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`UNITED STATES PATENT AND TRADEMARK OFFICE
`_________________________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`_________________________
`
`SUN PHARMACEUTICAL INDUSTRIES LTD.
`Petitioner,
`v.
`MERCK SHARP & DOHME CORP.
`Patent Owner.
`_________________________
`Case IPR2020-01072
`Patent No. 7,326,708
`_________________________
`
`PETITION FOR INTER PARTES REVIEW
`
`
`Mail Stop PATENT BOARD
`Patent Trial and Appeal Board
`U.S. Patent and Trademark Office
`P.O. Box 1450
`Alexandria, VA 22313-1450
`Submitted Electronically via the PTAB E2E System
`
`
`
`

`

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`IPR2020-01072 (7,326,708)
`
`TABLE OF CONTENTS
`
`I.
`
`INTRODUCTION ............................................................................................... 1
`
`II. OVERVIEW ....................................................................................................... 1
`
`III. STANDING (37 C.F.R. § 42.104(A)); PROCEDURAL STATEMENTS ..... 5
`
`IV. MANDATORY NOTICES (37 C.F.R. § 42.8(A)(1)) ..................................... 6
`
`A. Each Real Party in Interest (37 C.F.R. § 42.8(b)(1)) ....................................... 6
`
`B. Notice of Related Matters (37 C.F.R. § 42.8(b)(2)) ........................................ 6
`
`1. Judicial Matters Involving the ʼ708 Patent .................................................. 6
`
`2. Administrative Matters ................................................................................. 7
`
`C. Designation of Lead and Back-Up Counsel and Service (37 C.F.R. §§
`42.8(b)(3), 42.8(b)(4)) ............................................................................................ 8
`
`V. STATEMENT OF THE PRECISE RELIEF REQUESTED AND THE
`REASONS THEREFOR (37 C.F.R. § 42.22(A)) ...................................................... 9
`
`VI. THE ʼ708 PATENT ......................................................................................... 9
`
`VII. CLAIM CONSTRUCTION .......................................................................... 11
`
`VIII. PERSON OF ORDINARY SKILL IN THE ART (“POSA”) ....................... 11
`
`IX.
`
`IDENTIFICATION OF CHALLENGE (37 C.F.R. § 42.104(B)) ................ 12
`
`X. INVALIDITY ANALYSIS ............................................................................... 13
`
`A. Ground 1: Claims 1-3, 17, 19, and 21-23 Are Anticipated by WO ʼ498 ...... 13
`
`1. Disclosure of WO ʼ498 .............................................................................. 14
`
`2. Claim 1 ....................................................................................................... 17
`
`3. Claim 2 ....................................................................................................... 25
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`IPR2020-01072 (7,326,708)
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`4. Claim 3 ....................................................................................................... 25
`
`5. Claim 17 ..................................................................................................... 26
`
`a) A pharmaceutical composition comprising .......................................... 26
`
`a therapeutically effective amount of the salt according to
`b)
`claim 2 ............................................................................................................ 27
`
`in association with one or more pharmaceutically acceptable
`c)
`carriers. .......................................................................................................... 27
`
`6. Claim 19 ..................................................................................................... 28
`
`a) A method for the treatment of type 2 diabetes comprising .................. 28
`
`administering to a patient in need of such treatment a
`b)
`therapeutically effective amount of the salt according to claim 2
`or a hydrate thereof. ....................................................................................... 28
`
`7. Claims 21-22 .............................................................................................. 28
`
`8. Claim 23 ..................................................................................................... 31
`
`B. Ground 2: Claims 1-3, 17, 19 and 21-23 Are Anticipated by
`the ʼ871 Patent ...................................................................................................... 31
`
`1. Disclosure of the ʼ871 Patent ..................................................................... 31
`
`2. Claims 1 and 2 ............................................................................................ 33
`
`3. Claim 3 ....................................................................................................... 34
`
