Case 1:14-cv-02758-PAC Document 138 Filed 02/21/17 Page 1 of 86
`
`UNITED STATES DISTRICT COURT
`FOR THE SOUTHERN DISTRICT OF NEW YORK
`
`
`
`Kowa Company, Ltd.,
`Kowa Pharmaceuticals America, Inc., and
`Nissan Chemical Industries, Ltd.,
`
`
`Plaintiffs,
`
`v.
`
`Amneal Pharmaceuticals, LLC,
`
`
`Defendants.
`
`
`Kowa Company, Ltd.,
`Kowa Pharmaceuticals America, Inc., and
`Nissan Chemical Industries, Ltd.,
`
`
`Plaintiffs,
`
`
`v.
`
`Apotex, Inc. and Apotex Corp.,
`
`
`Civil Action No. 14-CV-2758 (PAC)
`
`Civil Action No. 14-CV-7934 (PAC)
`
`Defendants.
`
`
`
`DEFENDANTS AMNEAL’S AND APOTEX’S
`PROPOSED FINDINGS OF FACT AND CONCLUSIONS OF LAW
`REGARDING ANTICIPATION AND OBVIOUSNESS OF THE ASSERTED
`“FORM A CLAIMS” OF U.S. PATENT NO. 8,557,993
`
`
`
`
`
`
`
`

`

`Case 1:14-cv-02758-PAC Document 138 Filed 02/21/17 Page 2 of 86
`
`TABLE OF CONTENTS
`
`I. 
`
`II. 
`
`INTRODUCTION ........................................................................................................................... 1 
`
`PROPOSED FINDINGS OF FACT REGARDING ANTICIPATION OF THE
`“FORM A” CLAIMS OF THE ’993 PATENT ........................................................................... 2 
`
`A. 
`
`Background ........................................................................................................................... 2 
`
`1. 
`
`2. 
`
`3. 
`
`4. 
`
`The ’993 Patent ....................................................................................................... 2 
`
`Asserted “Form A Claims” of the ’993 Patent ................................................... 2 
`
`The Specification of the ’993 Patent .................................................................... 4 
`
`The Prosecution History of the ’993 Patent ....................................................... 6 
`
`B. 
`
`Nissan Itself Proved that Example 3 of EP ’406 Anticipates Claims 1 and 22-25 of
`the ’993 Patent. ..................................................................................................................... 7 
`
`1. 
`
`2. 
`
`3. 
`
`4. 
`
`5. 
`
`6. 
`
`EP ’406 Discloses a Process for Making a Crystalline Form of Pitavastatin
`Calcium. .................................................................................................................... 8 
`
`Plaintiff Nissan’s Testing, Conclusion, and Unambiguous Representation
`that Example 3 of EP ’406 Inherently Anticipates Claims Identical to the
`Form A Claims of the ’993 Patent. ...................................................................... 8 
`
`The EPO Accepted Nissan’s Showing that Example 3 Anticipates the
`Claims 1, 2 and 37 of the ’232 Application. ...................................................... 12 
`
`After Acquiring the ’232 Application, Nissan Argued that EP ’406 Could
`Not Anticipate Example 3—Precisely the Opposite of What Nissan Had
`Previously Insisted and Demonstrated. ............................................................. 13 
`
`The EPO Rejected Nissan’s Flip-Flop, and Reiterated that Example 3
`Anticipates the Original Claims. ......................................................................... 14 
`
`Nissan Gave Up on Disavowing Its Scientific Proof, But Misled the EPO
`in the Process. ....................................................................................................... 15 
`
`C. 
`
`Defendants’ Experts Confirmed that Example 3 of EP ’406 Anticipates the Form A
`Claims of the ’993 Patent. ................................................................................................. 16 
`
`1. 
`
`2. 
`
`Dr. Sessler Confirmed that Nissan Faithfully Followed Example 3. ............ 16 
`
`Dr. Roberts Confirmed that Nissan Obtained Form A from its Replications
`of Example 3. ........................................................................................................ 17 
`
`
`
`ii
`
`

