On behalf of: Par Pharmaceutical, Inc. et al.
`
`
`
`
`
`
`Entered: January 3, 2017
`
`
`
`UNITED STATES PATENT AND TRADEMARK OFFICE
`_______________________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`_______________________
`
`PAR PHARMACEUTICAL, INC., BRECKENRIDGE PHARMACEUTICAL,
`INC., AND ROXANE LABORATORIES, INC.
`Petitioners
`
`v.
`
`NOVARTIS AG
`Patent Owner
`_______________________
`Case IPR2016-000841
`U.S. Patent No. 5,665,772
`_______________________
`
`Before LORA M. GREEN, CHRISTOPHER L. CRUMBLEY, and
`ROBERT A. POLLOCK, Administrative Patent Judges.
`
`
`
`PETITIONERS’ UPDATED EXHIBIT LIST
`
`
`
`
`
`
`1 Breckenridge Pharmaceutical, Inc. was joined as a party to this proceeding via a
`Motion for Joinder in IPR2016-01023; Roxane Laboratories, Inc. was joined as a
`party via a Motion for Joinder in IPR2016-01102.
`
`
`
`
`
`
`
`
`
`
`Entered: January 3, 2017
`
`
`
`UNITED STATES PATENT AND TRADEMARK OFFICE
`_______________________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`_______________________
`
`PAR PHARMACEUTICAL, INC., BRECKENRIDGE PHARMACEUTICAL,
`INC., AND ROXANE LABORATORIES, INC.
`Petitioners
`
`v.
`
`NOVARTIS AG
`Patent Owner
`_______________________
`Case IPR2016-000841
`U.S. Patent No. 5,665,772
`_______________________
`
`Before LORA M. GREEN, CHRISTOPHER L. CRUMBLEY, and
`ROBERT A. POLLOCK, Administrative Patent Judges.
`
`
`
`PETITIONERS’ UPDATED EXHIBIT LIST
`
`
`
`
`
`
`1 Breckenridge Pharmaceutical, Inc. was joined as a party to this proceeding via a
`Motion for Joinder in IPR2016-01023; Roxane Laboratories, Inc. was joined as a
`party via a Motion for Joinder in IPR2016-01102.
`
`
`
`
`
`Case IPR2016-00084
`U.S. Patent No. 5,665,772
`
`
`Pursuant to 37 C.F.R. § 42.63(e), Petitioners Par Pharmaceutical, Inc. et al.
`
`respectfully submit the following current exhibit list.
`
`Exhibit Description
`1001
`U.S. Patent No. 5,665,772 (“the ’772 Patent”)
`
`1002
`
`1003
`
`1004
`
`1005
`
`1006
`
`1007
`
`1008
`
`1009
`
`1010
`
`1011
`
`1012
`
`1013
`
`File History for the ’772 Patent
`
`Declaration of William L. Jorgensen, Ph.D. in Support of Petition for
`Inter Partes Review of U.S. Patent No. 5,665,772
`
`Curriculum Vitae of William L. Jorgensen
`
`Randall Ellis Morris, Rapamycins: Antifungal, Antitumor, Antiprolif-
`erative, and Immunosuppressive Macrolides, 6 TRANSPLANTATION RE-
`VIEWS 39 (1992) (“Morris”)
`
`Gregory D. Van Duyne et al., Atomic Structure of the Rapamycin Hu-
`man Immunophilin FKBP-12 Complex, 113 J. AM. CHEMICAL SOC’Y
`7433 (1991) (“Van Duyne”)
`
`Samuel H. Yalkowsky, Estimation of Entropies of Fusion of Organic
`Compounds, 18 INDUS. & ENG’G CHEMISTRY FUNDAMENTALS 108
`(1979) (“Yalkowsky”)
`
`Thomas L. Lemke, Chapter 16: Predicting Water Solubility, REVIEW
`OF ORGANIC FUNCTIONAL GROUPS 113 (2d ed. 1988)
