UNITED STATES PATENT AND TRADEMARK OFFICE
`__________________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`__________________
`
`MYLAN PHARMACEUTICALS INC., DR. REDDY’S
`LABORATORIES, INC., DR. REDDY’S LABORATORIES, LTD., and
`SUN PHARMACEUTICALS INDUSTRIES LTD.,
`Petitioners,
`
`v.
`
`MERCK SHARP & DOHME CORP.,
`Patent Owner.
`__________________
`
`IPR2020-000401
`Patent 7,326,708
`__________________
`
`
`
`PATENT OWNER’S SEVENTH AMENDED EXHIBIT LIST
`
`
`
`1 Dr. Reddy’s Laboratories, Inc. and Dr. Reddy’s Laboratories, Ltd. were joined as
`parties to this proceeding via a Motion for Joinder in IPR2020-01060; and Sun
`Pharmaceuticals Industries Ltd. was joined as a party to this proceeding via Motion
`for Joinder in IPR2020-01072.
`
`

`

`
`
`IPR2020-00040 | Patent 7,326,708
`
`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 (’708 & ’921)
`EX2006
`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))
`EX2014 Declaration of Anthony H. Sheh
`EX2015 U.S. District Court for the District of Delaware, Civil Docket for
`Case # 1:19-md-2902-RGA (as of April 13, 2020)
`Stipulation and [Proposed] Order to Amend Scheduling Order, In
`re Sitagliptin Phosphate (’708 & ’921) Patent Litigation, No. 19-
`2902-RGA (D. Del. Mar. 16, 2020), ECF No. 83
`EX2017 U.S. District Court for the Northern District of West Virginia,
`Civil Docket for Case # 1:19-cv-00101-IMK (as of April 13, 2020)
`EX2018 Defendant’s Answer to Plaintiff’s Complaint and Counterclaims,
`Merck Sharp & Dohme Corp. v. Mylan Pharmaceuticals Inc., No.
`19-cv-101-IMK (N.D. W. Va. May 31, 2019), ECF No. 32
`Joint Quarterly Status Report, Merck Sharp & Dohme Corp. v.
`Mylan Pharmaceuticals Inc., No. 19-cv-101-IMK (N.D. W. Va.
`Jan. 3, 2020), ECF No. 50
`
`EX2019
`
`EX2016
`
`1
`
`

`

`
`
`IPR2020-00040 | Patent 7,326,708
`
`Description
`Exhibit
`EX2020 REDACTED VERSION, Brief in Support of Mylan
`Pharmaceuticals Inc. and Mylan Inc.’s Motion to Dismiss for
`Improper Venue and Failure to State a Claim, Merck Sharp &
`Dohme Corp. v. Mylan Pharmaceuticals, Inc., No. 19-cv-315-
`RGA (D. Del. Mar. 28, 2019), ECF No. 15
`EX2021 U.S. Judicial Panel on Multidistrict Litigation, Civil Docket for
`Case # MDL No. 2902
`EX2022 Memorandum in Support of Motion to Transfer, In re Sitagliptin
`Phosphate (’708 & ’921) Patent Litigation, MDL No. 2902
`(J.P.M.L. May 15, 2019), ECF No. 1-1
`In re Sitagliptin Phosphate (’708 & ’921) Patent Litigation, 402 F.
`Supp. 3d 1366 (J.P.M.L. 2019)
`EX2024 Oral Order, Plastic Omnium Advanced Innovation and Research v.
`Donghee America Inc., No. 16-187-LPS (D. Del. Oct. 27, 2017),
`ECF No. 196
`EX2025 Declaration of Alexander S. Zolan in Support of Pro Hac Vice
`Admission
`EX2026 Declaration of Elise M. Baumgarten in Support of Pro Hac Vice
`Admission
`
`EX2023
`
`
`EX2027 TO EX2031 Reserved
`EX2032 U.S. Patent No. 8,309,724
`EX2033 WO 2013/001457
`
`EX2033 to EX2040 Reserved
`Transcript of July 15, 2020 Telephonic Hearing
`EX2041
`EX2042 A.T.M. Serajuddin & Pudipeddi, Salt-Selection Strategies, in
`HANDBOOK OF PHARMACEUTICAL SALTS (P.H. Stahl & C.G.
`Wermuth, eds., 2002)
`EX2043 U.S. Patent No. 8,329,696
`EX2044 WO 2012/166420
`Pandey et al., Importance of Polymorphs and Salts in the
`EX2045
`Pharmaceutical Industry, in DRUG DISCOVERY AND
`DEVELOPMENT, VOLUME 2: DRUG DEVELOPMENT (Mukund S.
`Chorghade ed., 2007)
`EX2046 Vippagunta et al., Crystalline Solids, 48 ADVANCED DRUG
`DELIVERY REVIEWS 3 (2001)
`EX2047 Reutzel-Edens et al., Anhydrates and Hydrates of Olanzapine:
`Crystallization, Solid-State Characterization, and Structural
`Relationships, 3 CRYSTAL GROWTH & DESIGN 897 (2003)
`
`2
`
`