`4. Claims 17 and 19 ........................................................................................ 35
`
`5. Claims 21-23 .............................................................................................. 37
`
`C. Ground 3: Claims 3, 17, 19, and 21-23 Would Have Been
`Obvious in View of WO ʼ498 .............................................................................. 39
`
`1. The Level of Ordinary Skill in the Pertinent Art ....................................... 39
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`IPR2020-01072 (7,326,708)
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`2. The Scope and Content of the Prior Art ..................................................... 39
`
`a) WO ʼ498 (EX1004) ............................................................................... 39
`
`b) Claim 3 .................................................................................................. 40
`
`c) Claim 17 ................................................................................................ 42
`
`(1) A pharmaceutical composition comprising ....................................... 42
`
`(2) a therapeutically effective amount of the salt
`according to claim 2 ................................................................................... 42
`
`in association with one or more pharmaceutically
`(3)
`acceptable carriers. ..................................................................................... 43
`
`d) Claim 19 ................................................................................................ 43
`
`(1) A method for the treatment of type 2 diabetes comprising ............... 43
`
`(2) administering to a patient in need of such treatment
`a therapeutically effective amount of the salt according to
`claim 2 or a hydrate thereof. ...................................................................... 43
`
`e) Claims 21-23 ......................................................................................... 44
`
`D. Ground 4: Claims 1-3, 17, 19, and 21-23 Would Have Been
`Obvious in View of WO ʼ498 and Bastin ............................................................ 46
`
`1. The Level of Ordinary Skill in the Pertinent Art ....................................... 46
`
`2. The Scope and Content of the Prior Art ..................................................... 47
`
`a) WO ʼ498 (EX1004) ............................................................................... 47
`
`b) Bastin (EX1006) ................................................................................... 47
`
`3. The Differences Between the Claims and Prior Art .................................. 48
`
`a) Claim 1 .................................................................................................. 48
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`IPR2020-01072 (7,326,708)
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`(1) There Is No Requirement to Select a Lead
`Compound in Salt Selection Cases ............................................................ 48
`
`(2) WO ʼ498 and Bastin Would Have Rendered the
`Phosphoric Acid Salt Obvious ................................................................... 51
`
`b) Claims 2 and 3 ....................................................................................... 57
`
`c) Claims 17 and 19 ................................................................................... 57
`
`d) Claims 21-23 ......................................................................................... 58
`
`E. Ground 5: Claim 4 Would Have Been Obvious in View
`of WO ʼ498, Bastin and Brittain........................................................................... 59
`
`1. The Level of Ordinary Skill in the Pertinent Art ....................................... 59
`
`2. The Scope and Content of the Prior Art ..................................................... 60
`
`a) WO ʼ498 (EX1004) and Bastin (EX1006) ........................................... 60
`
`b) Brittain (EX1005) ................................................................................. 60
`
`3. The Differences Between the Claim and Prior Art .................................... 61
`
`F. Ground 6: Claim 4 Would Have Been Obvious in View
`of WO ʼ498 and Brittain ....................................................................................... 62
`
`1. The Level of Ordinary Skill in the Pertinent Art ....................................... 62
`
`2. The Scope and Content of the Prior Art ..................................................... 62
`
`a) WO ʼ498 (EX1004) and Brittain (EX1005) ......................................... 62
`
`3. The Differences Between the Claim and Prior Art .................................... 62
`
`G. Secondary Considerations of Nonobviousness ............................................. 64
`
