UNITED STATES PATENT AND TRADEMARK OFFICE
`___________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`___________
`
`
`
`MYLAN PHARMACEUTICALS INC.,
`Petitioner,
`
`v.
`
`ASTRAZENECA AB,
`Patent Owner.
`____________________________________________
`
`Case IPR2015-01340
`Patent RE44,186
`
`____________________________________________
`
`
`
`PATENT OWNER ASTRAZENECA AB’S EXHIBIT LIST
`(as of September 25, 2015)
`
`
`
`
`
`
`___________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`___________
`
`
`
`MYLAN PHARMACEUTICALS INC.,
`Petitioner,
`
`v.
`
`ASTRAZENECA AB,
`Patent Owner.
`____________________________________________
`
`Case IPR2015-01340
`Patent RE44,186
`
`____________________________________________
`
`
`
`PATENT OWNER ASTRAZENECA AB’S EXHIBIT LIST
`(as of September 25, 2015)
`
`
`
`
`
`
`
`
`
`
`Exhibit
`
`Description
`
`Case No. IPR2015-01340
`Patent RE44,186
`
`Exhibit 2001
`
`Doreen M. Ashworth et al., 4-Cyanothiazolidides as Very
`Potent, Stable Inhibitors of Dipeptidyl Peptidase IV, 6 BIOORG.
`& MED. CHEM. LETT. 2745 (1996)
`
`Exhibit 2002
`
`David R. Magnin et al., Synthesis of Novel Potent Dipeptidyl
`Peptidase IV Inhibitors with Enhanced Chemical Stability:
`Interplay Between the N-Terminal Amino Acid Alkyl Side Chain
`and the Cyclopropyl Group of α-Aminoacyl-L-cis-4,5-
`methanoprolinenitrile-Based Inhibitors, 47 J. MED. CHEM. 2587
`(2004)
`
`Exhibit 2003
`
`Jeffrey A. Robl & Lawrence G. Hamann, The Discovery of the
`Dipeptidyl Peptidase-4 (DPP4) Inhibitor Onglyza™: From
`Concept to Market, in ACCOUNTS IN DRUG DISCOVERY: CASE
`STUDIES IN MEDICINAL CHEMISTRY 1 (Joel C. Barrish et al. eds.,
`2011)
`Exhibit 2004 ASTRAZENECA ANNUAL REPORT AND FORM 20-F INFORMATION
`2014, available at www.astrazeneca.com/annualreport2014
`
`Exhibit 2005
`
`Jens J. Holst & Carolyn F. Deacon, Inhibition of the Activity of
`Dipeptidyl-Peptidase IV as a Treatment for Type 2 Diabetes, 47
`DIABETES 1663 (1998)
`
`Exhibit 2006
`
`Kathleen Aertgeerts et al., Crystal Structure of Human
`Dipeptidyl Peptidase IV in Complex with a Decapeptide
`Reveals Details on Substrate Specificity and Tetrahedral
`intermediate Formation, 13 PROTEIN SCI. 412 (2004)
`
`Exhibit 2007
`
`K. Augustyns et al., The Unique Properties of Dipeptidyl-
`Peptidase IV (DPP IV / CD26) and the Therapeutic Potential of
`DPP IV Inhibitors, 6 CURR. MED. CHEM. 311 (1999)
`
`Exhibit 2008
`
`George R. Flentke et al., Inhibition of Dipeptidyl
`Aminopeptidase IV (DP-IV) by Xaa-boroProdipeptides and Use
`of These Inhibitors to Examine the Role of DP-IV in T-cell
`Function, 88 PROC. NAT’L ACAD. SCI. 1556 (1991)
`
`
`
`1
`
`
`
`
`Exhibit
`
`Exhibit 2009
`
`Case No. IPR2015-01340
`Patent RE44,186
`
`Description
`
`Robert P. Pauly et al., Improved Glucose Tolerance in Rats
`Treated With the Dipeptidyl Peptidase IV (CD26) Inhibitor Ile-
`Thiazolidide, 48 METABOLISM 385 (1999)
`
`Exhibit 2010
`
`Hans-U Demuth et al., Abstract, Single Dose Treatment of
`Diabetic Patients by the DP IV Inhibitor P32/98, 49 DIABETES
`413-P (2000)
`
`Exhibit 2011 U.S. Patent No. 5,939,560
`
`Exhibit 2012
`
`Paul Rothenberg et al., Abstract, Treatment with a DPP-IV
`Inhibitor, NVP-DPP728, Increases Prandial Intact GLP-1
`Levels and Reduced Glucose Exposure in Humans, 49
`DIABETES 160-OR (2000)
`
`Exhibit 2013 U.S. Patent No. 6,166,063
`
`Exhibit 2014
`
`Ligaya M. Simpkins et al., Potent Non-Nitrile Dipeptidic
`Dipeptidyl Peptidase IV Inhibitors, 17 BIOORG. & MED. CHEM.