`

`
`
`IPR2020-00040 | Patent 7,326,708
`
`Description
`
`Exhibit
`EX2048 U.S. Patent No. 7,056,942
`EX2049 Bernstein, Crystal Growth, Polymorphism and Structure-Property
`Relationships in Organic Crystals, 26 J. PHYS. D. APPL. PHYS. B66
`(1993)
`EX2050 Bernstein, POLYMORPHISM IN MOLECULAR CRYSTALS (2002)
`(Chapter 3)
`Transcript of Aug. 6, 2020 Deposition of Mukund Chorghade,
`Ph.D.
`EX2101 Declaration of Allan S. Myerson, Ph.D.
`EX2102 Curriculum Vitae of Allan S. Myerson, Ph.D.
`EX2103 Declaration of Adam J. Matzger, Ph.D.
`EX2104 Curriculum Vitae of Adam J. Matzger, Ph.D.
`EX2105 Declaration of Lou Ann Eader
`EX2106
`Synopsis and Comprehensive Study Summary from the Clinical
`Study Report for Protocol 005, dated November 15, 2005 (excerpt)
`Synopsis and Comprehensive Study Summary from the Clinical
`Study Report for Protocol 006, dated April 1, 2005 (excerpt)
`EX2108 Module 3.2.P.5.4 Batch Analyses from Januvia® NDA, dated
`November 14, 2005 (excerpt)
`EX2109 Declaration of Gary Herman, M.D.
`EX2110
`Email Summary of December 9, 2002, Meeting Re: Clinical
`Development of MK-0431
`January 3, 2003 Email Re: DRAFT Preliminary Interim Analysis
`Memo/RMC Background Slides - L-224715
`EX2112 Demuth et al., Single Dose Treatment of Diabetic Patients by the
`DP IV Inhibitor P32/98, 49 DIABETES A102 (2000)
`Pospisilik et al., Long-Term Treatment with the Dipeptidyl
`Peptidase IV Inhibitor P32/98 Causes Sustained Improvements in
`Glucose Tolerance, Insulin Sensitivity, Hyperinsulinemia, and β-
`Cell Glucose Responsiveness in VDF (fa/fa) Zucker Rats, 51
`DIABETES 943 (2002)
`Thornberry & Weber, Discovery of JANUVIA (Sitagliptin), a
`Selective Dipeptidyl Peptidase IV Inhibitor for the Treatment of
`Type 2 Diabetes, 7 CURRENT TOPICS IN MEDICINAL CHEMISTRY
`557 (2007)
`EX2115 Rothenberg et al., Treatment with a DPP-IV Inhibitor, NVP-
`DPP728, Increases Prandial Intact GLP-1 Levels and Reduces
`Glucose Exposure in Humans, 49 DIABETES 160-OR (2000)
`
`EX2051
`
`EX2107
`
`EX2111
`
`EX2113
`
`EX2114
`
`3
`
`