`XI. THE BOARD SHOULD INSTITUTE TRIAL BASED
`ON SUN’S PETITION (35 U.S.C. § 325(D) OR § 314(A)) ................................... 67
`
`XII. CONCLUSION .............................................................................................. 70
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`IPR2020-01072 (7,326,708)
`
`TABLE OF AUTHORITIES
`
`Page(s)
`
`Cases
`Acorda Therapeutics Inc. v. Roxane Laboratories, Inc.,
`903 F.3d 1310 (Fed. Cir. 2018) .......................................................................... 66
`Amgen Inc. v. Alexion Pharmaceuticals Inc.,
`IPR2019-00740, Paper 15 (P.T.A.B. Aug. 20, 2019) ................................... 67, 69
`Amgen Inc. v. F. Hoffmann-La Roche Ltd.,
`580 F.3d 1340 (Fed. Cir. 2009) .............................................................. 30, 38, 46
`Amneal Pharm. LLC v. Purdue Pharma L.P.,
`IPR2016-01412, Paper 9 (P.T.A.B. Feb. 14, 2017) ............................................ 49
`Amneal Pharmaceuticals, LLC v. Supernus Pharmaceuticals, Inc.,
`IPR2013-00368, Paper 8 (P.T.A.B. Dec. 2013) ................................................. 64
`Amneal Pharms. LLC v. Hospira, Inc.,
`IPR2016-01577, Paper 11 (P.T.A.B. at Feb. 9, 2017) ........................................ 65
`Apotex Inc. v. UCB Biopharma SPRL,
`IPR2019-00400, Paper 17 (P.T.A.B. July 15, 2019) .......................................... 68
`Associated British Foods, PLC v. Cornell Research Foundation Inc.,
`IPR2019-00578, Paper 25 (P.T.A.B July 25, 2019) ............................... 15, 32, 33
`Bayer Pharma AG v. Watson Laboratories, Inc.,
`874 F.3d 1316 (Fed. Cir. 2017) .......................................................................... 49
`Bayer Schering Pharma AG v. Barr Laboratories,
`575 F.3d 1341 (Fed. Cir. 2008) .......................................................................... 56
`Becton, Dickinson and Company v. B. Braun Melsungen AG,
`IPR2017-01586, slip op. (P.T.A.B. Dec. 15, 2017) ............................................ 67
`Boston Scientific Scimed, Inc. v. Cordis Corp.,
`554 F.3d 982 (Fed. Cir. 2009) ............................................................................ 42
`Bristol-Myers Squibb Co. v. Ben Venue Labs., Inc.,
`246 F.3d 368 (Fed. Cir. 2001) ...................................................................... 13, 14
`
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`Celanese Int’l Corp. v. Daicel Corp.,
`IPR2017-00163, Paper 46 (P.T.A.B. May 3, 2018) ........................................... 49
`Cohesive Techs., Inc. v. Waters Corp.,
`543 F.3d 1351 (Fed. Cir. 2008) .......................................................................... 64
`Constant v. Advanced Micro-Devices, Inc.,
`848 F.2d 1560 (Fed. Cir. 1988) ...................................................................... 2, 51
`Custom Accessories, Inc. v. Jeffrey-Allan Indus., Inc.,
`807 F.2d 955 (Fed. Cir. 1986) ............................................................................ 11
`Dr. Falk Pharma GmbH v. GeneriCo, LLC,
`2019 WL 2452362 (Fed. Cir. June 12, 2019) ..................................................... 65
`Dr. Reddy's Laboratories, Inc. et al v. Merck Sharp & Dohme Corp.,
`IPR2020-01060 (P.T.A.B.) ................................................................................... 8
`Glaxo Group Ltd. v. Apotex, Inc.,
`376 F.3d 1339 (Fed. Cir. 2004) .................................................................... 19, 34
`Gnosis SPA v. South Alabama Medical Science Foundation,
`IPR2013-00116, Paper 68 (P.T.A.B. June 20, 2014) ......................................... 49
`Google Inc. v. Jongerius Panoramic Techs, LLC,
`IPR2013-00191, Paper 70 (P.T.A.B. Aug. 12, 2014) ................................... 14, 61
`Graham v. John Deere Co. of Kansas City,
`383 U.S. 1 (1966) ................................................................................................ 39
`Greenliant Sys., Inc. v. Xicor LLC,
`692 F.3d 1261 (Fed. Cir. 2012) .................................................................... 30, 38
`Grunenthal GMBH v. Alkem Labs. Ltd.,
`919 F.3d 1333 (Fed. Cir. 2019) .................................................................... 55, 56
`In re Aller,
`220 F.2d 454 (C.C.P.A. 1955) ...................................................................... 44, 55
`In re Cyclobenzaprine Hydrochloride,
`676 F.3d 1063 (Fed. Cir. 2012) .......................................................................... 56
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`IPR2020-01072 (7,326,708)
`
`In re Fong,
`378 F.2d 977 (CCPA 1967) ................................................................................ 32
`In re Fout,
`675 F.2d 297 (C.C.P.A. 1982) ...................................................................... 51, 54
`In re Gleave,
`560 F.3d 1331 (Fed. Cir. 2009) .......................................................................... 24
