UNITED STATES PATENT AND TRADEMARK OFFICE
`__________________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`__________________
`
`MYLAN PHARMACEUTICALS INC.,
`Petitioner,
`
`v.
`
`MERCK SHARP & DOHME CORP.,
`Patent Owner.
`__________________
`
`Case No. IPR2020-00040
`U.S. Patent No. 7,326,708
`__________________
`
`PATENT OWNER’S PRELIMINARY RESPONSE
`
`
`
`
`

`

`Case No. IPR2020-00040
`U.S. Patent No. 7,326,708
`
`
`
`TABLE OF CONTENTS
`
`
`INTRODUCTION ..................................................................................................... 1
`
`BACKGROUND ....................................................................................................... 4
`
`
`
`
`
`
`
`
`
`Sitagliptin and the ’708 Patent .............................................................. 4
`
`’708 Patent Prosecution History ............................................................ 5
`
`Summary of Mylan’s Grounds and Asserted Art .................................. 7
`
`Related District Court Litigation ......................................................... 10
`
`ARGUMENT ........................................................................................................... 13
`
`I.
`
`The Board Should Exercise Its Discretion Pursuant to §ֻ§ 325(d) and
`314(a) to Deny Institution. ............................................................................. 13
`
`
`
`
`
`The Board Should Reject Mylan’s Petition Under § 325(d) as a
`Mere Rehash of the Same Prior Art and Arguments Previously
`Presented to the Office. ....................................................................... 13
`
`The Board Should Exercise Its Discretion and Decline to
`Institute Trial Under § 314(a) .............................................................. 23
`
`1.
`
`2.
`
`Instituting Trial on Mylan’s Petition Would be an
`Inefficient Use of the Board’s Limited Resources ................... 24
`
`The Board Should Deny Institution Rather Than Institute
`Trial on Clearly Meritless Grounds .......................................... 31
`
`II. Mylan’s Petition Fails Because It Does Not Address the Claimed 1:1
`Stoichiometric Ratio of Sitagliptin and Phosphoric Acid ............................. 46
`
` Mylan Does Not Argue that WO ’498 or the ’871 Patent
`Expressly Disclose the Claimed 1:1 Salt ............................................ 48
`
` Mylan Does Not Explain How WO ’498 or the ’871 Patent
`Inherently Disclose the Claimed 1:1 DHP Salt ................................... 50
`
` Mylan’s Obviousness Grounds Incorporate Its Defective
`Anticipation Arguments and Should be Denied ................................. 52
`
`CONCLUSION ........................................................................................................ 54
`
`
`
`
`
`
`
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`Case No. IPR2020-00040
`U.S. Patent No. 7,326,708
`
`
`
`TABLE OF AUTHORITIES
`
`
`Arendi S.A.R.L. v. Apple Inc.,
`832 F.3d 1355 (Fed. Cir. 2016) .......................................................................... 51
`
`Constant v. Advanced Micro-Devices, Inc.,
`848 F.2d 1560 (Fed. Cir. 1988) .......................................................................... 43
`
`Cooper v. Goldfarb,
`154 F.3d 1321 (Fed. Cir. 1998) .................................................................... 34, 35
`
`Dynamic Drinkware LLC v. Nat’l Graphics, Inc.,
`800 F.3d 1375 (Fed. Cir. 2015) .......................................................................... 33
`
`Harmonic Inc. v. Avid Tech, Inc.,
`815 F.3d 1356 (Fed. Cir. 2016) .................................................................... 13, 31
`
`In re Steed, 802 F.3d 1311 (Fed. Cir. 2015) ...................................................... 32, 34
`
`Neptune Generics, LLC v. Eli Lilly & Co.,
`921 F.3d 1372 (Fed. Cir. 2019) .......................................................................... 27
`
`Nidec Motor Corp. v. Zhongshan Broad Ocean Motor Co.,
`851 F.3d 1270 (Fed. Cir. 2017) .......................................................................... 46
`
`Oil States Energy Servs., LLC v. Greene’s Energy Grp.,
`LLC, 138 S. Ct. 1365 (2018) ............................................................................... 13
`
`Organik Kimya AS v. Rohm & Haas Co.,
`873 F.3d 887 (Fed. Cir. 2017) ............................................................................ 52
