`_______________________________
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`_______________________________
`SAWAI USA, INC. AND
`SAWAI PHARMACEUTICAL CO., LTD.
`Petitioners,
`
`v.
`
`BIOGEN MA, INC.
`Patent Owner.
`_______________________________
`Patent No. 8,399,514
`_______________________________
`Inter Partes Review IPR2019-00789
`_______________________________
`
`PETITIONERS’ EXHIBIT LIST AS OF MAY 6, 2019
`
`US_139279447v1_385667-00004
`
`
`
`EXHIBIT
`NO.
`
`DESCRIPTION
`
`1001
`
`1002
`
`1003
`
`1004
`
`1005
`
`1006
`
`1007
`
`1008
`
`1009
`
`1010
`
`1011
`
`U.S. Patent No. 8,399,514, Treatment for Multiple
`Sclerosis (filed Feb. 13, 2012) (issued Mar. 19, 2013)
`
`Declaration of John R. Corboy, M.D.
`
`Declaration of Leslie Benet, Ph.D.
`
`Declaration of Ian McKeague, Ph.D.
`
`Biogen News Release, Phase II Study of Oral Compound
`BG-12 Meets Primary Endpoint in Multiple Sclerosis (Jan. 9,
`2006)
`
`S. Schimrigk et al., A Prospective, Open-Label, Phase II
`Study of Oral Fumarate Therapy for the Treatment of
`Relapsing-Remitting Multiple Sclerosis, 10 (Suppl. 2)
`MULTIPLE SCLEROSIS CLIN. & LAB. RES. S258, Abstract
`P642 (2004)
`
`L. Kappos et al., Efficacy of a Novel Oral Single-Agent
`Fumarate, BG00012, in Patients with Relapsing-Remitting
`Multiple Sclerosis: Results of a Phase 2 Study, 253 (Suppl.
`2) J. NEUROL. II27, O108 (2006)
`
`International Publication No. WO 2006/0037342 A2
`(published Apr. 13, 2006)
`
`U.S. Patent No. 7,320,999, Dimethyl Fumarate for the
`Treatment of Multiple Sclerosis (filed July 17, 2002)
`(issued Jan. 22, 2008)
`
`NCT00168701, CLINICALTRIALS.GOV,
`https://clinicaltrials.gov/ archive/NCT00168701/2005_09_14
`
`ICH HARMOISED TRIPARITE GUIDELINE – DOSE-RESPONSE
`INFORMATION TO SUPPORT DRUG REGISTRATION E4 (Mar. 10,
`1994)
`
`US_139279447v1_385667-00004
`
`
`
`EXHIBIT
`NO.
`
`DESCRIPTION
`
`1012
`
`1013
`
`1014
`
`1015
`
`1016
`
`1017
`
`1018
`
`S. Schimrigk et al., A Prospective, Open-Label, Phase II
`Study of Oral Fumarate Therapy for the Treatment of
`Relapsing-Remitting Multiple Sclerosis (2004), available at
`http://web.archive.org/web/
`20041021033354/http://www.fumapharm.ch:80/pdf/BG-12_
`Schimrigk_Poster_Final.pdf (“Schimrigk 2004 Poster”)
`
`N. Brune et al., Oral Fumarate Therapy Alters Cytokine
`Production in Patients with Relapsing-Remitting Multiple
`Sclerosis, 10 (suppl. 2) MULTIPLE SCLEROSIS CLIN & LAB.
`RES. S259, ABSTRACT P643 (2004)
`
`S. Schimrigk et al., An Open-Label, Prospective Study of
`Oral Fumaric Acid Therapy for the Treatment Relapsing-
`Remitting Multiple Sclerosis (RRMS), 64(6)(Suppl. 1)
`NEUROLOGY A392, S46.003 (2005)
`
`L. Kappos et al., A Randomised, Placebo-controlled Phase II
`Trial of a Novel Oral Single-Agent Fumarate Therapy,
`BG00012, in Patients with Relapsing-Remitting Multiple
`Sclerosis, 252 (Suppl. 2) J. NEUROL. II/148, P574 (2005)
`
`Biogen News Release, Oral Compound BG-12 Achieves
`Primary Endpoint in Phase II Study of Relapsing-Remitting
`Multiple Sclerosis; Treatment with BG-12 Led to Statistically
`Significant Reductions in MRI Measures (May 30, 2006)
`
`C. Nieboer et al., Fumaric Acid Therapy in Psoriasis: A
`Double-Blind Comparison between Fumaric Acid Compound
`Therapy and Monotherapy with Dimethylfumaric Acid Ester,
`181 DERMATOLOGICA 33 (1990)
`
`S. Schimrigk et al., Oral Fumaric Acid Esters for the
`Treatment of Active Multiple Sclerosis: An Open-Label,
`Baseline-Controlled Pilot Study, 13 EUR. J. NEUOL. 604
`(2006)
`
`US_139279447v1_385667-00004
`
`
`
`EXHIBIT
`NO.