`LETT. 6476 (2007)
`Exhibit 2015 Pioneer and Analogue Drugs, in ANALOGUE-BASED DRUG
`DISCOVERY III 3 (János Fischer et al. eds., 2013)
`
`Exhibit 2016
`
`Thomas E. Hughes et al., NVP-DPP728: (1-[[[2-[(5-
`Cyanopyridin-2-yl)amino ]ethyl]amino ]acetyl]-2-cyano-(S)-
`pyrrolidine ), a Slow-Binding Inhibitor of Dipeptidyl Peptidase
`IV, 38 BIOCHEM. 11597 (1999)
`
`Exhibit 2017
`
`Coralie Nguyen et al., Specific and Irreversible Cyclopeptide
`Inhibitors of Dipeptidyl Peptidase IV Activity of the T-Cell
`Activation Antigen CD26, 41 J. MED. CHEM. 2100 (1998)
`
`Exhibit 2018
`
`Aiying Wang et al., Potency, Selectivity and Prolonged Binding
`of Saxagliptin to DPP4: Maintenance of DPP4 Inhibition by
`Saxagliptin In Vitro and Ex Vivo When Compared to a Rapidly-
`Dissociating DPP4 Inhibitor, 12 BMC PHARM. 1 (2012)
`
`
`
`2
`
`
`
`Case No. IPR2015-01340
`Patent RE44,186
`
`
`Exhibit
`Description
`Exhibit 2019 Defendants Joint Initial Invalidity Contentions Regarding U.S.
`Patent No. RE44,186
`
`Exhibit 2020
`
`M.A. Nauck et al., Effects of Subcutaneous Glucagon-Like
`Peptide 1(GLP-1 [7–36 Amide]) in Patients with NIDDM, 39
`DIABETOLOGIA 1546 (1996)
`
`Exhibit 2021
`
`Nancy L. Thompson et al., A Fischer Rat Substrain Deficient in
`Dipeptidyl Peptidase IV Activity Makes Normal Steady-State
`RNA Levels and an Altered Protein: Use as a Liver-Cell
`Transplantation Model, 273 J. BIOCHEM. 497 (1991)
`
`Exhibit 2022
`
`Int’l Pub. No. WO 95/15309
`
`Exhibit 2023 U.S. Patent No. 6,011,155
`
`Exhibit2024
`
`Von R. Hiltmann et al., 2-Acylaminopyridin-Derivate mit
`morphinagonistischer und -antagonistischer Wirksamkeit, 24
`ARZNEIM. FORSCH. 584 (1974)
`
`Exhibit 2025 U.S. Patent No. 4,591,598
`
`Exhibit 2026 German Patent Pub. No. 25 21 895 A1
`
`Exhibit 2027 U.S. Patent No. 3,325,478
`
`Exhibit 2028
`
`Stephen Hanessian et al., Probing the Importance of Spacial
`and Conformational Domains in Captopril Analogs for
`Angiotensin Converting Enzyme Activity, 8 BIOORG. & MED.
`CHEM. LETT. 2123 (1998)
`
`Exhibit 2029
`
`Koert Gerzon et al., The Adamantyl Group in Medicinal Agents
`I. Hypoglycemic N-Arylsulfonyl-N’adamantylureas, 6 J. MED.
