456 F.Supp.2d 644
`(Cite as: 456 F.Supp.2d 644)
`
`United States District Court,
`D. New Jersey.
`JANSSEN PHARMACEUTICA N.V., and Janssen
`Pharmaceutica Products, L.P., Plaintiffs,
`v.
`MYLAN PHARMACEUTICALS., INC., Defend-
`ants.
`Janssen Pharmaceutica N.V., and Janssen Pharma-
`ceutica Products, L.P., Plaintiffs,
`v.
`Dr. Reddy's Laboratories, Ltd., and Dr. Reddy's
`Laboratories, Inc., Defendants.
`
`Civil Action Nos. 03–6220 (JCL), 03–6185(JCL).
`Oct. 13, 2006.
`
`Background:
`Inventors and producers of name
`brand drug for
`the treatment of schizophrenia
`brought infringement action against drug manufac-
`turers which sought to market a generic version of
`the patented drug. Generic manufacturers admitted
`infringement but claimed that patent was invalid
`due to obviousness, and alternatively, was unen-
`forceable due to alleged inequitable conduct.
`
`Holdings: The District Court, Lifland, J., held that:
`(1) claims of patented schizophrenia drug were not
`invalid for obviousness, and
`(2) patent applicant's nondisclosure of prior art re-
`garding the dopamine antagonism of lead chemical
`compound in patented schizophrenia drug did not
`constitute inequitable conduct.
`
`Judgment for plaintiffs.
`
`West Headnotes
`
`Page 1
`
`offset effect of decision in general. Most Cited
`Cases
`
`Party challenging patent bears the burden of
`proving by clear and convincing evidence the in-
`validity or unenforceability of the claims of a pat-
`ent; satisfaction of “clear and convincing” standard
`of proof requires evidence which produces in the
`mind of the trier of fact an abiding conviction that
`the truth of the factual contentions is highly prob-
`able. 35 U.S.C.A. § 282.
`
`[2] Patents 291
`
`16(3)
`
`291 Patents
`291II Patentability
`291II(A) Invention; Obviousness
`291k16 Invention and Obviousness in
`
`General
`
`291k16(3) k. View of person skilled in
`art. Most Cited Cases
`
`Claimed invention is unpatentable if the differ-
`ences between it 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 hav-
`ing ordinary skill in the art. 35 U.S.C.A. § 103(a).
`
`[3] Patents 291
`
`16(2)
`
`291 Patents
`291II Patentability
`291II(A) Invention; Obviousness
`291k16 Invention and Obviousness in
`
`General
`
`Cited Cases
`
`291k16(2) k. Prior art in general. Most
`
`[1] Patents 291
`
`112.5
`
`Patents 291
`
`16(3)
`
`291 Patents
`291IV Applications and Proceedings Thereon
`291k112 Conclusiveness and Effect of De-
`cisions of Patent Office
`291k112.5 k. Sufficiency of evidence to
`
`291 Patents
`291II Patentability
`291II(A) Invention; Obviousness
`291k16 Invention and Obviousness in
`
`General
`
`© 2014 Thomson Reuters. No Claim to Orig. US Gov. Works.
`
`NOVARTIS EXHIBIT 2081
`Par v Novartis, IPR 2016-00084
`Page 1 of 34
`
`

`
`456 F.Supp.2d 644
`(Cite as: 456 F.Supp.2d 644)
`
`Page 2
`
`291k16(3) k. View of person skilled in
`art. Most Cited Cases
`
`35 U.S.C.A. § 103(a).
`
`[5] Patents 291
`
`16(3)
`
`Patents 291
`
`16.13
`
`291 Patents
`291II Patentability
`291II(A) Invention; Obviousness
`291k16.13 k. Fact questions. Most Cited
`
`Cases
`
`Patents 291
`
`36.1(1)
`
`291 Patents
`291II Patentability
`291II(A) Invention; Obviousness
`291k36 Weight and Sufficiency
`291k36.1 Secondary Factors Affecting
`Invention or Obviousness
`291k36.1(1) k. In general. Most
`
`Cited Cases
`
`Obviousness determination in patent case de-
`pends on four underlying factual inquiries: (1) the
`scope and content of the prior art; (2) the level of
`ordinary skill in the prior art; (3) the differences
`between the claimed invention and the prior art;
`and (4) objective evidence of nonobviousness. 35
`U.S.C.A. § 103(a).
`
`[4] Patents 291
`
`16(2)
`
`291 Patents
`291II Patentability
`291II(A) Invention; Obviousness
`291k16 Invention and Obviousness in
`
`General
`
`Cited Cases
`
`291k16(2) k. Prior art in general. Most
`
`For purposes of obviousness determination in
`patent case, scope and content of the prior art is
`limited to art that is analogous to the claimed in-
`vention; analogous art is that which is from the
`same field of endeavor or, if not within the field of
`endeavor, is still reasonably pertinent to the partic-
`ular problem with which the inventor is involved.
