Petition for Inter Partes Review of U.S. Pat. No. 8,518,987 B2
`
`DOCUMENTS REVIEWED AND RELIED UPON BY
`TERENCE L. THRELFALL, PH.D.
`
`DOCUMENT DESCRIPTION
`Certified U.S. Patent No. 8,518,987 B2
`Certified File History of U.S. Patent No. 8,518,987 B2
`Arun K. Ghosh et al., Potent HIV Protease Inhibitors Incorporating
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`U.S. Patent No. 6,248,775 B1
`Elke Van Gyseghem et al., Solid State Characterization of the Anti-HIV
`Drug TMC114: Interconversion of Amorphous TMC114 Ethanolate
`and Hydrate, 38 EUR. J. PHARMACEUTICAL SCI. 489 (2009)
`Guideline for Submitting Supporting Documentation in Drug
`Applications for the Manufacture of Drug Substances, FOOD & DRUG
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`Stephen Byrn et al., Pharmaceutical Solids: A Strategic Approach to
`Regulatory Considerations, 12 PHARMACEUTICAL RES. 945 (1995)
`Gautam R. Desiraju, Hydration in Organic Crystals: Prediction from
`Molecular Structure, 6 J. CHEMICAL SOC’Y CHEMICAL COMM. 426
`(1991)
`Preface, in POLYMORPHISM IN PHARMACEUTICAL SOLIDS iii, iii-v (Harry
`G. Brittain ed., 1999)
`David J.W. Grant, Theory and Origin of Polymorphism, in
`POLYMORPHISM IN PHARMACEUTICAL SOLIDS 1 (Harry G. Brittain ed.
`1999)
`John Haleblian & Walter McCrone, Pharmaceutical Applications of
`Polymorphism, 58 J. PHARMACEUTICAL SCI. 911
`J. Keith Guillory, Generation of Polymorphs, Hydrates, Solvates, and
`Amorphous Solids, in POLYMORPHISM IN PHARMACEUTICAL SOLIDS 183
`(Harry G. Brittain ed., 1999)
`Örn Almarsson & Michael J. Zaworotko, Crystal Engineering of the
`Composition of Pharmaceutical Phases. Do Pharmaceutical Co-
`crystals Represent a New Path to Improved Medicines?, CHEMICAL
`COMM. 1889 (2004)
`Stephen R. Byrn et al., Hydrates and Solvates, in SOLID-STATE
`CHEMISTRY OF DRUGS 233 (2d ed. 1999)
`Steven S. Zumdahl, CHEMISTRY 31-59, 295-347, 383-433, 559-613
`(1986)
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`Lupin Ex. 1027 (Page 1 of 4)
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`DOCUMENT DESCRIPTION
`R. Docherty, The Application of Computational Chemistry to the Study
`of Molecular Materials, in CRYSTAL GROWTH OF ORGANIC MATERIALS
`2 (Allan S. Myerson et al. eds., 1996)
`Terence L. Threlfall, Analysis of Organic Polymorphs: A Review, 120
`ANALYST 2435 (1995)
`Gregory A. Stephenson et al., Formation of Isomorphic Desolvates:
`Creating a Molecular Vacuum, 87 J. PHARMACEUTICAL SCI. 536 (1998)
`Sherry L. Morissette et al., High Throughput Crystallization:
`Polymorphs, Salts, Co-crystals and Solvates of Pharmaceutical Solids,
`56 ADVANCED DRUG DELIVERY REVIEWS 275 (2004)
`Stephen R. Byrn et al., Solid-State Pharmaceutical Chemistry, 6
`CHEMISTRY MATERIALS 1148 (1994)
`P. Heinrich Stahl, The Problems of Drug Interactions with Excipients,
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`PRODUCTS 265 (D.D. Breimer ed., 1980)
`Bruno C. Hancock & Michael Parks, What is the True Solubility
`Advantage for Amorphous Pharmaceuticals?, 17 PHARMACEUTICAL
`RES. 397 (2000)
`Harry G. Brittain & Eugene F. Fiese, Effects of Pharmaceutical
`Processing on Drug Polymorphs and Solvates, in POLYMORPHISM IN
`PHARMACEUTICAL SOLIDS 331 (Harry G. Brittain ed., 1999)
`Joel Bernstein, Polymorphism of Pharmaceuticals, in POLYMORPHISM
`IN MOLECULAR CRYSTALS 240 (2002)
`HANDBOOK OF PHARMACEUTICAL EXCIPIENTS xv-xvi (Arthur H. Kibbe
`ed., 3d ed. 2000)
`Sudha R. Vippagunta et al., Crystalline Solids, 48 ADVANCE DRUG
`DELIVERY REVIEWS 3 (2001)
`Certified U.S. Patent No. 7,700,645 B2
`Certified File History of U.S. Patent No. 7,700,645 B2
`European Patent Application No. EP 02076929.5
`International Publication No. WO 95/06030 A1
`European Patent No. 1 567 529 B1
`File History of European Patent No. 1 567 529 B1
`Matti U.A. Ahlqvist & Lynne S. Taylor, Water Dynamics in Channel
`Hydrates Investigated Using H/D Exchange, 241 INT’L J.