`

`Case 1:14-cv-02758-PAC Document 138 Filed 02/21/17 Page 3 of 86
`
`D. 
`
`Plaintiffs Have Not Established Any Failure by Defendants to Prove Anticipation
`of Claims 1 and 22–25 by Clear and Convincing Evidence. ........................................ 18 
`
`1. 
`
`2. 
`
`3. 
`
`Dr. Byrn’s Untimely Theory Is Unsupported by the Record. ........................ 19 
`
`Dr. Byrn’s Theory Contradicts Plaintiffs’ FDA Communications and Dr.
`Byrn’s Own Patents. ............................................................................................. 26 
`
`The Court Does Not Accept Dr. Byrn’s Theory Based on Unpublished,
`Unverified, and Unreviewed Indian Patent Applications. .............................. 27 
`
`III. 
`
`PROPOSED CONCLUSIONS OF LAW REGARDING ANTICIPATION OF THE
`ASSERTED “FORM A CLAIMS” OF THE ’993 PATENT. ................................................ 28 
`
`A. 
`
`Legal Standards ................................................................................................................... 28 
`
`1. 
`
`2. 
`
`The Law of Anticipation...................................................................................... 28 
`
`The Admissibility, Reliability and Credibility of Expert Evidence. ............... 29 
`
`B. 
`
`Example 3 of EP ’406 Inherently Anticipates Claims 1 and 22-25 of the ’993
`Patent. .................................................................................................................................. 30 
`
`1. 
`
`2. 
`
`3. 
`
`4. 
`
`Nissan’s Own Scientific Conclusions and Representations to the European
`Patent Office: Unrebutted and Scientifically Confirmed. ............................... 31 
`
`Nissan’s Trial Evidence Does Not Refute Nissan’s Own Clear and
`Convincing Evidence of Anticipation. .............................................................. 34 
`
`There Is No Heightened Burden to Show Invalidity. ..................................... 40 
`
`EP ’406 Also Inherently Anticipates Claim 22. ................................................ 41 
`
`IV. 
`
`PROPOSED FINDINGS OF FACT REGARDING OBVIOUSNESS OF THE “FORM
`A” CLAIMS OF THE ’993 PATENT. ........................................................................................ 43 
`
`A. 
`
`B. 
`
`C. 
`
`D. 
`
`E. 
`
`The Person of Ordinary Skill in the Art of the ’993 Patent. ........................................ 43 
`
`Pitavastatin Calcium and Other Crystalline Statins Known in the Art ...................... 43 
`
`Motivation to Perform Routine Polymorph Screens on Prior Art Crystalline
`Pitavastatin Calcium. .......................................................................................................... 44 
`
`The Person of Ordinary Skill’s Reasonable Expectation that a Routine Polymorph
`Screen Would Produce the Polymorphs of Pitavastatin Calcium, Including
`Form A. ................................................................................................................................ 49 
`
`Form A of Pitavastatin Calcium Was Sufficiently Obvious as to Have Been
`Invented Nearly Simultaneously with the ’993 Patentee’s Conception of the
`Form. .................................................................................................................................... 50 
`
`iii
`
`