`

`
`
`IPR2020-00040 | Patent 7,326,708
`
`EX2120
`
`EX2121
`EX2122
`
`Description
`Exhibit
`Second Declaration of Robert M. Wenslow, Ph.D.
`EX2116
`EX2117 WO 2005/020920
`EX2118 WO 2005/072530
`EX2119 Compilation of L-224715 Phosphate Salt Anhydrous Polymorph
`Data
`Physical Characterization of L-224715-66839-113 (115) and -125
`(from ISAA)
`L-000224715 Monohydrate Evaluation
`Parallel Development of Multiple Crystal Forms for a New Drug
`Candidate: Selection of the Final Form via Integrated Chemical
`and Pharmaceutical Process Evaluation
`L-000224715 (MK-0431) Preliminary Market Formulation
`Development Report
`EX2124 Declaration of Stephen Howard Cypes
`EX2125 Merck Lab Notebook 66839 (Excerpt)
`EX2126
`S. Cypes Weekly Reports
`EX2127 Declaration of Karl B. Hansen, Ph.D.
`EX2128 Merck Lab Notebook 70130 (Excerpt)
`EX2129 Merck Lab Notebook 70316 (Excerpt)
`EX2130 Merck Lab Notebook 72471 (Excerpt)
`EX2131 K. Hansen Weekly Reports
`EX2132
`Email from M. Palucki to K. Hansen re Acid Salt Screen of L-
`224715 Free Base (and Attachment)
`Email from L. Shultz to K. Hansen re L-224715 salt selection
`EX2133
`Email from K. Hansen re L-224715 meeting follow-up
`EX2134
`EX2135 Delivery Sheet Lot 006F007
`EX2136 Delivery Sheet Lot 006F017
`EX2137
`L-000224715 Phosphate Salt Polymorph Screen
`EX2138
`Symyx Presentation L224715 H3PO4 Salt
`EX2139
`Email from C. Starbuck to K. Hansen re L-224,715 drying
`EX2140 Declaration of Rebecca Leigh Shultz, Ph.D.
`EX2141 Merck Lab Notebook 60659 (Excerpt)
`EX2142 Merck Lab Notebook 60659 Supplemental Data (Excerpt)
`EX2143 Merck Lab Notebook 26180 (Excerpt)
`EX2144 Merck Lab Notebook 26180 Supplemental Data (Excerpt)
`EX2145 Merck Lab Notebook 72917 (Excerpt)
`EX2146
`Preliminary Pharmaceutical Assessment of L-224715
`EX2147
`Pharmaceutical Evaluation of L-224715
`
`EX2123
`
`4
`
`

`

`
`
`IPR2020-00040 | Patent 7,326,708
`
`Exhibit
`EX2148
`EX2149
`
`EX2150
`
`EX2151
`
`EX2152
`
`EX2153
`
`EX2154
`
`EX2155
`
`EX2161
`
`Description
`L-000224715 Preformulation Report
`Physico-chemical characteristics of L-000224715 phosphate salt,
`monohydrate form
`L. Shultz Merck Research Laboratories Progress Report December
`2001
`L. Shultz Merck Research Laboratories Progress Report January
`2002
`L. Shultz Merck Research Laboratories Progress Report February
`2002
`L. Shultz Merck Research Laboratories Progress Report March
`2002
`L. Shultz Merck Research Laboratories Progress Report September
`2002
`Email from C. Lindemann re: L-224715 Quick Update (and
`Attachment)
`Salt Selection for L-224715 and L-221869
`EX2156
`Email from I. Santos re: Salt selection for L-224715
`EX2157
`EX2158 December 7, 2002 Email re: Background Slides for Monday’s
`Meeting
`EX2159 Email from D. Zhang re: Physical Characterization of L-224715
`Phosphate
`EX2160 Rocco et al., Solid-State Characterization of Zanoterone, 122 INT’L
`J. PHARMACEUTICS 17 (1995)
`Poole et al., Dissolution Behavior and Solubility of Anhydrous and
`Trihydrate Forms of Ampicillin, 57 J. PHARM. SCIS. 1945 (1968)
`EX2162 Kobayashi, Physiochemical Properties and Bioavailability of
`Carbamazepine Polymorphs and Dihydrate, 193 INT’L J.
`PHARMACEUTICS 137 (2000)
`EX2163 Morris et al., Advances in Pharmaceutical Materials and
`Processing, 1 PSTT 235 (1998)
`EX2164 Gavezzotti, Are Crystal Structures Predictable?, 27 ACC. CHEM.
`RES. 309 (1994)
`EX2165 Day, Investigating the Latent Polymorphism of Maleic Acid,
`CHEM. COMMUN. 54 (2006)
`EX2166 Vishweshwar et al., The Predictably Elusive Form II of Aspirin,
`127 J. AM. CHEM. SOC. 16802 (2005)
`
`5
`
`

