`
`
`
`
`Paper No. ___
`Filed: April 6, 2018
`
`UNITED STATES PATENT AND TRADEMARK OFFICE
`_____________________________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`_____________________________
`
`APOTEX INC., APOTEX CORP., ARGENTUM PHARMACEUTICALS
`LLC, ACTAVIS ELIZABETH LLC, TEVA PHARMACEUTICALS USA,
`INC., SUN PHARMACEUTICAL INDUSTIRES, LTD., SUN
`PHARMACEUTICAL INDUSTRIES, INC., AND SUN PHARMA GLOBAL
`FZE,
`Petitioners,
`
`v.
`
`NOVARTIS A.G.,
`Patent Owner.
`_____________________________
`
`IPR2017-008541
`Patent No. 9,187,405
`_____________________________
`
`PETITIONERS’ UPDATED EXHIBIT LIST
`
`
`1 Cases IPR2017-01550, IPR2017-01946, and IPR2017-01929 have been joined
`
`with this proceeding.
`
`
`
`LIST OF EXHIBITS
`
`Exhibit No.
`
`Description
`
`1001
`
`1002
`
`1003
`
`1004
`
`1005
`
`1006
`
`1007
`
`1008
`
`1009
`
`1010
`
`1011
`
`1012
`
`1013
`
`U.S. Patent No. 9,187,405, “S1P Receptor Modulators for Treating
`Relapsing-Remitting Multiple Sclerosis” (filed April 21, 2014)
`(issued November 17, 2015)
`
`Declaration of Dr. Barbara S. Giesser
`
`Curriculum Vitae of Dr. Barbara S. Giesser
`
`John Kovarik and Silke Appel-Dingemanse: International
`Publication No. WO 2006/058316 (published June 1, 2006)
`
`Thomson, FTY720 in Multiple Sclerosis: The Emerging Evidence of
`its Therapeutic Value, CORE EVIDENCE, 1(3):157-167 (2006)
`
`U. S. Patent No. 6,004,565 (Chiba) “Compositions and Methods of
`Using Compositions with Accelerated Lymphocyte Homing
`Immunosuppressive Properties” (filed September 23, 1997) (issued
`December 21, 1999)
`
`Kappos, L., et al., FTY720 in Relapsing MS: Results of a Double-
`Blind Placebo-Controlled Trial with a Novel Oral
`Immunomodulator, JOURNAL OF NEUROLOGY 252(Suppl 2):11/41,
`Abstract O141 (2005)
`
`Budde, et al., First Human Trial of FTY720, a Novel
`Immunomodulatory, in Stable Renal Transplant Patients, JOURNAL
`OF THE AMERICAN SOCIETY OF NEPHROLOGY, 13:1073-1083 (2002)
`
`File History U.S. Patent Application No. 12/303,765
`
`File History U.S. Patent Application No. 13/149,468
`
`File History U.S. Patent Application No. 14/257,342
`
`GB 0612721.1
`
`U.S. Pat. No. 8,741,963 “S1P Receptor Modulators for Treating
`Multiple Sclerosis” (filed May 31, 2011) (issued June 3, 2014)
`
`-1-
`
`
`
`1014
`
`1015
`
`1016
`
`1017
`
`1018
`
`1019
`
`1020
`
`1021
`
`1022
`
`1023
`
`1024
`
`File History of U.S. Patent Application No. 11/720,205
`
`Provisional Patent Application No. 60/631,483 (filed November 29,
`2004)
`
`Virley, Developing Therapeutics for the Treatment of Multiple
`Sclerosis, NEURORX, 2:638-649 (2005)
`
`Adachi, et al., Design, Synthesis, and Structure-Activity
`Relationships of 2-Substituted-2-amino-1,3-propanediols: Discovery
`of a Novel Immunosuppressant, FTY720, BIOORGANIC AND
`MEDICINAL CHEMISTRY LETTERS, 5(8):853-856 (1995)
`
`Dumont, Fingolimod Mitsubishi Pharma/Novartis, IDRUGS,
`8(3):236-253 (2005)
`
