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`
`UNITED STATES PATENT AND TRADEMARK OFFICE
`
`___________________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`___________________
`
`Alkermes Pharma Ireland Ltd.
`and Alkermes, Inc.
`Petitioners,
`
`v.
`
`Otsuka Pharmaceutical Co., Ltd.
`Patent Owner
`
`Patent No. 9,125,939 B2
`Issued: September 8, 2015
`Filed: August 2, 2006
`Inventors: Tetsuro Kikuchi, Taro Iwamoto, Tsuyoshi Hirose
`
`Title: CARBOSTYRIL DERIVATIVES AND MOOD STABILIZERS FOR
`TREATING MOOD DISORDERS
`
`___________________
`
`Inter Partes Review No. IPR2017-00287
`
`
`
`PETITIONERS’ UPDATED EXHIBIT LIST
`
`
`
`
`
`
`Mail Stop PATENT BOARD
`Patent Trial and Appeal Board
`United States Patent and Trademark Office
`P.O. Box 1450
`Alexandria, VA 22313-1450
`
`
`
`
`
`

`

`
`
`Alkermes
`Ex. No.
`Ex. 1001
`Ex. 1002
`
`Ex. 1003
`Ex. 1004
`
`Ex. 1005
`Ex. 1006
`
`Ex. 1007
`
`Ex. 1008
`
`Ex. 1009
`
`Ex. 1010
`
`Ex. 1011
`
`Ex. 1012
`
`Description
`
`U.S. Patent 9,125,939
`Declaration of Allen Frances, M.D. in Support of the Petition for
`Inter Partes Review of U.S. Patent No. 9,125,939
`Allen Frances, M.D., Curriculum Vitae
`Declaration of Jessie Au in Support of the Petition for Inter Partes
`Review of U.S. Patent No. 9,125,939
`Jessie Au, Curriculum Vitae
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`or lithium in the treatment of mania in patients partially
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`“Tohen”
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`Abstracts of the 2002 Annual Meeting of the American Psychiatric
`Association; Philadelphia, PA. USA (2002) (New Research
`Abstract 314 (NR314)).
`“Keck”
`Citrome et al., Pharmacokinetics and safety of aripiprazole and
`concomitant mood stabilizers, Abstracts of the 2002 Annual
`Meeting of the American Psychiatric Association; Philadelphia,
`PA. USA (2002) (New Research Abstract 317 (NR317)).
`“Citrome”
`American Psychiatric Association, Practice guideline for the
`treatment of patients with bipolar disorder (Revision), Am. J.
`Psychiatry, 159:4, April 2002 Supplement
`“Practice Guidelines 2002”
`Kowatch R.A. et al., The use of mood stabilizers and atypical
`antipsychotics in children and adolescents with bipolar disorders,
`CNS Spectrums, 8(4): 273-280 (2003)
`“Kowatch”
`Vieta, Eduard, et al., Olanzapine as long-term adjunctive therapy in
`treatment-resistant bipolar disorder, J. CLIN. PSYCHOPHARMACOL.,
`v.21(5): 469-473 (2001).
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`nonpsychotic bipolar mixed states [letter], J. CLIN. PSYCHIATRY,
`59:83-85. (1998)
`
`
`
`
`
`

