Case 1:19-md-02902-RGA Document 136 Filed 07/17/20 Page 1 of 82 PageID #: 1915
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`IN THE UNITED STATES DISTRICT COURT
`FOR THE DISTRICT OF DELAWARE
`
`
`
`IN RE: SITAGLIPTIN PHOSPHATE (’708
`& ’921) PATENT LITIGATION
`
`
`
`
`
`
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`
`
`MDL No. 19-2902-RGA
`
`C.A. Nos. 19-311-RGA,
`
`19-312-RGA,
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`19-313-RGA,
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`19-314-RGA,
`
`19-317-RGA,
`
`19-318-RGA,
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`19-319-RGA,
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`19-347-RGA,
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`19-1489-RGA.
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`
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`JOINT CLAIM CONSTRUCTION BRIEF
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`Case 1:19-md-02902-RGA Document 136 Filed 07/17/20 Page 2 of 82 PageID #: 1916
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`TABLE OF CONTENTS
`
`MERCK’S INTRODUCTION.............................................................................................1
`I.
`DEFENDANTS’ INTRODUCTION ...................................................................................2
`II.
`III. MERCKS’S PERSON OF ORDINARY SKILL .................................................................3
`IV.
`DEFENDANTS’ PERSON OF ORDINARY SKILL .........................................................3
`V.
`REPRESENTATIVE CLAIMS ...........................................................................................4
`A.
`’708 Patent ...............................................................................................................4
`1.
`Claim 1 .........................................................................................................4
`2.
`Claim 2 .........................................................................................................4
`3.
`Claim 4 .........................................................................................................4
`4.
`Claim 5 .........................................................................................................4
`5.
`Claim 24 .......................................................................................................5
`’921 Patent ...............................................................................................................5
`1.
`Claim 1 .........................................................................................................5
`2.
`Claim 11 .......................................................................................................5
`3.
`Claim 22 .......................................................................................................5
`AGREED-UPON CONSTRUCTIONS ...............................................................................6
`VI.
`VII. DISPUTED CLAIM TERMS ..............................................................................................6
`A.
`’708 Patent ...............................................................................................................6
`1.
`“the salt of claim 1 [or 2] . . .” (claims 2, 3, and 21) ...................................6
`2.
`“crystalline monohydrate [of the dihydrogen phosphate salt of
`sitagliptin]” (claims 4 and 24) ....................................................................25
`“characteristic absorption bands obtained from the X-ray powder
`diffraction pattern at spectral d-spacings of” (claims 5-7) .........................33
`“crystallizing the dihydrogenphosphate salt of [sitagliptin] at
`25°C” (claim 24) ........................................................................................42
`’921 Patent .............................................................................................................48
`1.
`Merck’s Introductory Statement ................................................................48
`2.
`Defendants’ Introductory Statement ..........................................................49
`3.
`“surfactant” (claims 1, 3, 5-8, 10, 11, and 21) ...........................................49
`4.
`“sitagliptin” (claims 1, 3, 5, 7, 10, and 12-14) ...........................................63
`5.
`“sodium lauryl sulfate” (claims 11, 22, 24, and 26) ..................................69
`6.
`“sitagliptin phosphate monohydrate” (claims 22, 24-26) ..........................70
`
`3.
`
`4.
`
`B.
`
`B.
