have inherently

coproduced Doxycycline. He also identified the Ste-

phens’ applications, disclosed that part of the conclusion

of the Murai 1964 investigation which showed by ultra-

onitine

violet data that there was no inherent coproduction,

and offered to apprise the Examiner of any further

information he might request. Examiner Modance stated

that the Patent Office could not consider the question

of inherent coproduction since it was not suggested

by any prior art and declined Pfizer’s offer to make

the facts respecting inherent coproduction of record

(Oglesby Affidavit dated March 18, 1975, paragraphs

57 and 72, p. 10).

19. In its third amendment dated July 23, 1964

Pfizer made the fact of the July 1964 interview of

record, but did not mention in that amendment any

of Oglesby’s discussion with Examiner Modance on

July 9, 1964 (DX 5, pp. 89-90).

20. On February 23, 1965 Oglesby interviewed

Examiner Adams (the February 1965 interview) and

disclosed that Stephens’ prior work might possibly have

inherently coproduced Doxycycline, identified the Ste-

phens’ applications, again disclosed that part of the

results of the Murai 1964 investigation, which showed

by ultraviolet data that there was no inherent coproduc-

tion, and offered to apprise him of any further in-

formation he might request. Examiner Adams, like

Examiner Modance, stated that the Patent Office could

not consider the question of inherent coproduction

since it was not suggested by any prior art and declined

Pfizer’s offer to make the facts respecting inherent

coproduction of record (Oglesby Affidavit dated March

18, 1974, paragraph 72, p. 10).

21. Inthe July 1964 and February 1965 interviews,

Oglesby did not disclose Stephens’ belief or Stephens’

further belief. ‘

22. In its fifth amendment dated March 5, 1965,

responsive to the final rejection of January 19, 1965,

_

(DX 5, pp. 98-108) Pfizer made the February 1965

interview of record (DX 5, pp. 99, 106-107) stating

that Pfizer could not state unequivocally that the “ad-

ditional active entity” identified in the Stephens’ prior

work was not Doxycycline but that based on the Murai

1964 investigation it had concluded from the differences

in ultraviolet spectra, that the “additional active entity”

was not Doxycycline (DX 5, pp. 106-107). In that

amendment Pfizer also offered to prc vide the Patent

Office, upon request, with additional information re-

specting the experimental techniques used in the Murai

1964 investigaticn (DX 5, p. 107). The Patent Office

did not request any further information.

In that amendment Pfizer did not state that it had

identified the Stephens’ applications at the July 1964

and February 1965 interviews and did not disclose

Stephens’ belief or Stephens’ further belief.

23. Pfizer did not disclose any of the facts respect-

ing the possible inherent coproduction of Doxycycline

to the Patent Office until the July 1964 and the Febru-

ary 1965 interviews, and Pfizer did not make any

facts respecting the possible inherent coproduction of

Doxycycline in Stephens’ prior work of record in the

Patent Office until March 5, 1965 (DX 5, pp. 107-

108).

24. Pfizer did not, at any time during the prosecu-

tion of the Doxycycline application disclose to the

Patent Office Stephens’ belief or Stephens’ further belief

which Stephens maintained from prior to the filing

of the Doxycycline application and until June 1964.

25. Pfizer did not at any time during the prosecu-

tion of the Doxycycline application disclose to the

Patent Office the chromatographic evidence obtained

—_ =

in the Murai 1964 investigation tending to indicate

that the “additional active entity” in Stephens’ prior

work was Doxycycline.

26. The Patent Office knew from the March 5,

1965 amendment that Pfizer obtained chromatographic

data in Stephens’ prior work indicating that Doxycycline

might be inherently coproduced when following the

process disclosed in the Stephens’ applications. The

Patent Office did not know from that amendment or

from anything else that Pfizer disclosed to the Patent

Office, that chromatographic data was also obtained

in the Murai 1964 investigation which tended to indicate

that Doxycycline was inherently coproduced in Stephens’

prior work.

27. Examiner Adams understood the March 5, 1965

amendment to impliedly represent that there was no

data resulting from the Murai 1964 investigation which

tended to indicate that Doxycycline was inherently co-

produced in Stephens’ prior work (Adams Affidavit

dated February 3, 1975, paragraph 6, p. 3).

28. Examiner Adams understood the March 5, 1965

amendment to impliedly represent that there was no

data resulting from the Murai 1964 investigation which

tended to indicate that Doxycycline was inherently co-

produced in following the processes disclosed in the

cited references or the Belgian Patent (Adams Affidavit

dated February 3, 1975, paragraphs 5, 6, pp. 3-4).

29. Examiner Adams did not avail himself of Ogles-

by’s offer in the March 5, 1965 amendment to supply

additional information regarding the techniques em-

ployed in the Murai 1964 investigation and considered

the information provided from the Murai 1964 investiga-

tion sufficient to establish patentability, even if inherent

= =

coproduction had been in issue, because Examiner

Adams did not know of the chromatographic data

obtained in the Murai 1964 investigation and assumed

that Oglesby had fairly represented the results obtained

in the Murai 1964 investigation (Adams Affidavit dated

February 3, 1975, paragraphs 5 and 6, pp. 3-4; Adams

Affidavit dated February 24, 1975, paragraph 7, p.

7).

30. Examiner Adams did not know from the March

5, 1965 amendment or from anything else Pfizer dis-

closed to the Patent Office during the prosecution

of the Doxycycline application either Stephens’ belief

or Stephens’ further belief.

31. Had Pfizer disclosed to Examiner Adams that

chromatographic data, tending to indicate the inherent

coproduction of Doxycycline in Stephens’ prior work

and in following the process described in the Stephens’

applications, had been obtained in the Murai 1964

investigation, and had Pfizer further disclosed Stephens’

belief and Stephens’ further belief, Examiner Adams

would have been interested in and considered that

chromatographic data material (Adams Affidavit dated

February 3, 1975, paragraph 5, p. 3).