`
`291 Patents
`291II Patentability
`291II(A) Invention; Obviousness
`291k16 Invention and Obviousness in
`
`General
`
`291k16(3) k. View of person skilled in
`art. Most Cited Cases
`
`In patent case, obviousness analysis is conduc-
`ted from the perspective of a hypothetical person
`who is presumed to be aware of all the relevant pri-
`or art; however, that hypothetical person of ordin-
`ary skill in the art is presumed to be one who thinks
`along the line of conventional wisdom in the art and
`is not one who undertakes to innovate, whether by
`patient, and often expensive, systematic research or
`by extraordinary insights. 35 U.S.C.A. § 103(a).
`
`[6] Patents 291
`
`16(3)
`
`291 Patents
`291II Patentability
`291II(A) Invention; Obviousness
`291k16 Invention and Obviousness in
`
`General
`
`291k16(3) k. View of person skilled in
`art. Most Cited Cases
`
`Factors considered in defining the level of or-
`dinary skill in the art for purposes of obviousness
`analysis in patent case include: (1) the educational
`level of the inventor; (2) types of problems en-
`countered in the art; (3) prior art solutions to those
`problems; (4) rapidity with which innovations are
`made; (5) sophistication of the technology; and (6)
`educational level of active workers in the field. 35
`U.S.C.A. § 103(a).
`
`[7] Patents 291
`
`16.25
`
`291 Patents
`291II Patentability
`291II(A) Invention; Obviousness
`
`© 2014 Thomson Reuters. No Claim to Orig. US Gov. Works.
`
`NOVARTIS EXHIBIT 2081
`Par v Novartis, IPR 2016-00084
`Page 2 of 34
`
`

`
`456 F.Supp.2d 644
`(Cite as: 456 F.Supp.2d 644)
`
`291k16.25 k. Chemical compounds. Most
`Cited Cases
`
`For a chemical compound, a prima facie case
`obviousness
`requires
`structural
`similarity
`of
`between claimed and prior art subject matter where
`the prior art gives reason or motivation to make the
`claimed compositions. 35 U.S.C.A. § 103(a).
`
`[8] Patents 291
`
`16.5(1)
`
`291 Patents
`291II Patentability
`291II(A) Invention; Obviousness
`291k16.5 State of Prior Art and Advance-
`ment Therein
`
`291k16.5(1) k. In general. Most Cited
`
`Cases
`
`It is not enough for a party seeking to defeat a
`patent on obviousness grounds to merely identify
`each element of the invention in the prior art; in-
`stead, a prima facie case of obviousness requires
`the party to explain the reasons one of ordinary
`skill in the art would have been motivated to select
`the references and to combine them to render the
`claimed invention obvious. 35 U.S.C.A. § 103(a).
`
`[9] Patents 291
`
`16.25
`
`291 Patents
`291II Patentability
`291II(A) Invention; Obviousness
`291k16.25 k. Chemical compounds. Most
`Cited Cases
`
`Claims of patented schizophrenia drug were
`not invalid for obviousness; it would not have been
`obvious to the person of ordinary skill in the art
`that lead chemical compound was short-lasting and
`that that was a problem requiring a modification of
`its molecular structure, none of the cited references
`would convince the person of ordinary skill in the
`art that metabolism at the ketone was causing lead
`compound to be short acting, the solution to the
`lead compound's duration problem would not have
`been obvious to the person of ordinary skill in the
`
`Page 3
`
`art, and secondary considerations overwhelmingly
`demonstrated the nonobviousness of the patent. 35
`U.S.C.A. § 103(a).
`
`[10] Patents 291
`
`16.5(1)
`
`291 Patents
`291II Patentability
`291II(A) Invention; Obviousness
`291k16.5 State of Prior Art and Advance-
`ment Therein
`
`291k16.5(1) k. In general. Most Cited
`
`Cases
`
`the
`applying
`When
`in conduct-
`“motivation-suggestion-teaching” test
`ing obviousness analysis in patent case, court must
`ask whether the person of ordinary skill in the art at
`the relevant time, motivated by the general problem
`facing the inventor, would have been led to make
`the combination recited in the claims. 35 U.S.C.A.
`§ 103(a).