`
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`Case 1:19-md-02902-RGA Document 136 Filed 07/17/20 Page 3 of 82 PageID #: 1917
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`
`
`TABLE OF AUTHORITIES
`
`CASES
`
`Acceleration Bay v. Activision Blizzard,
`2018 WL 456035 (D. Del. Jan. 17, 2018) ..........................................................................37, 40
`
`Acromed Corp. v. Sofamor Danek Grp. Inc.,
`253 F.3d 1371 (Fed. Cir. 2001)................................................................................................18
`
`Advanced Fiber Techs. Trust v. J&L Fiber Servs., Inc.,
`674 F.3d 1365 (Fed. Cir. 2012)..........................................................................................56, 67
`
`Advanced Med. Optics, Inc. v. Alcon Inc.,
`361 F. Supp. 2d 370 (D. Del. 2005) ...................................................................................39, 41
`
`AK Steel Corp. v. Sollac &Ugine,
`344 F.3d 1234 (Fed. Cir. 2003)..................................................................................................9
`
`Akzo Nobel Coatings, Inc. v. Dow Chem. Co.,
`811 F.3d 1334 (Fed. Cir. 2016)....................................................................................15, 50, 64
`
`Alcon Research, Ltd. v. Apotex Inc.,
`687 F.3d 1362 (Fed. Cir. 2012)............................................................................................9, 11
`
`Alcon, Inc. v. Teva Pharm. USA, Inc.,
`664 F. Supp. 2d 443 (D. Del. 2009) .........................................................................................40
`
`Allen Eng’g Corp. v. Bartell Indus., Inc.,
`299 F.3d 1336 (Fed. Cir. 2002)....................................................................................36, 40, 42
`
`Allergan Sales, LLC v. Lupin Ltd.,
`2013 WL 4519609 (E.D. Tex. Aug. 21, 2013) ........................................................................20
`
`Altiris, Inc. v. Symantic Corp.,
`318 F.3d 1363 (Fed. Cir. 2003)................................................................................................12
`
`Amgen Inc. v. Hospira, Inc.,
`2016 WL 7013483 (D. Del. Nov. 30, 2016) ......................................................................15, 19
`
`Amgen Inc. v. Hospira, Inc.,
`232 F. Supp. 3d 621 (D. Del. 2017) .........................................................................................18
`
`Asyst Techs., Inc. v. Emtrak, Inc.,
`544 F.3d 1310 (Fed. Cir. 2008)................................................................................................68
`
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`Case 1:19-md-02902-RGA Document 136 Filed 07/17/20 Page 4 of 82 PageID #: 1918
`
`
`
`Aventis Pharma S.A. v. Hospira, Inc.,
`675 F.3d 1324 (Fed. Cir. 2012)................................................................................................58
`
`Bayer Intellectual Prop. GmbH v. AuroBindo Pharma Ltd.,
`2017 WL 838662 (D. Del. Mar. 3, 2017) ......................................................................9, 11, 18
`
`Bicon, Inc. v. Straumann Co.,
`441 F.3d 945 (Fed. Cir. 2006)..................................................................................................12
`
`Bristol-Myers Squibb Co. v. Mylan Pharm., Inc.,
`2012 WL 1753670 (D. Del. May 16, 2012) .............................................................................31
`
`CBT Flint Partners, LLC v. Return Path, Inc.,
`654 F.3d 1353 (Fed. Cir. 2011)................................................................................................38
`
`Chamberlain Grp., Inc. v. Techtronic Indus.,
`676 F. App’x 980 (Fed. Cir. 2017) ............................................................................................9
`
`Chef Am., Inc. v. Lamb-Weston, Inc.,
`358 F.3d 1371 (Fed. Cir. 2004)....................................................................................36, 40, 42
`
`Cont’l Circuits LLC v. Intel Corp.,
`915 F.3d 788 (Fed. Cir. 2019)..................................................................................................59
`
`Creative Compounds, LLC v. Starmark Labs Inc.,
`2008 WL 4997185 (S.D. Fla. July 14, 2008) ...........................................................................26
`
`Eli Lilly & Co. v. Genentech, No. 13-07248,