`
`Par Pharm., Inc. v. TWI Pharm., Inc.,
`773 F.3d 1186 (Fed. Cir. 2014) .......................................................................... 47
`
`PersonalWeb Techs., LLC v. Apple, Inc.,
`917 F.3d 1376 (Fed. Cir. 2019) .......................................................................... 47
`
`PharmaStem Therapeutics, Inc. v. ViaCell, Inc.,
`491 F.3d 1342 (Fed. Cir. 2007) .......................................................................... 43
`
`Reading & Bates Constr. Co. v. Baker Energy Res. Corp.,
`748 F.2d 645 (Fed. Cir. 1984) ...................................................................... 42, 43
`
`ii
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`

`

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`U.S. Patent No. 7,326,708
`
`
`SAS Institute, Inc. v. Iancu,
`138 S. Ct. 1348 (2018) ........................................................................................ 24
`
`Sjolund v. Musland,
`847 F.2d 1573 (Fed. Cir. 1988) .......................................................................... 43
`
`St. Regis Mohawk Tribe v. Mylan Pharm. Inc.,
`896 F.3d 1322 (Fed. Cir. 2018) .......................................................................... 13
`
`XY, LLC v. Trans Ova Genetics, L.C.,
`890 F.3d 1282 (Fed. Cir. 2018) .......................................................................... 26
`
`Alarm.com Inc. v. Vivint, Inc.,
`IPR2015-01967, Paper 12 (P.T.A.B. Mar. 30, 2016) ......................................... 21
`
`Amgen Inc. v. Alexion Pharmaceuticals Inc.,
`IPR2019-00740, Paper 15 (P.T.A.B. Aug. 20, 2019) ............................. 21, 22, 23
`
`Amneal Pharmaceuticals LLC v. Alkermes Pharma Ireland Limited,
`IPR2018-00943, Paper 8 (P.T.A.B. Nov. 7, 2018) ............................................. 22
`
`Apple Inc. v. SightSound Techs., LLC,
`CBM2013-00021, Paper 13 (P.T.A.B. Oct. 8, 2013) ......................................... 27
`
`Aquestive Therapeutics, Inc., v. Neurelis, Inc.,
`IPR2019-00450, Paper 8 (P.T.A.B. Aug. 1, 2019) ............................................. 18
`
`Arctic Cat, Inc. v. Polaris Indus. Inc.,
`IPR2014-01427, Paper 58 (P.T.A.B. Feb. 4, 2016) ............................................ 48
`
`Associated British Foods plc v. Cornell Research Foundation, Inc.,
`IPR2019-00578, Paper 25 (P.T.A.B. July 25, 2019) .......................................... 44
`
`Becton, Dickinson & Co. v. B. Braun Melsungen AG,
`IPR2017-01586, Paper 8 (P.T.A.B. Dec. 15, 2017) ..................................... 14, 20
`
`Biodelivery Scis. Int’l v. Aquestive Therapeutics, Inc.,
`IPR2015-00165, Paper 91 (P.T.A.B. Feb. 7, 2019) ............................................ 32
`
`C.R. Bard, Inc. v. Med. Components, Inc.,
`IPR2015-01660, Paper 9 (P.T.A.B. Feb. 9, 2016) .............................................. 51
`
`iii
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`

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`U.S. Patent No. 7,326,708
`
`
`Cambrios Film Sols. Corp. v. C3Nano Inc.,
`IPR2019-00709, Paper 15 (P.T.A.B. Aug. 26, 2019) ......................................... 51
`
`Chevron Oronite Co. LLC, v. Infineum USA L.P.,
`IPR2018-00923, Paper 9 (P.T.A.B. Nov. 7, 2018) ....................................... 32, 44
`
`Clim-A-Tech Ind., Inc. v. William A. Ebert,
`IPR2017-01863, Paper 13 (P.T.A.B. Feb. 12, 2018) .......................................... 21
`
`Comcast Cable Commc’ns, LLC v. Veveo, Inc.,
`IPR2017-00932, Paper 10 (P.T.A.B. Sept. 7, 2017)..................................... 46, 51
`
`Corning Inc. v. DSM IP Assets B.V.,
`IPR2013-00053, Paper 66 (P.T.A.B. May 1, 2014) ........................................... 40
`
`Cosmax Co. v. AmorePacific Corp.,
`IPR2018-01516, Paper 8 (P.T.A.B. Feb. 20, 2019) ............................................ 16
`
`Cultec, Inc. v. StormTech LLC,
`IPR2017-00777, Paper 7 (P.T.A.B. Aug. 22, 2017) ........................................... 16
`
`Deeper, UAB v. Vexilar, Inc.,
`IPR2018-01310, Paper 7 (P.T.A.B. Jan. 24, 2019) ...................................... 32, 44
`
`Digital Check Corp. v. e-ImageData Corp.,
`IPR2017-00178, Paper 6 (P.T.A.B. Apr. 25, 2017) ..................................... 22, 23
`
`E-One, Inc. v. Oshkosh Corp.,
`IPR2019-00161, Paper 16 (P.T.A.B. May 15, 2019) ....................... 24, 25, 28, 29
`
`Fortinet Inc. v. British Telecomms. Pub. Ltd.,