`In re Graves,
`69 F.3d 1147 (Fed. Cir. 1995) ............................................................................ 13
`Iron Grip Barbell Co., Inc. v. USA Sports, Inc.,
`392 F.3d 1317 (Fed. Cir. 2004) .......................................................................... 66
`In re Harris,
`409 F.3d 1339 (Fed. Cir. 2005) .......................................................................... 66
`In re Nomiya,
`509 F.2d 566 (C.C.P.A. 1975) ............................................................................ 51
`In re O’Farrell,
`853 F.2d 894 (Fed. Cir. 1988) ............................................................................ 39
`In re Peterson,
`315 F.3d 1325 (Fed. Cir. 2003) .......................................................................... 45
`In re Preda,
`401 F.2d 825 (C.C.P.A. 1968) ............................................................................ 13
`In re Sitagliptin Phosphate (ʼ708 & ʼ921) Patent Litigation,
`C.A. No. 19-md-2902 (D. Del.) ............................................................................ 7
`In re Thorpe,
`777 F.2d 695 (Fed. Cir. 1985) ...................................................................... 30, 38
`In re Wesslau,
`353 F.2d 238 (C.C.P.A. 1965) ............................................................................ 39
`In re Williams,
`36 F.2d 436 (C.C.P.A. 1929) .............................................................................. 66
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`Kao Corp. v. Unilever United States, Inc.,
`441 F.3d 963 (Fed. Cir. 2006) ............................................................................ 66
`Kashiv Biosciences, LLC v. Amgen Inc.,
`IPR2019-00791, Paper 15 (P.T.A.B. Sept. 11, 2019) ......................................... 68
`Kennametal, Inc. v. Ingersoll Cutting Tool Co.,
`780 F.3d 1376 (Fed. Cir. 2015) .............................................................. 13, 22, 23
`KSR Int’l Co. v. Teleflex, Inc.,
`550 U.S. 398 (2007) ............................................................................................ 11
`Merck Sharp & Dohme Corp. v. Accord Healthcare, Inc.,
`1:19-cv-02192 (D. Del.) ........................................................................................ 7
`Merck Sharp & Dohme Corp. v. Anchen Pharmaceuticals, Inc. et al.,
`1:19-cv-00311 (D. Del.) ........................................................................................ 6
`Merck Sharp & Dohme Corp. v. Apotex Inc. et al.,
`1:19-cv-00313 (D. Del.) ........................................................................................ 6
`Merck Sharp & Dohme Corp. v. Apotex Inc.,
`1:20-cv-00749 (D. Del.) ........................................................................................ 7
`Merck Sharp & Dohme Corp. v. Lupin Ltd. et al.,
`1:19-cv-00347 (D. Del.) ........................................................................................ 7
`Merck Sharp & Dohme Corp. v. Lupin Ltd.,
`1:20-cv-00776 (D. Del.) ........................................................................................ 7
`Merck Sharp & Dohme Corp. v. Macleods Pharmaceuticals, Ltd. et al.,
`1:19-cv-00316 (D. Del.) ........................................................................................ 6
`Merck Sharp & Dohme Corp. v. Mylan Pharmaceuticals Inc. et al.,
`1:19- cv-01489 (D. Del.) ....................................................................................... 7
`Merck Sharp & Dohme Corp. v. Mylan Pharmaceuticals Inc. et al.,
`1:19-cv-00101 (N.D. W. Va.) ............................................................................... 6
`Merck Sharp & Dohme Corp. v. Sandoz, Inc.,
`1:19-cv-00312 (D. Del.) ........................................................................................ 6
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`Merck Sharp & Dohme Corp. v. Sun Pharmaceutical Industries Ltd.,
`1:19-cv-00319 (D. Del.) ........................................................................................ 6
`Merck Sharp & Dohme Corp. v. Teva Pharmaceuticals USA, Inc.,
`1:19-cv-00318 (D. Del.) ........................................................................................ 6
`Merck Sharp & Dohme Corp. v. Torrent Pharmaceuticals Limited et al.,
`1:19-cv-00320 (D. Del.) ........................................................................................ 7
`Merck Sharp & Dohme Corp. v. Torrent Pharmaceuticals Limited et al.,
`1:19-cv-00872 (D. Del.) ........................................................................................ 7
`Merck Sharp & Dohme Corp. v. Watson Pharmaceuticals, Inc. et al.,
`1:19-cv-00317 (D. Del.) ........................................................................................ 6
`Merck Sharp & Dohme Corp. v. Wockhardt Bio AG et al.,