`
`U.S. Patent No. 5,233,036 (“Hughes”)
`
`U.S. Patent No. 4,650,803 (“Stella”)
`
`U.S. Patent No. 5,100,883 (“Scheihser”)
`
`Stuart L. Schreiber, Chemistry and Biology of the Immunophilins and
`Their Immunosuppressive Ligands, 251 SCI. 283 (1991) (“Schreiber”)
`
`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) (“Moon”)
`
`1
`
`
`
`Case IPR2016-00084
`U.S. Patent No. 5,665,772
`
`Exhibit Description
`Hans-Joachim Böhm, LUDI: rule-based automatic design of new sub-
`1014
`stituents for enzyme inhibitor leads, 6 J. COMPUTER-AIDED MOLECULAR
`DESIGN 593 (1992) (“Böhm”)
`
`1015
`
`1016
`
`1017
`
`1018
`
`1019
`
`1020
`
`1021
`
`1022
`
`1023
`
`1024
`
`Silverman, Chapter 2: Drug Discovery, Design, and Development,
`THE ORGANIC CHEMISTRY OF DRUG DESIGN & ACTION 4 (1992) (“Sil-
`verman”)
`
`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)
`
`William L. Jorgensen, Rusting of the Lock and Key Model for Protein-
`Ligand Binding, 254 SCI. 954 (1991)
`
`Modesto Orozco et al., Mechanism for the Rotamase Activity of FK506
`Binding Protein from Molecular Dynamics Simulations, 32 BIOCHEM-
`ISTRY 12864 (1993)
`
`Michelle L. Lamb & William L. Jorgensen, Investigations of Neu-
`rotrophic Inhibitors of FK506 Binding Protein via Monte Carlo Simu-
`lations, 41 J. MED. CHEMISTRY 3928 (1998)
`
`Michelle L. Lamb et al., Estimation of Binding Affinities of FKBP12
`Inhibitors Using a Linear Response Method, 7 BIOORGANIC & MEDICI-
`NAL CHEMISTRY 851 (1999)
`
`Thomas W. Bell, Construction of a Soluble Heptacyclic Terpyridine, 51
`J. ORGANIC CHEMISTRY 764 (1986) (“Bell”)
`
`M. Ballauff, Phase Equilibria in Rodlike Systems with Flexible Side
`Chains, 19 MACROMOLECULES 1366 (1986) (“Ballauff”)
`
`R. Stern et al., Rigid rod polymers with flexible side chains, 32 POLY-
`MER 2096 (1991) (“Stern”)
`
`Michael G. Rossmann et al., Three-Dimensional Coordinates from Ste-
`reodiagrams of Molecular Structures, B36 ACTA CRYSTALLOGRAPHICA
`819 (1980) (“Rossmann”)
`
`2
`
`
`
`Case IPR2016-00084
`U.S. Patent No. 5,665,772
`
`Exhibit Description
`William L. Jorgensen & Julian Tirado-Rives, The OPLS Potential
`1025
`Functions for Proteins. Energy Minimizations for Crystals of Cyclic
`Peptides and Crambin, 110 J. AM. CHEMICAL SOC’Y 1657 (1988)
`
`1026
`
`1027
`
`1028
`
`1029
`
`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)
`
`Michael L. Connolly, Solvent-Accessible Surfaces of Proteins and Nu-
`cleic Acids, 221 SCI. 709 (1983)
`
`Yoshihiko Nisibata et al., Automatic Creation of Drug Candidate
`Structures Based on Receptor Structure. Starting Point for Artificial
`Lead Generation., 47 TETRAHEDRON 8985 (1991)
`
`Stephen W. Michnick et al., Solution Structure of FKBP, a Rotamase
`Enzyme and Receptor for FK506 and Rapamycin, 252 SCI. 836 (1991)
`
`10302
`
`Declaration of Scott Bennett, Ph.D.
