IN THE UNITED STATES PATENT AND TRADEMARK OFFICE
`___________________
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`___________________
`MYLAN PHARMACEUTICALS INC.
`Petitioner,
`v.
`MERCK SHARP & DOHME CORP.
`Patent Owner.
`U.S. Patent No. 7,326,708 to Cypes et al.
`Issue Date: February 5, 2008
`Title: Phosphoric acid salt of a dipeptidyl peptidase-IV inhibitor
`Inter Partes Review No.: IPR2020-00040
`
`Petition for Inter Partes Review of U.S. Patent No. 7,326,708
`Under 35 U.S.C. §§ 311-319 and 37 C.F.R. §§ 42.1-.80, 42.100-.123
`
`Mail Stop “PATENT BOARD”
`Patent Trial and Appeal Board
`U.S. Patent and Trademark Office
`P.O. Box 1450
`Alexandria, VA 22313-1450
`
`

`

`Petition for Inter Partes Review of USPN 7,326,708
`
`C.
`
`V.
`
`I.
`II.
`III.
`
`TABLE OF CONTENTS
`INTRODUCTION ........................................................................................... 1
`OVERVIEW .................................................................................................... 1
`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 ’708 Patent ................................. 6
`2.
`Administrative Matters ............................................................... 7
`Designation of Lead and Back-Up Counsel and Service
`(37 C.F.R. §§ 42.8(b)(3), 42.8(b)(4)) .................................................... 7
`STATEMENT OF THE PRECISE RELIEF REQUESTED AND THE
`REASONS THEREFOR (37 C.F.R. § 42.22(A)) ........................................... 8
`THE ’708 PATENT ......................................................................................... 8
`VI.
`VII. CLAIM CONSTRUCTION ..........................................................................10
`VIII. PERSON OF ORDINARY SKILL IN THE ART (“POSA”) .......................11
`IX.
`IDENTIFICATION OF CHALLENGE (37 C.F.R. § 42.104(B)) ................11
`X.
`INVALIDITY ANALYSIS ...........................................................................12
`A.
`Ground 1: Claims 1-3, 17, 19, and 21-23 Are Anticipated by
`WO ’498 ..............................................................................................12
`1.
`Disclosure of WO ’498 .............................................................14
`2.
`Claim 1 ......................................................................................16
`3.
`Claim 2 ......................................................................................24
`4.
`Claim 3 ......................................................................................25
`i
`
`

`

`Petition for Inter Partes Review of USPN 7,326,708
`
`c)
`
`b)
`
`5.
`
`6.
`
`Claim 17 ....................................................................................26
`a)
`A pharmaceutical composition comprising ....................26
`b)
`a therapeutically effective amount of the salt
`according to claim 2 .......................................................26
`in association with one or more pharmaceutically
`acceptable carriers. .........................................................27
`Claim 19 ....................................................................................27
`a)
`A method for the treatment of type 2 diabetes
`comprising ......................................................................27
`administering to a patient in need of such treatment
`a therapeutically effective amount of the salt
`according to claim 2 or a hydrate thereof. ......................27
`Claims 21-22 .............................................................................28
`7.
`Claim 23 ....................................................................................30
`8.
`Ground 2: Claims 1-3, 17, 19 and 21-23 Are Anticipated by the
`’871 Patent ...........................................................................................31
`1.
`Disclosure of the ’871 Patent ....................................................31
`2.
`Claims 1 and 2 ...........................................................................33
`3.
`Claim 3 ......................................................................................34
`4.
`Claims 17 and 19.......................................................................35
`5.
`Claims 21-23 .............................................................................37
`Ground 3: Claims 3, 17, 19, and 21-23 Would Have Been
`Obvious in View of WO ’498 .............................................................38
`1.
`The Level of Ordinary Skill in the Pertinent Art ......................39
`2.
`The Scope and Content of the Prior Art ...................................39
`a) WO ’498 (EX1004) ........................................................39
`
`B.
`
`C.
`
`ii
`
`