`Park, et al., Pharmacokinetic/Pharmacodynamic Relationships of
`FTY720 in Kidney Transplant Patients, BRAZILIAN JOURNAL OF
`MEDICAL AND BIOLOGICAL RESEARCH, 38: 683-694 (2005)
`
`Yanagawa, et al., FTY720, a Novel Immunosuppressant, Induces
`Sequestration of Circulating Mature Lymphocytes by Acceleration
`of Lymphocyte Homing in Rats, III. Increase in Frequency of
`CD62L-Positive T Cells in Peyer’s Patches by FTY720-Induced
`Lymphocyte Homing, IMMUNOLOGY, 95: 591-594 (1998)
`
`“Clinical Pharmacology in the Critically Ill Child,” in CRITICAL
`CARE PEDIATRICS, Zimmerman and Gildea eds. (Saunders Company
`1985)
`
`Chiba, FTY720, a New Class of Immunomodulatory, Inhibits
`Lymphocyte Egress from Secondary Lymphoid Tissues and Thymus
`by Agonistic Activity at Sphingosine 1-Phosphate Receptors,
`PHARMACOLOGY & THERAPEUTICS, 108:308-319 (2005)
`
`MCALPINE’S MULTIPLE SCLEROSIS, 4th Edition, Compston, ed
`(Elsevier, Inc., December 2005)
`
`Frohman, et al., Multiple Sclerosis – The Plaque and its
`Pathogenesis, NEW ENGLAND JOURNAL OF MEDICINE, 354: 942-955
`(2006)
`
`-2-
`
`
`
`1025
`
`1026
`
`1027
`
`1028
`
`1029
`
`1030
`
`1031
`
`1032
`
`1033
`
`1034
`
`1035
`
`Inglese, Multiple Sclerosis: New Insights and Trends, AMERICAN
`JOURNAL OF NEURORADIOLOGY, 27: 954-957 (2006)
`
`Dragun, D., et al., FTY720: Early Clinical Experience,
`TRANSPLANT. PROC., 36 (Suppl 2S), 554S-548S (2004)
`
`Kahan, B.D., FTY720: A New Dimension in Transplantation,
`TRANSPLANT. PROC., 33, 3081-3083 (2001)
`
`Fujino, et al., Amelioration of Experimental Autoimmune
`Encephalomyelitis in Lewis Rats by FTY720 Treatment, JOURNAL OF
`PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 305(1):70-77
`(2003)
`
`Kataoka, et al., FTY720, Sphingosine 1-Phosphate Receptor
`Modulator, Ameliorates Experimental Autoimmune
`Encephalomyelitis by Inhibition of T Cell Infiltration, CELLULAR
`AND MOLECULAR IMMUNOLOGY, 2(6):439-448 (2005)
`
`Kahan, B.D., Sirolimus and FTY720: New Approaches to
`Transplant Immunosuppression, TRANSPLANT. PROC., 34, 2520-
`2522 (2002)
`
`Kahan, et al., Pharmacodynamics, Pharmacokinetics, and Safety of
`Multiple Doses of FTY720 in Stable Renal Transplant Patients: A
`Multicenter, Randomized, Placebo-Controlled, Phase I Study,
`TRANSPLANTATION, 76(7): 1079-1084 (2003)
`
`Final Written Decision, Paper 112, IPR2014-00784
`
`PHYSICIAN’S DESK REFERENCE, 59th Edition (Thomson PDR,
`January 1, 2005)
`
`“Introduction to Pharmacokinetics” in BIOPHARMACEUTICS AND
`CLINICAL PHARMACOKINETICS, Gibaldi (Lea & Febiger, 1991)
`
`Orange Book entry for Fingolimod
`(http://www.accessdata.fda.gov/scripts/cder/ob/patent_info.cfm?Pro
`duct_No=001&Appl_No=022527&Appl_type=N) (last accessed
`February 2, 2017)
`
`-3-
`
`
`
`1036
`
`1037
`
`1038
`
`1039
`
`1040
`
`FDA approval letter for Tysabri, obtained from the Food and Drug
`Administration website
`http://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=ov
`erview.process&ApplNo=125104 (last accessed January 30, 2017)
