Case 1:19-cv-00101-TSK Document 123 Filed 11/17/21 Page 1 of 19 PageID #: 8507
`
`IN THE UNITED STATES DISTRICT COURT
`FOR THE NORTHERN DISTRICT OF WEST VIRGINIA
`AT CLARKSBURG
`
`
`
`
`
`
`
`C.A. No. 1:19-cv-00101 (IMK)
`
`
`MERCK SHARP & DOHME CORP.,
`
`
`
`Plaintiff,
`
`
`
`MYLAN PHARMACEUTICALS INC.,
`
`
`
`
`v.
`
`
`
`Defendant.
`
`
`STIPULATIONS OF FACT
`
`
`Pursuant to the Court’s Scheduling Order dated August 30, 2021, and for the purpose of
`
`this case only (which shall not be used for any other proceeding, including any appeal
`
`concerning IPR2020-00040 and/or before the PTAB),1 the parties stipulate to the following facts,
`
`which require no proof at trial:
`
`I.
`
`PARTIES
`
`1.
`
`Plaintiff Merck Sharp & Dohme Corp. (“Merck”) is a corporation organized and
`
`existing under the laws of the State of New Jersey, having its corporate offices and principal
`
`place of business at One Merck Drive, Whitehouse Station, New Jersey 08889.
`
`2.
`
`Defendant Mylan Pharmaceuticals Inc. (“Mylan”) is a corporation organized and
`
`existing under the laws of the State of West Virginia, having its corporate offices and a place of
`
`business at 781 Chestnut Ridge Road, Morgantown, West Virginia 26505.
`
`
`1 Neither party will use nor refer to any stipulated fact(s) herein before the PTAB or the Federal
`Circuit in connection with IPR2020-00040 or any appeal of IPR2020-00040. Both sides may
`refer to this document in any appeal from this Action.
`
`1
`
`

`

`Case 1:19-cv-00101-TSK Document 123 Filed 11/17/21 Page 2 of 19 PageID #: 8508
`
`II. MERCK’S PRODUCTS
`
`3.
`
`Merck is the holder of New Drug Application (“NDA”) No. 21995 for
`
`JANUVIA®, which has been approved by the U.S. Food and Drug Administration (“FDA”).
`
`4.
`
`Merck is the holder of NDA No. 22044 for JANUMET®, which has been
`
`approved by the FDA.
`
`5.
`
`JANUVIA® and JANUMET® are indicated as an adjunct to diet and exercise to
`
`improve glycemic control in adults with type 2 diabetes mellitus.
`
`6.
`
`Sitagliptin is an orally active inhibitor of the dipeptidyl peptidase (DPP-4)
`
`enzyme.
`
`7.
`
` JANUVIA® and JANUMET® contain as an active pharmaceutical ingredient the
`
`(R)-enantiomer of 1:1 sitagliptin phosphate monohydrate, which is known chemically as 7-[(3R)-
`
`3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-
`
`triazolo[4,3-a]pyrazine phosphate (1:1) monohydrate.
`
`III.
`
`PATENTS-IN-SUIT
`
`A.
`
`8.
`
`The ’708 Patent
`
`U.S. Patent No. 7,3626,708 (“the ’708 patent”) was issued by the U.S. Patent &
`
`Trademark Office on February 5, 2008.
`
`9.
`
`The title of the ’708 patent is “PHOSPHORIC ACID SALT OF A DIPEPTIDYL
`
`PEPTIDASE-IV INHIBITOR.”
`
`10.
`
`The ’708 patent lists Stephen Howard Cypes, Alex Minhua Chen, Russell R.
`
`Ferlita, Karl Hansen, Ivan Lee, Vicky K. Vydra, and Robert M. Wenslow, Jr. as the inventors.
`
`11.
`
`The ’708 patent issued from U.S. Patent Application No. 10/874,992, which was
`
`filed on June 23, 2004.
`
`2
`
`