`2015 WL 12672089 (C.D. Cal. Mar. 5, 2015) .............................................................13, 19, 20
`
`Endo Pharm. Inc. v. Mylan Pharm. Inc.,
`2013 WL 4402311 (D. Del. Aug. 7, 2013) ..............................................................................20
`
`Every Penny Counts, Inc. v. Am. Express Co.,
`563 F.3d 1378 (Fed. Cir. 2009)................................................................................................27
`
`Fenner Investments, Ltd. v. Cellco P’ship,
`778 F.3d 1320 (Fed. Cir. 2015)................................................................................................56
`
`GlaxoSmithKline LLC v. Banner Pharmacaps, Inc.,
`744 F.3d 725 (Fed. Cir. 2014)..................................................................................................20
`
`Guardant Health Inc. v. Found. Med., Inc.,
`2019 WL 5677748 (D. Del. Nov. 1, 2019) ..........................................................................9, 18
`
`Hockerson-Halberstadt, Inc. v. Converse Inc.,
`183 F.3d 1369 (Fed. Cir. 1999)................................................................................................38
`
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`Case 1:19-md-02902-RGA Document 136 Filed 07/17/20 Page 5 of 82 PageID #: 1919
`
`
`
`HTC Corp. v. IPCom GmbH & Co.,
`667 F.3d 1270 (Fed. Cir. 2012)................................................................................................58
`
`Innova/Pure Water, Inc. v. Safari Water Filtration Sys.,
`381 F.3d 1111 (Fed. Cir. 2004)................................................................................................16
`
`Intamin Ltd. v. Magnetar Techs., Corp.,
`483 F.3d 1328 (Fed. Cir. 2007)............................................................................................9, 44
`
`Inventio AG v. Thyssenkrupp Elevator Ams. Corp.,
`5 F. Supp. 3d 665 (D. Del. 2013) .......................................................................................39, 41
`
`Kaken Pharmaceutical Co. v. Iancu,
`952 F.3d 1346 (Fed. Cir. 2020)..........................................................................................63, 68
`
`Karlin Tech. Inc. v. Surgical Dynamics, Inc.,
`177 F.3d 968 (Fed. Cir. 1999)..................................................................................................32
`
`Kim v. ConAgra Foods, Inc.,
`465 F.3d 1312 (Fed. Cir. 2006)................................................................................................59
`
`Laitram Corp. v. NEC Corp.,
`62 F.3d 1388 (Fed. Cir. 1995)..............................................................................................8, 18
`
`Lifestream Diagnostics, Inc. v. Polymer Tech. Sys., Inc.,
`109 F. App’x 411 (Fed. Cir. 2004) ..........................................................................................57
`
`Markman v. Westview Instruments, Inc.,
`52 F.3d 967 (Fed. Cir. 1995) (en banc)..............................................................................17, 35
`
`Massachusetts Inst. of Tech. v. Shire Pharm., Inc.,
`839 F.3d 1111 (Fed. Cir. 2016)....................................................................................48, 60, 65
`
`Merck & Co., Inc. v. Teva Pharm. USA, Inc.,
`347 F.3d 1367 (Fed. Cir. 2003)................................................................................................23
`
`Merck & Co. v. Teva Pharm. USA, Inc.,
`395 F.3d 1364 (Fed. Cir. 2005)....................................................................................15, 50, 64
`
`Merck Sharp & Dohme Corp. v. Hospira Inc.,
`221 F. Supp. 3d 497 (D. Del. 2016) .....................................................................................9, 11
`
`Microchip Tech. Inc. v. Aptiv Servs. US, LLC,
`2019 WL 2502417 (D. Del. June 17, 2019) .......................................................................39, 41
`
`Microsoft Corp. v. Multi-Tech Sys., Inc.,
`357 F.3d 1340 (Fed. Cir. 2004)................................................................................................67
`
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`Case 1:19-md-02902-RGA Document 136 Filed 07/17/20 Page 6 of 82 PageID #: 1920
`
`
`
`Mitek Sys., Inc. v. TIS Am. Inc.,
`2014 WL 3891237 (D. Del. Aug. 6, 2014) ........................................................................39, 41