`
`1031
`
`1032
`
`1033
`
`1034
`
`1035
`
`1036
`
`Transcript of June 1, 2016 Conference Call
`
`Transcript of June 17, 2016 Conference Call
`
`Transcript of November 8, 2016 Conference Call
`
`Heinz-Herbert Fiebig et al., In Vitro and In Vivo Evaluation of US-NCI
`Compounds in Human Tumor Xenografts, 17 CANCER TREATMENT
`REVS. 109 (1990)
`
`Transcript of the November 11, 2016 deposition of Howard A. Burris,
`III
`
`Robert C. Young et al., The Anthracycline Antineoplastic Drugs, 305
`NEW ENG. J. MED. 139 (1981)
`
`
`2 Ex. 1030 was served, but not filed, on May 27, 2016.
`
`3
`
`
`
`Case IPR2016-00084
`U.S. Patent No. 5,665,772
`
`Exhibit Description
`S. K. Carter The Clinical Evaluation of Analogs – III. Anthracyclines, 4
`1037
`CANCER CHEMOTHERAPY PHARMACOLOGY 5 (1980)
`
`1038
`
`1039
`
`1040
`
`1041
`
`1042
`
`1043
`
`1044
`
`1045
`
`1046
`
`Harinder S. Garewal et al., Phase I Trial of Esorubicin
`(4’Deoxydoxorubicin), 2. J. CLINICAL ONCOLOGY 1034 (1984)
`
`Elaine M. Rankin et al., A Phase II Study of 4-Deoxydoxorubicin in Ad-
`vanced Breast Cancer, 23 EUR. J. CANCER CLINICAL ONCOLOGY 1979
`(1987)
`
`Thomas P. Miller et al., Activity of Esorubicin in Recurrent Malignant
`Lymphoma: A Southwest Oncology Group Study, 9 J. CLINICAL ON-
`COLOGY 1204 (1991)
`
`S. T. Crooke et al., Structure-Activity Relationships of Anthracyclines
`Relative to Effects on Macromolecular Syntheses, 14 MOLECULAR
`PHARMACOLOGY 290 (1978)
`
`Toshikazu Oki et al., New Antitumor Antibiotics, Aclacinomycins A and
`B, 28 J. ANTIBIOTICS 830 (1975)
`
`Vivien H. Bramwell et al., Carminomycin vs Adriamycin in Advanced
`Soft Tissue Sarcomas: an EORTC Randomised Phase II Study, 19 EUR.
`J. CANCER CLINICAL ONCOLOGY 1097 (1983)
`
`European Soc’y for Med. Oncology & Anticancer Fund, Stomach Can-
`cer: A Guide for Patients (2012),
`https://www.esmo.org/content/download/6635/115239/file/EN-
`Stomach-Cancer-Guide-for-Patients.pdf
`
`Nat’l Comprehensive Cancer Network, Clinical Practice Guidelines in
`Oncology (NCCN Guidelines): Gastric Cancer – Version 3.2016 (2016)
`
`British Columbia Cancer Agency, Drug Manual - Epirubicin (Jan. 1,
`2015), http://www.bccancer.bc.ca/drug-database-
`site/Drug%20Index/Epirubicin_monograph_1Jan2015.pdf
`
`4
`
`
`
`Case IPR2016-00084
`U.S. Patent No. 5,665,772
`
`Exhibit Description
`Fabien Lamoureux et al., Sirolimus and Everolimus Intestinal Absorp-
`1047
`tion and Interaction with Calcineurin Inhibitors: A Differential Effect