`

`Case 1:14-cv-02758-PAC Document 138 Filed 02/21/17 Page 4 of 86
`
`F. 
`
`It Was Well Known in the Art that a “Pharmaceutical Composition” Including
`“Pharmaceutically Acceptable Carriers” Was Necessary to Administer an “Effective
`Amount” of Prior Art Crystalline Pitavastatin Calcium. .............................................. 51 
`
`G. 
`
`Plaintiffs’ Alleged Secondary Considerations of Non-Obviousness. ......................... 52 
`
`1. 
`
`2. 
`
`3. 
`
`4. 
`
`5. 
`
`No Nexus Exists Between Any Alleged Secondary Consideration and the
`Patents-in-Suit. ...................................................................................................... 52 
`
`Livalo is Not a Commercial Success. ................................................................. 53 
`
`There was No Long-Felt, But Unmet Need for Livalo. ................................. 55 
`
`Plaintiffs Have Failed to Demonstrate Any Unexpected Results .................. 60 
`
`Plaintiffs’ Licensing Evidence Does Not Support Non-Obviousness. ........ 62 
`
`V. 
`
`PROPOSED CONCLUSIONS OF LAW REGARDING OBVIOUSNESS OF THE
`“FORM A CLAIMS” OF THE ’993 PATENT. ........................................................................ 63 
`
`A. 
`
`B. 
`
`Legal Standards ................................................................................................................... 63 
`
`Claims 1 and 23-25 of the ’993 Patent Are Obvious in Light of EP ’406 and the
`Prior Art. .............................................................................................................................. 66 
`
`1. 
`
`2. 
`
`3. 
`
`4. 
`
`The Level of Ordinary Skill in the Art ............................................................... 66 
`
`The Scope and Content of the Prior Art .......................................................... 66 
`
`Differences Between the Prior Art and Claims at Issue ................................. 66 
`
`Motivation to Combine the Teachings of Prior Art to Achieve the Claimed
`Invention, and Whether a Person of Ordinary Skill Would Have a
`Reasonable Expectation of Success in So Doing. ............................................ 67 
`
`5. 
`
`Alleged Secondary Considerations. .................................................................... 69 
`
`
`
`C. 
`
`Claim 22 of the ’993 Patent Is Obvious in Light of EP ’406 and the Prior Art. ...... 75 
`
`
`iv
`
`

`

`Case 1:14-cv-02758-PAC Document 138 Filed 02/21/17 Page 5 of 86
`
`TABLE OF AUTHORITIES
`
`
`
`Page(s)
`
`Cases
`
`In re ’639 Patent Litig.,
`154 F. Supp. 2d 157 (D. Mass. 2001), aff’d sub nom. Smithkline Beecham Corp. v.
`Copley Pharm., Inc., 45 F. App’x 915 (Fed. Cir. 2002) ..................................................................... 32, 33
`
`ABT Sys. and Univ. Central Fla. v. Emerson Elec.,
`797 F.3d 1350 (Fed. Cir. 2015) ......................................................................................................... 73, 74
`
`AEP Energy Servs. Gas Holding Co. v. Bank of Am., N.A.,
`626 F.3d 699 (2d Cir. 2010) ..................................................................................................................... 36
`
`Amorgianos v. Nat’l R.R. Passenger Corp.,
`303 F.3d 256 (2d Cir. 2002) .............................................................................................................. 30, 65
`
`Anderson News, LLC v. Am. Media, Inc.,
`No. 09 Civ. 2227 (PAC), 2015 WL 5003528 (S.D.N.Y. Aug. 20, 2015) (Crotty, J.) ................ 30, 65
`
`In re Antor Media Corp.,
`689 F.3d 1282 (Fed. Cir. 2012) ................................................................................................................ 63
`
`Astra Aktiebolag v. Andrx Pharm., Inc.,
`222 F. Supp. 2d 423 (S.D.N.Y. 2002)..................................................................................................... 32
`
`AstraZeneca AB v. Andrx Labs., LLC,
`Nos. 14-08030, 15-1057, 2017 WL 111928 (D.N.J. Jan. 11, 2017) .................................................... 67
`
`Asyst Techs., Inc. v. Emtrak, Inc.,
`544 F.3d 1310 (Fed. Cir. 2008) ......................................................................................................... 64, 69
`
`In re Baxter Travenol Labs.,
`952 F.2d 388 (Fed. Cir. 1991) .................................................................................................................. 72
`
`Bayer Healthcare Pharm., Inc. v. Watson Pharm., Inc.,
`713 F.3d 1369 (Fed. Cir. 2013) ................................................................................................................ 75
`
`Borsack v. Ford Motor Co.,
`No. 04 Civ. 3255 (PAC), 2007 WL 2142070 (S.D.N.Y. July 26, 2007) (Crotty, J.) .................. 30, 65
`
`Bristol-Myers Squibb Co. v. Teva Pharm. USA, Inc.,
`752 F.3d 967 (Fed. Cir. 2014) ........................................................................................................... 72, 73
`
`Brooks v. Outboard Marine Corp.,
`234 F.3d 89 (2d Cir. 2000) ....................................................................................................................... 34
`
`v
`
`