`
`Multilayer Stretch Cling Film Holdings v. Berry Plastics Corp.,
`831 F.3d 1350 (Fed. Cir. 2016)................................................................................................34
`
`Nautilus Inc. v. Biosig Instruments, Inc.,
`572 U.S. 898 (2014) .....................................................................................................33, 34, 37
`
`Novo Indus, L.P. v. Micro Molds Corp.,
`350 F.3d. 1348 (Fed. Cir. 2003)...............................................................................................39
`
`Omega Eng’g, Inc. v. Raytek Corp.,
`334 F.3d 1314 (Fed. Cir. 2003)..........................................................................................52, 58
`
`Pause Tech., LLC v. TiVo, Inc.,
`419 F.3d 1326 (Fed. Cir. 2005)................................................................................................38
`
`Pfizer Inc. v. Apotex, Inc.,
`2019 WL 3369652 (D. Del. June 28, 2019) .............................................................................31
`
`Pfizer Inc. v. Dr. Reddy’s Labs Ltd.,
`2011 WL 767849 (D. Del. Feb. 28, 2011) ...............................................................................32
`
`Pfizer Inc. v. Ranbaxy Labs.,
`457 F.3d 1284 (Fed. Cir. 2006)........................................................................................ passim
`
`Phillips Petroleum Co. v. Huntsman Polymers Corp.,
`157 F.3d 866 (Fed. Cir. 1998)..................................................................................................48
`
`Phillips v. AWH Corp., 415 F.3d 1303
`(Fed. Cir. 2005) ................................................................................................................ passim
`
`Poly-Am., L.P. v. API Indus., Inc.,
`839 F.3d 1131 (Fed. Cir. 2016)................................................................................................66
`
`Power Integrations, Inc. v. ON Semiconductor Corp.,
`396 F. Supp. 3d. 851 (N.D. Cal. 2019) ....................................................................................60
`
`Power Mosfet Techs., L.L.C. v. Siemens AG,
`378 F.3d 1396 (Fed. Cir. 2004)..........................................................................................50, 64
`
`Purdue Pharma LP v. Endo Pharm Inc.,
`438 F.3d 1123 (Fed. Cir. 2006)................................................................................................60
`
`Rambus Inc. v. Infineon Techs AG,
`318 F.3d 1081 (Fed. Cir. 2003)................................................................................................46
`
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`Case 1:19-md-02902-RGA Document 136 Filed 07/17/20 Page 7 of 82 PageID #: 1921
`
`
`
`Ravo v. Covidien LP,
`2014 WL 198551 (W.D. Pa. Jan. 16, 2014) .................................................................17, 18, 23
`
`Regents of Univ. of Cal. v. Dakocytomation Cal., Inc.,
`517 F.3d 1364 (Fed. Cir. 2008)..........................................................................................15, 19
`
`S. Research Inst. v. Abon Pharm. LLC,
`2013 WL 4509925 (D.N.J. Aug. 22, 2013) .............................................................................60
`
`Salazar v. Procter & Gamble Co.,
`414 F.3d 1342 (Fed. Cir. 2005)................................................................................................60
`
`Schumer v. Lab. Computer Sys., Inc.,
`308 F.3d 1304 (Fed. Cir. 2002)..........................................................................................13, 19
`
`Shire ViroPharma Inc. v. CSL Behring LLC,
`2019 WL 266327 (D. Del. Jan. 18, 2019) ..................................................................................9
`
`SimpleAir, Inc. v. Sony Ericsson Mobile Commc’ns AB,
`820 F.3d 419 (Fed. Cir. 2016)..................................................................................................18
`
`Smartflash LLC v. Apple Inc.,
`77 F. Supp. 3d 535 (E.D. Tex. 2014) .......................................................................................41
`
`Spectrum Int’l Inc. v. Sterilite Corp.,
`164 F.3d 1372 (Fed. Cir. 1998)................................................................................................56
`
`Springs Window Fashions LP v. Novo Indus., L.P.,