`Between Cyclosporine and Tacrolimus, 28 FUNDAMENTAL & CLINICAL
`PHARMACOLOGY 463 (2012)
`
`1048
`
`1049
`
`1050
`
`1051
`
`1052
`
`1053
`
`1054
`
`1055
`
`John M. Kovarik et al., Influence of Delayed Initiation of Cyclosporine
`on Everolimus Pharmacokinetics in de Novo Renal Transplant Patients,
`3 AM. J. TRANSPLANTATION 1576 (2003)
`
`John M. Kovarik et al., Everolimus Drug Interactions: Application of a
`Classification System for Clinical Decision Making, 27 BIOPHARMA-
`CEUTICS & DRUG DISPOSITION 421 (2006)
`
`John M. Kovarik et al., Longitudinal Assessment of Everolimus in de
`novo Renal Transplant Recipients Over First Post-Transplant Year:
`Pharmacokinetics, Exposure-Response Relationships, and Influence on
`Cyclosporine, 69 CLINICAL PHARMACOLOGY & THERAPEUTICS 48
`(2001)
`
`K. Mross et al., Pharmacokinetics and Metabolism of Epidoxorubicin
`and Doxorubicin in Humans, 6 J. CLINICAL ONCOLOGY 517 (1988)
`
`Catharina Bäärnhielm & Christer Westerlund, Quantitative Relation-
`ships Between Structure and Microsomal Oxidation Rate of 1,4-
`Dihydropyridines, 58 CHEMICO-BIOLOGICAL INTERACTIONS 277 (1986)
`
`Peter A. Meredith et al., Application of Pharmacokinetic-
`Pharmacodynamic Modelling for the Comparison of Quinazoline α-
`Adrenoceptor Agonists in Normotensive Volunteers, 7 J. CARDIOVAS-
`CULAR PHARMACOLOGY 532 (1985)
`
`Abdulla Haj-Yehia & Meir Bialer, Structure-Pharmacokinetic Rela-
`tionships in a Series of Valpromide Derivatives with Antiepileptic Ac-
`tivity, 6 PHARMACEUTICAL RES. 683 (1989)
`
`Susanne Beckebaum et al., Efficacy, Safety, and Immunosuppressant
`Adherence in Stable Liver Transplant Patients Converted from a Twice-
`Daily Tacrolimus-Based Regimen to Once-Daily Tacrolimus Extended-
`Release Formulation, 24 TRANSPLANT INT’L 666 (2011)
`
`5
`
`
`
`Case IPR2016-00084
`U.S. Patent No. 5,665,772
`
`Exhibit Description
`Thomas E. Nevins et al., Predictive Patterns of Early Medication Ad-
`1056
`herence in Renal Transplantation, 98 TRANSPLANTATION 878 (2014)
`
`1057
`
`1058
`
`1059
`
`1060
`
`1061
`
`1062
`
`1063
`
`1064
`
`1065
`
`1066
`
`G. Corbetta & C. Ponticelli, Once-a-day Administration of Everolimus,
`Cyclosporine, and Steroid After Renal Transplantation: A Review of the
`Rationale, 42 TRANSPLANTATION PROC. 1303 (2010)
`
`Charles Grudzinskas, Chapter 33: Design of Clinical Development
`Programs, in PRINCIPLES OF CLINICAL PHARMACOLOGY 501 (2d ed.