`

`
`
`IPR2020-00040 | Patent 7,326,708
`
`Exhibit
`EX2167
`
`Description
`Fagan et al., An Ab Initio Approach to Crystal Structure
`Determination Using High-Resolution Powder Diffraction and
`Computational Chemistry Techniques: Application to 6,13-
`Dichlorotriphendioxazine, 7 CHEM. MATER. 2322 (1995)
`EX2168 Dunitz & Bernstein, Disappearing Polymorphs, 28 ACC. CHEM.
`RES. 193 (1995)
`EX2169 Bavin, Polymorphism in Process Development, CHEMISTRY &
`INDUSTRY 527 (Aug. 21, 1989)
`EX2170 Maddox, Crystals from First Principles, 335 NATURE 201 (1988)
`EX2171 U.S. Patent No. 6,861,426
`EX2172 Guillory, Generation of Polymorphs, Hydrates, Solvates, and
`Amorphous Solids, in POLYMORPHISM IN PHARMACEUTICAL SOLIDS
`(H.G. Brittain ed., 1st ed. 1999)
`EX2173 Kirwan & Orella, Crystallization in the Pharmaceutical and
`Bioprocessing Industries, in HANDBOOK OF INDUSTRIAL
`CRYSTALLIZATION (Allan S. Myerson ed., 2001)
`Taleb et al., Equilibrium Kinetics of Lysozome Crystallization
`Under an External Electrical Field, 232 J. CRYSTAL GROWTH 250
`(2001)
`EX2175 Garetz et al., Nonphotochemical, Polarization-Dependent, Laser-
`Induced Nucleation in Supersaturated Aqueous Urea Solutions, 77
`PHYS. REV. LETTERS 3475 (1996)
`EX2176 Ratsimba et al., Sonocrystallization: The End of Empiricism?, 17
`KONA POWDER & PARTICLE J. 38 (1999)
`International Conference on Harmonisation; Guidance on
`Impurities: Residual Solvents, 62 FR 67377 (Dec. 24, 1997)
`EX2178 Byrn et al., Solid-State Pharmaceutical Chemistry, 6 CHEM.
`MATER. 1148 (1994)
`EX2179 Myerson & Ginde, Crystals, Crystal Growth, and Nucleation, in
`HANDBOOK OF INDUSTRIAL CRYSTALLIZATION (Allan S. Myerson
`ed., 2001)
`EX2180 Rodriguez-Hornedo & Murphy, Significance of Controlling
`Crystallization Mechanisms and Kinetics in Pharmaceutical
`Systems, 88 J. PHARM. SCIS. 651 (1999)
`EX2181 Chopra, Surprises in Crystal Chemistry of Sugars, 17 ORG.
`PROCESS RES. DEV. 455 (2012)
`EX2182 U.S. Patent No. 7,157,429
`EX2183 U.S. Patent No. 5,939,560
`
`EX2174
`
`EX2177
`
`6
`
`