`
`1019
`
`DESCRIPTION
`
`U. Mrowietz et al., Dimethylfumarate for Psoriasis: More
`than a Dietary Curiosity, 11(1) TRENDS MOL. MED. 43
`(2005)
`
`1020
`
`Fumaderm® prescribing information
`
`1021
`
`1022
`
`1023
`
`1024
`
`1025
`
`1026
`
`1027
`
`1028
`
`1029
`
`H.M. Ockenfels et al., The Antipsoriatic Agent
`Dimethylfumarate Immunomodulates T-Cell Cytokine
`Secretion and Inhibits Cytokines of the Psoriatic Cytokine
`Network, 139 BR. J. DERM. 390 (1998)
`INTENTIONALLY LEFT BLANK
`R. de Jong et al., Selective Stimulation of T Helper 2
`Cytokine Responses by the Anti-Psoriasis Agent
`Monomethylfumarate, 26 EUR. J. IMMUNOL. 2067 (1996)
`
`P. Nibbering et al., Effects of Monomethylfumarate on
`Human Granulocytes, 101 J. INVEST. DERMATOL. 37 (1993)
`
`U.S. Patent No. 6,509,376, Utilization of Dialkyfumarates
`(filed Oct. 29, 1999) (issued Jan 21, 2003)
`
`Biogen News Release, BG-12 Psoriasis Study Meets Primary
`Endpoint; Oral Compound Also Being Studied for MS in
`Phase II Trial (Apr. 7, 2005)
`
`A.D. Ormerod et al., Fumaric Acid Esters, Their Place in the
`Treatment of Psoriasis, 150 Br. J. Dermatol. 630 (2004)
`
`U. Mrowietz et al., Treatment of Psoriasis with Fumaric Acid
`Esters: Results of a Prospective Multicentre Study,
`138(3) BR. J. DERMATOL. 456 (1998)
`
`W. Nugteren-Huying et al., Fumaric Acid Therapy for
`Psoriasis: A Randomized, Double-Blind, Placebo-
`Controlled Study,” 22(2) J. AM. ACAD. DERMATOL. 311
`(1990)
`
`US_139279447v1_385667-00004
`
`
`
`EXHIBIT
`NO.
`
`DESCRIPTION
`
`1030
`
`1031
`
`1032
`
`1033
`
`1034
`
`1035
`
`1036
`
`P. Altmeyer et al., Antipsoriatic Effect of Fumaric Acid
`Derivatives: Results of a Multicenter Double-Blind Study in
`100 Patients, 30 J. AM. ACAD. DERMATOL. 977 (1994)
`
`C. Nieboer et al., Systemic Therapy with Fumaric Acid
`Derivatives: New Possibilities in the Treatment of Psoriasis,
`20 J. AM. ACAD. DERM. 601 (1989)
`
`N. Brune et al., Detection of Altered Intracellular TH1- and
`TH2-Type Cytokine Production of Peripheral Blood
`Mononuclear cells (PBMCs) in Patients with Relapsing-
`Remitting Multiple Sclerosis (RRMS) Undergoing an Oral
`Fumaric-Acid Ester Therapy, 4(4) MULTIPLE SCLEROSIS:
`CLINICAL AND LABORATORY RESEARCH P3038 (1998)
`(ECTRIMS 98:14th Congress of the European Committee for
`Treatment and Research in Multiple Sclerosis, Sept. 9-12,
`1998, Stockholm, Sweden)
`
`S. Schimrigk et al., Oral Fumaric Acid Ester (FAE) in
`Relapsing-Remitting Multiple Sclerosis (RRMS). A Short
`Term, Open, clinical, Immunological and Magnetic
`Resonance Imaging (MRI) Controlled Phase II Trial, 246
`(Suppl. 1) J. NEUROL. I/36, 144 (1999) (Ninth Meeting of the
`European Neurological Society, June 5-9, 1999, Milan, Italy)
`
`L. Kappos et al., A Randomized, Placebo-Controlled Phase 2
`Trial of a Novel Oral Fumarate, BG00012, in Patients with
`Relapsing-Remitting Multiple Sclerosis (15th Meeting of the
`European Neurological Society, June 18-22, 2005), and
`Declaration of Gilmore O’Neill, M.D.
`
`A. Wierinckx et al., Detoxication Enzyme Inducers Modify
`Cytokine Production in Rat Mixed Glial Cells, 166 J.
`NEUROIMMUNOL. 132 (2005)
`
`R. Fox et al., Dimethyl Fumarate to Treat Multiple Sclerosis,
`in MULTIPLE SCLEROSIS THERAPEUTICS 387 (Jeffrey A.
`Cohen et al. eds., 4th ed. 2011)
`
`US_139279447v1_385667-00004
`
`
`
`EXHIBIT
`NO.
`1037
`
`1038
`
`1039
`
`1040
`
`1041
`
`1042
`
`1043
`
`1044
`
`1045
`
`DESCRIPTION
`
`European Medicines Agency, Assessment Report, Tecfidera
`(Nov. 26, 2013)
`
`R. Gold et al., Placebo-Controlled Phase 3 Study of Oral
`BG-12 for Relapsing Multiple Sclerosis, 367 NEW ENG. J.