`323 F.3d 989 (Fed. Cir. 2003)..................................................................................................56
`
`Sprint Comms. v. Comcast IP Holdings, I, LLC,
`2014 WL 309432 (D. Del. Jan. 28, 2014) ..........................................................................37, 40
`
`Sprt, LLC v. B2 Networks, Inc.,
`2011 WL 7640123 (N.D.N.Y. Sept. 1, 2011) ......................................................................9, 14
`
`TecSec, Inc. v. Int’l Business Mach. Corp.,
`731 F.3d 1336 (Fed. Cir. 2013)................................................................................................66
`
`Teleflex, Inc. v. Ficosa N. Am. Corp.,
`299 F.3d 1313 (Fed. Cir. 2002)................................................................................................58
`
`Teva Pharm. USA, Inc. v. Sandoz, Inc.,
`574 U.S. 318 (2015) .................................................................................................................19
`
`Teva Pharm. USA Inc. v. Sandoz, Inc.,
`789 F.3d 1335 (Fed. Cir. 2015)................................................................................................12
`
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`Case 1:19-md-02902-RGA Document 136 Filed 07/17/20 Page 8 of 82 PageID #: 1922
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`
`
`Thorner v. Sony Comput. Entm’t Am. LLC,
`669 F.3d 1362 (Fed. Cir. 2012)................................................................................................60
`
`Tinnus Enters, LLC v. Telebrands Corp.,
`733 F. App’x. 1011 (Fed. Cir. 2018) .......................................................................................38
`
`TorPharm Inc. v. Ranbaxy Pharm., Inc.,
`336 F.3d 1322 (Fed. Cir. 2003)................................................................................................51
`
`ViiV Healthcare Co. v. Lupin Ltd.,
`Case No. 17-1576, D.I. 133 (D. Del. Jan. 9, 2019) ..................................................................33
`
`White v. Dunbar,
`119 U.S. 47 (1886) ...................................................................................................................31
`
`Wyeth LLC, v. Alembic Pharma, Ltd.,
`Case No. 16-cv-1305-RGA, D.I. 98 (D. Del. June 27, 2018) ..................................................26
`
`
`
`STATUTES
`
`37 C.F.R. § 1.75(c)...........................................................................................................................8
`
`35 U.S.C. § 112 ...................................................................................................................... passim
`
`35 USC § 103 .................................................................................................................................68
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`Case 1:19-md-02902-RGA Document 136 Filed 07/17/20 Page 9 of 82 PageID #: 1923
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`
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`I.
`
`MERCK’S INTRODUCTION
`
`This Hatch-Waxman case concerns three anti-diabetic drug products—Januvia®,
`
`Janumet®, and Janumet XR®—containing the active ingredient sitagliptin. Sitagliptin is a
`
`dipeptidyl-peptidase-4 (“DPP-4”) inhibitor, J.A. 1 (’708 Patent), 1:32-48, and was the first DPP-
`
`4 inhibitor approved by the FDA. Sitagliptin works by increasing incretin levels, which
`
`ultimately results in increased insulin levels and decreased blood glucose levels. J.A. 4
`
`(Januvia® Package Insert), 10. Januvia®, Janumet®, and Janumet XR® are approved to
`
`“improve glycemic control in adults with type 2 diabetes mellitus.” Id. at 1.
`
`This briefing concerns claim terms in two of the patents-in-suit.1 U.S. Patent No.
`
`7,326,708 (“the ’708 patent”), J.A. 1, and U.S. Patent No. 8,414,921 (“the ’921 patent”), J.A. 2.
`
`The ’708 patent covers, inter alia, the particular dihydrogenphosphate salt of sitagliptin in a 1:1
`
`stoichiometry and the crystalline monohydrate form of sitagliptin that is used in Januvia®,
`
`Janumet®, and Janumet XR®. The ’921 patent covers, inter alia, formulations of sitagliptin
`
`with another diabetes drug, metformin. Plaintiff Merck Sharp & Dohme Corp. (“Merck”) is the
`
`assignee of the ’708 and ’921 patents.