`

`Petition for Inter Partes Review of USPN 7,326,708
`
`b)
`c)
`
`d)
`
`(3)
`
`(2)
`
`Claim 3 ............................................................................39
`Claim 17 ..........................................................................41
`(1) A pharmaceutical composition comprising ..........41
`(2)
`a therapeutically effective amount of the salt
`according to claim 2 .............................................42
`in
`association with
`one
`or more
`pharmaceutically acceptable carriers. ..................42
`Claim 19 ..........................................................................42
`(1) A method for the treatment of type 2 diabetes
`comprising ............................................................42
`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
`Claims 21-23 ...................................................................43
`e)
`Ground 4: Claims 1-3, 17, 19, and 21-23 Would Have Been
`Obvious in View of WO ’498 and Bastin ...........................................46
`1.
`The Level of Ordinary Skill in the Pertinent Art ......................46
`2.
`The Scope and Content of the Prior Art ...................................46
`a) WO ’498 (EX1004) ........................................................46
`b)
`Bastin (EX1006) .............................................................46
`The Differences Between the Claims and Prior Art .................48
`a)
`Claim 1 ............................................................................48
`(1)
`There Is No Requirement to Select a Lead
`Compound in Salt Selection Cases ......................48
`(2) WO ’498 and Bastin Would Have Rendered
`the Phosphoric Acid Salt Obvious .......................51
`Claims 2 and 3 ................................................................56
`Claims 17 and 19 ............................................................57
`iii
`
`b)
`c)
`
`D.
`
`3.
`
`

`

`Petition for Inter Partes Review of USPN 7,326,708
`
`E.
`
`A.
`
`Claims 21-23 ...................................................................57
`d)
`Ground 5: Claim 4 Would Have Been Obvious in View of WO
`’498, Bastin and Brittain .....................................................................59
`1.
`The Level of Ordinary Skill in the Pertinent Art ......................59
`2.
`The Scope and Content of the Prior Art ...................................59
`a) WO ’498 (EX1004) and Bastin (EX1006) .....................59
`b)
`Brittain (EX1005) ...........................................................59
`The Differences Between the Claim and Prior Art ...................61
`3.
`Ground 6: Claim 4 Would Have Been Obvious in View of WO
`’498 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 ’498 (EX1004) and Brittain (EX1005) ...................62
`The Differences Between the Claim and Prior Art ...................62
`3.
`Secondary Considerations of Nonobviousness ...................................63
`B.
`THE BOARD SHOULD INSTITUTE TRIAL BASED ON
`MYLAN’S PETITION (35 U.S.C. § 325(D) OR § 314(A)) .........................66
`XII. CONCLUSION ..............................................................................................69
`
`XI.
`
`iv
`
`

`

`Petition for Inter Partes Review of USPN 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) ............................................ 48
`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) ............................... 14, 32, 33
`Bayer Pharma AG v. Watson Laboratories, Inc.,
`874 F.3d 1316 (Fed. Cir. 2017) .......................................................................... 48
`Bayer Schering Pharma AG v. Barr Laboratories,
`575 F.3d 1341 (Fed. Cir. 2008) .......................................................................... 55
`Becton, Dickinson and Company v. B. Braun Melsungen AG,
`IPR2017-01586, slip op. (P.T.A.B. Dec. 15, 2017) ........................................... 66
`Boston Scientific Scimed, Inc. v. Cordis Corp.,
`554 F.3d 982 (Fed. Cir. 2009) ............................................................................ 41
`Bristol-Myers Squibb Co. v. Ben Venue Labs., Inc.,
`246 F.3d 368 (Fed. Cir. 2001) ...................................................................... 12, 13
`v
`
`