`

`
`
`Ex. 1013
`
`Ex. 1014
`
`Ex. 1015
`
`Ex. 1016
`
`Ex. 1017
`
`Ex. 1018
`
`Ex. 1019
`
`Ex. 1020
`
`Ex. 1021
`
`Ex. 1022
`
`Ex. 1023
`
`
`
`“Ketter”
`McElroy SL, et al., Olanzapine in treatment-resistant bipolar
`disorder, J. AFFECT DISORD. 49:119-122. (1998)
`“McElroy”
`Sachs, G.S. et al., Quetiapine versus placebo as adjunct to mood
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`Yatham, Lakshmi N. et al., The role of novel antipsychotics in
`bipolar disorder, J. CLIN. PSYCHIATRY 63: 10-14 (2002)
`“Yatham”
`Petrie, J.L. et al., Aripiprazole, a new atypical antipsychotic: phase
`II clinical trial results. EUR. NEUROPSYCHOPHARM 7 (Suppl
`2):S227 (1997)
`“Petrie”
`Goodwin, G.M., Typical and atypical antipsychotics in the
`treatment of mania, EUR. NEUROPSYCHOPHARM 11 (Suppl 3): S132
`(2001)
`“Goodwin”
`Chang, Kiki D. and Ketter, Terence A., Mood stabilizer
`augmentation with olanzapine in acutely manic children, J. CHILD
`AND ADOLESCENT PSYCHOPHARMACOLOGY, v:10(1): 45-49 (2000)
`“Chang”
`Del Bello M.P. et al., A double-blind, randomized, placebo-
`controlled study of quetiapine as adjunctive treatment for
`adolescent mania, J. AM. ACAD. CHILD ADOLESC. PSYCHIATRY, 41:
`1216-1223. (2002)
`“Del Bello”
`Tohen M. et al., Efficacy of olanzapine in acute bipolar mania: a
`double-blind, placebo-controlled study, ARCH GEN PSYCHIATRY
`57(9): 841-849 (2000)
`“Tohen II”
`Haddad P. et al., Adjunctive use of olanzapine in the treatment of
`mania, INT. J. PSYCHIATRY IN CLIN PRACTICE, v3: 213-215 (1999)
`“Haddad”
`Excerpts from the Diagnostic and Statistical Manual of Mental
`Disorder-IV (DSM-IV)
`
`Jordan, S. et al., The antipsychotic aripiprazole is a potent, partial
`
`
`
`

`

`
`
`Ex. 1024
`
`Ex. 1025
`
`Ex. 1026
`
`Ex. 1027
`
`Ex. 1028
`
`Ex. 1029
`
`Ex. 1030
`
`Ex. 1031
`
`Ex. 1032
`
`Ex. 1033
`
`
`
`agonist at the human 5-HT1A receptor, EUR. J. PHARMACOL.,
`441(3):137-40 (2002)
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`Miller, D.S., et al., Comparative efficacy of typical and atypical
`antipsychotics as add-on therapy to mood stabilizers in the
`treatment of acute mania, J CLIN PSYCHIATRY, v62:975-980 (2001)
`“Miller”
`Carlson, G.A. et al., The stages of mania. A longitudinal analysis of
`the manic episode, ARCH. GEN. PSYCHIATRY, 28(2): 221-228 (1973)
`“Carlson”
`The Expert Consensus Guideline Series Medication Treatment of
`Bipolar Disorder 2000, A Postgraduate Medicine Special Report,
`April 2000
`“Expert Consensus”
`Griswold et al., Management of Bipolar Disorder, AM. FAM.
`PHYSICIAN 62(6):1343-1353 (2000)
`“American Family Physician”
`Data Demonstrate Aripiprazole Significantly Improved Symptoms
`of Acute Mania in Patients With Bipolar Disorder; New Data
`Presented Today at American Psychiatric Association Annual
`Meeting, PR Newswire, May 22, 2002,
`“BMS/Otsuka Press Release”
`Frye et al., The Increasing Use of Polypharmacotherapy for
`Refractory Mood Disorders: 22 Years of Study, J CLIN PSYCHIATRY
`61(1): 9-15 (2000)
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`Shimokawa, High Performance Liquid Chromatographic Methods
`for the Determination of Aripiprazole with Ultraviolet Detection in
`Rat Plasma and Brain: Application to the Pharmacokinetic Study,
`JOURNAL OF CHROMATOGRAPHY 21, 8-14, 13 (2005).
`(“Shimokawa”)
`Chiu and Franklin, Analysis and Pharmacokinteics of Olanzapine
`(LY170053) and Two Metabolites in Rat Plasma Using Reversed-
`Phase HPLC with Electrochemical Detection, JOURNAL OF
`PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, 14, 609-615
`(1996). (“Chiu and Franklin”)
`Mattiuz et al., Disposition and Metabolism of Olanzapine in Mice,
`
`
`
`