J. Conclusions of Law Concerning Pfizer’s Misrepre-

sentations to the Patent Office Respecting the

Prior Inherent Coproduction of Doxycycline

1. At all times during the prosecution of the Doxy-

cycline application Pfizer deliberately withheld from

the Patent Office Stephens’ belief that Doxycycline

was inherently coproduced in Stephens’ prior work and

in following the process disclosed in the Stephens’ ap-

plications, and further deliberately withheld from the

Patent Office Stephens’ further belief that if Doxycycline

-

was inherently coproduced in Stephens’ prior work and

in the process described in the Stephens applications,

that Doxycycline was also inherently coproduced in

the processes disclosed in the cited references and the

Belgian Patent, which beliefs Stephens maintained from

prior to the filing of the Doxycycline application and

until June, 1964.

2. Pfizer had a duty to disclose Stephens’ belief

and Stephens’ further belief to the Patent Office with

reasonable diligence after the filing of the Doxycycline

application and at all times thereafter during the prose-

cution of the Doxycycline application.

3. In the March 5, 1965 amendment reporting

the results of the Murai 1964 investigation, Pfizer

deliberately disclosed only the favorable ultraviolet data

which indicated that inherent coproduction did not

occur, which deliberately withholding the unfavorable

chromatographic data obtained during the same investi-

gation, which tended to indicate that inherent coproduc-

tion did occur.

4. Pfizer had a duty to disclose that part of the

Murai 1964 investigation which tended to indicate the

inherent coproduction of Doxycycline by chromato-

graphic data in the July 1964 and February 1965

interviews and in its March 5, 1965 amendment and

at all times thereafter during the prosecution of the

Doxycycline application.

5. The cited references and the Belgian Patent

were prior art as to the Doxycycline application under

35 U.S.C. $102.

6. Stephens’ prior work and the Stephens’ applica-

tions were not prior art as to the Doxycycline applica-

tion under 35 U.S.C. §102.

= =

7. Pfizer’s offers to apprise the Patent Office of

any further information it might request concerning

the Murai 1964 investigation in the July 1964 and

the February 1965 interviews and in the March 5,

1965 amendment is insufficient to satisfy Pfizer’s un-

compromising duty of absolute candor and full and

complete disclosure. It was Pfizer’s duty to disclose

that in the Murai 1964 investigation chromatographic

data tended to indicate inherent coproduction, and since

the reported results of the Murai 1964 investigation

did not indicate any contradictory data, the Patent

Office had no duty to inquire further.

8. Pfizer is estopped to assert that it disclosed

to Examiners Modance and Adams in the July 1964

and the February 1965 interviews that Stephens’ prior

work might possibly have inherently coproduced Doxy-

cycline and that it identified the Stephens applications

because Pfizer failed to state in writing and of record

that it brought that information to the attention of

the Patent Office in those interviews.

9. By disclosing only the possibility of inherent

coproduction by chromatographic data at the time of

Stephens’ prior work, and by withholding Stephens’

belief and Stephens’ further belief, and dy deliberately

withholding that part of the Murai 1964 investigation

which tended to indicate the inherent coproduction

of Doxycycline by chromatographic data in Stephens’

prior work, Pfizer deliberately withheld from the Patent

Office the facts and Stephens’ beliefs on which the

Patent Office might have concluded that the cited

references and the Belgian Patent were prior art which

anticipated the Doxycycline application under 35

U.S.C. $102. Pfizer therefore deliberately withheld facts

and beliefs which were material to the issue of whether

—_ In

or not Doxycycline was anticipated under 35 U.S.C.

§102.

10. Pfizer's deliberate withholding of Stephens’ be-

lief that Doxycycline was inherently coproduced in

Stephens’ prior work and Stephens’ further belief that

if Doxycycline was inherently coproduced in accordance

with the process described in Stephens’ application it

was also inherently coproduced in following the proc-

esses of the cited references and the Belgian Patent

and its deliberate withholding of that part of the Murai

1964 investigation which tended to indicate the inherent

coproduction of Doxycycline by chromatographic data

in Stephens’ prior work constitutes inequitable conduct

which fails to satisfy an applicant’s uncompromising

duty of absolute candor and full and complete disclosure

to the Patent Office of all facts which may be relevant

to an issue of patentability.

K. The Facts Respecting Pfizer’s Withholding of Ex-

perimental Data Evidencing Its Inability to Carry

Out Portions of the Patented Process

Use of a Ruthenium Catalyst

1. The Doxycycline patent application and patent

states that Doxycycline and the further compounds

claimed therein may be produced by the hydrogenation

of certain other compounds in the presence of “noble

metal” catalysts (DX 67, column 1, lines 21-30 and

51-65). The patent application and patent further iden-

tify ruthenium as one of the preferred noble metal

catalysts (DX 67, column 2, lines 26-28 and 38-

40).

2. The Doxycycline patent claims, in addition to

Doxycycline and other related compounds, the process

for producing such compounds by hydrogenating cer-

= =

tain other compounds with “a catalytic amount of

a noble metal catalyst” (DX 67, claims 1, 4 and

5).

3. Prior to filing the Doxycycline application Pfizer

had been unsuccessful after a number of experiments

in its efforts to use ruthenium to catalyze the hy-

drogenation process disclosed and claimed in the patent

application and patent (DX 60, 62, 63 and 64).

4. Pfizer did not succeed in using ruthenium to

catalyze the hydrogenation process disclosed and

claimed in the Doxycycline patent application and pat-

ent at any time prior to or during the prosecution

of the Doxycycline application (DX 65, 66 and 75).

5. Pfizer did not disclose to the Patent Office at

any time during the prosecution of the Doxycycline

application its unsuccessful efforts to use ruthenium

to catalyze the hydrogenation process disclosed and

claimed in the Doxycycline patent application and pat-

ent.