`

`
`
`IPR2020-00040 | Patent 7,326,708
`
`EX2185
`
`EX2189
`
`Description
`Exhibit
`EX2184 Yu, Amorphous Pharmaceutical Solids: Preparation,
`Characterization and Stabilization, 48 ADVANCED DRUG
`DELIVERY REVIEWS 27 (2001)
`Smith & March, MARCH’S ADVANCED ORGANIC CHEMISTRY:
`REACTIONS, MECHANISMS, AND STRUCTURE (2001) (excerpt)
`EX2186 WO 2010/131035
`EX2187 U.S. Patent No. 8,334,319
`EX2188 Muhtadi & Hassan, Codeine Phosphate, 10 ANALYTICAL PROFILES
`OF DRUG SUBSTANCES 93 (1981)
`Langes et al., Codeine Dihydrogen Phosphate Hemihydrate, C65
`ACTA CRYST. O419 (2009)
`EX2190 Caira, Crystalline Polymorphism of Organic Compounds, 198
`TOPICS IN CURRENT CHEMISTRY, 163 (1998)
`EX2191 U.S. Patent No. 6,124,305
`EX2192 Chyall Second Declaration, March 7, 2012
`EX2193 A.T.M. Serajuddin, Salt Formation to Improve Drug Solubility, 59
`ADVANCED DRUG DELIVERY REVIEWS, 603 (2007)
`S.M. Berge, L.D. Bighley, & D.C. Monkhouse, Pharmaceutical
`Salts, 66 J. PHARM. SCIS 1 (1977)
`EX2195 G. Davies, Changing the Salt, Changing the Drug, 266 PHARM. J.
`322 (2001)
`EX2196 R.K. Verbeeck, I. Kanfer, & R.B. Walker, Generic substitution:
`The use of medicinal products containing different salts and
`implications for safety and efficacy, 28 EURO J. PHARM. SCIS 1
`(2006)
`P.L. Gould, Salt selection for basic drugs, 33 INT’L J.
`PHARMACEUTICS 201 (1986)
`EX2198 Ammonium phosphate monobasic, Sigma Aldrich Catalog
`EX2199 Ammonium phosphate dibasic, Sigma Aldrich Catalog
`EX2200
`Triammonium phosphate trihydrate, Combi-Blocks
`EX2201 Handbook of Pharmaceutical Excipients (4th ed.)
`J.A. Tamada & C.J. King, Extraction of Carboxylic Acids by
`EX2202
`Amine Extractants, Lawrence Berkeley Laboratory University of
`California Ph.D. Thesis, Received March 27, 1999
`EX2203 B. Grimball et al., Cyclohexylamine inexplicably induces antennae
`loss in Formosan subterranean termites (Coptotermes formosanus
`Shiraki): cyclohexylamine hydrogen phosphate salts are novel
`termiticides, 73 SOC. CHEM. INDUS. 2039 (2017)
`
`EX2194
`
`EX2197
`
`7
`
`

`

`
`
`IPR2020-00040 | Patent 7,326,708
`
`EX2205
`
`EX2206
`
`Description
`Exhibit
`EX2204 A.B. Bjåen et al., Polymorphism of chloroquine diphosphate, 92
`INT’L J. PHARMACEUTICS 183 (1993)
`F. Takusagawa & T. F. Koetzle, A Study of the Charge Density in
`Putrescine Diphosphate at 85 K, 35 ACTA CRYST. 867 (1979)
`J.R. Rubin, Structure of the Anti-Malarial Drug Primaquine
`Diphosphate, 48 ACTA CRYST. 379 (1992)
`EX2207 Khan et al., The Crystal Structure of Diammonium Hydrogen
`Phosphate, (NH4)2HPO4, 28 ACTA CRYST. 2065 (1972)
`EX2208 Cotton et al., Structure of Bis(methylguanidinium) Monohydrogen
`Orthophosphate. A Model for the Arginine-Phosphate Interactions
`at the Active Site of Staphyloccocal Nuclease and Other
`Phosphohydrolytic Enzymes, 96 J. AM. CHEM. SOC. 4471 (1974)
`Low et al., Structure of Bis(guaninium) Hydrogenphosphate 2.5-
`Hydrate, 42 ACTA CRYST. 1045 (1986)
`EX2210 Adams & Small, The Crystal Structure of Bisguanidinium
`Hydrogen Phosphate Monohydrate, B32 ACTA CRYST. 832 (1976)
`EX2211 Averbuch-Pouchot & Durif, Structures of Ethylenediammonium
`Monohydrogentetraoxophosphate(V) and Ethylenediammonium
`Monohydrogentetraoxoarsenate, C43 ACTA CRYST. 1894 (1987)
`EX2212 Baouab & Jouini, Crystal Structures and Thermal Behavior of Two
`New Organic Monophosphates, 141 J. SOLID STATE CHEM., 343
`(1998)
`EX2213 Demir et al., N-(2-Hydroxyethyl)ethylene-diammonium
`hydrogenphosphate monohydrate, C58 ACTA CRYSTA. o407 (2002)
`EX2214 Kamoun et al., Chemical Preparations, Main Crystallographic and
`Structural Features of Two New Monophosphates:
`[NH3(CH2)3NH3].HPO4.H2O and
`[NH3(CH2)2NH(CH2)2NH3].HPO4.2H2O, 310 C.R. ACAD. SCI.
`PARIS 733 (1990)
`EX2215 M. L. Mrad et al., Tris(5-amino-1H-1,2,4-triazol-4-ium)
`dihydrogenphosphate hydrogenphosphate trihydrate, 68 ACTA
`CRYSTA. o3257 (2012)
`J. Fábry R. Krupková, P. Vanek, & M. Dusek,
`Tris(methylammonium) hydrogenphosphate dihydrogenphosphate,
`62 ACTA CRYSTA. o73 (2006)
`EX2217 A.E. Cohen et al., Structure and Thermal Vibrations of Spermine
`Phosphate Hexahydrate from Neutron Diffraction Data at 125 K,
`B53 ACTA CRYST. 787 (1997)
`
`EX2209
`
`EX2216
`
`8
`
`