`1:19-cv-00321 (D. Del.) ........................................................................................ 7
`Merck Sharp & Dohme Corp. v. Zydus Pharmaceuticals (USA) Inc. et al.,
`1:19-cv-00314 (D. Del.) ........................................................................................ 6
`Modernatx Inc. v. Curevac AG,
`IPR2017-02194, Paper 45 (P.T.A.B. April 16, 2019) ........................................ 66
`Mylan Pharmaceuticals Inc. et al. v. UCB Pharma GMBH,
`IPR2016-00510, Paper No. 45 (P.T.A.B. July 19, 2017) ....................... 50, 55, 56
`Mylan Pharmaceuticals Inc. v. Cosmo Technologies Ltd.,
`IPR2017-01035, Paper 17 (P.T.A.B. Sept. 21, 2017) ......................................... 14
`Mylan Pharmaceuticals Inc. v. Sanofi-Aventis Deutschland GMBH,
`IPR2018-01680, Paper 22 (P.T.A.B. Apr. 3, 2019) ..................................... 68, 69
`Mylan Pharmaceuticals Inc. v. Merck Sharp & Dohme Corp.,
`IPR2020-00040 (P.T.A.B.) ....................................................................... 7, 67, 71
`Newell Cos., Inc. v. Kenney Mfg. Co.,
`864 F.2d 757 (Fed. Cir. 1988) ............................................................................ 64
`NHK Spring Co., Ltd. v. Intri-Plex Techs., Inc.,
`Case IPR2018-00752, Paper 8 (P.T.A.B. Sept. 12, 2018) ............................ 68, 69
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`One World Technologies Inc. v. The Chamberlain Group Inc.,
`IPR2017-00126, Paper 67 (P.T.A.B. Apr. 4, 2019) ....................................passim
`Otsuka Pharm. Co. v. Sandoz, Inc.,
`678 F.3d 1280 (Fed. Cir. 2012) .......................................................................... 49
`Perricone v. Medicis Pharmaceuticals Corp.,
`432 F.3d 1368 (Fed. Cir. 2005) .......................................................................... 18
`Pfizer, Inc. v. Apotex, Inc.,
`480 F.3d 1348 (Fed. Cir. 2007) ...................................................................passim
`PharmaStem Therapeutics, Inc. v. ViaCell, Inc.,
`491 F.3d 1342 (Fed. Cir. 2007) ............................................................................ 2
`Phillips v. AWH Corp.,
`415 F.3d 1303 (Fed. Cir. 2005) (en banc) .......................................................... 10
`Provepharm Inc. v. Wista Laboratories Ltd.,
`IPR2018-00182, Paper 16 (P.T.A.B. July 5, 2018) ............................................ 15
`Purdue Pharma Prods. L.P. v. Par Pharm., Inc.,
`377 F. App’x 978 (Fed. Cir. 2010) ..................................................................... 64
`Quanergy Systems, Inc. v. Velodyne Lidar, Inc.,
`IPR2018-00256, Paper 14 (P.T.A.B. May 25, 2018) ......................................... 64
`Rasmusson v. SmithKline Beecham Corp.,
`413 F.3d 1318 (Fed. Cir. 2005) .......................................................................... 14
`Realtime Data, LLC v. Iancu,
`912 F.3d 1368 (Fed. Cir. 2019) .......................................................................... 39
`Sandoz Inc. v. Pharmacylics LLC,
`IPR2019-00865, Paper 8 (P.T.A.B. Sept. 26, 2019) ........................................... 69
`Sinclair & Carroll Co. v. Interchemical Corp.,
`325 U.S. 327 (1945) ............................................................................................ 24
`Sjolund v. Musland,
`847 F.2d 1573 (Fed. Cir. 1988) ............................................................................ 2
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`IPR2020-01072 (7,326,708)
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`Spezialpräparate mbH,
`IPR2016-01370, Paper 13 (P.T.A.B. Feb. 8, 2017) ............................................ 64
`Teva Pharmaceuticals USA, Inc. et al v. Merck Sharp & Dohme Corp.,
`IPR2020-01045 (P.T.A.B.) ................................................................................... 7
`Titanium Metals Corp. of America v. Banner,
`778 F.2d 775 (Fed. Cir. 1985) ............................................................................ 45
`Valve Corp. v. Elec. Scripting Prods., Inc.,
`IPR2019-00062, -00063, -00084 ........................................................................ 68
`Warner Chilcott Co. v. Teva Pharmaceuticals USA,
`89 F. Supp. 3d 641 (D.N.J. 2015) ....................................................................... 22
`Watson Labs., Inc. v. United Therapeutics Corp.,
`IPR2017-01621, Paper 10 (P.T.A.B. Jan. 11, 2018) .......................................... 32
`Statutes
`35 U.S.C. § 102 ............................................................................................ 10, 12, 15
`35 U.S.C. § 102(a) ............................................................................................... 2, 14
`35 U.S.C. § 102(b) ............................................................................................. 47, 60