`

`Case 1:14-cv-02758-PAC Document 138 Filed 02/21/17 Page 6 of 86
`
`Brown v. 3M,
`265 F.3d 1349 (Fed. Cir. 2001) ................................................................................................................ 28
`
`Caldwell v. U.S.,
`481 F.2d 898 (Ct. Cl. 1973) ...................................................................................................................... 71
`
`Caterpillar Tractor Co. v. Berco, S.p.A.,
`714 F.2d 1110 (Fed. Cir. 1983) ................................................................................................................ 32
`
`In re Cavanagh,
`436 F.2d 491 (C.C.P.A. 1971) ........................................................................................................... 71, 72
`
`Cont’l Can Co. v. Monsanto Co.,
`948 F.2d 1264 (Fed. Cir. 1991) ................................................................................................................ 28
`
`Cucuras v. Sec’y of Dep’t of Health & Human Servs.,
`993 F.2d 1525 (Fed. Cir. 1993) ................................................................................................................ 36
`
`In re Cyclobenzaprine Hydrochloride Extended-Release Capsule Patent Litig.,
`676 F.3d 1063 (Fed. Cir. 2012) ................................................................................................................ 64
`
`Daubert v. Merrell Dow Pharm., Inc.,
`509 U.S. 579 (1993) ...................................................................................................................... 29, 30, 65
`
`Demarco Corp. v. F. Von Langsdorff Licensing Ltd.,
`851 F.2d 1387 (Fed. Cir. 1988) ................................................................................................................ 70
`
`Ecolochem, Inc. v. S. Cal. Edison Co.,
`227 F.3d 1361 (Fed. Cir. 2000), cert. denied, 532 U.S. 974 (2001) ........................................... 64, 69, 74
`
`Eli Lilly & Co. v. Zenith Goldline Pharm., Inc.,
`471 F.3d 1369 (Fed. Cir. 2006) ................................................................................................................ 28
`
`Envtl. Designs, Ltd. v. Union Oil Co. of Cal.,
`713 F.2d 693 (Fed. Cir. 1983) .................................................................................................................. 75
`
`In re Geisler,
`116 F.3d 1465 (Fed. Cir. 1997) ................................................................................................................ 73
`
`General Elec. Co. v. Joiner,
`522 U.S. 136 (1997) ............................................................................................................................ 30, 65
`
`Geo M Martin v. Alliance Mach.,
`618 F.3d 1294 (Fed. Cir. 2010) ................................................................................................................ 75
`
`In re Gershon,
`372 F.2d 535 (C.C.P.A. 1967) .................................................................................................................. 71
`
`vi
`
`

`

`Case 1:14-cv-02758-PAC Document 138 Filed 02/21/17 Page 7 of 86
`
`Glaxo Inc. v. Novopharm Ltd.,
`52 F.3d 1043 (Fed. Cir. 1995) .................................................................................................................. 33
`
`In re GPAC, Inc.,
`57 F.3d 1573 (Fed. Cir. 1995) .................................................................................................................. 70
`
`Graham v. John Deere Co.,
`383 U.S. 1 (1966) ....................................................................................................................................... 64
`
`Howmedica Osteonics Corp. v. Zimmer, Inc.,
`640 F. App’x 951 (Fed. Cir. 2016) .......................................................................................................... 33
`
`In re Huang,
`100 F.3d 135 (Fed. Cir. 1996) .................................................................................................................. 70
`
`Iron Grip Barbell Co. v. USA Sports, Inc.,
`392 F.3d 1317 (Fed. Cir. 2004) ......................................................................................................... 71, 73
`
`J.T. Eaton & Co. v. Atl. Paste & Glue Co.,
`106 F.3d 1563 (Fed. Cir. 1997) ................................................................................................................ 70
`
`Kansas Jack, Inc. v. Kuhn,
`719 F.2d 1144 (Fed. Cir. 1983) ................................................................................................................ 70
`
`Koa Corp. v. Unilever U.S., Inc.,
`441 F.3d 963 (Fed. Cir. 2006) .................................................................................................................. 72
`
`KSR Int’l Co. v. Teleflex Inc.,
`550 U.S. 398 (2007) ...................................................................................................................... 63, 66, 75
`
`Kumho Tire Co., Ltd. v. Carmichael,
`526 U.S. 137 (1999) ...................................................................................................................... 30, 34, 65
`
`Lindemann Maschinenfabrik GMBH v. Am. Hoist and Derrick Co.,
`730 F.2d 1452 (Fed. Cir. 1984) ................................................................................................................ 64
`
`Merck & Cie v. Watson Labs., Inc.,
`822 F.3d 1347 (Fed. Cir. 2016) ................................................................................................................ 36
`
`Microsoft Corp. v. i4i Ltd. P’ship,
`131 S. Ct. 2238 (2011) .............................................................................................................................. 29
`
`Minn. Mining & Mfg. Co. v. Johnson & Johnson Orthopedics, Inc.,
`976 F.2d 1559 (Fed. Cir. 1992) ................................................................................................................ 29
`
`Mintz v. Dietz & Watson, Inc.,
`679 F.3d 1372 (Fed. Cir. 2012) ................................................................................................................ 64
`
`vii
`
`