`PHARMACEUTICS 253 (2002)
`Rajendra K. Khankari & David J.W. Grant, Pharmaceutical Hydrates,
`248 THERMOCHIMICA ACTA 61 (1995)
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`DOCUMENT DESCRIPTION
`Kenneth R. Morris & Nair Rodríguez-Hornedo, Hydrates, in
`ENCYCLOPEDIA OF PHARMACEUTICAL TECHNOLOGY 393 (James
`Swarbrick & James C. Boylan eds., 1993)
`Albert J. Fry, Solvents and Supporting Electrolytes, in LABORATORY
`TECHNIQUES IN ELECTROANALYTICAL CHEMISTRY 469 (Peter T.
`Kissinger & William R. Heineman eds., 2d ed. 1996)
`Charles Cougnon & Jacques Simonet, Cathodic Reactivity of Platinum
`and Palladium in Electrolytes in Superdry Conditions, 46 PLATINUM
`METALS REV. 94 (2002)
`Dian J. Gaffen et al., Annual Cycles of Tropospheric Water Vapor, 97 J.
`GEOPHYSICAL RES. 18185 (1992)
`Svante Arrhenius, On the Influence of Carbonic Acid in the Air Upon
`the Temperature of the Ground, in CLIMATE CHANGE: CRITICAL
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`Agenerase® Prescribing Information (April 1999)
`Kenneth R. Morris, Structural Aspects of Hydrates and Solvates, in
`POLYMORPHISM IN PHARMACEUTICAL SOLIDS 125 (Harry G. Brittain
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`RES. 146 (1983)
`Trial Transcripts from March 18, 2014 – April 2, 2014 trial proceedings
`in Janssen Products, L.P. et al. v. Lupin Ltd. et al., Consolidated Case
`No. 10-5954 (D.N.J.)
`Declaration of Frederick J. Northrup, Ph.D. in Support of Lupin
`Limited’s Petition for Inter Partes Review of U.S. Patent No. 8,518,987
`B2
`Printout of Data File of Dr. Northrup’s Powder X-Ray Diffraction
`testing on “Compound 13” (Apr. 8, 2015)
`Printout of Data File of Dr. Northrup’s Powder X-Ray Diffraction
`testing on “Compound 13 EtOH recrystallized” (Apr. 8, 2015)
`Printout of Data File of Dr. Northrup’s Powder X-Ray Diffraction
`testing on “Compound 13 iPrOH recrystallized” (Apr. 8, 2015)
`Printout of Data File of Dr. Northrup’s Thermogravimetric Analysis
`
`Lupin Ex. 1027 (Page 3 of 4)
`
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`Petition for Inter Partes Review of U.S. Pat. No. 8,518,987 B2
`
`Doc. No.
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`DOCUMENT DESCRIPTION
`sample mass testing on “Compound 13” (Apr. 8, 2015)
`Printout of Data File of Dr. Northrup’s Thermogravimetric Analysis
`sample mass testing on “Compound 13 EtOH recrystallized” (Apr. 8,
`2015)
`Printout of Data File of Dr. Northrup’s Thermogravimetric Analysis
`sample mass testing on “Compound 13 iPrOH recrystallized” (Apr. 8,
`2015)
`Printout of Data File of Dr. Northrup’s Thermogravimetric Analysis /
`Mass Spectrometry testing on “Compound 13” (Apr. 8, 2015)
`Printout of Data File of Dr. Northrup’s Thermogravimetric Analysis /
`Mass Spectrometry testing on “Compound 13 EtOH recrystallized”
`(Apr. 8, 2015)
`Printout of Data File of Dr. Northrup’s Thermogravimetric Analysis /
`Mass Spectrometry testing on “Compound 13 iPrOH recrystallized”
`(Apr. 8, 2015)
`Declaration of Aristotle G. Kalivretenos, Ph.D. in Support of Lupin
`Limited’s Petition for Inter Partes Review of U.S. Patent No. 8,518,987
`B2
`Packing Slip from Aurora Analytics, LLC to Frederick Northrup, Ph.D.
`(Apr. 4, 2015)
`Certificate of Analysis of “Compound 13 Darunavir” (Apr. 8, 2015)
`Certificate of Analysis of “Compound 13 Darunavir, ethanol
`recrystallized” (Apr. 8, 2015)
`Certificate of Analysis of “Compound 13 Darunavir, isopropyl
`recrystallized” (Apr. 8, 2015)
`
`Lupin Ex. 1027 (Page 4 of 4)
`
`