`
`[11] Patents 291
`
`36.1(1)
`
`291 Patents
`291II Patentability
`291II(A) Invention; Obviousness
`291k36 Weight and Sufficiency
`291k36.1 Secondary Factors Affecting
`Invention or Obviousness
`291k36.1(1) k. In general. Most
`
`Cited Cases
`
`Patents 291
`
`36.2(1)
`
`291 Patents
`291II Patentability
`291II(A) Invention; Obviousness
`291k36 Weight and Sufficiency
`291k36.2 Commercial Success
`291k36.2(1) k. In general. Most
`
`Cited Cases
`
`Objective evidence of nonobviousness in patent
`case includes commercial success, long felt, but un-
`solved need, failure of others, copying, acclaim,
`
`© 2014 Thomson Reuters. No Claim to Orig. US Gov. Works.
`
`NOVARTIS EXHIBIT 2081
`Par v Novartis, IPR 2016-00084
`Page 3 of 34
`
`

`
`456 F.Supp.2d 644
`(Cite as: 456 F.Supp.2d 644)
`
`and unexpected superior results. 35 U.S.C.A. §
`103(a).
`
`[12] Patents 291
`
`97.14
`
`291 Patents
`291IV Applications and Proceedings Thereon
`291k97.7 Unenforceability of Patent; Inequit-
`able Conduct or Fraud on Office
`291k97.14 k. Determination; summary
`judgment. Most Cited Cases
`(Formerly 291k97)
`
`In order to find inequitable conduct in patent
`case, there must have been a misrepresentation or
`omission of a material fact, the misrepresentation or
`omission must have been made with an intent to de-
`ceive the Patent and Trademark Office (PTO), and
`the equities must warrant a conclusion that the pat-
`entee has engaged in inequitable conduct. 37 C.F.R.
`§ 1.56(a).
`
`[13] Patents 291
`
`97.9
`
`291 Patents
`291IV Applications and Proceedings Thereon
`291k97.7 Unenforceability of Patent; Inequit-
`able Conduct or Fraud on Office
`291k97.9 k. What information is material.
`Most Cited Cases
`(Formerly 291k97)
`
`For purposes of inequitable conduct analysis in
`patent case, materiality does not require that any
`withheld information,
`if
`it had been provided,
`would have resulted in a rejection of the patent
`claims by the patent examiner; information can be
`“material” even if a patent examiner would find the
`claimed invention to be patentable after considering
`such information. 37 C.F.R. § 1.56(a).
`
`[14] Patents 291
`
`97.9
`
`291 Patents
`291IV Applications and Proceedings Thereon
`291k97.7 Unenforceability of Patent; Inequit-
`able Conduct or Fraud on Office
`
`Page 4
`
`291k97.9 k. What information is material.
`Most Cited Cases
`(Formerly 291k97)
`
`Patents 291
`
`97.12
`
`291 Patents
`291IV Applications and Proceedings Thereon
`291k97.7 Unenforceability of Patent; Inequit-
`able Conduct or Fraud on Office
`291k97.12 k. Failure to disclose material
`information. Most Cited Cases
`(Formerly 291k97)
`
`Patents 291
`
`97.13
`
`291 Patents
`291IV Applications and Proceedings Thereon
`291k97.7 Unenforceability of Patent; Inequit-
`able Conduct or Fraud on Office
`291k97.13 k. Evidence. Most Cited Cases
`(Formerly 291k97)
`
`Patent applicant's nondisclosure of prior art re-
`garding the dopamine antagonism of lead chemical
`compound in patented schizophrenia drug did not
`constitute inequitable conduct rendering the patent
`unenforceable; information that applicant failed to
`disclose to the Patent and Trademark Office (PTO)
`during the patent prosecution was not material since
`such information taught away from the invention,
`not towards it, and there was no clear and convin-
`cing evidence that anyone acted with an intent to
`deceive the PTO. 37 C.F.R. § 1.56(a).
`
`[15] Patents 291
`
`97.8
`
`291 Patents
`291IV Applications and Proceedings Thereon
`291k97.7 Unenforceability of Patent; Inequit-
`able Conduct or Fraud on Office
`291k97.8 k. In general. Most Cited Cases
`(Formerly 291k97)
`
`Because non-inventor was not substantively in-
`volved in the prosecution of patent for chemical
`compound, he had no disclosure obligations im-
`
`© 2014 Thomson Reuters. No Claim to Orig. US Gov. Works.
`
`NOVARTIS EXHIBIT 2081
`Par v Novartis, IPR 2016-00084
`Page 4 of 34
`
`

`
`456 F.Supp.2d 644
`(Cite as: 456 F.Supp.2d 644)
`
`posed on him by the Patent and Trademark Office
`and could not have committed inequitable conduct.
`37 C.F.R. § 1.56(a).