`

`Petition for Inter Partes Review of USPN 7,326,708
`
`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 1351,1364 (Fed. Cir. 2008) ................................................................. 63
`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,
`No. 2017-2312, 2019 WL 2452362 (Fed. Cir. June 12, 2019) ........................... 65
`Eli Lilly & Co. v. Zenith Goldline Pharm., Inc.,
`471 F.3d 1369 (Fed. Cir. 2006) .......................................................................... 21
`Glaxo Group Ltd. v. Apotex, Inc.,
`376 F.3d 1339 (Fed. Cir. 2004) ........................................................ 18, 20, 21, 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) ..................................passim
`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) .................................................................... 54, 55
`Hologic Inc. v. Becton, Dickinson and Co.,
`IPR2016-00820, Paper 52 (P.T.A.B. Sept. 28, 2017)......................................... 40
`In re Aller,
`220 F.2d 454 (C.C.P.A. 1955) ...................................................................... 44, 56
`
`vi
`
`

`

`Petition for Inter Partes Review of USPN 7,326,708
`
`In re Cyclobenzaprine Hydrochloride,
`676 F.3d 1063 (Fed. Cir. 2012) .......................................................................... 55
`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
`In re Harris,
`409 F.3d 1339 (Fed. Cir. 2005) .......................................................................... 65
`In re Nomiya,
`509 F.2d (C.C.P.A. 1975) ................................................................................... 50
`In re O’Farrell,
`853 F.2d 894 (Fed. Cir. 1988) ............................................................................ 39
`In re Petering,
`301 F.2d 676 (C.C.P.A. 1962) ................................................................ 23, 25, 35
`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 (’708 & ’921) Patent Litigation,
`C.A. No. 19-md-2902-RGA (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
`
`vii
`
`

`

`Petition for Inter Partes Review of USPN 7,326,708
`
`In re Williams,
`36 F.2d 436 (C.C.P.A. 1929) .............................................................................. 65
`Iron Grip Barbell Co., Inc. v. USA Sports, Inc.,
`392 F.3d 1317 (Fed. Cir. 2004) .......................................................................... 65
`Kao Corp. v. Unilever United States, Inc.,
`441 F.3d 963 (Fed. Cir. 2006) ............................................................................ 65
`Kashiv Biosciences, LLC v. Amgen Inc.,
`IPR2019-00791, Paper 15 (P.T.A.B. Sept. 11, 2019)................................... 67, 68
`Kennametal, Inc. v. Ingersoll Cutting Tool Co.,
`780 F.3d 1376 (Fed. Cir. 2015) .............................................................. 13, 21, 22
`KSR Int’l Co. v. Teleflex, Inc.,
`550 U.S. 398 (2007) ............................................................................................ 11
`
`Merck Sharp & Dohme Corp. v. Alvogen Pine Brook f/k/a Alvogen
`Pine Brook, Inc. et al.,
`1:19-cv-00310 (D. Del.) ........................................................................................ 6
`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. Lupin Ltd. et al.,
`1:19-cv-00347 (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-00101 (N.D. W. Va.) ......................................................................... 6, 68
`Merck Sharp & Dohme Corp. v. Mylan Pharmaceuticals Inc. et al.,
`1:19-cv-01489 (D. Del.) ........................................................................................ 6
`Merck Sharp & Dohme Corp. v. Sandoz, Inc.,
`1:19-cv-00312 (D. Del.) .................................................................................. 6, 68
`
`viii
`
`

`

`Petition for Inter Partes Review of USPN 7,326,708
`
`Merck Sharp & Dohme Corp. v. Sun Pharma Global FZE et al.,
`1:19-cv-00319 (D. Del.) ........................................................................................ 7
`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) .................................. 65, 66
`Mylan Pharmaceuticals Inc. et al. v. UCB Pharma GMBH,
`IPR2016-00510, Paper No. 45 (P.T.A.B. July 19, 2017) ....................... 50, 54, 55
`Mylan Pharmaceuticals Inc. v. Cosmo Technologies Ltd.,
`IPR2017-01035, Paper 17 (P.T.A.B. Sept. 21, 2017)......................................... 13
`Mylan Pharmaceuticals Inc. v. Sanofi-Aventis Deutschland GMBH,
`IPR2018-01680, Paper 22 (P.T.A.B. Apr. 3, 2019) ..................................... 67, 68
`Newell Cos., Inc. v. Kenney Mfg. Co.,
`864 F.2d 757 (Fed. Cir. 1988) ............................................................................ 63
`NHK Spring Co., Ltd. v. Intri-Plex Techs., Inc.,
`Case IPR2018-00752, Paper 8 (P.T.A.B. Sept. 12, 2018) ............................ 67, 68
`
`ix
`
`