6. Had Pfizer diclosed to the Patent Office that

all all times prior to the issuance of the patent it

had been unsuccessful in using ruthenium in all of

its experiments and had not been successful in any

of its experiments in using ruthenium to catalyze the

claimed hydrogenation process, Examiner Adams would

have rejected at least the principal process claim (Claim

1) of the Doxycycline application under 35 U.S.C.

$112 (Adams Affidavit dated February 3, 1975, para-

graph 8, pp. 4-5).

Preparation of 7-Chloro-Doxycycline

7. Example XXXV of the Doxycycline patent appli-

cation and patent describes a detailed procedure for

the preparation of a compound known as 7-chloro-

doxycycline (7-chloro-6-epi-6-deoxy-5-oxytetracycline )

by the hydrogenation of a compound known as

7-chloro-methacycline _(7-chloro-6-deoxy-6-demethyl-6-

methylene-5-oxytetracycline hydrochloride), and speci-

fies the exact conditions to be used in the hydrogena-

tion reaction (DX 5, p. 38, Example XXXV; DX

67, Example XXXV, column 18, lines 10-21).

8. The process for producing 7-chloro-doxycycline

from 7-chloro-methacycline as described in Example

XXXV is claimed in the Doxycycline application and

patent (DX 67, Claims 1-4).

9. In March, April and May of 196°, Pfizer at-

tempted in five separate experiments to make 7-chloro-

doxycycline using the process described in Example

XXXV of the Doxycycline patent application and pat-

ent. In four of the five experiments the presence of

only the 7-chloro-methacycline starting material was

identified and 7-chloro-doxycycline as not identified.

In the fifth experiment, only badly degraded materials,

which could not be identified as 7-chloro-doxycycline

were obtained. 7-chloro-doxycycline was not identified

or isolated in any of these five experiments (DX 68-

71).

10. Pfizer did not succeed in making 7-chloro-doxy-

cycline as disclosed in Example XXXV and as claimed

in the Doxycycline patent application and patent at

any time prior to or during the proggcution of the

Doxycycline application.

11. Pfizer did not disclose to the Patent Office

at any time during the prosecution of the Doxycycline

application its unsuccessful efforts to make 7-chloro-

doxycycline as disclosed in Example XXXV and as

claimed in the Doxycycline patent application and pat-

ent.

_ =

12. Had Pfizer disclosed to the Patent Office that

at all times prior to the issuance of the patent it

had been unsuccessful in making 7-chloro-doxycycline

by the procedure described in Example XXXV in

all of its experiments and had not been successful

in any of its experiments in making 7-chloro-doxycycline

by the procedure described in Example XXXV and

as claimed in the Doxycycline patent application and

patent, Examiner Adams would have rejected at least

the principal process claim (Claim 1) of the Doxycy-

cline application under 35 U.S.C. §112 (Adams Affi-

davit dated February 3, 1975, paragraph 9, p. 5).

L. Conclusions of Law Concerning Pfizer’s Inability

to Carry Out Portions of the Patented Process

Use of a Ruthenium Catalyst

1. From the filing date of the Doxycycline applica-

tion and thereafter throughout the prosecution of the

Doxycycline application Pfizer deliberately withheld

from the Patent Office the fact that in all of its

experiments it was unsuccessful in using ruthenium,

a designated preferred catalyst, in the hydrogenation

process for producing Doxycycline and the other claimed

compounds disclosed and claimed in the patent appli-

cation and patent.

2. Pfizer had a duty to disclose to the Patent

Office with reasonable diligence after the filing of

the Doxycycline application and thereafter during the

prosecution of the Doxycycline application that it had

never successfully used ruthenium to catalyze the hydro-

genation process to produce Doxycycline or any of

the other compounds claimed in the Doxycycline patent

application and patent.

—~ =

3. Had Pfizer disclosed to the Patent Office that

during the prosecution of the Doxycycline application

it had never successfully used ruthenium to catalyze

the hydrogenation process to produce Doxycycline or

any of the other claimed compounds, the Patent Office

would have rejected at least broad claim 1 of the

patent under 35 U.S.C. $112.

4. Pfizer’s deliberate withholding from the Patent

Office of its unsuccessful efforts to use ruthenium as

a catalyst in the process disclosed and claimed in

the Doxycycline patent application and patent was ma-

terial to the issue of whether or not at least broad

process claim 1 was patentable under 35 U.S.C. §112.

5. But for Pfizer’s deliberate withholding of its

unsuccessful efforts to use ruthenium to catalyze the

claimed hydrogenation process, the Doxycycline patent

with at least broad process claim 1 would not have

issued.

6. Pfizer's deliberate withholding and concealment

from the Patent Office during the prosecution of the

Doxycycline application thai it had never successfully

used ruthenium as a catalyst constitutes inequitable

conduct which does not satisfy an applicant’s uncom-

promising duty of absolute candor and full and complete

disclosure to the Patent Office of all facts which may

be relevant to an issue of patentability.

Preparation of 7-chloro-doxycycline

7. From the filing date of the Doxycycline appli-

cation and thereafter throughout the prosecution of the

Doxycycline application Pfizer deliberately withheld

——

from the Patent Office that in all of its experiments

it was unsuccessful in making 7-chloro-doxycycline as

described in Example XXXV of the specification of

the Doxycycline patent application and patent and as

claimed in the patent application and patent.

8. Pfizer had a duty to disclose to the Patent

Office with reasonable diligence after the filing of

the Doxycycline application and thereafter during the

prosecution of the Doxycycline application that it had

never successfully made 7-chloro-doxycycline as de-

scribed in Example XXXV of the Doxycycline patent

application and patent and claimed in the Doxycycline

patent application and patent.