`IPR2019-01326, Paper 8 (P.T.A.B. Jan. 7, 2020) .............................................. 19
`
`Fox Factory, Inc. v. SRAM, LLC,
`IPR2016-01876, Paper 8 (P.T.A.B. Apr. 3, 2017) ............................................. 23
`
`FreeBit AS v. Bose Corp.,
`IPR2017-01307, Paper 8 (P.T.A.B. Nov. 14, 2017) ..................................... 32, 45
`
`General Plastic Indus. Co., Ltd. v. Canon Kabushiki Kaisha,
`IPR2016-01357, Paper 19 (P.T.A.B. Sept. 6, 2017)........................................... 29
`
`iv
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`

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`
`
`HyperBranch Medical Technology v. Confluent Surgical, Inc.,
`IPR2018-01099, Paper 14 (P.T.A.B. Nov. 27, 2018) ......................................... 23
`
`Jiawei Tech. (HK) Ltd. v. Richmond,
`IPR2014-00937, Paper 24 (P.T.A.B. Feb. 6, 2014) ................................ 46, 51, 52
`
`LG Elecs. Inc. v. Wi-LAN Inc.,
`IPR2018-00704, Paper 13 (P.T.A.B. Sept. 5, 2018)........................................... 45
`
`Limelight Networks, Inc., v. Akamai Techs., Inc.,
` IPR2017-00349, Paper 7 (P.T.A.B. May 30, 2017) .......................................... 40
`
`Microsoft Corp. v. IPA Tech. Inc.,
`IPR2019-00839, Paper 9 (P.T.A.B. Nov. 8, 2019) ............................................. 15
`
`Microsoft Corp., v. Koninklijke Philips N.V.,
`IPR2018-00279, Paper 11 (P.T.A.B. June 8, 2018) ........................................... 17
`
`NHK Spring Co., Ltd. v. Intri-Plex Techs., Inc.,
`IPR2018-00752, Paper 8 (P.T.A.B. Sept. 12, 2018)....................................passim
`
`One World Techs. Inc. v. Chamberlain Grp. Inc.,
`IPR2017-00126, Paper 67 (P.T.A.B. Apr. 4, 2019) ........................................... 43
`
`Praxair Distribution, Inc. v. Ino Therapeutics, LLC,
`IPR2015-00893, Paper 14 (P.T.A.B. Sept. 22, 2015)......................................... 23
`
`RJ Reynolds Vapor Co. v. Fontem Holdings 1 BV,
`IPR2017-01642, Paper 10 (P.T.A.B. Jan. 16, 2018) .......................................... 21
`
`Siemens Healthcare Diagnostics Inc. v. Radiometer Medical APS,
`IPR2018-00311, Paper 6 (P.T.A.B. June 25, 2018) ........................................... 19
`
`Unified Patents Inc. v. Dynamic Data Techs., LLC,
`IPR2019-01085, Paper 12 (P.T.A.B. Dec. 3, 2019) ..................................... 33, 45
`
`35 U.S.C. § 102 ...................................................................................... 32, 33, 39, 42
`
`35 U.S.C. § 103 .................................................................................................passim
`
`35 U.S.C. § 314(a) ............................................................................................passim
`
`35 U.S.C. § 315(e)(2) ............................................................................................... 27
`
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`
`35 U.S.C. § 316(b) ................................................................................................... 44
`
`35 U.S.C. § 318(b) ................................................................................................... 26
`
`35 U.S.C. § 325(d) ............................................................................................passim
`
`37 C.F.R. § 42.65(a) ................................................................................................. 51
`
`157 Cong. Rec. S1376 (daily ed. Mar. 8, 2011) ...................................................... 20
`
`MPEP §§ 704.01, 706 .............................................................................................. 17
`
`MPEP § 706(I)(2) ..................................................................................................... 42
`
`MPEP § 706.04 ........................................................................................................ 21
`
`Joe Matal, A Guide to the Legislative History of the America Invents
`Act: Part II of II, 21 Fed. Cir. B.J. 539, 615 (2012) ........................................... 21
`
`
`
`
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`
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`PATENT OWNER’S EXHIBIT LIST
`
`Description
`Exhibit
`EX2001 Declaration of Bruce R. Genderson in Support
`of Pro Hac Vice Admission
`EX2002 Declaration of Vicky K. Vydra
`EX2003 Declaration of Robert M. Wenslow, Ph.D.