`2007)
`
`Public Assessment Report of the Medicines Evaluation Board in the
`Netherlands – Epirubicin Hydrochloride (Aug. 27, 2009), http://db.cbg-
`meb.nl/Pars/h108079.pdf
`
`Meds. & Healthcare Prods. Regulatory Agency (MHRA), United King-
`dom Public Assessment Report – Epirubicin Hydrochloride 10 mg and
`50 mg Powder for Solution for Injection,
`http://www.mhra.gov.uk/home/groups/par/documents/websiteresources
`/con213154.pdf
`
`Pfizer Canada, Product Monograph for Pharmorubicin PFS (Epirubi-
`cin Hydrochloride Injection) (2014),
`http://www.pfizer.ca/sites/g/files/g10017036/f/201410/pharmorubicin-
`pm-173657-E.pdf
`
`U.S. Patent No. 4,885,171
`
`U.S. Patent No. 5,206,018
`
`Curriculum Vitae of Mark J. Ratain
`
`Robert S. Kerbel, Human Tumor Xenografts as Predictive Preclinical
`Models for Anticancer Drug Activity in Humans, 2 CANCER BIOLOGY &
`THERAPY S134 (2003)
`
`H. Charles Manning et al., Mouse Models of Breast Cancer: Platforms
`for Discovering Precision Imaging Diagnostics and Future Cancer
`Medicine, 57 J. NUCLEAR MED. 60S (2016)
`
`6
`
`
`
`Case IPR2016-00084
`U.S. Patent No. 5,665,772
`
`Exhibit Description
`Matthew Trendowski et al., Effects of mTOR Inhibitors and Cytoskele-
`1067
`tal-Directed Agents Alone and in Combination Against Normal and
`Neoplastic Hematopoietic Cells In Vitro, 33 INVESTIGATIONAL NEW
`DRUGS 1162 (2015)
`
`1068
`
`1069
`
`1070
`
`1071
`
`1072
`
`1073
`
`1074
`
`1075
`
`1076
`
`1077
`
`Dirk P. Dittmer et al., Rapalogs in Viral Cancers, 21 EXPERT OPINION
`INVESTIGATIONAL DRUGS 135 (2012)
`
`C. M. Hartford & M. J. Ratain, Rapamycin: Something Old, Something
`New, Sometimes Borrowed and Now Renewed, 82 CLINICAL PHARMA-
`COLOGY & THERAPEUTICS 381 (2007)
`
`U.S. Patent No. 5,100,899
`
`Transcript of August 30, 2016 Trial Testimony of Dr. Howard A. Bur-
`ris
`
`2011 European Multidisciplinary Cancer Congress, 23-27 September
`2011, Stockholm, Sweden, EUR. SOC’Y FOR MED. ONCOLOGY (2011)
`
`European Multidisciplinary Cancer Cong., Congress Update Service,
`Issue for October 2011 (2011), http://www.ecco-
`org.eu/~/media/Documents/ECCO%20sections/Stockholm%202011/Ne
`ws%20and%20alerts/Congress%20update%20services/Issue7_August2
`011_rev3.pdf
`
`Paul E. Goss et al., Aromatase Inhibitors in the Treatment and Preven-
`tion of Breast Cancer, 19 J. CLINICAL ONCOLOGY 881 (2001)
`
`Femara Package Insert (Revised 01/2014)
`
`Arimidex Package Insert (Revised 10/2010)
`
`Howard A. Burris, III et al., Health-Related Quality of Life of Patients
`With Advanced Breast Cancer Treated With Everolimus Plus Exemes-
`tane Versus Placebo Plus Exemestane in the Phase 3, Randomized,
`Controlled, BOLERO-2 Trial, 119 CANCER 1908 (2013)
`
`7
`
`
`
`Case IPR2016-00084
`U.S. Patent No. 5,665,772
`
`Exhibit Description
`Howard A. Burris III et al., Pegfilgrastim on the Same Day Versus Next
`1078
`Day of Chemotherapy in Patients With Breast Cancer, Non–Small-Cell
`Lung Cancer, Ovarian Cancer, and Non-Hodgkin’s Lymphoma: Results
`of Four Multicenter, Double-Blind, Randomized Phase II Studies, 6 J.