`

`Petition for Inter Partes Review of USPN 7,326,708
`
`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) .......................................................................... 48
`Perricone v. Medicis Pharmaceuticals Corp.,
`432 F.3d 1368 (Fed. Cir. 2005) .......................................................................... 17
`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) .......................................................................... 13
`Realtime Data, LLC v. Iancu,
`912 F.3d 1368 (Fed. Cir. 2019) .......................................................................... 38
`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) ............................................................................ 3
`
`x
`
`

`

`Petition for Inter Partes Review of USPN 7,326,708
`
`Spezialpräparate mbH,
`IPR2016-01370, Paper 13 (P.T.A.B. Feb. 8, 2017) ............................................ 64
`Syntex (U.S.A.) LLC v. Apotex Inc.,
`407 F.3d 1371 (Fed. Cir. 2005) .......................................................................... 18
`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 ........................................................................ 67
`Warner Chilcott Co. v. Teva Pharmaceuticals USA,
`89 F. Supp. 3d 641 (D.N.J. 2015) ................................................................. 22, 23
`Watson Labs., Inc. v. United Therapeutics Corp.,
`IPR2017-01621, Paper 10 (P.T.A.B. Jan. 11, 2018) .......................................... 32
`Wm. Wrigley Jr. Co. v. Cadbury Adams USA LLC,
`683 F.3d 1356 (Fed. Cir. 2012) .................................................................... 20, 22
`Statutes
`35 U.S.C. § 102 ............................................................................................ 10, 12, 15
`35 U.S.C. § 102(a) ............................................................................................... 2, 14
`35 U.S.C. § 102(b) ............................................................................................. 46, 59
`35 U.S.C. § 102(e)(2) ......................................................................................... 14, 32
`35 U.S.C. § 325(D) ................................................................................ 66, 67, 68, 69
`Regulations
`37 C.F.R. § 42.6(d) .................................................................................................. 11
`37 C.F.R. § 42.100(b) .............................................................................................. 10
`37 C.F.R. § 42.106(a) ................................................................................................. 5
`
`xi
`
`

`

`Petition for Inter Partes Review of USPN 7,326,708
`
`Petitioner’s Exhibit List
`
`Petitioner
`Exhibit #
`1001
`1002
`1003
`1004
`1005
`1006
`
`1007
`1008
`1009
`1010
`
`1011
`1012
`1013
`1014
`1015
`
`1016
`
`Description
`U.S. Patent No. 7,326,708
`Declaration of Dr. Mukund Chorghade
`CV of Dr. Mukund Chorghade
`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 ’708 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)
`
`xii
`
`

`

`Petition for Inter Partes Review of USPN 7,326,708
`
`I.
`
`INTRODUCTION
`
`Mylan Pharmaceuticals Inc. (“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 ’708 patent”) (EX1001), which is assigned to
`
`Merck, Sharpe & Dohme Corp. (“Merck” or “Patent Owner”).
`
`II. OVERVIEW
`
`The ’708 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,
`
`¶65.
`
`1
`
`