9.. Had Pfizer disclosed to the Patent Office that

during the prosecution of the Doxycycline application

it had never successfully made 7-chloro-doxycycline as

disclosed in Example XXXV and as claimed in the

Doxycycline patent application and patent, the Patent

Office would have rejected at least broad claim 1

of the patent under 35 U.S.C. $112.

10. Pfizer's deliberate withholding from the Patent

Office of its unsuccessful efforts to make 7-chloro-

doxycycline as described in Example XXXV of the

Doxycycline patent application and patent and as

claimed in the Doxycyline patent application and patent

was material to the issue of whether or not at least

the broad process claim 1 was patentable under 35

U.S.C. §112.

11. But for Pfizer’s deliberate withholding of its

unsuccessful efforts to make 7-chloro-doxycycline as

—_— =

described in Example XXXV and as claimed in the

Doxycycline patent application and patent, the Doxycy-

cline patent with at least broad process claim 1 would

not have issued.

12. Pfizer's deliberate withholding and concealment

from the Patent Office during the prosecution of the

Doxycycline application that it had never successfully

made 7-chloro-doxycycline as described in Example

XXXV constitutes inequitable conduct which fails to

satisfy an applicant’s uncompromising duty of absolute

candor and full and complete disclosure to the Patent

Office of all facts which may be relevant to an issue

of patentability.

M. The Facts Respecting Pfizer’s Withholding of and

Misrepresentation of the Facts in this Court Con-

cerning the Significance of the 5-Position Stereo-

chemistry of Doxycycline During Prosecution in

the Patent Office

1. Pfizer is represented of record in this proceeding

by two firms of attorneys Gibson, Dunn & Crutcher

(attorneys Gibson) by J. von Kalinowski, R. Cooper,

and J. Martin, among others, and Cushman, Darby

& Cushman by P. Kokulis and E. Martin, among

others.

2. On November 9, 1973, Defendant USV filed

a Request for Production of Documents seeking all

of the patent prosecution files relating to the Doxy-

cycline patent including Oglesby’s prosecution files and

Oglesby’s internal notes and memoranda (Defendant

USV’s Request for Production of Documents No. 3).

Pfizer responded on December 12, 1973 and refused

to produce these documents on the grounds, among

others, that the Request “seeks documents which are

— =

irrelevant” (Plaintiff Pfizer's Response to Defendant

USV’s Request for Production of Documents No. 3).

3. On December 15, 1973 Defendant USV noticed

Oglesby’s deposition and informally requested Pfizer

to voluntarily produce all of the Oglesby prosecution

files including his internal notes and memoranda on

the understanding that there would be no waiver of

any claim of work product or attorney client privilege

(DX 16). Pfizer refused (Oglesby deposition of March

4, 1974, p. 39).

4. During Oglesby’s deposition on March 4, 1974,

Pfizer’s counsel J. Martin informed Defendant USV’s

counsel that Connolly & Hutz refused to produce certain

documents from Oglesby’s prosecution files, stating that

such documents were Oglesby’s internal memoranda

(the Oglesby internal memoranda) which had never

been disclosed or communicated to Pfizer, but main-

tained solely within Connolly & Hutz’ offices, and that

Connolly & Hutz regarded the Oglesby internal mem-

oranda as its property and also protected by the

attorney-client and work product privileges and refused

to produce them. At that time Connolly and Hutz

produced only a group of documents which consisted

primarily of letters between Oglesby and Pfizer (DX

61, Oglesby deposition of March 4, 1974, pp. 32-

33).

During Oglesby’s deposition Mr. Hutz (Oglesby’s

law partner in Connolly & Hutz) stated that J. Martin’s

statement that the Oglesby internal memoranda had

never been disclosed or communicated to Pfizer and

that Connolly & Hutz regarded them as their property

and protected by the attorney-client and work product

privileges was correct (DX 61, Oglesby deposition,

March 4, 1974, p. 39).

a.

Both statements were made in the presence of Ogles-

by, Knuth and Kokulis. Knuth was present at Oglesby’s

deposition to assist Pfizer’s counsel on technical ques-

tions (Knuth Affidavit dated April 19, 1975, paragraph

2, p. 1). Kokulis participated in the deposition for

Pfizer. Knuth and Kokulis do not deny hearing those

statements, although as of April 19, 1975, Knuth had

no present independent recollection of those statements

(Knuth Affidavit, supra, paragraph 2, p. 1).

During Oglesby’s deposition on March 4, 1974, nei-

ther Kokulis nor Knuth said that the statements that

no one outside Connolly & Hutz had seen the Oglesby

internal memoranda was true or false. Rather, both

remained silent on that subject.

None of the Oglesby internal memoranda were pro-

duced during Oglesby’s deposition (Pfizer Brief dated

April 21, 1975, p. 10).

5. Prior to his deposition on March 4, 1974, Ogles-

by had reviewed only the file wrapper and none of

the Oglesby internal memoranda and only Hutz had

reviewed Oglesby’s files and deleted from the documents

produced all of the Oglesby internal memoranda without

reading them (Oglesby deposition March 4, 1974, p.

93; Hutz Affidavit dated April 28, 1975, paragraph

2,p.2).

6. During his deposition on March 4, 1974, Oglesby

was questioned about what transpired in his interviews

with the Patent Office Examiners and Oglesby testified

that his practice was to quickly prepare an amendment

rather than a document and incorporate in the amend-

ment all that transpired which was germane to the

issues at hand and then file the amendment in the

Patent Office. Oglesby further stated that if something

—s5—

unusual occurred, which he didn’t believe happened

at the March 29, 1962 interview, he might have pre-

pared a memo but did not believe he did for that

interview and could recall nothing other than what

was recorded in the amendment filed on April 26,

1962 (Oglesby deposition, March 4, 1974, pp. 107-

108, 119).