`
`Fourteen defendant groups filed Abbreviated New Drug Applications seeking to market
`
`generic versions of Januvia®, Janumet®, and/or Janumet XR® before the expiration of one or
`
`both of the ’708 and ’921 patents. Merck has sued all fourteen defendant groups for
`
`
`1 Merck recently amended its Complaint against Teva to allege infringement of a third patent,
`U.S. Patent No. 7,468,459. The Court has entered a Scheduling Order where the claim
`construction briefing related to terms in the claims of the ’459 patent will occur on a separate,
`expedited schedule. No. 19-cv-00318-RGA, D.I. 55 (D. Del. Feb. 18, 2020).
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`
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`infringement of the ’708 patent2 and five defendant groups (Mylan, Macleods, Teva, Watson,
`
`and Sun) for infringement of the ’921 patent.
`
`There are eight claim terms at issue in this Markman proceeding. For each disputed term,
`
`Merck seeks a plain and ordinary meaning, or if necessary, a construction that is supported by
`
`the claim text, the specification, and the prosecution history. By contrast, Defendants’ proposed
`
`constructions seek to read in limitations that are not supported by the claim language or the rest
`
`of the intrinsic record. Defendants’ proposed constructions for the terms in the ’921 patent are
`
`based on a misreading of the prosecution history.
`
`That Defendants’ claim-construction positions lack merit is suggested by the fact that the
`
`Defendants do not present a united claim-construction front. Mylan does not join in any of
`
`Defendants’ proposed constructions and does not separately propose its own constructions for
`
`any of the terms in dispute. And Zydus does not join in Defendants’ proposed construction for
`
`one disputed ’708 patent term and does not separately propose its own construction for that term.
`
`II.
`
`DEFENDANTS’ INTRODUCTION
`
`Claim construction starts with the intrinsic evidence: the claims, the specification, and
`
`the prosecution history. While Defendants’3 constructions are faithful to the intrinsic evidence,
`
`Merck’s are not. Some of Merck’s proposed constructions ignore the plain language of the
`
`claims and instead seek to redraft the claims to cover what Merck wishes it had claimed. Merck
`
`
`2 Merck recently entered into a Consent Judgment with Torrent, Macleods, Accord, Wockhardt,
`and Alvogen thus only ten defendant Groups remain in the litigation. Case Nos. 19-cv-320-
`RGA, D.I. 46 (D. Del. Feb. 19, 2020); 19-cv-872-RGA, D.I. 50 (D. Del. Feb. 19, 2020); 19-cv-
`0316-RGA, D.I. 58 (D. Del. Apr. 28, 2020); 19-cv-2192-RGA, D.I. 28 (D. Del. Mar. 27, 2020);
`19-cv-321-RGA, D.I. 54 (D. Del. May 28, 2020); 19-cv-310-RGA, D.I. 68 (D. Del. July 16,
`2020).
`
`3 Due to the pending IPR in connection with the ’708 patent, Mylan does not join in any of the
`claim constructions.
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`
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`proposes other constructions that ignore both the specification and plain meaning in an attempt to
`
`broaden the claims well beyond what the intrinsic evidence supports. Finally, Merck proposes
`
`several constructions that attempt to recover claim scope that was explicitly surrendered during
`
`prosecution. For all of these reasons, Defendants respectfully request that the Court adopt
`
`Defendants’ proposed constructions.
`
`III. MERCKS’S PERSON OF ORDINARY SKILL
`
`For the ’708 patent, the person of ordinary skill in the art (“POSA”) would have had a
`
`doctoral degree in chemistry, chemical engineering or a related field, with at least two years of
`
`laboratory experience working with pharmaceutical solids, including polymorphic forms, or
`
`would have had a master’s or bachelor’s degree in a similar field of study, with a commensurate
`
`increase in their years of post-graduate experience. Such a person also would have been familiar
`
`with a variety of issues relevant to developing pharmaceutical solids, including, among other
`
`things, analytical characterization techniques and pharmaceutical formulations. J.A. 3
`
`(“Myerson Decl.”), ¶55.