`

`Case 1:14-cv-02758-PAC Document 138 Filed 02/21/17 Page 8 of 86
`
`Newell Companies v. Kenney Mfg. Co.,
`864 F.2d 757 (Fed. Cir. 1988) ........................................................................................................... 71, 72
`
`In re Omeprazole Patent Litig.,
`483 F.3d 1364 (Fed. Cir. 2007) ......................................................................................................... 32, 37
`
`Ormco Corp. v. Align Tech., Inc.,
`463 F.3d 1299 (Fed. Cir. 2006) ......................................................................................................... 69, 70
`
`Orthopedic Equipment Co., Inc. v. All Orthopedic Appliances, Inc.,
`707 F.2d 1376 (Fed. Cir. 1983) ................................................................................................................ 71
`
`In re Paulsen,
`30 F.3d 1475 (Fed. Cir. 1994) .................................................................................................................. 70
`
`Perricone v. Medicis Pharm. Corp.,
`432 F.3d 1368 (Fed. Cir. 2005) ................................................................................................................ 28
`
`Pfizer, Inc. v. Apotex, Inc.,
`480 F.3d 1348 (Fed. Cir. 2007) ................................................................................................................ 63
`
`Power-One, Inc. v. Artesyn Techs., Inc.,
`599 F.3d 1343 (Fed. Cir. 2011) ................................................................................................................ 74
`
`PowerOasis, Inc. v. T-Mobile USA, Inc.,
`522 F.3d 1299 (Fed. Cir. 2008) ................................................................................................................ 40
`
`Purdue Pharma Prods. L.P. v. Par Pharm., Inc.,
`377 Fed. App’x 978 (Fed. Cir. 2010) ...................................................................................................... 75
`
`Sciele Pharma Inc. v. Andrx Corp.,
`684 F.3d 1253 (Fed. Cir. 2012) ................................................................................................................ 29
`
`Sheehan v. Daily Racing Form, Inc.,
`104 F.3d 940 (7th Cir 1997) ..................................................................................................................... 34
`
`SIBIA Neurosciences, Inc. v. Cadus Pharm. Corp.,
`225 F.3d 1349 (Fed. Cir 2000) ................................................................................................................. 73
`
`Sjolund v. Musland,
`847 F.2d 1573 (Fed. Cir. 1988) ................................................................................................................ 71
`
`Sparton Corp. v. United States,
`89 Fed. Cl. 196 (Ct. Cl. 2009) .................................................................................................................. 70
`
`Tanabe Seiyaku Co., Ltd. v. U.S. Intern. Trade Comm’n,
`109 F.3d 726 (Fed. Cir. 1997) .................................................................................................................. 31
`
`viii
`
`