`MED. 1098 (2012) (“Define Study”)
`
`R. Fox et al., Placebo-Controlled Phase 3 Study of Oral BG-
`12 or Glatiramer in Multiple Sclerosis, 367 NEW ENG. J.
`MED. 1087 (2012) (“Confirm Study”)
`
`E. Frohman et al., Multiple Sclerosis - The Plaque and its
`Pathogenesis, 354 NEW ENG. J. MED. 942 (2006)
`
`J. Miller, The Importance of Early Diagnosis of Multiple
`Sclerosis, 10(3) J. MANAG. CARE PHARM. S4 (2004)
`
`MS Prevalence, NATIONALMSSOCIETY.ORG,
`https://www.nationalmssociety.org/About-the-Society/MS-
`Prevalence (last visited July 9, 2018)
`
`S. Rich et al., Stepped-Care Approach to Treating MS: A
`Managed Care Treatment Algorithm, 10(3) J. MANAG. CARE
`PHARM. S26 (2004)
`
`D. Meier et al., Monitoring Treatment Efficacy with
`Magnetic Resonance Imaging (MRI) in an Open Phase II
`Study with Fumaric-Acid Esters (Fumaderm®) in Patients
`with relapsing-Remitting MS (RRMS), 4(4) MULTIPLE
`SCLEROSIS: CLINICAL AND LABORATORY RESEARCH P3037
`(1998) (ECTRIMS 98:14th Congress of the European
`Committee for Treatment and Research in Multiple Sclerosis,
`Sept. 9-12, 1998, Stockholm, Sweden)
`
`N. Brune et al., Oral Fumaric-Acid Ester Therapy (FAE)
`Influence T-Helper Cell Apoptosis in Peripheral Blood
`Lymphocytes (PBLS) and Soluble Intercellular Adhesion
`Molecule-I (SICAM-1) in Serum of Patients with Relapsing-
`Remitting Multiple Sclerosis (RRMS), 246 (Suppl. 1) J.
`
`US_139279447v1_385667-00004
`
`
`
`EXHIBIT
`NO.
`
`1046
`
`1047
`
`1048
`
`1049
`
`1050
`
`1051
`
`1052
`
`1053
`
`1054
`
`1055
`
`DESCRIPTION
`NEUROL. I/61, P272 (1999) (Ninth Meeting of the European
`Neurological Society, June 5-9, 1999, Milan, Italy)
`
`L. Kappos et al., Efficacy of a Novel Oral Single-Agent
`Fumarate, BG00012, in Patients with Relapsing-Remitting
`Multiple Sclerosis: Results of a Phase II Study (16th
`Meeting of the European Neurological Society, May 30,
`2006) attached as Exhibit C to the Declaration of Katherine
`T. Dawson in Biogen U.S. Patent App. No. 12/526,296 and
`marked as Ex. 1018 in Biogen MA Inc. v. Forward Pharma
`A/S, Interference No. 106,023 (“Kappos 2006 Presentation”)
`
`Leon Shargel et al., APPLIED BIOPHARMACEUTICS &
`PHARMAKINETICS 575-611 (5th ed. 2005)
`
`L. Kappos et al., Efficacy and Safety of Oral Fumarate in
`Patients with Relapsing-Remitting Multiple Sclerosis: A
`Multicentre, Randomised, Double-Blind, Placebo-Controlled
`Phase IIb Study, 372 LANCET 1463 (2008)
`
`FDA GUIDANCE FOR INDUSTRY - NON-INFERIORITY CLINICAL
`TRIALS TO ESTABLISH EFFECTIVENESS (Nov. 2016)
`
`E. de Klerk et al., Patient Compliance in Rheumatoid
`Arthritis, Polymyalgia Rheumatica, and Gout, 30 J.
`RHEUMATOLOGY 44 (2003)
`
`A. Paes et al., Impact of Dosage Frequency on Patient
`Compliance, 20(10) DIABETES CARE 1512 (1997)
`
`S. Eisen et al., The Effect of Prescribed Daily Dose
`Frequency on Patient Medication Compliance, 150 ARCH.
`INTERN. MED. 1881 (1990)
`
`Prosecution History Excerpts, U.S. Patent No. 8,399,514
`
`Declaration of Robert Mihail
`
`Declaration of Jennifer Rock
`
`US_139279447v1_385667-00004
`
`
`
`EXHIBIT
`NO.
`1056
`
`1057
`
`1058
`
`1059
`
`1060
`
`1061
`
`1062
`
`1063
`
`1064
`
`DESCRIPTION
`
`Declaration of Robert Walter Baumhefner, M.D.
`
`Declaration of Jacquelyn Bainbridge, Pharm.D.
`
`Declaration of Ronald G. Marks, Ph.D.
`
`Declaration of Jennifer Rock
`
`Declaration of Tatsufumi Hiramatsu
`
`2019.04.08 – E-mail to Mylan
`
`2019.04.24 – E-mail from PTAB
`
`2019.04.25 – E-mail to Biogen and Mylan
`
`2019.05.01 – E-mail to Biogen
`
`US_139279447v1_385667-00004
`
`