`35 U.S.C. § 102(e)(2) ......................................................................................... 15, 32
`35 U.S.C. § 325(d) ............................................................................................. 67, 69
`Other Authorities
`37 C.F.R. § 41.10(b) .................................................................................................. 8
`37 C.F.R. § 42.6(d) .................................................................................................. 12
`37 C.F.R. § 42.6(e) ................................................................................................... 71
`37 C.F.R. § 42.8(a)(1) ................................................................................................ 6
`37 C.F.R. § 42.8(b)(1) ................................................................................................ 6
`37 C.F.R. § 42.8(b)(3) ................................................................................................ 7
`37 C.F.R. § 42.8(b)(4) .......................................................................................... 7, 71
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`37 C.F.R. § 42.22(a) ................................................................................................... 8
`37 C.F.R. § 42.22(a) ................................................................................................... 8
`37 C.F.R. § 42.24 ..................................................................................................... 70
`37 C.F.R. § 42.24 ..................................................................................................... 70
`37 C.F.R. § 42.100(b) ........................................................................................ 10, 11
`37 C.F.R. §42.100(b) ........................................................................................ 10, 11
`37 C.F.R. § 42.104(A)................................................................................................ 5
`37 C.F.R. § 42.104(A) ................................................................................................ 5
`37 C.F.R. § 42.104(B) .............................................................................................. 12
`37 C.F.R. § 42.104(B) .............................................................................................. 12
`37 C.F.R. § 42.105 ................................................................................................... 71
`37 C.F.R. § 42.105 ................................................................................................... 71
`37 C.F.R. § 42.106(a) ................................................................................................. 5
`37 C.F.R. § 42.106(a) ................................................................................................. 5
`37 C.F.R. § 42.8(b)(2) ................................................................................................ 6
`37 C.F.R. § 42.8(b)(2) ................................................................................................ 6
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`IPR2020-01072 (7,326,708)
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`LIST OF EXHIBITS
`
`Description
`U.S. Patent No. 7,326,708
`Declaration of Dr. Steven M. Baldwin
`CV of Dr. Steven M. Baldwin
`WO 03/004498 to Edmonson
`Brittain, “Polymorphism in Pharmaceutical Solids”
`Bastin et al. “Salt Selection and Optimisation [sic] Procedures for
`Pharmaceutical New Chemical Entities”
`U.S. Patent No 6,699,871
`Orange Book Entry for Janumet®
`Orange Book Entry for Januvia®
`Complete copy of the prosecution history of the ʼ708 patent as
`available for download from the USPTO website
`U.S. Patent No. 4,572,909
`U.S. Provisional Application No. 60/303,474, filed July 6, 2001
`Prescribing Information for Janumet®
`Prescribing Information for Januvia®
`Merck Sharpe & Dohme’s Responses and Objections to
`Defendants’ First Set of Joint Interrogatories (1-10)
`Brown et al., Chemistry: The Central Science, 8th Revised
`Edition, 615-618 (2002)
`Mylan Pharmaceuticals Inc. v. Merck Sharp & Dohme Corp.,
`IPR2020-00040, Ex. 1002, Declaration of Dr. Mukund
`Chorghade, Ph.D. (Oct. 29, 2019)
`
`Exhibit No.
`1001
`1002
`1003
`1004
`1005
`1006
`
`1007
`1008
`1009
`1010
`
`1011
`1012
`1013
`1014
`1015
`
`1016
`
`1017
`
`
`
`
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`I.
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`IPR2020-01072 (7,326,708)
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`INTRODUCTION
`Sun Pharmaceutical Industries Ltd. (“Petitioner”) petitions for Inter Partes
`
`Review (“IPR”) seeking cancellation of Claims 1-4, 17, 19, and 21-23 (“challenged
`
`claims”) of U.S. Patent No. 7,326,708 (“the ʼ708 patent”) (EX1001), which is
`
`assigned to Merck, Sharpe & Dohme Corp. (“Merck” or “Patent Owner”).