`

`Case 1:14-cv-02758-PAC Document 138 Filed 02/21/17 Page 9 of 86
`
`Therasense, Inc. v. Becton, Dickinson & Co.,
`593 F.3d 1289 (Fed. Cir. 2010) ................................................................................................................ 69
`
`Titanium Metals Corp. of Am. v. Banner,
`778 F.2d 775 (Fed. Cir. 1985) .................................................................................................................. 28
`
`Tokai Corp. v. Easton Enterprises,
`632 F.3d 1358 (Fed. Cir. 2011) ................................................................................................................ 64
`
`Turpin v. Merrell Dow Pharm., Inc.,
`959 F.2d 1349 (6th Cir. 1992) ................................................................................................................. 34
`
`UBS AG v. HealthSouth Corp.,
`645 F. Supp. 2d 135 (S.D.N.Y. 2008)..................................................................................................... 36
`
`Vulcan Eng’g Co. v. Fata Aluminum Inc.,
`278 F.3d 1366 (Fed. Cir. 2002) ................................................................................................................ 74
`
`Wm. Wrigley Jr. Co. v. Cadbury Adams USA LLC,
`683 F.3d 1356 (Fed. Cir. 2012) ................................................................................................................ 64
`
`Statutes
`
`35 U.S.C. § 102 ............................................................................................................................................. 1, 28
`
`35 U.S.C. § 103 ................................................................................................................................................... 2
`
`Other Authorities
`
`Fed. R. Evid. 702(c) .................................................................................................................................. 29, 65
`
`Fed. R. Civ. P. 26 ...................................................................................................................................... 35, 37
`
`ix
`
`

`

`Case 1:14-cv-02758-PAC Document 138 Filed 02/21/17 Page 10 of 86
`
`I.
`
`INTRODUCTION
`1.
`
`This is a patent infringement case under the Hatch-Waxman Act. Plaintiff-patentee
`
`Nissan Chemical Industries, Ltd. (“Nissan”) sued defendants Apotex, Inc. and Apotex Corp.
`
`(collectively, “Apotex”) and Amneal Pharmaceuticals, LLC (“Amneal”) for infringement of U.S.
`
`Patent No. 8,557,993 (“the ’993 patent”), based on defendants having each filed Abbreviated New
`
`Drug Applications (“ANDAs”) with the Food and Drug Administration (“FDA”). Plaintiffs Kowa
`
`Company, Ltd. and Kowa Pharmaceuticals America, Inc. (“Kowa”) are licensees of Plaintiff Nissan
`
`Chemical Industries, Ltd (“ Nissan”), and the owners of the New Drug Application (“NDA”) for
`
`pitavastatin calcium tablets sold under the tradename Livalo®, which allegedly is or contains an
`
`embodiment of the invention claimed in the ’993 patent. By their respective ANDAs, Amneal and
`
`Apotex each seek FDA approval to market lower cost pitavastatin calcium tablets to compete with
`
`Livalo®. As authorized by the Hatch-Waxman Act, Amneal and Apotex each included in their
`
`respective ANDAs a certification that their proposed ANDA products would not infringe any valid
`
`claim of the ’993 patent, and served notice of the same on Plaintiffs.
`
`2.
`
`Plaintiffs then sued within the statutory period, availing themselves of the Hatch-
`
`Waxman Act’s automatic 30-month stay of FDA approval of Amneal’s and Apotex’s respective
`
`ANDAs. If you credit Plaintiffs’ testimony about Livalo® revenues, this two-and-a-half year period
`
`of no competition was worth approximately $500 million of sales at patent-protected prices.
`
`3.
`
`This Court held a 10-day bench trial on January 17–30, 2017, and held closing
`
`arguments on February 3, 2017. As explained below, the Court finds that Amneal and Apotex have
`
`proven by clear and convincing evidence that Example 3 of EP ’406 inherently anticipates claims 1
`
`and 22–25 of the ’993 patent. Accordingly, the Court concludes that claims 1 and 22–25 of the ’993
`
`patent are invalid under 35 U.S.C. § 102(b).
`
`4.
`
`The Court also finds that Amneal and Apotex have proven by clear and convincing
`
`1
`
`

