UNITED STATES PATENT AND TRADEMARK OFFICE
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`
`
`
`
`
`COALITION FOR AFFORDABLE DRUGS VIII, LLC
`Petitioner,
`
`v.
`
`THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
`Patent Owner
`
`
`
`Case: IPR2015-01836
`Patent No. 7,932,268
`
`
`
`UPDATED LIST OF PATENT OWNER’S EXHIBITS
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`
`
`
`
`
`COALITION FOR AFFORDABLE DRUGS VIII, LLC
`Petitioner,
`
`v.
`
`THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
`Patent Owner
`
`
`
`Case: IPR2015-01836
`Patent No. 7,932,268
`
`
`
`UPDATED LIST OF PATENT OWNER’S EXHIBITS
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`PATENT OWNER’S LIST OF EXHIBITS
`
`University of Pennsylvania Patent License Agreement (May 19,
`2006)
`NDA #203858, Sponsor’s Background Package For the
`Endocrinologic and Metabolic Drugs Advisory Committee
`Meeting, Advisory Committee Briefing Materials (Oct. 17, 2012)
`ClinicalTrials.gov: Safety, Tolerability, and Efficacy of
`Microsomal Triglyceride Protein (MTP) Inhibitor, available at
`https://clinicaltrials.gov/ct2/show/NCT01556906?term=NCT015
`56906&rank=1
`Marina Cuchel et al., Inhibition of Microsomal Triglyceride
`Transfer Protein in Familial Hypercholesterolemia, 356 (2) N.
`ENG. J. MED. 148-56 (Jan. 11, 2007).
`U.S. Appl. No. 14/075,483, Amendment and Response to Final
`Office Action (Nov. 30, 2015)
`FDA News Release, FDA approves new orphan drug for rare
`cholesterol disorder, available at
`http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncement
`s/ucm333285.htm (Dec. 26, 2012)
`Marina Cuchel et al., Efficacy and safety of a microsomal
`triglyceride transfer protein inhibitor in patients with
`homozygous familial hypercholesterolemia: a single-arm, open-
`label, phase 3 study, 381 THE LANCET 40-46 (Jan. 5, 2013)
`Joseph Walker et al., New Hedge Fund Strategy: Dispute the
`Patent, Short the Stock, THE WALL STREET JOURNAL, available at
`http://www.wsj.com/articles/hedgefundmanagerkylebasschalleng
`esjazzpharmaceuticalspatent1428417408 (Apr. 7, 2015)
`U.S. Appl. No. 13/046,118: Information Disclosure Statement
`(IDS) (Sept. 28, 2011)
`Patentee’s Observations in reply to the Notice of Opposition by
`Dr. Evan Stein, European Patent No. 1 725 234
`
`Ex. 2001
`
`Ex. 2002
`
`Ex. 2003
`
`Ex. 2004
`
`Ex. 2005
`
`Ex. 2006
`
`Ex. 2007
`
`Ex. 2008
`
`Ex. 2009
`
`Ex. 2010
`
`2
`
`
`
`Ex. 2011
`
`Ex. 2012
`
`Ex. 2013
`
`Ex. 2014
`
`Ex. 2015
`
`Ex. 2016
`
`Ex. 2017
`
`Ex. 2018
`
`Ex. 2019
`
`Ex. 2020
`
`Ex. 2021
`
`Ex. 2022
`
`Ex. 2023
`
`The Pink Sheet, MTP inhibitor research discontinued (July 31,
`2000)
`Aegerion Pharmaceuticals, Inc., U.S. Securities and Exchange
`Commission, Form 10-K (March 2, 2015)
`Aegerion Pharmaceuticals, Inc., U.S. Securities and Exchange
`Commission, Form 10-K (March 18, 2013)
`Aegerion Pharmaceuticals, Inc., Third Quarter 2015 Earnings
`Conference Call, available at
`http://files.shareholder.com/downloads/AEGR/0x0x860375/8F9
`C1576-D084-454D-BBCF-
`C656C341E238/AEGR_Q3_15_Slides_Final.pdf (Nov. 9, 2015)
`JUXTAPID label (2012)
`Center For Drug Evaluation And Research, Application Number
`203858Orig1s00, Summary Basis for Regulatory Action (Dec.