`

`Case 1:19-cv-00101-TSK Document 123 Filed 11/17/21 Page 3 of 19 PageID #: 8509
`
`12.
`
`The ’708 patent claims priority and/or benefit to U.S. Provisional Application No.
`
`60/482,161, which was filed on June 24, 2003.
`
`13. Merck is the owner and assignee of the ’708 patent.
`
`14.
`
`The ’708 patent has been listed in connection with JANUVIA® and JANUMET®
`
`in the FDA’s Approved Drug Products with Therapeutic Equivalence Evaluations (“Orange
`
`Book”).2
`
`15.
`
`The Orange Book lists the expiration date of the ’708 patent, excluding pediatric
`
`exclusivity, as November 24, 2026.
`
`16.
`
`The Orange Book lists the expiration date of the ’708 patent, inclusive of pediatric
`
`exclusivity, as May 24, 2027.
`
`17.
`
`At the time of this stipulation, Merck is asserting each of claims 1–7 and 19 of the
`
`’708 patent against Mylan.
`
`B.
`
`18.
`
`The ’921 Patent
`
`U.S. Patent No. 8,414,921 (“the ’921 patent”) was issued by the U.S. Patent &
`
`Trademark Office on April 9, 2013.
`
`19.
`
`The title of the ’921 patent is “PHARMACEUTICAL COMPOSITIONS OF
`
`COMBINATIONS OF DIPEPTIDYL PEPTIDASE-4 INHIBITORS WITH METFORMIN.”
`
`20.
`
`The ’921 patent lists Ashkan Kamali, Laman Alani, Kyle A. Fliszar, Soumojeet
`
`Ghosh, and Monica Tijerina as the inventors.
`
`
`2 Merck is also the holder of NDA No. 202270 for JANUMET® XR, which has been approved
`by the FDA. The ’708 patent has also been listed in connection with JANUMET® XR in the
`FDA’s Orange Book.
`
`3
`
`

`

`Case 1:19-cv-00101-TSK Document 123 Filed 11/17/21 Page 4 of 19 PageID #: 8510
`
`21.
`
`The ’921 patent issued from U.S. Patent Application No. 12/085,722, which is the
`
`national stage entry under 35 U.S.C. § 371 of international application PCT/US2006/047380,
`
`filed on May 29, 2008.
`
`22.
`
`The ’921 patent claims priority and/or benefit to U.S. Provisional Application No.
`
`60/750,954 filed on December 16, 2005.
`
`23. Merck is the owner and assignee of the ’921 patent.
`
`24.
`
`The ’921 patent has been listed in connection with JANUMET® in the FDA’s
`
`Orange Book.
`
`25.
`
`The Orange Book lists the expiration date of the ’921 patent, excluding pediatric
`
`exclusivity, as July 21, 2028.
`
`26.
`
`The Orange Book lists the expiration date of the ’921 patent, inclusive of pediatric
`
`exclusivity, as January 21, 2029.
`
`27.
`
`At the time of this stipulation, Merck is asserting claim 1 of the ’921 patent
`
`against Mylan.
`
`IV. ASSERTED CLAIMS
`
`A.
`
`28.
`
`’708 Patent
`
`Claim 1 of the ’708 patent recites the following:
`
`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:
`
`
`
`4
`
`

`

`Case 1:19-cv-00101-TSK Document 123 Filed 11/17/21 Page 5 of 19 PageID #: 8511
`
`or a hydrate thereof.
`
`
`
`29.
`
`Claim 2 of the ’708 patent recites the following:
`
`The salt of claim 1 of structural formula II having the (R)-
`configuration at the chiral center marked with an *
`
`
`Claim 3 of the ’708 patent recites the following:
`
`30.
`
`The salt of claim 1 of structural formula III having the (S)-
`configuration at the chiral center marked with an *
`
`
`Claim 4 of the ’708 patent recites the following:
`
`31.
`
`The salt of claim 2 characterized in being a crystalline
`monohydrate.
`
`32.
`
`Claim 5 of the ’708 patent recites the following:
`
`
`
`
`
`The salt of claim 4 characterized by characteristic diffraction peaks
`obtained from the X-ray powder diffraction pattern corresponding
`to d-spacings of 7.42, 5.48, and 3.96 angstroms.
`
`5
`
`

`

`Case 1:19-cv-00101-TSK Document 123 Filed 11/17/21 Page 6 of 19 PageID #: 8512
`
`33.
`
`Claim 6 of the ’708 patent recites the following:
`
`The salt of claim 5 further characterized by characteristic
`diffraction peaks obtained from the X-ray powder diffraction
`pattern corresponding to d-spacings of 6.30, 4.75, and 4.48
`angstroms.
`
`34.
`
`Claim 7 of the ’708 patent recites the following:
`
`The salt of claim 6 further characterized by characteristic
`diffraction peaks obtained from the X-ray powder diffraction
`pattern corresponding to d-spacings of 5.85, 5.21, and 3.52
`angstroms.
`
`35.
`
`Claim 19 of the ’708 patent recites the following:
`
`A method for the treatment of type 2 diabetes comprising
`administering to a patient in need of such treatment a
`therapeutically effective amount of the salt according to claim 2 or
`a hydrate thereof.
`
`36. Merck is not asserting infringement of the ’708 patent under any theory of
`
`doctrine of equivalents.
`
`37. Mylan is not contesting infringement of any of claims 1, 2, or 19 of the ’708
`
`patent.3
`
`38. Mylan is not asserting invalidity of any of claims 4–7 of the ’708 patent.
`
`B.
`
`39.
`
`’921 Patent
`
`Claim 1 of the ’921 patent recites the following:
`
`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.
`
`
`3 The parties are presently working on a separate infringement stipulation that will be submitted
`at a later date.
`
`6
`
`