`

`Petition for Inter Partes Review of USPN 7,326,708
`
`Dependent claims 2-3, 17, 19, and 21-23 recite the phosphate salt of sitagliptin while
`
`Claims 4-16, 18, 20, and 24 recite the monohydrate thereof or various monohydrate
`
`forms thereof. EX1001, 15:63-18:36. The ’708 patent, however, is not the first
`
`disclosure of sitagliptin phosphate. WO 03/004498 (“WO ’498”) (EX1004), prior
`
`art to the ’708 patent under 35 U.S.C. § 102(a), discloses sitagliptin and its
`
`“pharmaceutically acceptable salts.” Patent Owner can hardly dispute otherwise
`
`since the ’708 patent plainly admits these facts in the “Background of the Invention”:
`
`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
`
`prior art are binding on the patentee.” PharmaStem Therapeutics, Inc. v. ViaCell,
`
`Inc., 491 F.3d 1342, 1362 (Fed. Cir. 2007); Constant v. Advanced Micro-Devices,
`
`Inc., 848 F.2d 1560, 1570 (Fed. Cir. 1988) (“A statement in the patent that
`
`something is in the prior art is binding on the applicant and patentee for
`
`2
`
`

`

`Petition for Inter Partes Review of USPN 7,326,708
`
`determinations of anticipation and obviousness.”); Sjolund v. Musland, 847 F.2d
`
`1573, 1577-79 (Fed. Cir. 1988) (patent specification admitted that certain matter was
`
`prior art, and thus “the jury was not free to disregard [that matter]” and “must have
`
`accepted [it] as prior art, as a matter of law”); One World Technologies Inc. v. The
`
`Chamberlain Group Inc., IPR2017-00126, Paper 67 at 14-15 (P.T.A.B. Apr. 4,
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`2019) (“[T]he Court of Customs and Patent Appeals [has] long held that admissions
`
`in a patent may be considered prior art for any purpose.”).2
`
`As to “pharmaceutically acceptable salts,” WO ’498 teaches the term can refer
`
`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).
`
`And much like the ’708 patent, the compounds of WO ’498 are dipeptidyl peptidase-
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`IV enzyme inhibitors that are useful for the treatment or prevention of diseases such
`
`as diabetes and particularly type 2 diabetes. EX1004, Abstract.
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`2 The fact that the patentee’s admissions about WO ’498 were made in the
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`“Background of the Invention” of the ’708 patent gives further weight to this prior
`
`art admission. One World Technologies Inc., IPR2017-00126, Paper 67 at 15.
`
`3
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`Petition for Inter Partes Review of USPN 7,326,708
`
`As to salts of sitagliptin specifically, WO ’498 exemplifies one of the
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`“[p]articularly preferred” salts (i.e., the hydrochloride salt) of sitagliptin as Example
`
`7:
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`Id. at 46:1-4. There is no dispute about this fact either; the ’708 patent admits it.
`
`EX1001, 4:19-22. Further, WO ’498 claims sitagliptin and its “pharmaceutically
`
`acceptable salts.” EX1004, Claim 15 (7th structure), 55 (bottom structure); id., 60:5
`
`(“pharmaceutically acceptable salts thereof”).
`
`In reference to WO ’498, the ’708 patent inventors may state: “there is no
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`specific disclosure in the above reference of the newly discovered monobasic
`
`dihydrogen
`
`phosphate
`
`salt
`
`of
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`4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro
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`[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine.”
`
`EX1001, 1:58-62. However, WO ’498 teaches and claims sitagliptin and its
`
`“pharmaceutically acceptable salts” and then identifies the phosphoric acid salt as a
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`“[p]articularly preferred” salt. Id., 10:14-15. Under applicable legal precedents,
`
`4
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`