`

`
`
`IPR2020-00040 | Patent 7,326,708
`
`Description
`Exhibit
`EX2218 Newman & Stahly, Form Selection of Pharmaceutical
`Compounds, in HANDBOOK OF PHARMACEUTICAL ANALYSIS
`(Ohannesian ed., 2002)
`EX2219 Cruz-Cabeza, Acid-Base Crystalline Complexes and the pKa rule,
`14 CRYSTENGCOMM. 6362 (2012)
`EX2220 WO 2012/166420
`EX2221 Atwood First Affidavit, June 6, 2011
`EX2222 Atwood Second Affidavit, August 20, 2012
`EX2223 Atwood Third Affidavit, September 13, 2013
`EX2224 Chyall Third Declaration, February 19, 2013
`EX2225 Chyall First Declaration, August 3, 2010
`EX2226 Chyall Lab Notebook 4031
`EX2227
`Transcript of Jan. 29, 2015 Chyall Testimony
`EX2228 Matzger Lab Notebook 3
`EX2229 Matzger Lab Notebook 4
`EX2230 Wong-Foy Notebook
`EX2231 Collection of underlying data related to the Declaration of Adam J.
`Matzger
`EX2232 Galbraith Lab Notebook
`EX2233 D.E. Newberry & N.W.M. Ritchie, Performing elemental
`microanalysis with high accuracy and high precision by scanning
`electron microscopy/silicon drift detector energy-dispersive X-ray
`spectrometry (SEM/SDD-EDS), 50 J. MATERIAL SCI. 493 (2015)
`P.K. Kipkemboi & A.J. Easteal, Vibrational spectroscopic studies
`of aqueous solutions of tert-butyl alcohol and terti-butylamine, 80
`CANADIAN J. CHEM. 789 (2002)
`T. Visser & J.H. van der Maas, Systematic Interpretation of Raman
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`EX2236 M. Xie, Y. Qi & Y. Hu, Conformational Equilibrium and
`Hydrogen Bonding in Liquid 2-Phenylethylamine Explored by
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`CHEM., 3060 (2011)
`EX2237 C. Perchard & J.P. Perchard, Liquid-Phase Hydrogen Bonding and
`Raman Spectrometry, 6 J. RAMAN SPECTROSCOPY 74 (1977)
`
`EX2234
`
`EX2235
`
`9
`
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`