`

`Case 1:19-cv-00101-TSK Document 123 Filed 11/17/21 Page 7 of 19 PageID #: 8513
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`40. Merck is not asserting infringement of claim 1 of the ’921 patent under any theory
`
`under the doctrine of equivalents for the limitation “about 0.5 to 1% by weight of a surfactant.”
`
`41. Mylan is not asserting invalidity of any claim of the ’921 patent.
`
`V.
`
`RELATED PROCEEDINGS
`
`A. Multidistrict Litigation
`
`42.
`
`This action was transferred on August 9, 2019, to the United States District Court
`
`for the District of Delaware and assigned to Judge Richard G. Andrews as part of MDL No. 19-
`
`2902 for coordinated and consolidated pretrial proceedings. Dkt. No. 49.
`
`43.
`
`On August 20, 2021, the United States District Court for the District of Delaware
`
`advised the Judicial Panel on Multidistrict Litigation that coordinated and consolidated pretrial
`
`proceedings had been completed and this was action was remanded to this Court. Dkt. No. 71.
`
`The jointly designated record on remand of the pretrial proceedings that took place before the
`
`United States District Court for the District of Delaware are present in Docket Nos. 77, 83, 84,
`
`86, 91, 92, 93, 94, and 95.
`
`B.
`
`44.
`
`Inter Partes Review
`
`Claims 1–4, 17, 19, and 21–23 of the ’708 patent were the subject of a petition for
`
`inter partes review (“IPR”) submitted by Mylan to the Patent Trial & Appeal Board requesting
`
`that the Board cancel those claims as either anticipated under 35 U.S.C. § 102 and/or obvious
`
`under 35 U.S.C. § 103.
`
`45.
`
`In its IPR petition, Mylan asserted the following grounds of invalidity concerning
`
`certain claims of the ’708 patent:
`
`a.
`
`Claims 1–3, 17, 19, and 21–23 are unpatentable as anticipated under 35 U.S.C.
`§ 102 over WO 03/004498 (“WO ’498,” DEFS-JANUMET_00000785).
`
`7
`
`

`

`Case 1:19-cv-00101-TSK Document 123 Filed 11/17/21 Page 8 of 19 PageID #: 8514
`
`b.
`
`c.
`
`d.
`
`e.
`
`f.
`
`Claims 1–3, 17, 19, and 21–23 are unpatentable as anticipated under 35 U.S.C.
`§ 102 over U.S. Patent No. 6,699,871 (“the ’871 patent,” DEFS-
`JANUMET_00000743).
`
`Claims 3, 17, 19, and 21–23 are unpatentable as obvious under 35 U.S.C. § 103
`over WO ’498.
`
`Claims 1–3, 17, 19, and 21–23 are unpatentable as obvious under 35 U.S.C. § 103
`over WO ’498 and Bastin (DEFS-JANUMET_00000044).
`
`Claim 4 is unpatentable as obvious under 35 U.S.C. § 103 over WO ’498, Bastin,
`and Brittain (DEFS-JANUMET_00001107).
`
`Claim 4 is unpatentable as obvious under 35 U.S.C. § 103 over WO ’498 and
`Brittain.
`
`46.
`
`On May 7, 2021, the Board entered a final written decision pursuant to 35 U.S.C.
`
`§ 318(a) holding that Mylan had failed to prove by a preponderance of the evidence that claims
`
`1–4, 17, 19, and 21–23 of the ’708 patent are unpatentable. See Mylan Pharms. Inc. v. Merck
`
`Sharp & Dohme Corp., IPR2020-00040, 2021 WL 1833325 (P.T.A.B. May 7, 2021).
`
`47. Mylan has appealed the Board’s final written decision. Mylan Pharms. Inc. v.
`
`Merck Sharp & Dohme Corp., No. 21-2121 (Fed. Cir.).
`
`VI. CLAIM CONSTRUCTION
`
`48.
`
`The following terms of the asserted claims were construed by the United States
`
`District for the District of Delaware as part of the consolidated and coordinated pretrial
`
`proceedings in MDL No. 19-2902. Dkt. No. 93-20.
`
`A.
`
`“crystalline monohydrate [of the dihydrogenphosphate salt of sitagliptin]”
`(’708 patent, claims 4 and 24)
`
`49.
`
`The term “crystalline monohydrate [of the dihydrogenphosphate salt of
`
`sitagliptin]” in claims 4 and 24 of the ’708 patent were construed as “a repeating unit cell
`
`incorporating a 1:1 ratio of water to a dihydrogenphosphate salt of sitagliptin.”
`
`8
`
`