`
`Patents 291
`
`328(2)
`
`291 Patents
`291XIII Decisions on the Validity, Construction,
`and Infringement of Particular Patents
`291k328 Patents Enumerated
`291k328(2) k. Original utility. Most Cited
`
`Cases
`
`4,335,127, 4,342,870, 4,352,811. Cited as Prior
`
`Art.
`
`Patents 291
`
`328(2)
`
`291 Patents
`291XIII Decisions on the Validity, Construction,
`and Infringement of Particular Patents
`291k328 Patents Enumerated
`291k328(2) k. Original utility. Most Cited
`
`Cases
`
`4,804,663. Valid and Infringed.
`
`*647 Douglas Scott Eakeley, John R. Middleton,
`Kaylynn Sun–Lee Yoon, Matthew Jonathan Atlas,
`Rita Marie Jennings, Lowenstein Sandler PC, Rose-
`land, NJ, Gregory L. Diskant, Scott B. Howard,
`Stuart E. Pollack, Melissa Mandgroc, Irena Royz-
`man, Patterson, Belknap, Webb, & Taylor, New
`York, NY, for Plaintiffs.
`
`Arnold B. Calmann, Jeffrey Soos, Saiber, Schle-
`singer, Satz & Goldstein, LLC, Newark, NJ, Robert
`F. Gree, John E. Rosenquist, Christopher T. Grif-
`fith, Peter H. Domer, Leydig, Voit & Mayer, Chica-
`go, IL, for Mylan Pharmaceuticals., Inc.
`
`Alan Henry Pollack, Budd Larner, Short Hills, NJ,
`for Dr. Reddy's Laboratories, Ltd., and Dr. Reddy's
`Laboratories, Inc.
`
`OPINION
`LIFLAND, District Judge.
`
`Page 5
`
`I. Introduction
`Plaintiffs, Janssen Pharmaceutica, N.V., a Bel-
`gian corporation, and its New Jersey-based subsidi-
`ary,
`Janssen Pharmaceutica, L.P.
`(collectively
`“Janssen”), are the inventors and producers of
`risperidone, the active ingredient in Janssen's suc-
`cessful drug for the treatment of schizophrenia,
`Risperdal. It is perhaps an understatement to de-
`scribe Risperdal as merely “successful.” The drug
`has been described by the American Chemical So-
`ciety as “a standard in the treatment of psychosis,
`revolutionizing anti-psychotic treatments.” Pl.'s Ex.
`(“PX”) 309. In 2005 alone, Risperdal accounted for
`over $3 billion in worldwide sales for Janssen's par-
`ent company, Johnson & Johnson. Vergis Tr.
`78:9–16.
`
`Inc.
`Pharmaceuticals,
`Defendants, Mylan
`(“Mylan”),
`a West Virginia
`corporation, Dr.
`Reddy's Laboratories, Ltd., an Indian corporation,
`and its New Jersey-based subsidiary, Dr. Reddy's
`Laboratories, Inc. (collectively, “DRL”), are drug
`manufacturers seeking to market a generic version
`of risperidone. Janssen filed this suit claiming in-
`fringement of its U.S. Patent No. 4,804,663 (“the
`'663 patent”), which claims risperidone, among oth-
`er chemical compounds. Mylan and DRL concede
`they have infringed the '663 patent; they counter,
`however, that the '663 patent is invalid due to obvi-
`ousness, and alternatively, Mylan argues that the
`'663 patent is unenforceable due to Janssen's al-
`leged inequitable conduct.
`
`The parties tried the case before the Court from
`June 28, 2006 through June 30, 2006 and on July 5,
`2006. Thereafter, they submitted proposed findings
`of fact and conclusions of law. The parties' submis-
`sions and the record evidence have been carefully
`considered. For the reasons set forth below,FN1 the
`Court finds that Mylan and DRL have failed to
`prove by clear and convincing evidence that the
`'663 patent is obvious under 35 U.S.C. § 103(a),
`and that Mylan has failed to prove by clear and
`convincing evidence that Janssen engaged in in-
`the '663 patent*648 is
`equitable conduct. Thus,
`
`© 2014 Thomson Reuters. No Claim to Orig. US Gov. Works.
`
`NOVARTIS EXHIBIT 2081
`Par v Novartis, IPR 2016-00084
`Page 5 of 34
`
`

`
`456 F.Supp.2d 644
`(Cite as: 456 F.Supp.2d 644)
`
`neither invalid nor unenforceable, and as a result,
`Mylan and DRL have infringed that patent under 35
`U.S.C. § 271(e)(2).
`
`FN1. This opinion shall constitute the
`Court's findings of fact and conclusions of
`law pursuant to Federal Rule of Civil Pro-
`cedure 52(a).