`EX2004 Declaration of Russell R. Ferlita
`EX2005 Declaration of Joanne Diddle
`Scheduling Order, In re Sitagliptin Phosphate
`EX2006
`(’708 & ’921) Patent Litigation, No. 1:19-md-
`02902-RGA (D. Del. Aug. 23, 2019)
`EX2007 Order, Merck Sharp & Dohme Corp. v. Mylan
`Pharmaceuticals, Inc., No. 1:19-cv-00101-IMK
`(N.D. W. Va. Aug. 2, 2019)
`EX2008 Defendants’ Initial Invalidity Contentions, In re
`Sitagliptin Phosphate (’708 & ’921) Patent
`Litigation, No. 1:19-md-02902-RGA (D. Del.
`Oct. 25, 2019) (Excerpt)
`EX2009 Certified Assignment Record – US 7,326,708
`EX2010 Certified Assignment Record – WO 03/004498
`EX2011 U.S. Patent No. 9,718,880 (cited in Amgen Inc.
`v. Alexion Pharms. Inc., IPR2019-00740, Paper
`15 (P.T.A.B. Aug. 20, 2019))
`EX2012 U.S. Patent No. 7,919,499 (cited in Amneal
`Pharmaceuticals LLC v. Alkermes Pharma
`Ireland Limited, IPR2018-00943, Paper 8
`(P.T.A.B. Nov. 7, 2018))
`EX2013 U.S. Patent No. 9,182,027 (cited in Fox
`Factory, Inc. v. SRAM, LLC, IPR2016-01876,
`Paper 8 (P.T.A.B. Apr. 3, 2017))
`
`Short Name
`
`
`Vydra Decl.
`Wenslow Decl.
`Ferlita Decl.
`Diddle Decl.
`
`
`
`
`
`
`
`
`
`
`
`
`
`
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`Case No. IPR2020-00040
`U.S. Patent No. 7,326,708
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`
`
`INTRODUCTION
`
`Mylan Pharmaceuticals Inc.’s (“Mylan”) Petition for IPR of U.S. Patent No.
`
`7,326,708 (“the ’708 patent”) is the quintessential case in which the Board should
`
`exercise its discretion to deny institution. The Board has denied institution for a
`
`number of independent reasons; virtually all of them are present in this case. The
`
`art Mylan asserts in its Petition was the primary art before the examiner during
`
`prosecution of the ’708 patent; the arguments and art raised here are duplicative of
`
`those raised in related district court proceedings against Mylan and thirteen other
`
`generic drug companies; and because Mylan relies on a reference that is not prior art
`
`for purposes of obviousness, trial would necessarily be instituted on facially
`
`defective grounds. In addition, Mylan fails to provide evidence that a key limitation
`
`present in all claims of the ’708 patent is either anticipated or obvious based on the
`
`asserted art. In sum, the Board should reject Mylan’s Petition.
`
`1. Mylan principally relies on the same art and arguments that were before
`
`the Office during examination: WO 03/004498 (“WO ’498”) and U.S. Patent No.