`ONCOLOGY PRACTICE 133 (2010)
`
`1079
`
`1080
`
`1081
`
`1082
`
`1083
`
`1084
`
`1085
`
`1086
`
`José Baselga et al., Everolimus in Postmenopausal Hormone-Receptor–
`Positive Advanced Breast Cancer, 366 NEW ENG. J. MED. 520 (2012)
`
`C. Villarreal-Garza et al., mTOR Inhibitors in the Management of Hor-
`mone Receptor-Positive Breast Cancer: The Latest Evidence and Fu-
`ture Directions, 23 ANNALS ONCOLOGY 2526 (2012)
`
`Francis Arena, Clinical Implications of Recent Studies Using mTOR In-
`hibitors to Treat Advanced Hormone Receptor-Positive Breast Cancer,
`6 CANCER MGMT. & RES. 389 (2014)
`
`Carlo Palmieri et al., Breast Cancer: Current and Future Endocrine
`Therapies, 382 MOLECULAR & CELLULAR ENDOCRINOLOGY 695 (2014)
`
`Elisavet Paplomata & Ruth O’Regan, New and Emerging Treatments
`for Estrogen Receptor-Positive Breast Cancer: Focus on Everolimus, 9
`THERAPEUTICS & CLINICAL RISK MGMT. 27 (2013)
`
`K. I. Pritchard et al., Endocrine Therapy for Postmenopausal Women
`with Hormone Receptor-Positive HER2-Negative Advanced Breast
`Cancer After Progression or Recurrence on Nonsteroidal Aromatase
`Inhibitor Therapy: A Canadian Consensus Statement, 20 CURRENT ON-
`COLOGY 48 (2013)
`
`Rowan T. Chlebowski, Strategies to Overcome Endocrine Therapy Re-
`sistance in Hormone Receptor-Positive Advanced Breast Cancer, 4
`CLINICAL INVESTIGATION 19 (2014)
`
`Stephen Chan et al., Phase II Study of Temsirolimus (CCI-779), a Novel
`Inhibitor of mTOR, in Heavily Pretreated Patients with Locally Ad-
`vanced or Metastatic Breast Cancer, 23 J. CLINICAL ONCOLOGY 5314
`(2005)
`
`8
`
`
`
`Case IPR2016-00084
`U.S. Patent No. 5,665,772
`
`Exhibit Description
`1087
`Torisel Package Insert (Revised 05/2007)
`
`1088
`
`1089
`
`1090
`
`1091
`
`1092
`
`1093
`
`1094
`
`1095
`
`1096
`
`1097
`
`1098
`
`K. Öberg, Treatment of Neuroendocrine Tumours of the Gastrointesti-
`nal Tract, 27 ONCOLOGIA 57 (2004)
`
`Nexavar Package Insert (Revised 10/2010)
`
`Sutent Package Insert (Revised 05/2011)
`
`Nat’l Comprehensive Cancer Network, Clinical Practice Guidelines in
`Oncology: Kidney Cancer – Version 1.2017 (Sept. 26, 2016),
`www.nccn.org/patients
`
`Michael B. Atkins et al., Randomized Phase II Study of Multiple Dose
`Levels of CCI-779, a Novel Mammalian Target of Rapamycin Kinase
`Inhibitor, in Patients With Advanced Refractory Renal Cell Carcinoma,
`22 J. CLINICAL ONCOLOGY 909 (2004)
`
`John J. Bissler et al., Sirolimus for Angiomyolipoma in Tuberous Scle-
`rosis Complex or Lymphangioleiomyomatosis, 358 NEW ENG. J. MED.