`

`
`
`Ex. 1034
`
`Ex. 1035
`
`Ex. 1036
`
`Ex. 1037
`
`Ex. 1038
`
`Ex. 1039
`
`Ex. 1040
`
`Ex. 1041
`
`Ex. 1042
`
`Ex. 1043
`
`Ex. 1044
`
`Dogs, and Rhesus Monkeys, DRUG METABOLISM AND DISPOSITION,
`25: 573-583 (1997). (“Mattiuz”)
`Aravagiri et al., Pharmacokinetics and Tissue Distribution of
`Olanzapine in Rats, BIOPHARMACEUTICS & DRUG DISPOSITION, 20:
`369–377 (1999). (“Aravagiri”)
`Gunaratna et al., An automated blood sampler for simultaneous
`sampling of systemic blood and brain microdialysates for drug
`absorption, distribution, metabolism, and elimination studies,
`JOURNAL OF PHARMACOLOGICAL AND TOXICOLOGICAL METHODS
`49: 57-64 (2004). (“Gunaratna”)
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`Methamphetamine and Tetrabenazine, PSCYHOPHARMACOLOGIA,
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`Okada, Inhibition by Antimanic Drugs of Hyperactivity Induced by
`Methampehtamine-Chlordiazepoxide Mixture in Mice,
`PHARMACOLOGY BIOCHEMISTRY & BEHAVIOR, 35, 897-901
`(1990). (“Okada”)
`Takigawa, Intracranial Self-Stimulation and Locomotor Traces as
`Indicators for Evaluating and Developing Antipsychotic Drugs,
`JAPANESE JOURNAL OF PSYCHIATRY AND NEUROLOGY, 48, 1,
`127-132 (1994). (“Takigawa”)
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`Hyperlocomotion and Behavioral Sensitization Via Modulation of
`Prefrontal Monoamine Release, NEUROPHARMACOLOGY 62, 1634-
`1639 (2012). (“Ago”)
`Zhao et al., Comparison of Methods for Evaluating Drug-Drug
`Interaction, FRONTIERS IN BIOSCIENCE E2, 241-249 (2010).
`Fraser, The Antagonism Between the Actions of Active Substances,
`THE BRITISH MEDICAL JOURNAL, 457-459 (1872). (“Fraser”)
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`of Agents, JOURNAL OF INFECTIOUS DISEASES,137, 2, 122-130,
`(1978). (“Berenbaum”)
`Chou and Talalay, Quantitative Analysis of Dose-Effect
`Relationships: the Combined Effects of Multiple Drugs or Enzyme
`Inhibitors, in ADVANCES IN ENZYME REGULATION, Vol. 22,
`1983). (“Chou and Talalay”)
`Greco, Application of a New Approach for the Quantitation of
`Drug Synergism to the Combination of cis-
`Diamminedichloroplatium and 1-b-D-Arabinofuranosylcytosine,
`
`
`
`
`
`

`

`
`
`Ex. 1045
`
`Ex. 1046
`
`Ex. 1047
`
`Ex. 1048
`
`Ex. 1049
`
`Ex. 1050
`
`Ex. 1051
`
`Ex. 1052
`
`Ex. 1053
`
`Ex. 1054
`
`Ex. 1055
`
`Ex. 1056
`
`Ex. 1057
`
`CANCER RESEARCH 50, 5318-5327, (1990). (“Greco 1990”)
`Greco, The Search for Synergy: A Critical Review from a
`Response Surface Perspective, PHARMACOLOGICAL REVIEWS, 47,
`2, 331-385 (1995). (“Greco 1995”)
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`of Nonlinear Regression, Curve Shift, Isobologram, and
`Combination Index Analyses, CLINICAL CANCER RESEARCH, 10,
`7994-8004, (2004). (“Zhao 2004”)
`Johnston et al., Synergy Between 3’-Azido-3’-deoxythymidine and
`Paclitaxel in Human Pharynx FaDu Cells, PHARM. RESEARCH
`20(7):957-61 (2003). (“Johnston”)
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`http://www.kaspercpa.com/statisticalreview.htm (last visited on
`October 16, 2016
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`(last visited October 16, 2016)
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`Expression Induced by Methamphetamine in Mice, BRAIN
`RESEARCH, 782, 83-90 (1998). (“Namima”)
`Da-Rosa, Effects of Lithium and Valproate on Oxidative Stress and
`Behavioral Changes Induced by Administration of m-AMPH,
`PSYCHIATRY RESEARCH, 198, 521-526 (2012). (“Da-Rosa”)
`Feier, Lithium and Valproate Modulate Energy Metabolism in an
`Animal Model of Mania Induced by Methamphetamine,
`PHARMACOLOGY, BIOCHEMISTRY AND BEHAVIOR, 103, 589-596
`(2013). (“Feier”)
`Lim et al., Medication Prescribing Patterns for Patients with
`Bipolar I Disorder in Hospital Settings: Adherence to Published
`Practice Guidelines, Bipolar Disorders 2001: 3 (2001) 165-173
`Leucht, S. et al, Second-Generation Antipsychotic Agents in the
`Treatment of Acute Mania: A Systematic Review and Meta-
`analysis of Randomized Controlled Trials, Arch Gen Psychiatry
`64:4 (2007), 442-455 at 450.
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`“Pharmacological Therapy,” pp. 620-638 at 632.
`Kaplan et al, Comprehensive Textbook of Psychiatry, 3rd Ed.
`(1980)
`
`
`
`
`
`