`
`
`IPR2020-00040 | Patent 7,326,708
`
`EX2239
`
`Description
`Exhibit
`EX2238 A.M. Amado, M.M. Nolasco & P.J.A. Ribeiro-Claro, Proving
`Pseudopolymorphic transitions in Pharmaceutical Solids using
`Raman Spectroscopy: Hydration and Dehydration of Theophylline,
`96 J. PHARM. SCIS. 1366 (2007)
`J.M. Rollinger & A. Burger, Physico-Chemical Characterization
`of Hydrated and Anhydrous Crystal Forms of Amlodipine Besylate,
`68 J. THERMAL ANALYSIS & CALORIMETRY 361 (2002)
`EX2240 C. Lester et al., Dehydration of Risedronate Hemi-Pentahydrate:
`Analytical and Physical Characterization, 95 J. PHARM. SCIS. 2631
`(2006)
`EX2241 A.M. Amado, M.M. Nolasco & P.J.A. Ribeiro-Claro, Insights into
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`methodology, 41 J. RAMAN SPECTROSCOPY, 340 (2010)
`EX2242 N.C.F. Stofella et al., Solid-State Characterization of Different
`Crystalline Forms of Sitagliptin, 12 MATERIALS 1 (2019)
`EX2243 B. Rees, L. Jenner & m. Yusupov, Bulk-solvent correction in large
`macromolecular structures, 61 ACTA CRYSTA. 1299 (2005)
`EX2244 NIST Solubility Table (excerpt)
`EX2245 Balkan et al., Inhibition of Dipeptidyl Peptidase IV with NVP-
`DPP728 Increases Plasma GLP-1 (7-36 Amide) concentrations
`and Improves Oral Glucose Tolerance in Obese Zucker Rats, 42
`DIABETOLOGIA 1324 (1999)
`EX2246 R.I. Ellin and J. H. Wills, Oximes Antagonistic to Inhibitors of
`Cholinesterase, 53 J. PHARM. SCI. 1143 (1964)
`EX2247 H.M. Koehler & J.J. Hefferren, Mineral Acid Salts of Lidocaine,
`53 J. PHARM. SCIS 1126 (1964)
`EX2248 V.C. Walton, M.R. Howlett, & G.B. Selzer, Anhydrotetracycline
`and 4-Epianhydrotetracycline in Market Tetracyclines and Aged
`Tetracycline Products, 59 J. PHARM. SCIS, 1160 (1970)
`EX2249 B. Hoener, T.D. Sokoloski, L.A. Mitscher & L. Malspeis, Kinetics
`of Dehydration of Epitetracycline in Solution, 63 J. PHARM. SCIS.
`1901 (1974)
`EX2250 U. V. Shah et al., Effect of crystal habits on the surface energy and
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`EX2251 N. Rasenack and B.W. Muller, Crystal habit and tableting
`behavior, 244 INT’L J. PHARMACEUTICS 45 (2002)
`
`10
`
`

`

`
`
`IPR2020-00040 | Patent 7,326,708
`
`Exhibit
`EX2252
`
`
`EX2273
`
`Description
`F. Podczeck and Y. Miah, The influence of particle size and shape
`on the angle of internal friction and the flow factor of unlubricated
`and lubricated powders, 144 INT’L J. PHARMACEUTICS 187 (1996)
`EX2253 U.S. Patent No. 8,518,987
`Janczak & Perpetuo, Hexakis(melaminium)
`EX2254
`Tetrakis(dihydrogenphosphate) Monohydrogenphosphate
`Tetrahydrate, C58 ACTA CRYST. o455 (2002)
`EX2255 TO EX2272 Reserved
`Teva Pharmaceutical Industries, API Division, Chemical Pilot
`R&D, Assia, Petach Tikva, Sitagliptin Sulphate Pilot Concise
`Report (TEVASITAIPR000088–TEVASITAIPR00127)
`EX2274 Oct. 2, 2011 Email re Sitaglipin sulfate (TEVASITAIPR000088–
`TEVASITAIPR000131)
`Transcript of Nov. 6, 2020 Telephonic Hearing
`Tentative Markman Order, In re Sitagliptin Phosphate (’708 &
`’921) Patent Litigation, No. 1:19-md-02902-RGA (D. Del. Aug.
`17, 2020), ECF No. 167
`Transcript of Aug. 18, 2020 Markman Hearing Videoconference,
`In re Sitagliptin Phosphate (’708 & ’921) Patent Litigation, No.
`1:19-md-02902-RGA (D. Del. Aug. 18, 2020)
`EX2278 Declaration of Professor Allan S. Myerson, Ph.D. Regarding Claim
`Construction, In re Sitagliptin Phosphate (’708 & ’921) Patent
`Litigation, No. 1:19-md-02902-RGA (D. Del. July 17, 2020), ECF
`No. 93-1 at 37–62
`EX2279 Declaration of Graham Buckton, Ph.D., D.Sc., In re Sitagliptin
`Phosphate (’708 & ’921) Patent Litigation, No. 1:19-md-02902-
`RGA (D. Del. July 17, 2020), ECF No. 94-1 at 2–27
`EX2280 Reply Declaration of Professor Allan S. Myerson, Ph.D. Regarding
`Claim Construction, In re Sitagliptin Phosphate (’708 & ’921)
`Patent Litigation, No. 1:19-md-02902-RGA (D. Del. July 17,
`2020), ECF No. 94-1 at 236–253
`Third Declaration of Robert M. Wenslow, Ph.D.
`EX2281
`EX2282 Memorandum Opinion, In re Sitagliptin Phosphate (’708 & ’921)
`Patent Litigation, No. 1:19-md-02902-RGA (D. Del. Nov. 17,
`2020), ECF No. 310
`Transcript of Dec. 15, 2020 Deposition of Mukund Chorghade,
`Ph.D.
`
`EX2275
`EX2276
`
`EX2277
`
`EX2283
`
`11
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`