`

`Case 1:19-cv-00101-TSK Document 123 Filed 11/17/21 Page 9 of 19 PageID #: 8515
`
`B.
`
`50.
`
`“the salt of claim 1 [or 2]” (’708 patent, claims 2, 3, and 21)
`
`The term “the salt of claim 1 [or 2]” in claims 2, 3, and 21 of the ’708 patent was
`
`construed not to exclude hydrates.
`
`C.
`
`51.
`
`“surfactant” (’921 patent, claims 1 and 21)
`
`The term “surfactant” in claims 1 and 21 of the ’921 patent was construed as
`
`“surfactant that works as a wetting agent to increase the dissolution of sitagliptin.”
`
`D.
`
`52.
`
`“sitagliptin” (’921 patent, claim 1)
`
`The term “sitagliptin” in claim 1 of the ’921 patent was construed as “sitagliptin.”
`
`*
`
`*
`
`*
`
`53.
`
`In addition to the claim terms above, the term “characteristic absorption bands
`
`obtained from the X-ray powder diffraction pattern at spectral d-spacings of,” which was
`
`previously recited in claims 5–7 of the ’708 patent, were construed as indefinite. See Dtk. No.
`
`93-20 at 7. The U.S. Patent & Trademark subsequently issued a certificate of correction for the
`
`’708 patent on February 9, 2021, to replace the term “absorption bands obtained from the X-ray
`
`powder diffraction pattern at spectral” with “diffraction peaks obtained from the X-ray powder
`
`diffraction pattern corresponding to” in claims 5–7. See Dkt. Nos. 94-9, 94-15.
`
`VII. THE ’871 PATENT
`
`54.
`
`U.S. Patent No. 6,699,871 (“the ’871 patent”) was issued by the U.S. Patent &
`
`Trademark Office on March 2, 2004.
`
`55.
`
`The title of the ’871 patent is “BETA-AMINO HETEROCYCLIC DIPEPTIDYL
`
`PEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES.”
`
`56.
`
`The ’871 patent issued from U.S. Patent Application No. 10/189,603, which was
`
`filed on July 5, 2002.
`
`9
`
`

`

`Case 1:19-cv-00101-TSK Document 123 Filed 11/17/21 Page 10 of 19 PageID #: 8516
`
`57.
`
`The ’871 patent claims priority and/or benefit to U.S. Provisional Application No.
`
`60/303,474, which was filed on July 6, 2001.
`
`58.
`
`The ’871 patent has been listed in connection with JANUVIA® and JANUMET®
`
`in the FDA’s Orange Book.
`
`59.
`
`The Orange Book lists the expiration date of the ’871 patent, excluding pediatric
`
`exclusivity, as July 26, 2022.
`
`60.
`
`The Orange Book lists the expiration date of the ’871 patent, inclusive of pediatric
`
`exclusivity, as January, 26, 2023.
`
`61.
`
`Claim 17 of the ’871 patent recites:
`
`A compound which is:
`
`or a pharmaceutically acceptable salt thereof.
`
`62.
`
`Claim 20 of the ’871 patent recites:
`
`
`
`A pharmaceutical composition which comprises an inert carrier
`and a compound of claim 16.
`
`Through a Certificate of Correction, claim 20 of the ’871 patent does not depend
`
`63.
`
`from claim 16 as originally recited but now depends from claim 17.
`
`VIII. THE ’528 PUBLICATION
`
`64.
`
`Robert M. Wenslow, Joseph D. Armstrong III, Alex M. Chen, Stephen Cypes,
`
`Russell R. Ferlita, Karl Hansen, Christopher Lindemann, Evangelia Spartalis are the named
`
`10
`
`

