`Matthew L. Fedowitz, Esq.
`Daniel R. Evans, Esq.
`MERCHANT & GOULD P.C.
`1900 Duke Street, Suite 600
`Alexandria, VA 22314
`Main Telephone: (703) 684-2500
`Main Facsimile: (703) 684-2501
`
`
`
`
`
`
`
`
`
`UNITED STATES PATENT AND TRADEMARK OFFICE
`_____________________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`_____________________
`
`
`
`BRECKENRIDGE PHARMACEUTICAL, INC.
`Petitioner
`
`v.
`
`
`
`NOVARTIS AG
`Patent Owner
`
`_____________________
`
`Case No. To Be Assigned
`Patent No. 5,665,772
`_____________________
`
`
`
`APPENDIX OF EXHIBITS
`
`
`
`
`
`1001 U.S. Patent No. 5,665,772
`
`1002 File History for U.S. Patent No. 5,665,772
`
`1003 Declaration of William L. Jorgensen, Ph.D. in Support of Petition for
`Inter Partes Review of U.S. Patent No. 5,665,772
`
`1004 Curriculum Vitae of William L. Jorgensen
`
`1005 Randall Ellis Morris, Rapamycins: Antifungal, Antitumor,
`Antiproliferative, and Immunosuppressive Macrolides, 6
`TRANSPLANTATION REVIEWS 39 (1992)
`
`1006 Gregory D. Van Duyne et al., Atomic Structure of the Rapamycin Human
`Immunophilin FKBP-12 Complex, 113 J. AM. CHEMICAL SOC’Y 7433
`(1991)
`
`1007 Samuel H. Yalkowsky, Estimation of Entropies of Fusion of Organic
`Compounds, 18 INDUS. & ENG’G CHEMISTRY FUNDAMENTALS
`108 (1979)
`
`1008 Thomas L. Lemke, Chapter 16: Predicting Water Solubility, REVIEW OF
`ORGANIC FUNCTIONAL GROUPS 113 (2d ed. 1988)
`
`1009 U.S. Patent No. 5,233,036
`
`1010 U.S. Patent No. 4,650,803
`
`1011 U.S. Patent No. 5,100,883
`
`1012 Stuart L. Schreiber, Chemistry and Biology of the Immunophilins and
`Their Immunosuppressive Ligands, 251 SCI. 283 (1991)
`
`1013
`
`Joseph B. Moon & W. Jeffrey Howe, Computer Design of Bioactive
`Molecules: A Method for Receptor-Based de Novo Ligand Design, 11
`PROTEINS: STRUCTURE, FUNCTION, & GENETICS 314 (1991)
`
`1014 Hans-Joachim Böhm, LUDI: rule-based automatic design of new
`substituents for enzyme inhibitor leads, 6 J. COMPUTER-AIDED
`MOLECULAR DESIGN 593 (1992)
`
`
`
`2
`
`
`
`1015 Silverman, Chapter 2: Drug Discovery, Design, and Development, THE
`ORGANIC CHEMISTRY OF DRUG DESIGN & ACTION 4 (1992)
`
`1016
`
`Julianto Pranata & William L. Jorgensen, Computational Studies on
`FK506: Conformational Search and Molecular Dynamics Simulation in
`Water, 113 J. AM. CHEMICAL SOC’Y 9483 (1991)
`
`1017 William L. Jorgensen, Rusting of the Lock and Key Model for Protein-
`Ligand Binding, 254 SCI. 954 (1991)
`
`1018 Modesto Orozco et al., Mechanism for the Rotamase Activity of FK506
`Binding Protein from Molecular Dynamics Simulations, 32
`BIOCHEMISTRY 12864 (1993)
`
`1019 Michelle L. Lamb & William L. Jorgensen, Investigations of
`Neurotrophic Inhibitors of FK506 Binding Protein via Monte Carlo
`Simulations, 41 J. MED. CHEMISTRY 3928 (1998)
`
`1020 Michelle L. Lamb et al., Estimation of Binding Affinities of FKBP12
`Inhibitors Using a Linear Response Method, 7 BIOORGANIC &
`MEDICINAL CHEMISTRY 851 (1999)
`
`1021 Thomas W. Bell, Construction of a Soluble Heptacyclic Terpyridine, 51 J.
`ORGANIC CHEMISTRY 764 (1986)
`
`1022 M. Ballauff, Phase Equilibria in Rodlike Systems with Flexible Side
`Chains, 19 MACROMOLECULES 1366 (1986)
`
`1023 R. Stern et al., Rigid rod polymers with flexible side chains, 32
`POLYMER 2096 (1991)
`
`1024 Michael G. Rossmann et al., Three-Dimensional Coordinates from
`Stereodiagrams of Molecular Structures, B36 ACTA
`CRYSTALLOGRAPHICA 819 (1980)
`
`1025 William L. Jorgensen & Julian Tirado-Rives, The OPLS Potential
`Functions for Proteins. Energy Minimizations for Crystals of Cyclic
`Peptides and Crambin, 110 J. AM. CHEMICAL SOC’Y 1657 (1988)
`
`
`
`3
`
`
`
`1026
`
`Julian Tirado-Rives & William L. Jorgensen, Molecular Dynamics of
`Proteins with the OPLS Potential Functions. Simulation of the Third
`Domain of Silver Pheasant Ovomucoid in Water, 112 J. AM. CHEMICAL
`SOC’Y 2773 (1990)
`
`1027 Michael L. Connolly, Solvent-Accessible Surfaces of Proteins and Nucleic
`Acids, 221 SCI. 709 (1983)
`
`1028 Yoshihiko Nisibata et al., Automatic Creation of Drug Candidate
`Structures Based on Receptor Structure. Starting Point for Artificial
`Lead Generation., 47 TETRAHEDRON 8985 (1991)
`
`1029 Stephen W. Michnick et al., Solution Structure of FKBP, a Rotamase
`Enzyme and Receptor for FK506 and Rapamycin, 252 SCI. 836 (1991)
`
`
`
`
`
`
`
`4
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