7. During Oglesby’s deposition on March 4, 1974,

Pfizer’s counsel J. Martin sought to stop further ques-

tioning of Oglesby about what had transpired in inter-

views with the Patent Office Examiners, stating that

it was a waste of time since Oglesby had testified

that the amendments filed in the Patent Office reflected

the substance of the interviews and as contemporaneous

documents were more reliable than Oglesby’s recollec-

tion of events occurring 12 years ago (Oglesby deposi-

tion, March 4, 1974, p. 268).

8. During Oglesby’s deposition on March 4, 1974,

and in accordance with the practice in the coordinated

and consolidated actions, Defendant USV’s attorneys

arranged a telephone conference with Pfizer’s attorneys

and with Special Master Heidenreich and requested

him to order the production of Oglesby’s internal mem-

oranda. At that time Pfizer counsel J. Martin repre-

sented to Special Master Heidenreich that the Oglesby

internal memoranda had never been transmitted to

nor seen by Pfizer, or by anyone else, and that Con-

nolly & Hutz regarded them as its property and refused

to produce them (DX 81, Tr. of Heidenreich Con-

ference call, p. 2).

9. During Oglesby’s deposition on March 4, 1974,

Pfizer produced a letter from Knuth to Oglesby dated

July 6, 1964 (DX 20). Oglesby’s handwritten notes

—

(upon which Pfizer subsequently sought to rely in_

connection with these motions) had been deleted from

the bottom of that letter (the Oglesby handwritten

notes) by Hutz prior to its production (DX 15; Hutz

Affidavit dated April 28, 1975, paragraph 2, p. 2).

Counsel for USV were not advised that the Oglesby

handwritten notes had been deleted (Pfizer Brief dated

April 21, 1975, p. 7).

10. The Original Motion filed on May 29, 1974

involved, inter alia, the charge by Defendant USV

that Pfizer had not provided the Patent Office with

all of the facts concerning its knowledge and beliefs

as to the absolute stereochemical configuration of Doxy-

cycline at the 5-position (USV Brief, May 29, 1974,

p. 10; USV Reply Brief, p. 13).

11. In early 1974 Defendant USV spent many days

taking the depositions of Pfizer’s scientists and patent

agents and thereafter extensively briefed the Original

Motion.

12. On July 30, 1974 Pfizer filed an affidavit

executed by Oglesby in opposition to the Original Mo-

tion. That affidavit did not state or indicate that dur-

ing the prosecution of the Doxycycline application Pfizer

had an uncertain belief as to the absolute stereochemi-

cal configuration of Doxycycline at the 5-position or

that Oglesby had ever discussed 5-position stereochem-

istry with any of the Patent Examiners.

13. On September 11, 1974, the first day of argu-

ment on the Original Motion, Pfizer’s counse! Cooper

stated that the 5-position stereochemistry “. . . has

at all times been irrelevant to the patentability of

Doxycycline . . .” and that “. . . the whole point

regarding the 5-position stereochemistry is not relevant

—_— =

to the prosecution history” (Tr. September 11, 1974,

pp. 111, 115).

14. On September 13, 1974, the second day of

argument on the Original Motion, Pfizer’s counsel

Cooper for the first time disclosed that two of the

Oglesby internal memoranda (the two documents) sup-

ported Pfizer’s assertion to the Court that Oglesby

had discussed the 5-position stereochemistry with the

Patent Examiner in the March 1962 interview (Tr.

September 13, 1974, pp. 182, 199).

The Court inquired whether Pfizer should be per-

mitted to produce only selected Oglesby internal memo-

randa which happened to support its position.

Pfizer’s counsel Cooper then stated to the Court

that they had never previously seen the two documents

and that Pfizer had never had or seen the two documents

and that he had recently learned about the two docu-

ments in a telephone conversation with Oglesby (Tr.

September 13, 1974, pp. 168-170), pp. 119-200, p. 226.

(See Also, Tr. January 24, 1975, p. 73). Knuth was

present at the September 13, 1974 hearing (Tr. Septem-

ber 13, 1974, p. 2), but did not state whether or

not the statement that Pfizer had never seen the two

documents was true or false. Rather he remained silent.

15. On September 20, 1974 Pfizer produced the

two documents which relate to Oglesby’s March 29,

1962 interview with Examiner Adams and indicate

that Oglesby discussed the stereochemical formula de-

picted in the Belgian Patent at the 5-position with

Examiner Adams (DX 18, 6, 12).

Pfizer’s first amendment dated April 26, 1962 does

not disclose that Oglesby discussed the stereochemical

formula depicted in the Belgian Patent at the 5-position

with Examiner Adams in the March 1962 interview.

—

16. On January 3, 1975 Pfizer produced another

copy of the Oglesby handwritten note letter to Defend-

ant USV containing the handwritten notes previously

deleted by Hutz, together with other documents (Pfizer

Brief dated April 21, 1975, pp. 8, 9). The handwritten

note letter containing the handwritten notes had never

been produced to the Masters (Tr. January 25, 1975,

pp. 303-304). The handwritten notes relate to Oglesby’s

July 9, 1964 interview with Examiner Modance and

indicate that Oglesby discussed the stereochemical con-

figuration of Doxycycline at the 5-position with Ex-

aminer Modance (DX 15).

Pfizer’s third amendment dated July 23, 1964 does

not disclose that Oglesby discussed the stereochemical

configuration of Doxycycline at the 5-position with

Examiner Modance on July 9, 1964.

17. On January 24, 1975, the fourth day of oral

argument on the Original Motion, Pfizer’s attorneys

J. Martin and E. Martin again represented that the

Oglesby internal memoranda had never been produced

to Pfizer or Pfizer’s attorneys, and that Connolly &

Hutz had just recently produced them to Pfizer’s attor-

neys (Tr. January 24, 1975, pp. 114-117). Kokulis

was present at the January 24, 1975 hearing (Tr.