`140 (2008)
`
`Transcript of August 30, 2016 Trial Testimony of Dr. John J. Bissler
`
`U.S. Nat’l Inst. of Health, Rapamycin Therapy for Patients With Tu-
`berous Sclerosis Complex and Sporadic LAM (2007),
`https://clinicaltrials.gov/ct2/show/NCT00457808?term=NCT00457808
`&rank=1
`
`U.S. Nat’l Inst. of Health, RAD001 Therapy of Angiomyolipomata in
`Patients with TS Complex and Sporadic LAM (2013),
`https://clinicaltrials.gov/ct2/show/NCT00457964?term=NCT00457964
`&rank=1
`
`John J. Bissler & John C. Kingswood, Optimal Treatment of Tuberous
`Sclerosis Complex Associated Renal Angiomyolipomata: A Systematic
`Review, 8 THERAPEUTIC ADVANCES IN UROLOGY 279 (2016)
`
`David Neal Franz et al., Rapamycin Causes Regression of Astrocytomas
`in Tuberous Sclerosis Complex, 59 ANNALS NEUROLOGY 490 (2006)
`
`9
`
`
`
`Case IPR2016-00084
`U.S. Patent No. 5,665,772
`
`Exhibit Description
`Catherine Lam et al., Rapamycin (Sirolimus) in Tuberous Sclerosis As-
`1099
`sociated Pediatric Central Nervous System Tumors, 54 PEDIATRIC
`BLOOD CANCER 476 (2010)
`
`1100
`
`1101
`
`1102
`
`1103
`
`1104
`
`1105
`
`1106
`
`1107
`
`1108
`
`Andrew J. Wagner et al., Clinical Activity of mTOR Inhibition With Si-
`rolimus in Malignant Perivascular Epithelioid Cell Tumors: Targeting
`the Pathogenic Activation of mTORC1 in Tumors, 28 J. CLINICAL ON-
`COLOGY 835 (2010)
`
`AADi Launches Its Phase 2 Registration Trial for ABI-009, a Targeted
`mTOR Inhibitor, for Patients with Advanced PEComa, a Rare Form of
`Sarcoma, BUS. WIRE (Nov. 2, 2015),
`http://www.businesswire.com/news/home/20151102005411/en/AADi-
`Launches-Phase-2-Registration-Trial-ABI-009
`
`S. Vignot et al., mTOR-Targeted Therapy of Cancer With Rapamycin
`Derivatives, 16 ANNALS ONCOLOGY 525 (2005)
`
`Ravi D. Rao et al., Mammalian Target of Rapamycin (mTOR) Inhibi-
`tors as Anti-Cancer Agents, 4 CURRENT CANCER DRUG TARGETS 621
`(2004)
`
`Shile Huang et al., Rapamycins: Mechanism of Action and Cellular Re-
`sistance, 2 CANCER BIOLOGY & THERAPY 222 (2003)
`
`David M. Sabatini, mTOR and Cancer: Insights Into a Complex Rela-
`tionship, 6 NATURE REVIEWS: CANCER 729 (2006)
`
`U.S. Patent Application Publication No. US 2015/0140036
`
`Alice Goodman, Novel Initiative to Address Oncology Drug Crisis,
`ASCO POST (May 15, 2012), available at
`http://www.ascopost.com/issues/may-15-2012/novel-initiative-to-
`address-oncology-drug-crisis.aspx
`
`David I. Quinn and Primo N. Lara, Jr., Renal-Cell Cancer – Targeting
`an Immune Checkpoint or Multiple Kinases, 373 NEW ENG. J. MED
`1872 (2015)
`
`10
`
`
`
`Case IPR2016-00084
`U.S. Patent No. 5,665,772
`
`Exhibit Description
`T. K. Choueiri et al., Cabozantinib versus Everolimus in Advanced Re-
`1109
`nal-Cell Carcinoma, 373 NEW ENG. J. MED 1814 (2015)
`
`1110
`
`1111
`
`1112
`
`1113
`
`1114
`
`1115
`
`1116
`
`1117
`
`1118
`
`1119
`
`1120
`
`1121
`
`1122
`
`R. J. Motzer et al., Nivolumab versus Everolimus in Advanced Renal-
`Cell Carcinoma, 373 NEW ENG. J. MED 1803 (2015)
`
`Cometriq Package Insert (Revised 11/2012)
`
`Opdivo (nivolumab) Package Insert (Revised 12/2014).
`
`C. P. Eng et al., Activity of Rapamycin (AY-22,989) Against Trans-
`planted Tumors, 37 J. ANTIBIOTICS 1231 (1984)
`
`Deposition of Alexander M. Klibanov (November 14, 2016)
`
`Deposition of William R. Roush (November 21, 2016)
`
`Transcript of August 30, 2016 Trial Testimony of Dr. William R.
`Roush
`
`Peter A. Schwartz & Anthony N. Paruta, Solution Thermodynamics of
`Alkyl p-Aminobenzoates, 65 J. PHARMACEUTICAL SCI. 252 (1976)
`
`Supplemental Declaration of William L. Jorgensen, Ph.D. in Support of
`Petitioner’s Reply in the Inter Partes Review of U.S. Patent No.