`
`II. Background
`
`A. The '663 Patent
`
`On February 14, 1989, the United States Patent
`and Trademark Office (“PTO”) issued the '663 pat-
`ent
`to its inventors Ludo E.J. Kennis and Jan
`Vandenberk and assignee, Janssen. PX 1. The '663
`patent originated from a patent application filed
`with the PTO on March 27, 1985. Stipulations of
`Fact (“SF”) 14–15; PX 1.
`
`The '663 patent's 18 claims encompass com-
`pounds “having useful antipsychotic properties and
`being useful in the treatment of a variety of com-
`plaints in which serotonin release is of predominant
`importance.” PX 1. Among those compounds are
`risperidone and compound 11, which are included
`in each of the patent's 18 claims.FN2 SF–17. There
`is no claim in the ' 663 patent in which risperidone
`is the only compound. PX 1; Wolff Tr. 546:1–10.
`
`FN2. In the '663 patent, the chemical name
`for
`Risperidone
`is
`3–[2–[4–(6–fluoro–1,2–benzisoxazol–3–yl
`)–1–piperidinyl]
`ethyl]–6,7,8,9–tetrahydro–2–methyl–4H–p
`yrido[1,2–a]–pyrimidin–4–one;
`the chem-
`ical
`name
`for
`Compound
`11
`is
`3–[2–[4–(6–fluoro–1,2–benzisoxazol–3–yl
`)–1–piperidinyl]
`ethyl]–2–methyl–4H–pyrido[1,
`2–a]pyrimidin–4–one. Defs.' Ex. (“DX”) 1.
`
`The compounds claimed in the '663 patent were
`the result of Janssen's efforts to invent an effective
`antipsychotic drug, with few side effects, for the
`treatment of Schizophrenia. Tamminga Tr. 53:4–22.
`
`Page 6
`
`B. Schizophrenia
`Schizophrenia is a debilitating disease of the
`brain characterized by hallucinations, delusions and
`other symptoms that impair a person's capacity for
`thought, attention, memory, emotion and social
`functioning. Tamminga Tr. 46:19–47:1. Despite
`much research, the cause, mechanism, and etiology
`of the disease remain unknown. Tamminga Tr.
`47:2–3.
`
`People who suffer from schizophrenia exhibit a
`wide array of symptoms that can be classified into
`three major categories: positive symptoms, negative
`symptoms, and cognitive symptoms. Tamminga Tr.
`47:4–7.
`
`Positive symptoms include extreme hallucina-
`tions and paranoid delusions. Hallucinations are
`auditory, visual or both. Schizophrenics do not just
`hear voices in their mind, “they believe that there
`are people actually talking to them.” Tamminga Tr.
`47:8–16. In addition, schizophrenics believe in the
`false realities created by their delusions, sometimes
`causing the delusions to take over their lives. Id. at
`47:17–18.
`
`Negative symptoms include the complete loss
`of all emotion and lack of spontaneous thought,
`both of which “result in a loss of social skills and
`really an entire loss of social functioning.” Tam-
`minga Tr. 47:19–24.
`
`Cognitive symptoms include the impairment of
`memory and attention. These cognitive deficits
`cause schizophrenics to become unable to use in-
`formation and to have great difficulty making de-
`cisions. Tamminga Tr. 47:25–48:4.
`
`These symptoms can entirely take over the
`lives of persons with schizophrenia, preventing
`them from working or developing social networks.
`Less than 20 percent of schizophrenics have jobs,
`less than 15 percent ever marry, and approximately
`10 percent eventually commit suicide. Tamminga
`Tr. 48:5–15.
`
`© 2014 Thomson Reuters. No Claim to Orig. US Gov. Works.
`
`NOVARTIS EXHIBIT 2081
`Par v Novartis, IPR 2016-00084
`Page 6 of 34
`
`

`
`456 F.Supp.2d 644
`(Cite as: 456 F.Supp.2d 644)
`
`*649 C. Early Treatments
`Schizophrenia is a disease as old as mankind.
`For most of that time, there were no effective med-
`ical treatments. The only option was compassionate
`care, placing schizophrenics into protected environ-
`ments such as government hospitals that quickly
`became overcrowded. But compassionate care did
`nothing to treat the symptoms and the patients did
`not get better. Tamminga Tr. 48:18–49:2.
`
`Beginning in the 1930s, doctors attempted
`medical treatments. These treatments included in-
`duced fever, electroconvulsive shock therapy and
`frontal lobotomy. None of these attempts to treat
`the disease was effective. To the contrary, these
`treatments could even worsen the symptoms of
`schizophrenia. Tamminga Tr. 49:3–12.