`

`
`
`Ex. 1058
`
`Ex. 1059
`
`Ex. 1060
`
`Ex. 1061
`
`Ex. 1062
`
`Ex. 1063
`
`Ex. 1064
`
`Ex. 1065
`Ex. 1066
`
`Ex. 1067
`
`Ex. 1068
`
`Ex. 1069
`
`Ex. 1070
`
`Ex. 1071
`
`Ex. 1072
`
`Ex. 1073
`
`Ex. 1074
`
`Kaplan et al, Comprehensive Textbook of Psychiatry, 4th Ed.
`(1985).
`Kaplan et al, Comprehensive Textbook of Psychiatry, 5th Ed.
`(1989).
`Kaplan et al, Comprehensive Textbook of Psychiatry, 6th Ed.
`(1995).
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`Ed. (2000).
`Talbott et al, The American Psychiatric Press Textbook of
`Psychiatry, 1st Ed. (1988).
`Hales et al, American Psychiatric Press Textbook of Psychiatry,
`2nd Ed. (1994).
`Hales et al, The American Psychiatric Press Textbook of
`Psychiatry, 3rd Ed. (1999).
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`and Feasibility Testing of a Treatment Algorithm for Patients with
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`Medication Treatment of Bipolar Disorder 2000, J Clin Psychiatry
`63:4 (Apr. 2002).
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`Management of Bipolar Disorder, J Clin Psychiatry 2000;61 (suppl
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`Bauer et al., Clinical Practice Guidelines for Bipolar Disorder from
`the Department of Veteran Affairs, J Clin Psychiatry 60:1 (Jan.
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`W. Konig et al., Long-term Therapy of Affective Disorders:
`Monotherapy or Polypharmacy?, Pharmacopsychiat. 21 (1988).
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`10 (1990).
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`(1977), Chap. 32, “Pharmacological Therapy,”
`Lawrence C. Kolb, M.D., Modern Clinical Psychiatry, 10th Ed.
`(1982), Chap. 32, “Pharmacological Therapy,”
`
`
`
`
`
`

`

`Sachs, G.S. et al., Combination of a Mood Stabilizer with
`Risperidone or Haloperidol for Treatment of Acute Mania: A
`Double-Blind, Placebo-Controlled Comparison of Efficacy and
`Safety, AM. J. PSYCHIATRY 159:7 (July 2002)
`“Sachs III”
`File History 9,125,939
`Declaration of Nicholas K. Mitrokostas in Support of Petitioners’
`Motion for Pro Hac Vice Admission Under 37 C.F.R. § 42.10(c)
`
`
`
`
`
`
`
`Ex. 1075
`
`Ex. 1076
`Ex. 1077
`
`
`
`
`
`

`

`
`
`CERTIFICATION OF SERVICE
`The undersigned hereby certifies that “PETITIONERS’ UPDATED
`
`EXHIBIT LIST” was served electronically via e-mail on January 31, 2017 on the
`
`/Sarah Fink/
`Sarah Fink (Reg. No. 64,886)
`
`following:
`
`Erin M. Sommers
`James B. Monroe
`Finnegan, Henderson, Farabow,
`Garrett & Dunner, LLP
`901 New York Ave, NW
`Washington, DC 20001
`Tel: 202-408-4292
`Fax: 202-408-4400
`erin.sommers@finnegan.com
`james.monroe@finnegan.com
`
`Counsel for Patent Owner
`Otsuka Pharmaceutical Co. Ltd.
`
`
`
`Dated: January 31, 2017
`
`
`
`
`
`
`
`
`

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