`

`Case 1:19-cv-00101-TSK Document 123 Filed 11/17/21 Page 11 of 19 PageID #: 8517
`
`inventors of U.S. Patent Application Number 10/569,566, published as Patent Application
`
`Publication No. 2006/0287528 (“the ’528 publication”), entitled “Novel crystalline forms of a
`
`phosphoric acid salt of a dipeptidyl peptidase-IV inhibitor.”
`
`65.
`
`The ’528 publication claims priority and/or benefit to U.S. Provisional
`
`Application No. 60/499,629, which was filed on September 2, 2003.
`
`66.
`
`On March 18, 2008, the U.S. Patent & Trademark Office issued a Notice of
`
`Abandonment in U.S. Patent Application Number 10/569,566 due to Applicant’s failure to
`
`timely pay the required issue fee and publication fee, if applicable, within the statutory period of
`
`three months from the mailing date of the Notice of Allowance, which was mailed on November
`
`21, 2007.
`
`IX. MYLAN’S ANDA PRODUCTS
`
`67. Mylan submitted ANDA No. 202473 (“Mylan’s JANUVIA ANDA”) to the FDA
`
`seeking approval to commercially manufacture, use, offer for sale, sell, and/or import generic
`
`versions of Merck’s JANUVIA® (“Mylan’s JANUVIA ANDA Products”) prior to the expiration
`
`of the ’708 patent.
`
`68. Mylan submitted ANDA No. 202478 (“Mylan’s JANUMET ANDA,” and
`
`collectively with Mylan’s JANUVIA ANDA, “Mylan’s ANDAs”) to the FDA seeking approval
`
`to commercially manufacture, use, offer for sale, sell, and/or import generic versions of Merck’s
`
`JANUMET® (“Mylan’s JANUMET ANDA Products,” and collectively with Mylan’s
`
`JANUVIA ANDA Products, “Mylan’s ANDA Products”) prior to the expiration of the ’708 and
`
`’921 patents. Mylan notified Merck that Mylan’s ANDAs contain certifications described in
`
`Section 505(j)(2)(A)(vii)(IV) of the Federal Food Drug and Cosmetic Act, 21 U.S.C.
`
`§ 355(j)(2)(A)(vii)(IV) (“Paragraph IV certifications”) with respect to the ’708 and ’921 patents,
`
`11
`
`

`

`Case 1:19-cv-00101-TSK Document 123 Filed 11/17/21 Page 12 of 19 PageID #: 8518
`
`asserting that the ’708 and ’921 patents are invalid, unenforceable, and/or will not be infringed
`
`by the manufacture, use, offer for sale, sale, and/or importation of Mylan’s ANDA Products.
`
`X.
`
`PRIORITY DATE
`
`A.
`
`The ’708 patent
`
`69. Merck reduced to practice an anhydrous form of 1:1 sitagliptin
`
`dihydrogenphosphate, within the scope of claims 1 and 2 of the ’708 patent, prior to January 16,
`
`2003, and by no later than February 2002. See, e.g., Vydra IPR Decl. (MRK-STG-02029572);
`
`Hansen IPR Decl. (MRK-STG-02031996); Shultz IPR Decl. (MRK-STG-02032532); Myerson
`
`Rep. ¶¶ 212–219, 234–235 (Apr. 16, 2021); Mylan Pharms. Inc. v. Merck Sharp & Dohme
`
`Corp., IPR2020-00040, Paper 91 at 43–52, 2021 WL 1833325 (P.T.A.B. May 7, 2021).
`
`70. Merck reduced to practice an anhydrous form of the (S)-configuration of 1:1
`
`sitagliptin dihydrogenphosphate, within the scope of claim 3 of the ’708 patent, prior to January
`
`16, 2003, and by no later than March 2002. See, e.g., MRK-STG-01944132 (Lab Notebook
`
`70316) at *1944328, *1944494–95, *1944631; MRK-STG-01897287; MRK-STG-02017099;
`
`Myerson Rep. ¶¶ 220–221 (Apr. 16, 2021).
`
`71. Merck reduced to practice a method for the treatment of type 2 diabetes using an
`
`anhydrous form of 1:1 sitagliptin dihydrogenphosphate within the scope of claim 19 of the ’708
`
`patent prior to January 16, 2003, and by no later than December 2002. The inventors of the ’708
`
`patent had conceived of a method for the treatment of type 2 diabetes within the scope of claim
`
`19 of the ’708 patent by April 2002 and worked with reasonably continuous diligence to reduce
`
`that invention to practice. See, e.g., Myerson Rep. ¶¶ 231–233 (Apr. 16, 2021); Bloomgarden
`
`Rep. ¶¶ 31–51 (Apr. 16, 2021); Mylan Pharms. Inc. v. Merck Sharp & Dohme Corp., IPR2020-
`
`00040, Paper 91 at 43–52, 2021 WL 1833325 (P.T.A.B. May 7, 2021).
`
`12
`
`