`

`Case 1:14-cv-02758-PAC Document 138 Filed 02/21/17 Page 11 of 86
`
`evidence that claim 1 and 22–25 are obvious in light of EP ’406 and the prior art. Accordingly, the
`
`Court concludes that claims 1 and 22–25 of the ’993 patent are invalid under 35 U.S.C. § 103.
`
`II.
`
`PROPOSED FINDINGS OF FACT REGARDING ANTICIPATION OF THE
`“FORM A” CLAIMS OF THE ’993 PATENT
`A.
`
`Background
`1. The ’993 Patent
`
`5.
`
`The ’993 patent relates to “crystalline forms and the amorphous form of Pitavastatin
`
`calcium, processes for the preparation thereof and pharmaceutical compositions comprising these
`
`forms.” (DTX-0059 at 1:17-20.) The ’993 patent discloses that “Pitavastatin calcium is known by
`
`the chemical name: (3R,5S)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]-3,5-dihydroxy-6(E)-
`
`heptenoic acid hemicalcium salt.” (Id. at 1:24-26.) The phrase “pitavastatin calcium” means the
`
`same thing as the phrase “pitavastatin hemicalcium.”
`
`6.
`
`The ’993 patent issued on October 15, 2013, from U.S. Patent Application No.
`
`13/664,498 (“the ’498 application”), which was filed on October 31, 2012. The ’993 patent claims
`
`priority to PCT Application No. PCT/EP2004/050066, which was assigned European Patent
`
`Application No. 04707232.7 (“the ’232 Application”). The ’232 Application is a counterpart to the
`
`’498 application. Consequently, the specifications or disclosures of both applications are identical.
`
`7.
`
`The earliest priority date to which the ’993 patent claims entitlement is February 12,
`
`2003. The assignee and owner of the ’993 patent is Plaintiff Nissan.
`
`2. Asserted “Form A Claims” of the ’993 Patent
`
`8.
`
`Nissan asserts claims 1 and 22-25 against Amneal and Apotex. Each of these claims
`
`is directed to the “crystalline polymorph A” of pitavastatin calcium. Although claims 1, 22, and 23
`
`also claim other forms of pitavastatin calcium, Nissan asserts that infringement of these claims by
`
`Amneal and Apotex solely on the basis that the ANDA products contain “crystalline polymorph A”
`
`of pitavastatin calcium. The other forms claimed in claims 1, 22, and 23 are not discussed further
`
`2
`
`

`

`Case 1:14-cv-02758-PAC Document 138 Filed 02/21/17 Page 12 of 86
`
`herein. Accordingly, for simplicity, claims 1 and 22-25 are referred to herein as the “Form A
`
`Claims.”
`
`9.
`
`Claims 1, 22 and 24 claim Form A of pitavastatin hemicalcium salt as “polymorph A
`
`which exhibits a characteristic X-ray powder diffraction pattern with characteristic peaks expressed
`
`in 2θ at 5.0 (s), 6.8 (s), 9.1 (s), 10.0 (w), 10.5 (m), 11.0 (m), 13.3 (vw), 13.7 (s), 14.0 (w), 14.7 (w), 15.9
`
`(vw), 16.9 (w), 17.1 (vw), 18.4 (m), 19.1 (w), 20.8 (vs), 21.1 (m), 21.6 (m), 22.9 (m), 23.7 (m), 24.2 (s),
`
`25.2 (w), 27.1 (m), 29.6 (vw), 30.2 (w), 34.0 (w)” wherein “(vs) stands for very strong intensity; (s)
`
`stands for strong intensity; (m) stands for medium intensity; (w) stands for weak intensity; (vw)
`
`stands for very weak intensity.”
`
`
`
`1. A crystalline polymorph A, B, C, D, E, F, or the amorphous form,
`of [pitavastatin calcium] salt wherein
`A) polymorph A exhibits a characteristic X-ray powder diffraction
`pattern with characteristic peaks expressed in 2θ at 5.0 (s), 6.8 (s),
`9.1 (s), 10.0 (w), 10.5 (m), 11.0 (m), 13.3 (vw), 13.7 (s), 14.0 (w),
`14.7 (w), 15.9 (vw), 16.9 (w), 17.1 (vw), 18.4 (m), 19.1 (w), 20.8
`(vs), 21.1 (m), 21.6 (m), 22.9 (m), 23.7 (m), 24.2 (s), 25.2 (w), 27.1
`(m), 29.6 (vw), 30.2 (w), and 34.0 (w) . . . wherein, for each of said
`polymorphs, (vs) stands for very strong intensity; (s) stands for
`strong intensity; (m) stands for medium intensity; (w) stands for
`weak intensity; (vw) stands for very weak intensity.
`22. A pharmaceutical composition comprising an effective amount
`of the crystalline polymorph or amorphous form according to
`claim 1, and a pharmaceutically acceptable carrier.
`24. A crystalline polymorph A of [pitavastatin calcium] salt, which
`exhibits a characteristic X-ray powder diffraction pattern with
`characteristic peaks expressed in 2θ at 5.0 (s), 6.8 (s), 9.1 (s), 10.0
`(w), 10.5 (m), 11.0 (m), 13.3 (vw), 13.7 (s), 14.0 (w), 14.7 (w),
`15.9 (vw), 16.9 (w), 17.1 (vw), 18.4 (m), 19.1 (w), 20.8 (vs), 21.1
`(m), 21.6 (m), 22.9 (m), 23.7 (m), 24.2 (s), 25.2 (w), 27.1 (m), 29.6
`(vw), 30.2 (w), and 34.0 (w), wherein (vs) stands for very strong
`intensity; (s) stands for strong intensity; (m) stands for medium
`intensity; (w) stands for weak intensity; (vw) stands for very weak
`intensity.
`
`(DTX-0059 at 10:50–11:37; 13:7–10; 13:26–37 (emphasis added).)
`
`3
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`