January 24, 1975, p. 2), but did not state whether

or not the statement that the Oglesby internal memo-

randa had never been produced to Pfizer or Pfizer’s

attorneys until just recently was true or false. Rather

he remained silent.

18. On January 31, 1975, the sixth day of hearings

on the Original Motion, Pfizer’s counsel Cooper and

Oglesby disclosed for the first time that the complete

Oglesby prosecution files including Oglesby’s internal

—g9—

memoranda were delivered to Pfizer in the summer

of 1973 and at that time were reviewed by Pfizer’s

Knuth (Tr. January 31, 1975, pp. 313, 376-377).

Kokulis was present at the January 31, 1975 hearing

(Tr. January 31, 1975, p. 2), but did not state whether

or not he had also reviewed the complete Oglesby

prosecution files including some of Oglesby’s internal

memoranda in the summer of 1973. Rather he remained

silent.

19. On February 5, 1975 additional documents

from Oglesby’s prosecution files were produced for

the first time to defendants (Pfizer's Brief dated

April 21, 1975, p. 10). Some of these documents

(e.g., DX 8, 10) relate to Pfizer’s uncertainty con-

cerning the absolute stereochemistry at the 5-position.

A handwritten note (DX 19) in these files stated

that some of the Oglesby prosecution files, described

on the note as “drafts”, had been delivered to Pfizer

on February 27, 1974, five days before the commence-

ment of Oglesby’s deposition.

20. On February 13, 1975 the Present Motion

was filed by the I.R. Defendants and by Defendant

USV.

21. On April 20, 1975, Kokulis disclosed for the

first time that in August of 1973 he had received

the Connolly & Hutz files from Pfizer and reviewed

them and was aware that they contained “some memo-

randa” (Kokulis Affidavit dated April 20, 1975, para-

graphs 2, 3, p. 1).

22. The two documents first produced on September

20, 1974, the Oglesby handwritten notes first produced

on January 3, 1975, and the documents from the

Oglesby prosecution files first produced on February

5, 1975 revealed for the first time that Pfizer was

concerned from the date of the filing of the Doxycycline

—90—

application until at least June 1964 that the Belgian

Patent might be a complete anticipation of Doxycycline,

or at least might limit Pfizer to product-by-process

claims, because of its belief that the Belgian Patent

depicted the absolute stereochemical configuration of

Doxycycline at the 6-position, its uncertain belief that

the Belgian Patent did not depict the absolute stereo-

chemical configuration of Doxycycline at the 5-position,

and Oglesby’s uncertainty until June, 1964 whether

the Patent Office would follow the Le Grice and Brown

decisions and thus disregard the stereochemical formula

depicted in the Belgian Patent as an anticipation under

35 U.S.C. §102 or alternatively would limit Pfizer

to product-by-process claims.

N. Conclusions of Law Concerning Pfizer's Conceal-

ment and Misrepresentation of Facts in this Court

1. From the filing of the within action and until

January 31, 1975, Pfizer deliberately concealed from

attorneys Gibson that in the summer of 1973 Pfizer's

Knuth had received and reviewed Oglesby’s prosecution

files including all of the Oglesby internal memoranda.

2. From the filing of the within action and until

April 20, 1975, Kokulis deliberately concealed from

attorneys Gibson that in August of 1973 he had received

and reviewed Oglesby’s prosecution files including some

of the Oglesby internal memoranda.

3. From at least December 12, 1973 and until

January 31, 1975, Pfizer through its attorneys Gibson

and its patent agent Knuth deliberately concealed from

the Court that 11 of the Oglesby internal memoranda

were delivered to and reviewed by Pfizer's Knuth in

the summer of 1973.

=

4. From at least December 12, 1973 and until

January 31, 1975 Pfizer through its attorneys Gibson

and its patent agent Knuth deliberately misrepresented,

expressly and by its silence, to the Court that Pfizer

had not received or reviewed all of the Oglesby internal

memoranda in the summer of 1973.

5. From at least December 12, 1973 and until

April 20, 1975 Kokulis deliberately concealed from

the Court that some of Oglesby’s internal memoranda

were delivered to and reviewed by him in August

of 1973.

6. From at least December 12, 1973, and until

April 20, 1975 Kokulis deliberately misrepresented,

by his silence, to the Court that he had not received

or reviewed some of Oglesby’s internal memoranda

in August of 1973.

7. Pfizer and Kokulis had a duty to inform the

Court, at least as early as March 4, 1974, that they

had received and reviewed all or some, respectively,

of the Oglesby internal memoranda in the summer

of 1973.

8. Prior to Oglesby’s deposition on March 4,

1974, Hutz removed Oglesby’s handwritten notes from

the July 6, 1964 letter with deliberate and reckless

disregard about revealing the true and complete facts.

9. Prior to his deposition on March 4, 1974, Ogles-

by deliberately and with reckless disregard about reveal-

ing the true and complete facts, failed to review his

internal memoranda, and as a consequence, erroneously

testified that he did not believe that he had made

any file memoranda concerning the Doxycycline applica-

tion, and that the amendments filed in the Patent

Office stated the substance of his interviews with the

Examiners.

—

10. On July 30, 1974 Oglesby with deliberate and

reckless disregard for the true and complete facts,

misrepresented to the Court that the stereochemical

formula depicted in the Belgian patent at the 5-position

was irrelevant to any issue of patentability during the

prosecution of the Doxycycline application.

11. On September 11, 1974, Pfizer, through its

attorneys Gibson, deliberately misrepresented to the

Court that the stereochemical formula depicted in the

Belgian Patent at the 5-position was always irrelevant

to any issue of patentability during the prosecution of

the Doxycycline application.