`

`Case 1:19-cv-00101-TSK Document 123 Filed 11/17/21 Page 13 of 19 PageID #: 8519
`
`72.
`
`The crystalline monohydrate of the 1:1 DHP salt of sitagliptin was first created in
`
`March 2003. Wenslow Second IPR Declaration ¶ 27. Just prior to the monohydrate’s synthesis,
`
`three anhydrous forms had been identified and characterized: Form I, Form II, and Form
`
`III. Wenslow Second IPR Declaration ¶ 28. Anhydrous Forms I, II, and III were not publicly
`
`disclosed before the filing on June 24, 2003 of U.S. Provisional Application No. 60/482,161, to
`
`which the ’708 patent claims priority and/or benefit.
`
`73. WO ’498 (DEFS-JANUMET_00000785) is not prior art to claims 1–3 or 19 of
`
`the ’708 patent pursuant to 35 U.S.C. § 102(a). WO ’498 (DEFS-JANUMET_00000785) is prior
`
`art to claims 1–3 and 19 of the ’708 patent pursuant to 35 U.S.C. § 102(e).
`
`74.
`
`Brittain 2002 (DEFS-JANUMET_00000228) is not prior art to claims 1–3 or 19
`
`of the ’708 patent pursuant to 35 U.S.C. § 102(a).
`
`75.
`
`Ohannesian (DEFS-JANUMET_00000295) is not prior art to claims 1–3 or 19 of
`
`the ’708 patent pursuant to 35 U.S.C. § 102(a).
`
`76.
`
`EP ’036 (DEFS-JANUMET_00001211) is prior art to claims 1–3 and/or 19 of the
`
`’708 patent.
`
`77.
`
`Berge (DEFS-JANUMET_00000053) is prior art to claims 1–3 and/or 19 of the
`
`’708 patent.
`
`78.
`
`Gould (DEFS-JANUMET_00000252) is prior art to claims 1–3 and/or 19 of the
`
`’708 patent.
`
`79.
`
` Morris (DEFS-JANUMET_00000286) is prior art to claims 1–3 and/or 19 of the
`
`’708 patent.
`
`80.
`
`Shanker (DEFS-JANUMET_00000318) is prior art to claims 1–3 and/or 19 of the
`
`’708 patent.
`
`13
`
`

`

`Case 1:19-cv-00101-TSK Document 123 Filed 11/17/21 Page 14 of 19 PageID #: 8520
`
`81.
`
`Byrn (DEFS-JANUMET_00000242) is prior art to claims 1–3 and/or 19 of the
`
`’708 patent.
`
`82.
`
`Bighley (DEFS-JANUMET_00000072) is prior art to claims 1–3 and/or 19 of the
`
`’708 patent.
`
`83.
`
`Tong (DEFS-JANUMET_00000592) is prior art to claims 1–3 and/or 19 of the
`
`’708 patent.
`
`84.
`
`Rohloff (DEFS-JANUMET_00001261) is prior art to claims 1–3 and/or 19 of the
`
`’708 patent.
`
`85.
`
`Brittain 1999 (DEFS-JANUMET_00000121, DEFS-JANUMET_00000181,
`
`DEFS-JANUMET_00001107) is prior art to claims 1–3 and/or 19 of the ’708 patent.
`
`86.
`
`FDA Polymorphism Guidance 2000 (DEFS-JANUMET_00001238) is prior art to
`
`claims 1–3 and/or 19 of the ’708 patent.
`
`87.
`
`Aulton 1998 (D.I. 136, J.A. Ex. 43) is prior art to claims 1–3 and/or 19 of the ’708
`
`patent.
`
`88.
`
`Vippagunta (DEFS-JANUMET_00001267) is prior art to claims 1–3 and/or 19 of
`
`the ’708 patent.
`
`89.
`
`Bastin (DEFS-JANUMET_00000044) is prior art to claims 1–3 and/or 19 of the
`
`’708 patent.
`
`90.
`
`Zhang (DEFS-JANUMET_00001849) is prior art to claims 1–3 and/or 19 of the
`
`’708 patent.
`
`91. Moller (DEFS-JANUMET_00001433) is prior art to claims 1–3 and/or 19 of the
`
`’708 patent.
`
`14
`
`