`
`6,699,871 (“the ’871 patent”). Boiled down, Mylan asserts that each reference
`
`disclosed sitagliptin and pharmaceutically acceptable salts thereof, including the
`
`claimed dihydrogenphosphate (“DHP”) salt. But Patent Owner Merck Sharp &
`
`Dohme Corp. (“Merck”) put this argument before the Office on the first page of its
`
`application. The specification of the ’708 patent states that WO ’498 specifically
`
`1
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`disclosed sitagliptin, and that pharmaceutically acceptable salts of sitagliptin are
`
`generically encompassed within its scope, but that there was no specific disclosure
`
`in WO ’498 of the claimed DHP salt. WO ’498 and the ’871 patent were two of only
`
`three references listed on the first Information Disclosure Statement (“IDS”) and two
`
`of only seven references listed during examination. Given the prominence of this
`
`disclosure and its emphasis to the Office, it is inconceivable that the Office missed
`
`the arguments raised in Mylan’s Petition. The fact that the Office declined to reject
`
`any claims based on WO ’498 or the ’871 patent demonstrates that those arguments
`
`lacked merit, not that they were overlooked. The Board should exercise its discretion
`
`under 35 U.S.C. § 325(d) and deny institution.
`
`2.
`
`For numerous reasons, the Board should also deny institution in its
`
`discretion under 35 U.S.C. § 314(a). Mylan’s Petition for IPR is related to a larger
`
`Hatch-Waxman dispute pending in the district courts against Mylan and thirteen
`
`other generic defendants. Mylan and the other generic defendants in those lawsuits
`
`have raised the same arguments Mylan raises here (as well as other arguments based
`
`on the same art that cannot be raised here, e.g., obviousness-type double patenting
`
`or “OTDP”). Moreover, Mylan in the district court has challenged the validity of
`
`fifteen claims that its Petition leaves unaddressed—over the same prior art. Thus,
`
`even if Mylan were to prevail in a final written decision, the district court
`
`proceedings would continue, and Mylan (and its co-defendants) would make related
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`2
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`arguments on those other claims based on the same references. And were Merck to
`
`prevail, the inefficiency is even greater: along with having to litigate the exact same
`
`arguments against the other generic defendants, not bound by the estoppel
`
`provisions, Merck would likely still need to proceed against Mylan itself with
`
`respect to related arguments, like OTDP, based on the same prior art.
`
`3.
`
`Furthermore, any final written decision would likely issue after the
`
`completion of all discovery in the district court cases (except expert depositions),
`
`just five months before trial. Even then, any appeal to the Federal Circuit would not
`
`conclude until long after the district court’s trial on validity. Hence, substantial time
`
`and expense will be spent litigating in the district court before there is a final
`
`resolution of this IPR. The Office’s expenditure of its limited resources will lead to
`
`little, if any, efficiency and result in duplicative litigation, precisely contrary to the
`
`animating purposes of the America Invents Act (“AIA”).
`
`4. Mylan also relies on art that does not qualify as prior art for
`
`obviousness purposes to any of the claims in Grounds 3 and 4, and those grounds
`
`contain all but one of the claims Mylan asserts would have been obvious. The Board
`
`should follow its practice of not instituting trial on a Petition with facially defective
`
`grounds, especially in this case, where the same and related arguments have been
`
`raised in the district court.
`
`3
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`5.
`
`Finally, each of Mylan’s six grounds is fatally flawed because Mylan
`
`fails to establish that the 1:1 stoichiometry of the claimed DHP salt was disclosed
`
`either expressly or inherently in the asserted art. The only mention of this important
`
`limitation comes in a single conclusory sentence in a footnote in the anticipation
`
`section of Mylan’s Petition. The Petition lacks any argument that such stoichiometry
`
`would have been obvious. Mylan’s failure of proof regarding this limitation fatally
`
`undermines all of its grounds. The Board should reject Mylan’s Petition.
`
`BACKGROUND
`
`
`
`Sitagliptin and the ’708 Patent
`
`The chemical compound sitagliptin is the active ingredient in three Merck
`
`products used to treat type 2 diabetes: Januvia®, Janumet® and Janumet® XR.