`
`U. S. Pat. No. 8,324,283 (Oomura) Solid Pharmaceutical
`Compositions Comprising a SIP Receptor Agonist and a Sugar
`Alcohol (filed August 11, 2008) (issued December 4, 2012)
`
`Kappos, L., et al., A Placebo-Controlled Trial of Oral Fingolimod
`in Relapsing Multiple Sclerosis, NEW ENGLAND JOURNAL OF
`MEDICINE, 362(5):387-401 (2010)
`
`LaMontagne, et al., “Antagonism of Sphingosine-1-Phosphate
`Receptors by FTY720 Inhibits Angiogenesis,” Cancer Res., 66:221-
`231 (Jan. 2006)
`
`Thomson, FTY720 in Multiple Sclerosis: The Emerging Evidence of
`its Therapeutic Value, CORE EVIDENCE, 1(3):157-167 (2006)
`
`1041
`(served but
`not filed)
`
`“Clinical Pharmacology in the Critically Ill Child,” in CRITICAL
`CARE PEDIATRICS, Zimmerman and Gildea eds. (Saunders Company
`1985)
`
`1042
`
`1042
`
`1043
`
`1043
`
`1044
`
`1045
`
`PROTECTIVE ORDER MATERIAL: Transcript of December 15,
`2017 Deposition of Fred D. Lublin, M.D.
`
`REDACTED: Transcript of December 15, 2017 Deposition of Fred
`D. Lublin, M.D.
`
`PROTECTIVE ORDER MATERIAL: Transcript of January 10,
`2018 Conference Call with the Patent Trial and Appeal Board
`
`REDACTED: Transcript of January 10, 2018 Conference Call with
`the Patent Trial and Appeal Board
`
`PROTECTIVE ORDER MATERIAL: December 5, 2017 Email
`regarding document production
`
`PROTECTIVE ORDER MATERIAL: January 4, 2018 Email
`regarding discovery
`
`-4-
`
`
`
`1046
`
`1047
`
`1047
`
`1048
`
`1049
`
`1050
`
`1051
`
`Transcript of January 29, 2018 Deposition of Fred D. Lublin, M.D.
`
`PROTECTIVE ORDER MATERIAL: Reply Declaration of Leslie
`Z. Benet, Ph.D.
`
`REDACTED: Reply Declaration of Leslie Z. Benet, Ph.D.
`
`Curriculum Vitae of Leslie Z. Benet, Ph.D.
`
`FDA Guidance for Industry: Estimating the Maximum Safe Starting
`Dose in Initial Clinical Trials For Therapeutics in Adult Healthy
`Volunteers (July 2005)
`
`PROTECTIVE ORDER MATERIAL: Transcript of December 13,
`2017 Deposition of Christian Schnell
`
`PROTECTIVE ORDER MATERIAL: Novartis Clinical
`Development, Fingolimod (FTY720), Protocol No. CFTY720D2302
`(April 2006)
`
`1052
`
`Transcript of March 29, 2018 Conference Call with the Patent Trial
`and Appeal Board
`
`
`
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`-5-
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`
`
`CERTIFICATE OF SERVICE
`
`
`
`This is to certify that I caused to be served true and correct copies of the
`
`foregoing Updated Exhibit List and Exhibit 1052, on this 6th day of April, 2018,
`
`on the Patent Owner at the correspondence address of the Patent Owner as follows:
`
`Jane M. Love, Ph.D.
`Robert W. Trenchard
`GIBSON, DUNN & CRUTCHER LLP
`200 Park Avenue, 47th Floor
`New York, NY 10166
`Email: jlove@gibsondunn.com
`Email: rtrenchard@gibsondunn.com
`
`
`
`
`Dated: April 6, 2018
`
`
`
`
`
`
`
`
`/ Steven W. Parmelee /
` Steven W. Parmelee
` Reg. No. 31,990
`
`
`
`
`-6-
`
`
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