`

`Case 1:19-cv-00101-TSK Document 123 Filed 11/17/21 Page 15 of 19 PageID #: 8521
`
`92.
`
`’468 Patent (DEFS-JANUMET_00001601) is prior art to claims 1–3 and/or 19 of
`
`the ’708 patent.
`
`93.
`
`1992 FDA Policy Statement (DEFS-JANUMET_00001294) is prior art to claims
`
`1–3 and/or 19 of the ’708 patent.
`
`94.
`
`Zhu (DEFS-JANUMET_00001856) is prior art to claims 1–3 and/or 19 of the
`
`’708 patent.
`
`95.
`
`Stahl (DEFS-JANUMET_00000363) is prior art to claims 1–3 and/or 19 of the
`
`’708 patent.
`
`96.
`
`Demuth (MRK-STG-02031570) is prior art to claims 1–3 and/or 19 of the ’708
`
`patent.
`
`97.
`
`Rothenberg (MRK-STG-02031593) is prior art to claims 1–3 and/or 19 of the
`
`’708 patent.
`
`98.
`
`Davies (MRK-STG-02033939) is prior art to claims 1–3 and/or 19 of the ’708
`
`patent.
`
`patent.
`
`patent.
`
`patent.
`
`99.
`
`Rocco (MRK-STG-02033340) is prior art to claims 1–3 and/or 19 of the ’708
`
`100. Poole (MRK-STG-02033349) is prior art to claims 1–3 and/or 19 of the ’708
`
`101. Kobayashi (MRK-STG-02033353) is prior art to claims 1–3 and/or 19 of the ’708
`
`102. U.S. Patent No. 5,939,560 (MRK-STG-02033628) is prior art to claims 1–3
`
`and/or 19 of the ’708 patent.
`
`15
`
`

`

`Case 1:19-cv-00101-TSK Document 123 Filed 11/17/21 Page 16 of 19 PageID #: 8522
`
`103. U.S. Patent No. 6,124,305 (MRK-STG-02033812) is prior art to claims 1–3
`
`and/or 19 of the ’708 patent.
`
`104. Ellin (MRK-STG-02036029) is prior art to claims 1–3 and/or 19 of the ’708
`
`patent.
`
`patent.
`
`patent.
`
`patent.
`
`patent.
`
`patent.
`
`105. Koehler (MRK-STG-02036037) is prior art to claims 1–3 and/or 19 of the ’708
`
`106. Walton (MRK-STG-02036039) is prior art to claims 1–3 and/or 19 of the ’708
`
`107.
`
`Jones (MRK-STG-02559961) is prior art to claims 1–3 and/or 19 of the ’708
`
`108. Morris (MRK-STG-02033363) is prior art to claims 1–3 and/or 19 of the ’708
`
`109. Powell (MRK-STG-02559900) is prior art to claims 1–3 and/or 19 of the ’708
`
`110. Ashworth, 2-cyanopyrrolidides (MRK-STG-02560467) is prior art to claims 1–3
`
`and/or 19 of the ’708 patent.
`
`111. Ashworth, 4-cyanothiazolidides (MRK-STG-02560471) is prior art to claims 1–3
`
`and/or 19 of the ’708 patent.
`
`112. FDA and the Drug Development Process (MRK-STG-02560006) is prior art to
`
`claims 1–3 and/or 19 of the ’708 patent.
`
`113. DiMasi 2001 (MRK-STG-02560487) is prior art to claims 1–3 and/or 19 of the
`
`’708 patent.
`
`16
`
`

`

`Case 1:19-cv-00101-TSK Document 123 Filed 11/17/21 Page 17 of 19 PageID #: 8523
`
`114. U.S. Patent Application Publication No. 2002/0198205 (MRK-STG-02560326) is
`
`prior art to claims 1–3 and/or 19 of the ’708 patent.
`
`115. PDR 2001 (MRK-STG-02559773) is prior art to claims 1–3 and/or 19 of the ’708
`
`patent.
`
`XI. COMMON OWNERSHIP
`
`116. Each inventor of the ’871 patent, WO ’498, and the ’708 patent was under an
`
`obligation to assign their inventions, discoveries, patent applications, and patents to Merck, and
`
`the inventors did assign the subject matter of the ’871 patent, WO ’498, and the ’708 patent to
`
`Merck. See, e.g., Myerson Rep. ¶ 240 (Apr. 16, 2021).
`
`117. The subject matter of the ’871 patent, WO ’498, and the ’708 patent were
`
`commonly owned by Merck at the time of the inventions claimed in the ’708 patent.
`
`118. The ’871 patent and WO ’498 are not available as prior art under 35 U.S.C.
`
`§ 102(e) to the ’708 patent to prove obviousness under 35 U.S.C. § 103, pursuant to 35 U.S.C. §
`
`103(c). Nothing in this document is a statement by either party as to whether the ’871 patent
`
`and/or WO ’498 can be used as part of an obviousness-type double patenting invalidity
`
`challenge.
`
`XII. SALTS OF SITAGLIPTIN AND PHOSPHORIC ACID
`
`119. Using isopropanol, water, sitagliptin free base, and phosphoric acid, Dr. Adam
`
`Matzger synthesized a salt with a 3:2 stoichiometry of sitagliptin to phosphoric acid, with no 1:1
`
`sitagliptin dihydrogenphosphate salt present. For this experiment, Dr. Matzger followed the
`
`protocol set forth in Example 1 of WO 2012/166420 (WO ’420) (MRK-STG-02034546), which
`
`claims priority and/or benefit to U.S. Provisional Application No. 61/490,819, which was filed
`
`on May 27, 2011. This protocol used an approximately 2:1 ratio of sitagliptin free base to
`
`phosphoric acid, which is a non-equimolar amount of sitagliptin free base to phosphoric acid.
`
`17
`
`