`
`II. OVERVIEW
`The ʼ708 patent claims a compound commonly known as sitagliptin
`
`phosphate (depicted below), or a hydrate thereof. EX1001, Claim 1 at 16:1-14.1
`
`
`
`
`1 Sitagliptin
`is also known as 4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro
`
`[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine or
`
`7-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(trifluoromethyl)-5,6,7,8-
`
`tetrahydro-l,2,4-triazolo[4,3-a]pyrazine. EX1004, 15:64-66, Example 7; EX1002,
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`¶65.
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`1
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`IPR2020-01072 (7,326,708)
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`Dependent claims 2-3, 17, 19, and 21-23 recite the phosphate salt of sitagliptin while
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`Claims 4-16, 18, 20, and 24 recite the monohydrate thereof or various monohydrate
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`forms thereof. EX1001, 15:63-18:36. The ʼ708 patent, however, is not the first
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`disclosure of sitagliptin phosphate. WO 03/004498 (“WO ʼ498”) (EX1004), prior
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`art to the ʼ708 patent under 35 U.S.C. § 102(a), discloses sitagliptin and its
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`“pharmaceutically acceptable salts.” Patent Owner can hardly dispute otherwise
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`since the ʼ708 patent plainly admits these facts in the “Background of the Invention”:
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`WO 03/004498 (published 16 Jan. 2003), assigned to
`Merck & Co., describes a class of beta-amino
`tetrahydrotriazolo [4,3-a]pyrazines, which are potent
`inhibitors of DP IV and therefore useful for the treatment
`of Type 2 diabetes. Specifically disclosed in WO
`03/004498 is 4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro
`[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-
`trifluorophenyl)butan-2-amine.
`Pharmaceutically
`acceptable salts of this compound are generically
`encompassed within the scope of WO 03/004498.
`EX1001, 1:49-57 (emphasis added). “Admissions in the specification regarding the
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`prior art are binding on the patentee.” PharmaStem Therapeutics, Inc. v. ViaCell,
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`Inc., 491 F.3d 1342, 1362 (Fed. Cir. 2007); Constant v. Advanced Micro-Devices,
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`Inc., 848 F.2d 1560, 1570 (Fed. Cir. 1988) (“A statement in the patent that something
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`is in the prior art is binding on the applicant and patentee for determinations of
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`anticipation and obviousness.”); Sjolund v. Musland, 847 F.2d 1573, 1577-79 (Fed.
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`2
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`IPR2020-01072 (7,326,708)
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`Cir. 1988) (patent specification admitted that certain matter was prior art, and thus
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`“the jury was not free to disregard [that matter]” and “must have accepted [it] as
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`prior art, as a matter of law”); One World Technologies Inc. v. The Chamberlain
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`Group Inc., IPR2017-00126, Paper 67 at 14-15 (P.T.A.B. Apr. 4, 2019) (“[T]he
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`Court of Customs and Patent Appeals [has] long held that admissions in a patent
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`may be considered prior art for any purpose.”).2
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`As to “pharmaceutically acceptable salts,” WO ʼ498 teaches the term can refer
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`to salts generated from either bases or acids. EX1004, 9:27-30. As to the acid salts,
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`“[p]articularly preferred” are “citric, hydrobromic, hydrochloric, maleic,
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`phosphoric, sulfuric, fumaric, and tartaric acids.” Id., 10:14-15 (emphasis added).
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`And much like the ʼ708 patent, the compounds of WO ʼ498 are dipeptidyl peptidase-
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`IV enzyme inhibitors that are useful for the treatment or prevention of diseases such
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`as diabetes and particularly type 2 diabetes. EX1004, Abstract.
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`As to salts of sitagliptin specifically, WO ʼ498 exemplifies one of the
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`“[p]articularly preferred” salts (i.e., the hydrochloride salt) of sitagliptin as Example
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`7:
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`2
`The fact that the patentee’s admissions about WO ʼ498 were made in the
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`“Background of the Invention” of the ʼ708 patent gives further weight to this prior
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`art admission. One World Technologies Inc., IPR2017-00126, Paper 67 at 15.
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`3
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`Id. at 46:1-4. There is no dispute about this fact either; the ʼ708 patent admits it.
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`EX1001, 4:19-22. Further, WO ʼ498 claims sitagliptin and it