12. The deliberate misrepresentations, by expression

or by silence, and the acts of Knuth, Oglesby, Hutz,

Cooper, J. Martin, Kokulis and E. Martin are imputed

to Pfizer.

13. Pfizer's and Kokulis’ deliberate concealments

and misrepresentations, Oglesby’s and Hutz’ deliberate

and reckless disregard about revealing the true and

complete facts, and Pfizer's and Oglesby’s deliberate

misrepresentations that the absolute stereochemistry of

Doxycycline at the 5-position was always irrelevant

to any issue of patentability delayed production of

the two documents until September 20, 1974, delayed

production of the handwritten notes until January 3,

1975, and delayed the production of the documents

from the Oglesby prosecution files until February 5,

1975.

14. The two documents first produced on September

20, 1974, the Oglesby handwritten notes first produced

on January 3, 1975, and the documents from the

Oglesby prosecution files first produced on February

5, 1975 revealed for the first time that Pfizer was

~ SS

concerned from the date of the filing of the Doxycycline

application on May 5, 1961 until at least June 1964

that the Belgian Patent might be a complete anticipation

of Doxycycline under 35 U.S.C. §102, or at least

might limit Pfizer to product-by-process claims under

35 U.S.C. §112.

15. Pfizer's and Kokulis’ deliberate concealments

and misrepresentations, Oglesby’s and Hutz’ deliberate

and reckless disregard about revealing the true and

complete facts and Pfizer’s and Oglesby’s deliberate

misrepresentation that the absolute stereochemistry of

Doxycycline at the 5-position was always irrelevant

to any issue of patentability were material to the issue

of whether or not Doxycycline was anticipated under

35 U.S.C. §102 and whether or not Pfizer would

be limited to product-by-process claims under 35 U.S.C.

$112, and were also material to the issues presented

by the Original Motion, and therefore Pfizer’s and

Kokulis’ conduct constitutes fraud on the Court, unclean

hands and inequitable conduct.

16. Attorneys Gibson conduct did not intentionally

commit fraud on the Court.

O. Conclusions of Law Concerning Pfizer’s Overall

Course of Conduct Before the Patent Office

From the time of the filing of the Doxycycline

application and thereafter throughout the prosecution

thereof Pfizer deliberately embarked upon a course

of conduct to withhold from or to misrepresent to

the Patent Office prior art and facts which were material

to the issues of whether or not Doxycycline was antici-

pated under 35 U.S.C. §102 or obvious under 35

U.S.C. $103 or whether or not Pfizer was entitled

oniiinn

to claims of the broad scope solicited and obtained

under 35 U.S.C. $112, all as set forth in the preceding

Conclusions of Law. That entire course of conduct,

taken as a whole, constitutes fraudulent conduct, or

at the very least a calculated recklessness about the

truth for the purpose of obtaining a patent containing

the broadest possible product and process claims.

Pfizer’s entire course of conduct, taken as a whole,

also constitutes inequitable conduct which fails to satisfy

an applicant’s uncompromising duty of absolute candor

and full and complete disclosure to the Patent Office

of all facts which may be relevant to an issue of

patentability.

P. Conclusions of Law Applicable to Each of the

Above Lettered Sections of the Conclusions of

Law

1. The knowledge, beliefs and acts of each of

the named inventors on the Doxycycline application,

and the knowledge, beliefs and acts of Pfizer’s patent

agent Knuth and Pfizer’s scientists English, McBride,

Frost, Woodward, von Wittenau, Kent, Conover and

Murai is imputed to Oglesby and the knowledge, beliefs

and acts of all of the aforementioned persons is imputed

to Pfizer.

2. Pfizer's conduct in withholding from and in mis-

representing to the Patent Office prior art facts and

beliefs which were material to the issues of whether

or not Doxycycline was anticipated under 35 U.S.C.

$102 or obvious under 35 U.S.C. §103, or whether

or not Pfizer was entitled to claims of the broad

scope solicited and obtained under 35 U.S.C. §112

was material to the question of whether or not the

Patent Office might have stricken the Doxycycline appli-

cation under Patent Office Rule 56.

Oe

—_ =

Q. Pfizer’s Requests for Admissions

Pursuant to Rule 36, Fed.R. Civ. P., Pfizer has

made extensive requests for admissions which it claims

are germane to this motion. For the reasons stated

in the law section herein the admissions sought are

irrelevant to this motion.

R. Ultimate Conclusion of Law

The Doxycycline patent is invalid and unenforceable.

Let Judgment Be Entered Accordingly,

/s/ Miles W. Lord

Miles W. Lord

United States District Judge

JULY 16, 1975

Appeal From the United States District Court for the

District of Minnesota.

United States Court of Appeals for the Eighth Circuit.

In re: Coordinated Pretrial Proceedings in Antibiotic

Antitrust Actions. Pfizer, Inc., Appellant, v. Interna-

tional Rectifier Corp., Rachelle Laboratories Italia, S.p.

A., Rachelle Laboratories, Inc., Rachelle Pharmaceuti-

cals International, S.A., and USV Pharmaceutical Corp.,

Appellees. No. 75-1695.

Submitted: March 9, 1976

Filed: June 16, 1976

Before GIBSON, Chief Judge, HEANEY and WEB-

STER, Circuit Judges.

GIBSON, Chief Judge.

This patent infringement case was initially filed by

Pfizer, Inc. seeking damages and declaratory and in-

junctive relief in the Central District of California.