`
`Sitagliptin inhibits a protein known as dipeptidyl peptidase IV (“DPP-IV”), a
`
`regulatory enzyme involved in modulating the level of insulin (and thus glucose) in
`
`the human body. In 2006, Januvia® became the first DPP-IV inhibitor approved by
`
`the FDA for the treatment of diabetes.
`
`After synthesizing sitagliptin and identifying its biological activity, Merck
`
`worked to develop a stable solid form of the compound that could be formulated into
`
`a finished drug product. Merck’s efforts led to the synthesis and identification of
`
`the claimed DHP salt of sitagliptin as a lead solid form candidate and, eventually, to
`
`4
`
`

`

`
`the crystalline monohydrate form of the DHP salt, which is the solid form of
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`sitagliptin used today in Merck’s products.
`
`The claims of the ’708 patent are limited to a particular sitagliptin phosphate
`
`salt of defined stoichiometry. As recited and depicted in claim 1 of the ’708 patent,
`
`the challenged claims require a DHP salt with a 1:1 stoichiometric ratio of sitagliptin
`
`to phosphoric acid:
`
`
`
`’708 patent, Claim 1. Mylan acknowledges that claim 1 requires this particular
`
`stoichiometry. See Pet. at 19 n.8. The remaining claims that Mylan seeks to cancel
`
`are directed to the crystalline monohydrate form of the 1:1 DHP salt, pharmaceutical
`
`compositions containing the 1:1 DHP salt, a method of using the 1:1 DHP salt to
`
`treat type 2 diabetes, and a process for preparing the 1:1 DHP salt.
`
`
`
`’708 Patent Prosecution History
`
`Merck filed the patent application that became the ’708 patent on June 23,
`
`2004. The first page of the specification submitted with that application focused the
`
`Office’s attention on the same argument, based on the same art, that Mylan makes
`
`in its Petition. The specification states that “[s]pecifically disclosed in WO
`
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`03/004498 is [sitagliptin],” and that “[p]harmaceutically acceptable salts of this
`
`compound are generically encompassed within the scope of WO 03/004498.”
`
`EX1010 at 3–4. “However,” the specification continues, “there is no specific
`
`disclosure
`
`in
`
`the above reference of
`
`the newly discovered monobasic
`
`dihydrogenphosphate salt of [sitagliptin].” Id. at 4 (emphasis added).
`
`Merck also listed WO ’498 and the ’871 patent as two of only three references
`
`on the first IDS it submitted during examination. Id. at 46. The examiner
`
`demonstrated that he considered those references in numerous ways. First, he
`
`acknowledged receipt of the IDS listing WO ’498 and the ’871 patent. Id. at 147.
`
`Second, he signed that IDS. Id. at 157. Third, at the bottom of that IDS is the
`
`statement: “Examiner: Initial if reference considered,” and he placed his initials next
`
`to the ’871 patent, which is listed on the face of the ’708 patent. Id. The examiner
`
`did not initial WO ’498, but WO ’498 shares an identical specification with the ’871
`
`patent and it was not lined through on the IDS, which the examiner is instructed to
`
`do if a reference is “not in conformance and not considered.” Id. Merck filed only
`
`two other IDSs during the examination, disclosing just two additional references on
`
`each. Id. at 124, 166. In total, Merck listed seven references to the examiner, two
`
`of which correspond to Mylan’s primary references, and one of which was the
`
`publication of the application giving rise to the ’871 patent.
`
`6
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`Summary of Mylan’s Grounds and Asserted Art
`
`Mylan alleges six grounds of unpatentability—two based on anticipation and
`
`four based on obviousness—over WO ’498 (EX1004), the ’871 patent (EX1007),
`
`Bastin (EX1006), and Brittain (EX1005):
`
`Basis
`Ground References
`§ 102
`1
`WO ’498
`§ 102
`2
`’871 patent
`§ 103
`3
`WO ’498
`§ 103
`4
`WO ’498, Bastin
`5
`WO ’498, Bastin, Brittain § 103
`6
`WO ’498, Brittain
`§ 103
`
`Claims Challenged
`1–3, 17, 19, 21–23
`1–3, 17, 19, 21–23
`3, 17, 19, 21–23
`1–3, 17, 19, 21–23
`4
`4
`
`
`
`1.
`
`Grounds 1 and 2 assert parallel anticipation arguments against claims
`
`1–3, 17, 19, and 21–23 over WO ’498 and the ’871 patent, respectively.