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`Petition for Inter Partes Review of USPN 7,326,708
`
`sitagliptin phosphate was disclosed. For that matter, any attempt by Patent Owner
`
`to devalue the disclosure of WO ’498 and assert that it does not teach sitagliptin
`
`phosphate is belied by the fact that U.S. 6,699,871 (EX1007), which is related to
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`WO ’498, is listed in the FDA Orange Book along with the ’708 patent for Janumet®
`
`and Januvia®. EX1008 & EX1009.3
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`III.
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`STANDING (37 C.F.R. § 42.104(A)); PROCEDURAL STATEMENTS
`
`Petitioner certifies that: (1) the ’708 patent is available for IPR; and
`
`(2) Petitioner is not barred or estopped from requesting IPR of any claim of the
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`’708 patent on the grounds identified herein. This Petition is filed in accordance
`
`with 37 C.F.R. § 42.106(a). Filed herewith are a Power of Attorney and an Exhibit
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`List pursuant to Section 42.10(b) and Section 42.63(e), respectively. The required
`
`fee is paid when filing the Petition and the Office is authorized to charge any fee
`
`3 WO ’498 (EX1004) and U.S. 6,699,871 (EX1007) both claim priority to U.S.
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`Provisional Application No. 60/303,474 and share the same specification in all
`
`relevant material respects. Compare EX1004, 9:27-10:15 (“pharmaceutically
`
`acceptable salts”), 46:1-5 (Example 7, sitagliptin hydrochloride) with EX1007,
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`6:38-7:4 (“pharmaceutically acceptable salts”), 32:1-16 (Example 7, sitagliptin
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`hydrochloride). WO ’498 was not used by the Examiner during prosecution of the
`
`’708 patent to formulate any prior art rejection.
`
`5
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`Petition for Inter Partes Review of USPN 7,326,708
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`deficiencies and credit overpayments to Deposit Acct. No. DA501290 (Customer ID
`
`No. 27160).
`
`IV. MANDATORY NOTICES (37 C.F.R. § 42.8(A)(1))
`
`A.
`
`Each Real Party in Interest (37 C.F.R. § 42.8(b)(1))
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`The following real parties in interest are identified: Mylan Pharmaceuticals
`
`Inc., Mylan Inc., and Mylan N.V.
`
`B.
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`Notice of Related Matters (37 C.F.R. § 42.8(b)(2))
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`1.
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`Judicial Matters Involving the ’708 Patent
`
`The ’708 patent is currently the subject of the following litigations: Merck
`
`Sharp & Dohme Corp. v. Mylan Pharmaceuticals Inc. et al., 1:19-cv-00101 (N.D.
`
`W. Va.); Merck Sharp & Dohme Corp. v. Mylan Pharmaceuticals Inc. et al., 1:19-
`
`cv-01489 (D. Del.); Merck Sharp & Dohme Corp. v. Alvogen Pine Brook f/k/a
`
`Alvogen Pine Brook, Inc. et al., 1:19-cv-00310 (D. Del.); Merck Sharp & Dohme
`
`Corp. v. Anchen Pharmaceuticals, Inc. et al., 1:19-cv-00311 (D. Del.); Merck Sharp
`
`& Dohme Corp. v. Sandoz, Inc., 1:19-cv-00312 (D. Del.); Merck Sharp & Dohme
`
`Corp. v. Apotex Inc. et al., 1:19-cv-00313 (D. Del.); Merck Sharp & Dohme Corp.
`
`v. Zydus Pharmaceuticals (USA) Inc. et al., 1:19-cv-00314 (D. Del.); Merck Sharp
`
`& Dohme Corp. v. Macleods Pharmaceuticals, Ltd. et al., 1:19-cv-00316 (D. Del.);
`
`Merck Sharp & Dohme Corp. v. Watson Pharmaceuticals, Inc. et al., 1:19-cv-00317
`
`(D. Del.); Merck Sharp & Dohme Corp. v. Teva Pharmaceuticals USA, Inc.,
`
`6
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`

`Petition for Inter Partes Review of USPN 7,326,708
`
`1:19-cv-00318 (D. Del.); Merck Sharp & Dohme Corp. v. Sun Pharma Global FZE
`
`et al., 1:19-cv-00319 (D. Del.); Merck Sharp & Dohme Corp. v. Torrent
`
`Pharmaceuticals Limited et al., 1:19-cv-00320 (D. Del.); Merck Sharp & Dohme
`
`Corp. v. Wockhardt Bio AG et al., 1:19-cv-00321 (D. Del.); Merck Sharp & Dohme
`
`Corp. v. Lupin Ltd.