`

`Case 1:14-cv-02758-PAC Document 138 Filed 02/21/17 Page 13 of 86
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`10.
`
`Claims 23 and 25 claim Form A of Pitavastatin calcium as the Form A of claim 1
`
`which also has “an X-ray powder diffraction substantially as depicted in FIG. 1” of the ’993 patent
`
`(Claim 23), or simply the Form A of pitavastatin calcium which has the same X-ray powder
`
`diffraction (Claim 25).
`
`23. A crystalline polymorph A, B, C, D, E, E, or the amorphous
`form of [pitavastatin calcium] salt of claim 1, wherein polymorph
`A has an X-ray powder diffraction pattern substantially as
`depicted in FIG. 1 . . ..
`25. A crystalline polymorph A of [pitavastatin calcium] salt, having
`an X-ray powder diffraction substantially as depicted in FIG. 1.
`
`(DTX-0059 at 13:11–25 and 13:38–41.) Figure 1 is reproduced below:
`
`
`
`(DTX-0059 at Fig. 1.)
`
`3. The Specification of the ’993 Patent
`
`11.
`
`The specification of the ’993 Patent was copied almost in its entirety from a report of
`
`a routine polymorph screen prepared for Ciba by a contract laboratory called Solvias. (Tr. at
`
`799:16–800:7.) All nine figures and six tables of the ’993 patent were copied directly from the
`
`4
`
`

`

`Case 1:14-cv-02758-PAC Document 138 Filed 02/21/17 Page 14 of 86
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`contract laboratory report. All nine examples in the ’993 patent also were copied, with some
`
`simplification, from the report. (Tr. at 805:25–810:2 (comparing DTX-0351 with DTX-0059).)
`
`12.
`
`The specification discloses that pitavastatin calcium, and processes for its
`
`preparation, were known in the art by 2003. (DTX-0059 at 1:43–67.) For example, the ’993 patent
`
`discloses:
`
`A full synthetic procedure for the preparation of Pitavastatin calcium
`is described in EP-A-0520406. In the process described in this patent
`Pitavastatin calcium is obtained by precipitation from an aqueous
`solution as a white crystalline material with a melting point of 190-
`192 C.
`
`(Id. at 1:62–67.)
`13.
`European Patent Application EP-A-0520406 (“EP ’406”), referenced in the ’993
`
`patent above, was filed by Nissan back in 1992. As set forth in detail below, Nissan eventually
`
`insisted and demonstrated to the European Patent Office that EP ’406 inherently anticipated claims
`
`of the ’232 Application that were identical to the claims of the ’993 patent asserted here against
`
`Amneal and Apotex.
`
`14.
`
`The specification also discloses that “[i]t is known that pharmaceutical substances
`
`can exhibit polymorphism,” which it defines as “the ability of any substance to have two or more
`
`different crystal structures.” (DTX-0059 at 1:67–2:3.)
`
`15.
`
`The ’993 pate