`5,665,772
`
`Declaration of Mark J. Ratain, M.D. in Support of Petitioner’s Reply in
`the Inter Partes Review of U.S. Patent No. 5,665,772
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`J. Chris Kingswood et al., Review of the Tuberous Sclerosis Renal
`Guidelines from the 2012 Consensus Conference: Current Data and
`Future Study, 134 NEPHRON 51 (2016)
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`Physicians’ Desk Reference 742, 1348, 2138 (42d ed. 1988)
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`U.S. FDA, ICH, Guidance for Industry: S9 Nonclinical Evaluation for
`Anticancer Pharmaceuticals (Mar. 2010)
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`11
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`Case IPR2016-00084
`U.S. Patent No. 5,665,772
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`Exhibit Description
`Excerpts from Late Breaking and Best of 2011 European Multidiscipli-
`1123
`nary Cancer Congress and Award Abstracts, 47 (Supp. 2) EUR. J. CAN-
`CER 6-7, 9 (2011)
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`1124
`
`1125
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`Declaration of Jonathan M. Strang served in response to Objections
`served on December 12, 2016 (served, not filed)
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`Email chain between C. Schwarz, J. Strang and Board regarding request
`for teleconference (December 8-9, 2016)
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`Respectfully submitted,
`
`/Daniel G. Brown/
`By:
`Daniel G. Brown (Reg. No. 54,005)
`Latham & Watkins LLP
`885 Third Avenue
`New York, NY 10022-4834
`212-906-1200; 212-751-4864 (Fax)
`
`Counsel for Petitioner
`Par Pharmaceutical, Inc.
`
`/Matthew L. Fedowitz/
`By:
`Matthew L. Fedowitz
`(Reg. No. 61,386)
`Merchant & Gould P.C.
`1900 Duke Street, Ste. 600
`Alexandria, VA 22314
`703-684-2500; 703-684-2501 (Fax)
`
`Counsel for Petitioner
`Breckenridge Pharmaceutical, Inc.
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`/Keith A. Zullow/
`By:
`Keith A. Zullow (Reg. No. 37,975)
`Goodwin Procter LLP
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`Dated: January 3, 2017
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`Case IPR2016-00084
`U.S. Patent No. 5,665,772
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`The New York Times Building
`620 Eighth Avenue
`New York, NY 10018-1405
`212-813-8846; 646-558-4226 (Fax)
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`Counsel for Petitioner
`Roxane Laboratories, Inc.
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`13
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`Case IPR2016-00084
`U.S. Patent No. 5,665,772
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`CERTIFICATE OF SERVICE
`
`Pursuant to 37 C.F.R. § 42.6(e), I certify that on this 3rd day of January,
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`2017, a true and correct copy of the foregoing PETITIONERS’ UPDATED
`
`EXHIBIT LIST was served by electronic mail on Patent Owner’s lead and backup
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`counsel at the following email address:
`
`Nicholas N. Kallas (Reg. No. 31,530)
`Raymond R. Mandra (Reg. No. 34,382)
`Peter J. Waibel (Reg. No. 43,228)
`Christina Schwarz (pro hac vice)
`Charlotte Jacobsen (pro hac vice)
`Susanne L. Flanders (pro hac vice)
`Jared L. Stringham (pro hac vice)
`Fitzpatrick, Cella, Harper & Scinto
`1290 Avenue of the Americas
`New York, NY 10104-3800
`ZortressAfinitorIPR@fchs.com
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`By: /Daniel G. Brown/
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`Daniel G. Brown (Reg. No. 54,005)
`Latham & Watkins LLP
`885 Third Avenue
`New York, NY 10022-4834
`212-906-1200; 212-751-4864 (Fax)
`
`Counsel for Petitioner
`Par Pharmaceutical, Inc.
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