`
`IV. DEFENDANTS’ PERSON OF ORDINARY SKILL
`
`For the ’708 patent, the POSA would include a person having a doctoral degree in
`
`pharmaceutical sciences, a field of chemistry relating to physical form of crystals or drug
`
`delivery, or a related field with at least two years’ experience working with solid state materials
`
`for pharmaceuticals, including characterization thereof, in relation to the development of
`
`pharmaceutical formulations. A POSA may have an education level lower than a doctoral
`
`degree in pharmaceutical sciences, chemistry, or a related field if he or she has commensurately
`
`more relevant work experience. A POSA may also work as part of a multi-disciplinary team and
`
`draw upon not only his or her own skills, but also consult with others team members having
`
`specialized skills, to solve a given problem.
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`Case 1:19-md-02902-RGA Document 136 Filed 07/17/20 Page 12 of 82 PageID #: 1926
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`
`
`V.
`
`REPRESENTATIVE CLAIMS
`
`A.
`
`’708 Patent
`
`1.
`
`Claim 1
`
`A dihydrogenphosphate salt of 4-oxo-4-[3-(trifluoromethyl)-5,6-
`dihydro[1,2,4]triazolo[4,3-a]pyrazin-7 (8H)-yl]-l-(2,4,5-
`trifluorophenyl)butan-2-amine of structural formula I:
`
`
`
`or a hydrate thereof
`
`2.
`
`Claim 2
`
`The salt of claim 1 of structural formula II having the (R)-
`configuration at the chiral center marked with an *
`
`3.
`
`Claim 4
`
`“The salt of claim 2 characterized in being a crystalline
`monohydrate.”
`
`
`
`4.
`
`Claim 5
`
`“The salt of claim 4 characterized by characteristic absorption
`bands obtained from the X-ray powder diffraction pattern at
`spectral d-spacings of 7.42, 5.48, and 3.96 angstroms.”
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`4
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`Case 1:19-md-02902-RGA Document 136 Filed 07/17/20 Page 13 of 82 PageID #: 1927
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`
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`5.
`
`Claim 24
`
`(a) Crystallizing the dihydrogenphosphate salt of structural
`formula (II):
`
`
`at 25°C. from a mixture of isopropanol and water, such that the
`water concentration is above 6.8 weight percent;
`
`(b) recovering the resultant solid phase; and
`
`(c) removing the solvent therefrom.
`
`B.
`
`’921 Patent
`
`1.
`
`Claim 1
`
`A pharmaceutical composition comprising:
`(a) about 3 to 20% by weight of sitagliptin, or a pharmaceutically
`acceptable salt thereof;
`(b) about 25 to 94% by weight of metformin hydrochloride;
`(c) about 0.1 to 10% by weight of a lubricant;
`(d) about 0 to 35% by weight of a binding agent;
`(e) about 0.5 to 1 % by weight of a surfactant; and
`(f) about 5 to 15% by weight of a diluent.
`
`2.
`
`Claim 11
`
`The pharmaceutical composition of claim 10 wherein said
`lubricant is sodium stearyl fumarate, said binding agent is
`polyvinylpyrrolidone, said diluent is microcrystalline cellulose,
`and said surfactant is sodium lauryl sulfate.
`
`3.
`
`Claim 22
`
`A pharmaceutical composition in the form of a tablet
`comprising:
`a) 64.25 mg[*] of sitagliptin phosphate monohydrate, which is
`equivalent to 50 mg of sitagliptin free base anhydrate;
`b) 500 mg of metformin hydrochloride;
`c) 48.2 mg of polyvinylpyrrolidone;
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`Case 1:19-md-02902-RGA Document 136 Filed 07/17/20 Page 14 of 82 PageID #: 1928
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`d) 3.45 mg of sodium lauryl sulfate;
`e) 59.3 mg of microcrystalline cellulose;
`f) 13.8 mg of sodium stearyl fumarate; and
`g) 17 .2 mg of a film coating.