`
`
`Description
`Exhibit
`EX2284 Request for Certificate of Correction, U.S. Patent No. 7,326,708,
`U.S. Application No. 10/874,992 (Dec. 29, 2020)
`
`IPR2020-00040 | Patent 7,326,708
`
`
`Date: December 30, 2020
`
`
`
`
`
`
`
`Respectfully submitted,
`
`/Stanley E. Fisher/
`Stanley E. Fisher (Reg. No. 55,820)
`Bruce R. Genderson (Pro Hac Vice)
`David M. Krinsky (Reg. No. 72,339)
`Elise M. Baumgarten (Pro Hac Vice)
`Alexander S. Zolan (Pro Hac Vice)
`Shaun P. Mahaffy (Reg. No. 75,534)
`Anthony H. Sheh (Reg. No. 70,576)
`WILLIAMS & CONNOLLY LLP
`725 Twelfth Street, N.W.
`Washington, DC 20005
`T: (202) 434-5000
`F: (202) 434-5029
`sfisher@wc.com
`bgenderson@wc.com
`dkrinsky@wc.com
`ebaumgarten@wc.com
`azolan@wc.com
`smahaffy@wc.com
`asheh@wc.com
`
`Counsel for Patent Owner
`Merck Sharp & Dohme Corp.
`
`
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`12
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`

`
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`CERTIFICATION UNDER 37 C.F.R. § 42.24(d)
`
`Pursuant to 37 C.F.R. 42.6(e), the undersigned hereby certifies that a true
`
`IPR2020-00040 | Patent 7,326,708
`
`and correct copy of the foregoing was served on December 30, 2020, by delivering
`
`a copy via electronic mail on the following attorneys of record:
`
`Jitendra Malik
`Alissa M. Pacchioli
`Christopher W. West
`Heike S. Radeke
`KATTEN MUCHIN ROSEMAN LLP
`550 South Tryon, Street Suite 2900
`Charlotte, NC 28202-4213
`(704) 444-2000
`jitty.malik@kattenlaw.com
`alissa.pacchioli@kattenlaw.com
`christopher.west@katten.com
`heike.radeke@katten.com
`
`Jovial Wong
`Charles B. Klein
`Claire A. Fundakowski
`Zachary B. Cohen
`WINSTON & STRAWN LLP
`1901 L. Street, N.W.
`Washington, D.C. 20036
`(202) 282-5000
`Sunipr@winston.com
`
`
`
`
`
`
`Russell W. Faegenburg
`Tedd W. Van Buskirk
`Michael H. Teschner
`LERNER, DAVID, LITTENBERG,
`KRUMHOLZ & MENTLIK, LLP
`20 Commerce Drive
`Cranford, New Jersey 07016
`(908) 518-6367
`Rfaegenburg.ipr@ldlkm.com
`Tvanbuskirk@lernerdavid.com
`litigation@lernerdavid.com
`MTeschner.ipr@ldlkm.com
`
`
`
`/Stanley E. Fisher/
`Stanley E. Fisher
`Reg. No. 55,820
`
`
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`13
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