`
`D. First Generation, “Typical” Antipsychotic
`Drugs
`The lack of effective treatment options contin-
`ued into the 1950s. Then, for the first time, doctors
`developed an antipsychotic drug to treat schizo-
`phrenia, called chlorpromazine. Tamminga Tr.
`49:13–18. The discovery that chlorpromazine could
`treat some symptoms of schizophrenia was acci-
`dental. Physicians were testing chlorpromazine as a
`sedative when they noticed that chlorpromazine
`significantly reduced the hallucinations and delu-
`sions of their schizophrenic patients. Tamminga Tr.
`49:19–25.
`
`for
`treatment
`the first pharmaceutical
`As
`schizophrenia, chlorpromazine was rapidly adopted
`for use throughout the medical community. Phar-
`maceutical companies quickly began searching for
`similar drugs. This led to the development of new
`antipsychotics such as Janssen's haloperidol, mar-
`keted under
`the trade name, Haldol. Chlorpro-
`mazine, haloperidol, and other similar drugs be-
`came known as first generation, or typical, anti-
`psychotics. Tamminga Tr. 50:12–16, 21–25.
`
`While chlorpromazine and the other typical an-
`tipsychotics were an improvement over compas-
`sionate care and the early ineffective treatments,
`
`Page 7
`
`they were not perfect. A typical antipsychotic im-
`proved the positive symptoms of schizophrenia, but
`it had no effect on the negative or cognitive symp-
`toms that severely impaired the emotions, thoughts,
`and social functioning of schizophrenics. In fact, in
`some cases a typical antipsychotic could even
`worsen these symptoms. Tamminga Tr. 50:1–3.
`
`More significantly, even when typical anti-
`psychotics were successful at treating the positive
`symptoms of schizophrenia,
`they had many un-
`wanted and serious side effects, including sedation,
`cardiac side effects, and motor side effects. The
`motor-related side effects were the largest draw-
`back. Tamminga Tr. 51:1–5.
`
`For example, typical antipsychotics caused ex-
`trapyramidal symptoms (“EPS”) that caused pa-
`tients to experience rigidity and tremors similar to
`those of Parkinson's disease. The rigidity and
`tremors brought on by EPS were always uncomfort-
`able and often painful. EPS symptoms tended to
`cease when a patient stopped taking the medication.
`Tamminga Tr. 51:6–52:2.
`
`Even worse, EPS symptoms could also gradu-
`ally develop into a more serious motor syndrome
`called “tardive dyskinesia” (“TD”), characterized
`by motor difficulties such as, repetitive, involun-
`tary, and purposeless movements. Unlike EPS, tar-
`dive dyskinesia was frequently irreversible even
`after the medication was discontinued. Tamminga
`Tr. 51:13–23.
`
`These side effects had significant repercussions
`in the treatment of schizophrenia. Not surprisingly,
`patients disliked these motor side effects so much
`that they sometimes*650 stopped taking their med-
`ication altogether. Tamminga Tr. 52:3–5.
`
`E. Second Generation, “Atypical” Antipsychotic
`Drugs
`In the 1960s, scientists' search for an improved
`antipsychotic resulted in the development of the
`first second generation or “atypical” antipsychotic,
`clozapine. Clozapine was introduced in the 1960s
`
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`in Europe. Unlike the typical antipsychotics, cloza-
`pine had reduced motor side effects. Tamminga Tr.
`52:6–9, 52:25–53:1.
`
`Soon after clozapine was introduced, however,
`researchers discovered that while it had reduced
`motor side effects, it had a significant toxicity is-
`sue.
`It was found that clozapine could cause
`agranulocytosis, a sometimes deadly blood dis-
`order. Due to its toxicity, the Food and Drug Ad-
`ministration (“FDA”) did not approve clozapine in
`the United States until 1990. And even then, it was
`not approved for general use; its approval was lim-
`ited to use only with treatment-resistant patients.
`Tamminga Tr. 52:10–24.
`
`Despite this drawback, the discovery of cloza-
`pine demonstrated that it was possible to treat the
`positive symptoms of schizophrenia without serious
`motor side effects. It gave the medical community
`renewed hope
`for developing improved anti-
`psychotic drugs. Tamminga Tr. 53:2–8. For that
`reason, clozapine became the focus of researchers
`looking for new drugs that would incorporate cloza-
`pine's improvements without
`its toxicity. Strup-
`czewski Dep. (11/16/2004) Tr. 82:4–12. For ex-
`ample, both Eli Lilly and Sandoz spent years on re-
`search programs to modify clozapine to create a
`drug that would retain clozapine's benefits and
`eliminate its toxic effect. Meltzer Tr. 250:3–17;
`Tamminga Tr. 53:2–8.