`
`WO ’498, which is assigned to Merck, discloses a broad genus of compounds
`
`with DPP-IV inhibitory activity. In support of its anticipation and obviousness
`
`arguments, Mylan focuses on Example 7 of WO ’498. Example 7 discloses a
`
`sitagliptin hydrochloride salt:
`
`WO ’498 (EX1004) at 46:1–26. This hydrochloride salt is obviously not the same
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`DHP salt claimed in the ’708 patent. To get to the claimed DHP salt, Mylan argues
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`that WO ’498 “specifically claims sitagliptin and its ‘pharmaceutically acceptable
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`salts thereof’” based on WO ’498 claim 15, which lists sitagliptin among 32 other
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`compounds, id. at 54:17–60:4, and then points to WO ’498’s specification, which
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`lists “phosphoric” as one of eight “[p]articularly preferred” acids to use with one or
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`more of the genus of compounds of the invention, id. at 10:8–15. Pet. at 16.
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`The ’871 Patent, also assigned to Merck, has an identical specification to WO
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`’498. See Pet. at 33. In contrast to WO ’498, which Mylan relies upon in five of its
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`six asserted grounds, Mylan only relies on the ’871 patent in a single anticipation-
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`based ground. In addition to relying on Example 7 and the disclosure of sitagliptin
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`among 32 other compounds in claim 15, Mylan also points to claim 17 of the ’871
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`patent, which is an independent claim limited to the chemical structure of the
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`sitagliptin freebase “or a pharmaceutically acceptable salt thereof.” ’871 patent
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`(EX1007) at 41:1–14; see also Pet. at 33. Mylan contends that “[s]ince the ’871
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`patent teaches the phosphoric acid salt is a ‘[p]articularly preferred’ accompanying
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`salt, the ’871 patent teaches the phosphoric acid salt of sitagliptin.” Pet. at 34.
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`Mylan does not argue that WO ’498 or the ’871 patent contains any example
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`of a salt made by combining phosphoric acid and sitagliptin, much less the claimed
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`DHP salt of sitagliptin with its 1:1 stoichiometry. Instead, in a footnote, Mylan
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`appears to rely on a theory of inherency (without ever using the word) that the 1:1
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`stoichiometry of the claimed salt is the inherent result of combining sitagliptin and
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`phosphoric acid, an argument based solely on the conclusory assertion of its expert
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`that sitagliptin “can only be mono-protonated at the primary amine.” Pet. at 19.
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`2.
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`Ground 3 of Mylan’s Petition asserts obviousness of a subset of the
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`claims challenged in Ground 1 over WO ’498. Ground 3 does not assert the
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`obviousness of claim 1—the only independent claim in the ’708 patent. Instead,
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`Ground 1 expressly assumes the Board agrees with Mylan’s anticipation argument
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`regarding that claim (and claim 2). See, e.g., Pet. at 39. As a result, Ground 3
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`necessarily fails if the Board rejects Mylan’s anticipation argument in Ground 1.
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`3.
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`Ground 4 is an obviousness ground combining WO ’498 with Bastin.
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`Bastin is a general reference that Mylan says “teaches commonly used salts.”
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`Pet. at 47. Mylan does not argue that Bastin mentions or discusses sitagliptin.
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`Instead, Mylan argues that the POSA would have recognized that sitagliptin was
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`weakly basic, and would have therefore considered combining it with one of the salts
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`Bastin suggests for weakly basic drug substances. Pet. at 53–54. Mylan argues, but
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`does not explain why, the POSA would focus on the five inorganic salts (including
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`phosphate) listed in Bastin over the 21 other salts Bastin also says “could be
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`considered” for weakly basic drugs. See Pet. at 47; Bastin (EX1006) at 2.
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`4.
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`Finally, Grounds 5 and 6 assert the obviousness of the crystalline
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`monohydrate recited in claim 4 of the ’708 patent over the combination of WO ’498
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`and Brittain, with or without Bastin.
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`Brittain is another general reference that Mylan relies upon to show the
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`“prevalence of crystal hydrates of pharmaceutical substances,” and the relative
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`frequency of various hydration states. See Pet. at 59–60. Mylan does not argue that
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`Brittain mentions or discusses sitagliptin.