`

`Case 1:19-cv-00101-TSK Document 123 Filed 11/17/21 Page 18 of 19 PageID #: 8524
`
`See, e.g., Matzger Rep. ¶¶ 60–72 (Apr. 15, 2021). Prior to its disclosure in WO ’420, the 3:2 salt
`
`had not previously been publicly reported.
`
`120. By recrystallizing the 3:2 salt described in the aforementioned paragraph in water,
`
`Dr. Matzger synthesized a different salt with a 2:1 stoichiometry of sitagliptin to phosphoric
`
`acid, with no 1:1 sitagliptin dihydrogenphosphate salt present. See, e.g., Matzger Rep. ¶¶ 73–88
`
`(Apr. 15, 2021). This recrystallization experiment and the resulting 2:1 salt, using the particular
`
`3:2 salt described in the aforementioned paragraph, had not previously been publicly reported.
`
`121. Sitagliptin only has one chiral center.
`
`Dated: November 17, 2021
`
`Respectfully submitted,
`
`CAREY, DOUGLAS, KESSLER & RUBY, PLLC
`
`/s/ Steven R. Ruby
`Steven R. Ruby (WVSB #10752)
`901 Chase Tower, 707 Virginia Street,
`East P.O. Box 913
`Charleston, WV 25323
`Telephone: (304) 345-1234
`Facsimile: (304) 342-1105
`sruby@cdkrlaw.com
`
`OF COUNSEL:
`
`Bruce R. Genderson (admitted PHV)
`Jessamyn S. Berniker (admitted PHV)
`Stanley E. Fisher (admitted PHV)
`Alexander S. Zolan (admitted PHV)
`Elise Baumgarten (admitted PHV)
`Shaun P. Mahaffy (admitted PHV)
`Anthony H. Sheh (admitted PHV)
`WILLIAMS & CONNOLLY LLP
`725 Twelfth Street, N.W.
`Washington, DC 20005
`T: (202) 434-5000
`F: (202) 434-5029
`bgenderson@wc.com
`
`
`
`
`
`
`
`
`
`
`STEPTOE & JOHNSON, PLLC
`
`/s/ Gordon H. Copland
`Gordon H. Copland (WV Bar #828)
`William J. O’Brien (WV Bar #10549)
`400 White Oaks Blvd.
`Bridgeport, WV 26330
`(304) 933-8000
`gordon.copland@steptoe-johnson.com
`william.obrien@steptoe-johnson.com
`
`OF COUNSEL:
`
`Deepro R. Mukerjee (admitted PHV)
`Lance A. Soderstrom (admitted PHV)
`KATTEN MUCHIN ROSENMAN
`575 Madison Avenue
`New York, NY 10022
`(212) 940-8800
`deepro.mukerjee@katten.com
`lance.soderstrom@katten.com
`
`Jitendra Malik (admitted PHV)
`KATTEN MUCHIN ROSENMAN
`550 S. Tryon Street, Suite 2900
`Charlotte, NC 28202
`
`18
`
`

`

`Case 1:19-cv-00101-TSK Document 123 Filed 11/17/21 Page 19 of 19 PageID #: 8525
`
`jberniker@wc.com
`sfisher@wc.com
`azolan@wc.com
`ebaumgarten@wc.com
`smahaffy@wc.com
`asheh@wc.com
`
`Counsel for Plaintiff
`Merck Sharp & Dohme Corp.
`
`
`
`
`
`(704) 344-3182
`jitty.malik@katten.com
`
`Matthew M. Holub (admitted PHV)
`Jillian M. Schurr (admitted PHV)
`KATTEN MUCHIN ROSENMAN
`525 W. Monroe Street
`Chicago, IL 60661
`(312) 902-5200
`matthew.holub@katten.com
`jillian.schurr@katten.com
`
`Counsel for Defendant
`Mylan Pharmaceuticals Inc.
`
`
`
`
`19
`
`