`
`F. Risperidone
`Janssen was one of the companies attempting
`to develop a safe atypical antipsychotic. Following
`years of research and the testing of many potential
`compounds,
`two Janssen scientists, Kennis and
`Vandenberk, discovered risperidone. When ap-
`proved by the FDA, risperidone became the first
`atypical antipsychotic available for general use that
`effectively treated symptoms with reduced side ef-
`fects. Risperidone, sold by Janssen under the trade-
`mark Risperdal, was approved by the FDA in late
`1993 and was first sold in the United States in
`1994. Tamminga Tr. 53:9–13; Vergis Tr. 76:6–7,
`13–15, 76:24–77:5.
`
`Page 8
`
`Risperidone was a major advance over the typ-
`ical antipsychotic drugs. Tamminga Tr. 55:19–56:5.
`Like the typical antipsychotics, risperidone has a
`potent effect in treating the positive symptoms of
`schizophrenia. However, unlike the typical anti-
`psychotics, risperidone also improves the negative
`and
`cognitive
`symptoms
`of
`schizophrenia.
`Moreover, risperidone also has an extremely low
`side effect profile, with reduced EPS and almost no
`TD. Tamminga Tr. 53:14–22, 55:19–56:5.
`
`Risperdal had a revolutionary impact on the
`treatment
`of
`schizophrenia. Once
`risperidone
`entered the market,
`the medical community “set
`aside” the typical antipsychotics. Tamminga Tr.
`55:19–25.
`
`G. Mylan & DRL's Abbreviated New Drug Applic-
`ations
`Following Janssen's success with Risperdal,
`generic manufacturers began filing Abbreviated
`New Drug Applications (“ANDA”) with the FDA
`under
`the Hatch–Waxman Act, 28 U.S.C. §
`355(j)(1),
`seeking
`approval
`to
`sell
`generic
`risperidone products. Most of
`those companies
`chose not to challenge Janssen's '663 patent and
`*651 included a “paragraph III” certification under
`28 U.S.C. § 355(j)(2)(A)(vii)(III), indicating that
`the FDA should not approve their applications until
`after the expiration of the '663 patent. Vergis Tr.
`82:9–13; PX 75, PX 76, PX 77, PX 78, PX 85; PX
`396.
`
`On November 29, 2001, Mylan submitted an
`ANDA (No. 76–288) to the FDA seeking approval
`to market a generic risperidone tablet in various
`doses. Initially, Mylan also chose not to challenge
`the '663 patent by including a paragraph III certific-
`ation with its ANDA. SF 21.
`
`On October 24, 2003, DRL submitted an AN-
`DA (No. 76–879) to the FDA also seeking to sell a
`generic version of risperidone. SF–27. DRL's AN-
`DA, however, contained a “paragraph IV” certifica-
`tion pursuant to 28 U.S.C. § 355(j)(2)(A)(vii)(IV),
`challenging the validity of the '663 patent. FN3 SF
`
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`29. On November 19, 2003, Mylan followed DRL's
`lead and amended its ANDA (No. 76–288) to in-
`clude a paragraph IV certification. SF–23. Both De-
`fendants informed Janssen of its paragraph IV certi-
`fications shortly thereafter. SF 24, 29.
`
`FN3. DRL twice amended its ANDA to in-
`clude different doses and variations of a
`generic risperidone.
`
`H. The Current Litigation
`On December 30, 2003, Janssen filed separate
`patent
`infringement actions against Mylan (Civil
`No. 03–6220) and DRL (Civil No. 03–6185) under
`35 U.S.C. § 271(e)(2).FN4 On March 8, 2004, the
`two actions were consolidated for discovery and
`pre-trial purposes. Two additional actions filed by
`Janssen against DRL (Civil Nos. 05–0884, 5326)
`based on the filing of additional paragraph IV certi-
`fications for different forms of risperidone were
`consolidated with No. 03–6185 on March 9, 2006.
`
`FN4. Upon receiving notice of an applic-
`ant's paragraph IV certification, 35 U.S.C.
`§ 271(e)(2) permits the patent holder to
`immediately bring an action in a U.S. Dis-
`trict Court for a determination that the ap-
`plication infringes the patent. See, e.g.,
`SmithKline Beecham Corp.
`v. Apotex
`439
`F.3d
`1312,
`1314
`Corp.,
`(Fed.Cir.2006).
`
`In February 2004, Mylan and DRL filed separ-
`ate answers. Both Defendants asserted an affirmat-
`ive defense claiming that the '663 patent is invalid
`for obviousness under 35 U.S.C. § 103(a). Both De-
`fendants also asserted a counterclaim seeking a de-
`claration of invalidity.