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` Related District Court Litigation
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`Mylan’s Petition is part of ongoing litigation related to sitagliptin, as indicated
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`in the parties’ mandatory notices (e.g., Paper 7). Merck has filed Hatch-Waxman
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`suits alleging infringement of the ’708 patent, among others, against fourteen generic
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`drug companies including Mylan, Teva, Apotex, Par, Sun, and Sandoz. That
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`litigation has been consolidated for pretrial proceedings in a multidistrict litigation
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`(“MDL”) pending before Judge Richard G. Andrews in the United States District
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`Court for the District of Delaware.1 In re Sitagliptin Phosphate (’708 & ’921) Patent
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`Litigation, No. 19-md-2902-RGA (D. Del.).
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`The MDL proceedings in Delaware have been pending for roughly one year,
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`and are well underway. The parties have exchanged initial infringement and
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`1 That MDL and 13 of its constituent lawsuits are properly identified in Mylan’s
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`Petition, Pet. at 6–7, except Merck has now filed an additional lawsuit since Mylan
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`petitioned for IPR. See Merck Sharp & Dohme Corp. v. Accord Healthcare, Inc. et
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`al., No. 1:19-cv-02192-RGA (D. Del.).
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`invalidity contentions, engaged in substantial document discovery and production,
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`and are currently in the process of claim construction. See EX2006 at 2, 7–9. Fact
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`discovery concludes in November 2020, and expert reports will be served between
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`January and May 2021. See id. at 2, 9. The MDL is not in its “infant stages,” as
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`Mylan asserts. Pet. at 67. A three-day bench trial on validity against all MDL
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`defendants except Mylan is set to begin in the District of Delaware on October 4,
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`2021, with individual one-day infringement trials to be scheduled as necessary. See
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`id. at 10. Merck’s district court trial against Mylan on validity and infringement is
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`conditionally scheduled to begin in the Northern District of West Virginia on
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`December 13, 2021. See EX2007 at 1.
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`As a consequence of this schedule, Merck, Mylan, and the other MDL
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`defendants will necessarily expend significant resources litigating the district court
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`proceedings before the Board is likely to issue a final written decision in or around
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`May 2021.2 By that time, the parties will have concluded fact discovery, briefed and
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`argued any claim construction issues, and exchanged expert reports. Only expert
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`depositions will remain, with trial in Delaware five months away. Trial in the district
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`2 Assuming the Board adopts its customary schedule, the Board’s institution decision
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`is expected sometime in May 2020, and therefore the statutory deadline for a final
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`written decision will be sometime in May 2021.
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`court (at least on claims that Mylan has not challenged here) will occur before any
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`appeal of a final written decision to the Federal Circuit is resolved.
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`There is overlap between the claims, art, and arguments raised in this IPR and
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`in the MDL. The claims and art at issue in this IPR are a small and duplicative subset
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`of the claims asserted, and art identified, in the MDL. Mylan only seeks to cancel
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`nine of the ’708 patent’s claims here, namely claims 1–4, 17, 19, and 21–23; yet in
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`the MDL, Merck has asserted—and the MDL defendants (including Mylan) seek to
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`invalidate—each of the ’708 patent’s 24 claims. Mylan relies on four total
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`references here, and principally on two; the MDL defendants rely principally on the
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`same two references, and identify dozens of others.
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`Similarly, the arguments Mylan raises here are a duplicative subset of the
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`arguments raised in the MDL. For example, Mylan’s Petition argues that claim 1 of
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`the ’708 patent is invalid under § 102 because claim 17 of the ’871 patent claims
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`sitagliptin free base and pharmaceutically acceptable salts thereof, and the ’871
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`patent specification teaches sitagliptin combined with phosphoric acid. Pet. at 33–
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`34. The MDL defendants assert this same argument, and in addition raise it in the
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`context of OTDP, a ground of invalidity that cannot be raised here. This overlap
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`would lead to inefficient, duplicative proceedings.
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`
`
`I.
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`Case No. IPR2020-00040
`U.S. Patent No. 7,326,708
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`ARGUMENT
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`The Board Should Exercise Its Discretion Pursuant to §ֻ§ 325(d) and
`314(a) to Deny Institution.
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`The decision whether to institute an IPR is committe