`CHEM. 760 (1963)
`Exhibit 2030 F. R. Rubio et al., Urinary Metabolites of Rimantadine in
`Humans, 16 DRUG METABOLISM & DISPOSITION 773 (1988)
`
`
`
`3
`
`
`
`
`Exhibit
`
`Description
`
`Case No. IPR2015-01340
`Patent RE44,186
`
`Exhibit 2031
`
`Gunter Fischer et al., The Conformation Around the Peptide
`Bond Between the P1- And P2-Positions Is Important for
`Catalytic Activity of Some Proline-Specific Proteases, 742
`BBA 452 (1983)
`
`Exhibit 2032 U.S. Patent No. 4,954,158
`
`Exhibit 2033
`
`Masahiro Yoshioka et al., Role of Rat Intestinal Brush-Border
`Membrane Angiotensin-Converting Enzyme in Dietary Protein
`Digestion, 253 AM. J. PHYSIOL. G781 (1987)
`
`Exhibit 2034 German Patent Pub. No. 3324263 A1
`
`Exhibit 2035
`
`Stephen Hanessian et al., The Stereocontrolled Synthesis of
`Enantiopure α-Methano Heterocycles and Constrained Amino
`Acid Analogs, 37 TETRAHEDRON LETT. 8967 (1996)
`
`Exhibit 2036 Caplus Records for German Patent Pub. No. 3324263 A1
`
`Exhibit 2037
`
`Roberto Pellicciari et al., Synthesis of All Four
`Diastereoisomers of 4-(Carboxymethyl)proline, a
`Conformationally Constrained Analogue of 2-Aminoadipic
`Acid, 1 J. CHEM. SOC. 1251 (1995)
`
`Exhibit 2038
`
`Viacheslav V. Tverezovsky et al., Synthesis of (2S, 3R, 4S)-3,4-
`Methanoproline and Analogues by Cyclopropylidene Insertion,
`53 TETRAHEDRON 14773 (1997)
`
`Exhibit 2039
`
`Frank L. Switzer et al., Synthesis of (4)-2,3-Methanoproline: A
`Novel Inhibitor of Ethylene Biosynthesis, 45 TETRAHEDRON
`6091 (1989)
`
`Exhibit 2040
`
`Alain Hercouet et al., First Asymmetric Synthesis of (-)-(2S,
`3R)-Methanoproline, 7 TETRAHEDRON: ASYMMETRY 1267
`(1996)
`
`
`
`4
`
`
`
`
`Exhibit
`
`Description
`
`Case No. IPR2015-01340
`Patent RE44,186
`
`Exhibit 2041
`
`Raymond A. Pederson et al., Improved Glucose Tolerance in
`Zucker Fatty Rats by Oral Administration of the Dipeptidyl
`Peptidase IV Inhibitor Isoleucine Thiazolidide, 47 DIABETES
`1253 (1998)
`
`Exhibit 2042
`
`Jingrong Li et al., Aminoacylpyrrolidine-2-nitriles: Potent and
`Stable Inhibitors of Dipeptidyi-Peptidase IV (CD 26), 323
`ARCH. BIOCHEM. & BIOPHYSICS 148 (1995)
`
`Exhibit 2043
`
`Stephen Hanessian et al., The Synthesis of 4,5-Methano
`Congeners of α-Kainic and α-allo-Kainic Acids as Probes for
`Glutamate Receptors 37 TETRAHEDERON LETT. 8971 (1996)
`Exhibit 2044 Koppel et al., The Metabolism of Tromantadine 12 BIOMED.
`MASS. SPECTROM. 497 (1985)
`
`Exhibit 2045
`
`Su et al., Characterization of the In Vitro and In Vivo
`Metabolism and Disposition and Cytochrome P450
`Inhibition/Induction Profile of Saxagliptin in Human 40 DRUG
`METABOLISM AND DISPOSITION 1345 (2012)
`
`Exhibit 2046
`
`He et al., Absorption, Metabolism, and Excretion of
`[14C]Vildagliptin, a Novel Dipeptidyl Peptidase 4 Inhibitor, in
`Humans 37 DRUG METABOLISM AND DISPOSITION 536 (2009)
`Exhibit 2047 Onglyza® Prescribing Info., revised May 2013
`
`Exhibit 2048 Kombiglyze™ XR Prescribing Info., revised May 2013
`Januvia® Prescribing Info., revised Mar. 2015
`Exhibit 2049
`Exhibit 2050 Galvus® Prescribing Info.
`
`
`
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`
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`
`
`5
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`
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`Case No. IPR2015-01340
`Patent RE44,186
`
`Respectfully submitted,
`
`
`
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`
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`
`
`Dated: September 25, 2015 By: /Charles E. Lipsey/
`Charles E. Lipsey, Reg. No. 28,165
`Finnegan, Henderson, Farabow, Garrett &
`Dunner, L.L.P.
`11955 Freedom Drive
`Reston, VA 20190
`
`Counsel for Patent Owner
`
`
`
`
`
`6
`
`
`
`CERTIFICATE OF SERVICE
`
`The undersigned certifies that copies of the foregoing PRELIMINARY
`
`
`
`RESPONSE and Exhibits 2001-2050 were served electronically via e-mail
`
`directed to counsel of record for the Petitioner on September 25, 2015 at the
`
`following:
`
`Steven W. Parmelee
`Michael T. Rosato
`Wilson Sonsini Goodrich & Rosati
`701 Fifth Avenue, Suite 5100
`Seattle, WA 98104-7036
`sparmelee@wsgr.com
`mrosato@wsgr.com
`
`
`
`Mylan has agreed to electronic service.
`
`
`
`Dated: September 25, 2015
`
`
`
`
`
`By: /John W. Kozikowski/
` Litigation Legal Assistant
` FINNEGAN, HENDERSON, FARABOW,
` GARRETT & DUNNER, LLP
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