The defendants, International Rectifier Corp. (IRC)'

‘International Rectifier Corp. and its four subsidiaries, Ra-

chelle Laboratories Italia, S.p.A., Rachelle Laboratories, Inc

(This footnote is continued on next page)

a

—96—

and USV Pharmaceutical Corp. (USV), answered,

pleading that Pfizer's United States Patent No. 3,200,-

149? is invalid and unenforceable for failure to meet

statutory requirements of patentability and for fraud

and misconduct before the Patent Office. Both defend-

ants at first admitted infringement but subsequently

amended their answer to deny infringement and assert

unfair competition and antitrust counterclaims. Upon

defendants’ motion, the case was transferred to the

United States District Court for the District of Minne-

sota and assigned to District Judge Miles W. Lord

for coordinated pretrial proceedings with IRC’s antitrust

case and other antibiotic antitrust litigation, by order

of the Judicial Panel on Multidistrict Litigation dated

March 12, 1973. The case is scheduled to be returned

to the Central District of California for trial after

completion of coordinated pretrial proceedings.

While the case was pending for pretrial processing,

defendants filed successive motions for partial summary

judgment maintaining that Pfizer’s conduct in prose-

cuting the patent application before the Patent Office,

from the time the application was filed in May, 1961,

until the patent was issued in August, 1965, constituted

fraud, inequitable conduct and unclean hands, and

that Pfizer’s conduct before the District Court from

1973 until 1975 was also fraudulent and inequitable,

separately justifying refusal to enforce the patent.

Rachelle Pharmaceuticals International, $.A., and Rachelle Lab-

oratories (Philippines), Inc., are hereafter referred to jointly

as IRC.

2U.S. Patent No. 3,200,149 was issued on August 10, 1965,

for a chemical compound, and the process of producing the

compound, called doxycycline (Pfizer tradename Vibramycin),

a member of the tetracycline family of broad spectrum anti-

biotic drugs.

—97—

On July 16, 1975, in an extensive memorandum

opinion, the District Court granted partial summary

judgment and declared Pfizer’s doxycycline patent in-

valid and unenforceable. Pfizer, Inc. v. International

Rectifier Corp., 186 U.S.P.Q. 511 (D.Minn. 1975).

The court set forth more than 150 “uncontroverted”

facts from the record of documents’ and testimony

taken in eleven days of hearings on the summary

judgment and related discovery motions conducted inter-

mittently from September, 1974, through April, 1975.

On these 150 facts, deemed uncontroverted, Pfizer

was found guilty of five acts of inequitable conduct

before the Patent Office, each of which, standing alone,

the court considered sufficient to bar enforcement of

the patent. They are: (1) Pfizer’s alleged failure to

disclose both the existence of, and its inability to

distinguish, a prior Belgian patent of a similar com-

pound, in order to avoid Patent Office rejection for

anticipation (lack of “novelty”) under 35 U.S.C. §

102 (1964)* and “obviousness” under 35 U.S.C. §

’Pfizer opposed the motion with various memoranda, 54

exhibits and 24 affidavits. The affidavits were prepared by

Patent Examiner Adams, one of three Examiners (Adams, Berg

and Modance) who examined and allowed the doxycycline

patent, scientists employed by Pfizer, Pfizer managers, outside

patent counsel and outside legal counsel.

The defendants supported their motion with memoranda and

one affidavit of Examiner Adams, otherwise relying upon Pfiz-

er’s documents, deposition testimony of Pfizer’s representatives,

and the official prosecution record of the patent in the Patent

Office, called the “file wrapper.”

*35 U.S.C. § 102 states in relevant part as follows:

Conditions for patentability; novelty and loss of right to

patent

A person shall be entitled to a patent unless—

(a) the invention was known or used by others in

this country, or patented or described in a printed pub-

(This footnote is continued on next page)

—9g—

103 (1964);° (2) Pfizer’s argument of an allegedly

false and misleading analogy between doxycycline and

certain prior art epimers,’ similarly to avoid rejection

for anticipation and obviousness; (3) Pfizer’s alleged

concealment of test data concerning the antibacterial

activity of doxycycline, with similar motivation; (4)

Pfizer's alleged concealment of its scientists’ beliefs

that doxycycline may have been coproduced in prior

art processes, similarly motivated; and (5) Pfizer’s

alleged concealment of repeated experimental failures

of processes described and claimed in the doxycycline

patent with the motive of obtaining claims broader

than permissible under 35 U.S.C. § 112 (1964).’

lication in this or a foreign country, before the invention

thereof by the applicant for patent, or

* * *

(f) he did not himself invent the subject matter sought

to be patented, or

(g) before the applicant’s invention thereof the inven-

tion was made in this country by another who had not

abandoned, suppressed, or concealed it.

535 U.S.C. § 103 states in relevant part as follows:

Conditions for patentability; non-obvious subject matter

A patent may not be obtained though the invention

is not identically disclosed or described as set forth in

section 102 of this title, if the differences between the

subject matter sought to be patented and the prior art

are such that the subject matter as a whole would have

been obvious at the time the invention was made to a

person having ordinary skill in the art to which said

subject matter pertains. Patentability shall not be negatived

by the manner in which the invention was made.

®The term “epimer” is defined in part IIA., infra.

735 U.S.C. § 112 states in relevant part as follows:

Specification

The specification shall contain a written description of

the invention, and of the manner and process of making

and using it, in such full, clear, concise, and exact terms

as to enable any person skilled in the art to which it

pertains, or with which it is most nearly connected, to

make and use the same, and shall set forth the best

—99—

Additionally, Pfizer’s entire course of conduct before

the Patent Office was characterized as fraudulent or

“at the very least a calculated recklessness about the

truth” for the purpose of obtaining as broad a patent

as possible. Finally, Pfizer was summarily found guilty

of concealing critical facts from the court, amounting

to inequitable conduct and fraud on the court, that

independently justified refusal to enforce the doxycycline

patent.

On this appeal, Pfizer challenges the District Court's

rulings as violative of the cardinal principle that sum-

mary judgment is permitted only if there is “no genuine

issue as to any material fact,” Fed. R. Civ. P. 56(c),

and also the court’s interpretation of the principles

of law governing the patent infringement defense of

unclean hands resulting from fraud or inequitable con-

du

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