`
`
`VI. AGREED-UPON CONSTRUCTIONS
`
`The parties do not have any agreed-upon constructions.
`
`VII. DISPUTED CLAIM TERMS
`
`A.
`
`’708 Patent
`
`1.
`
`“the salt of claim 1 [or 2] . . .” (claims 2, 3, and 21)
`
`Merck
`Does not exclude hydrates.
`
`
`Defendants (excluding Mylan and Zydus)
`Excludes hydrates of the claimed salt.
`
`a.
`
`Merck’s Opening Position
`
`Ignoring the claim language, the specification, the prosecution history, and even their
`
`own statements, Defendants contend that claims 2, 3, and 21 of the ’708 patent exclude hydrates.
`
`Defendants’ only apparent reason for pressing this unsupported reading is to manufacture an
`
`improper dependency argument. The Court, as it has before in similar circumstances, should
`
`reject Defendants’ construction and find that these claims do not exclude hydrates.
`
`Claim 1 recites:
`
`A dihydrogenphosphate salt of 4-oxo-4-[3-(trifluoromethyl)-5,6-
`dihydro[1,2,4]triazolo[4,3-a]pyrazin-7 (8H)-yl]-l-(2,4,5-
`trifluorophenyl)butan-2-amine of structural formula I:
`
`
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`Case 1:19-md-02902-RGA Document 136 Filed 07/17/20 Page 15 of 82 PageID #: 1929
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`
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`or a hydrate thereof.4
`
`Claim 2, in turn, recites:
`
`The salt of claim 1 of structural formula II having the (R)-
`configuration at the chiral center marked with an *
`
`
`
`While not itself being construed, the language of claim 4 provides additional context for
`
`this dispute: “The salt of claim 2 characterized in being a crystalline monohydrate.”
`
`Claim 1, therefore, covers the dihydrogenphosphate salt of the recited compound, or
`
`hydrates thereof, irrespective of stereochemistry, whereas claim 2 requires that the compound of
`
`claim 1 have the enantiomeric (R)-configuration.5 The compound with the (R)-configuration is
`
`sitagliptin. Claim 3 is similar, except that it imposes a limitation requiring the (S)-configuration.
`
`And claim 21 recites a process for preparing “the salt of claim 2 comprising the step of
`
`contacting one equivalent of [sitagliptin] in an organic solvent or aqueous organic solvent with
`
`about a one equivalent of phosphoric acid at a temperature in the range of about 25-100ºC.” Id.,
`
`claim 21.
`
`
`4 A pharmaceutical salt is a combination of a drug with a counter-ion to form a neutral complex.
`In this case, the drug or free-base is 4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-
`a]pyrazin-7 (8H)-yl]-l-(2,4,5-trifluorophenyl)butan-2-amine, illustrated as the three-ring
`structure in structural formula I, and the counter-ion is phosphoric acid, H3PO4. J.A. 3 (Myerson
`Decl.), at ¶¶28-29.
`
`5 Enantiomers are a pair of compounds that have the same molecular formula but different
`spatial arrangements around a chiral center that are non-superimposable mirror images of each
`other. J.A. 3 (Myerson Decl.), ¶¶22-24.
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`Case 1:19-md-02902-RGA Document 136 Filed 07/17/20 Page 16 of 82 PageID #: 1930
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`
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`1)
`
`The Claim Language
`
`The starting point for claim construction is the language of the claims themselves. See
`
`e.g., Phillips v. AWH Corp., 415 F.3d 1303, 1321 (Fed. Cir. 2005). When interpreting dependent
`
`claims, the statute provides that such claims “shall be construed to incorporate by reference all
`
`the limitations of the claim to which it refers.” 35 U.S.C. § 112(4); 37 C.F.R. § 1.75(c).
`
`Applying this principle, the language “the salt of claim 1” in dependent claims 2 and 3 refers to
`
`claim 1 and should be construed to incorporate all its limitations, including the limitations to the
`
`dihydrogenphosphate salt of the depicted chemical