`
`On June 7, 2006, Mylan amended its answer to
`include the additional affirmative defense that the
`'663 patent is unenforceable due to Janssen's al-
`leged inequitable conduct. Mylan also seeks a de-
`claratory judgment to that effect. DRL did not join
`Mylan in asserting this defense and counterclaim.
`
`Page 9
`
`I. Jurisdiction, Venue and Applicable Law
`This Court has subject matter jurisdiction over
`Janssen's patent infringement claims and Mylan and
`DRL's counterclaims pursuant to 28 U.S.C. §§ 1331
`and 1338(a). Defendants have waived any objec-
`tions to this Court's exercise of personal jurisdic-
`tion, SF 11, and venue is proper under 28 U.S.C. §§
`1391(b)(1) and (c), and 1400(b).
`
`Because this action arises under the patent laws
`of the United States, this Court must apply the pre-
`cedents of the United States Court of Appeals for
`the Federal Circuit, which has jurisdiction over any
`appeal of this judgment. See 28 U.S.C. § 1295(a).
`
`III. Analysis
`
`A. Patent Infringement
`
`One is liable for patent infringement if he or
`she, “without authority makes, uses, *652 offers to
`sell, or sells any patented invention ... during the
`term of the patent therefor....” 35 U.S.C. § 271(a).
`Additionally, the filing of an application with the
`FDA under 21 U.S.C. § 355(j) “for a drug claimed
`in a patent” is an act of infringement “if the purpose
`of such submission”—as demonstrated in the ap-
`plicant's paragraph IV certification—“is to obtain
`approval ... to engage in the commercial manufac-
`ture, use, or sale of [that] drug ... before the expira-
`tion of such patent.” 35 U.S.C. § 271(e)(2)(A).
`
`Defendants concede infringing the claims of
`'663 patent with their proposed ANDA
`the
`products. SF 47. Thus, the only issues before the
`Court are those raised in Defendants' affirmative
`defenses to infringement: (1) whether the '663 pat-
`ent is invalid due to obviousness, as asserted by
`Mylan and DRL, and (2) whether the '663 patent is
`unenforceable due to inequitable conduct, as asser-
`ted only by Mylan.
`
`[1] “A patent shall be presumed valid.” 35
`U.S.C. § 282. The validity of each claim within a
`patent must be evaluated independently;
`the in-
`validity of one claim does not disturb the presump-
`
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`tion of validity of another. Id. The party challen-
`ging the patent bears the burden of proving by clear
`and convincing evidence the invalidity or unen-
`forceability of the claims of a patent. Id. “The
`‘clear and convincing’ standard of proof of facts is
`an intermediate standard which lies somewhere
`between ‘beyond a
`reasonable doubt’
`and a
`‘preponderance of the evidence’ ” and “has been
`described as evidence which produces in the mind
`of the trier of fact an abiding conviction that the
`truth of [the] factual contentions [is] ‘highly prob-
`able.’ ” Buildex, Inc. v. Kason Indus., Inc., 849 F.2d
`1461, 1463 (Fed.Cir.1988) (internal quotation omit-
`ted).
`
`B. Obviousness
`[2][3] “[A] claimed invention is unpatentable if
`the differences between it 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.’ ” Alza
`Corp. v. Mylan Labs., Inc., 464 F.3d 1286, 1289
`(Fed.Cir.2006) (quoting 35 U.S.C. § 103(a)). Obvi-
`ousness is a question of law. Id. at 1289–90. Its res-
`olution depends on four underlying factual inquir-
`ies, the so-called GrahamFN5 factors: “ ‘(1) the
`scope and content of the prior art; (2) the level of
`ordinary skill in the prior art; (3) the differences
`between the claimed invention and the prior art;
`and (4) objective evidence of nonobviousness.’ ”
`Id. at 1290 (quoting In re Dembiczak, 175 F.3d 994,
`998 (Fed.Cir.1999)).
`
`FN5. Graham v. John Deere Co., 383 U.S.
`1, 86 S.Ct. 684, 15 L.Ed.2d 545 (1966).
`
`1. The Scope and Content of the Prior Art
`[4] The scope and content of the prior art is
`limited to art that is analogous to the claimed in-
`vention. See In re Bigio, 381 F.3d 1320, 1325
`(Fed.Cir.2004). Analogous art is that which is from
`the same field of endeavor or, if not within the field
`of endeavor, is still reasonably pertinent to the par-
`ticular problem with which the inventor is involved.
`Id.
`
`Page 10
`
`The prior art includes (1) analogous patents or
`printed publications of a person besides the invent-
`or in this or a foreign country before March 27,
`1985