`21, 2012)
` Declaration of Nicholas K. Mitrokostas in support of Patent
` Owner’s Motion for Pro Hac Vice Admission of Nicholas K.
` Mitrokostas Under 37 C.F.R. § 42.10(c)
`Michael Mayersohn, Designing a Dosage Regimen: Drug
`Therapy, CLIN. THER., Vol. 10, No. 10 (Oct. 1980).
`Peter Jones et al., Comparative Dose Efficacy Study of
`Atorvastatin Versus Simvastatin, Pravastatin, Lovastatin, and
`Fluvastatin in Patients With Hypercholesterolemia (The
`CURVES Study, AM. J. CARDIOL., Vol. 81 (Mar. 1, 1998).
`Jeffrey A. Robl et al., A Novel Series of Highly Potent
`Benzimidazole-Based Microsomal Triglyceride Transfer Protein
`Inhibitors, J. MED. CHEM., Vol. 44, No. 6 (Mar. 15, 2001).
`Deposition Transcript of Michael Mayersohn, Ph. D. (May 16,
`2016).
`Deposition Transcript of Randall M. Zusman, M.D. (May 19,
`2016).
`Declaration of Dr. Frank Sacks, M.D.
`3
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`Ex. 2024
`
`Ex. 2025
`Ex. 2026
`Ex. 2027
`Ex. 2028
`Ex. 2029
`Ex. 2030
`Ex. 2031
`Ex. 2032
`Ex. 2033
`
`Ex. 2034
`
`Ex. 2035
`
`Ex. 2036
`
`Ex. 2037
`
`Ex. 2038
`
`Declaration of Dr. Thomas A. Baillie, Ph.D., D.SC.
`
`Declaration of S. David Kimball, Ph.D.
`Declaration of Daniel J. Rader, M.D.
`Dr. Frank Sacks, M.D., curriculum vitae
`Dr. Thomas A. Baillie, Ph.D., D.SC., curriculum vitae
`S. David Kimball, Ph.D., curriculum vitae
`Daniel J. Rader, M.D., curriculum vitae
`Dr. Frank Sacks, M.D., Materials Considered
`Dr. Thomas A. Baillie, Ph.D., D.SC., Materials Considered
`David Kimball, Ph.D., Materials Considered
`Malcolm Rowland et al., CLINICAL PHARMACOKINETICS:
`Concepts and Applications, William and Wilkins (1995).
`Sharon A. Huang et al., Phosphodiesterase-5 (PDE5) Inhibitors
`In the Management of Erectile Dysfunction, P T, Vol. 38, No. 7,
`pp. 407-419 (Jul. 2013).
`Heinz Lüllmann et al, Lipidosis Induced by Amphiphillic
`Cationic Drugs, BIOCHEM. PHARMACOL., Vol. 27, pp. 1103-08
`(1978).
`Jan-Peter H. T. M. Ploemen et al, Use of physiochemical
`calculation of pKa and CLogP to predict phospholipidosis-
`inducing potential: A case study with structurally related
`piperazines, EXP. TOXIC PATHOL., Vol. 55, pp. 347-55 (2004).
`Andrea Cavalli et al., Toward a pharmacophore for drugs
`inducing the long QT syndrome: insights from a CoMFA study
`of HERG K(+) channel blockers, J. MED. CHEM., Vol. 45, pp.
`3844-53 (2002).
`
`4
`
`
`
`
`
`
`
`Ex. 2039
`
`Ex. 2040
`
`Ex. 2041
`
`Ex. 2042
`
`Ex. 2043
`
`Ex. 2044
`
`Ex. 2045
`
`Ex. 2046
`
`Ex. 2047
`Ex. 2048
`Ex. 2049
`Ex. 2050
`
`Ex. 2051
`
`John S. Walsh et al., The Metabolic Activation of Abacavir by
`Human Liver Cytosol and Expressed Human Alcohol
`Dehydrogenase Isozymes, CHEM. BIOL. INTERACT., Vol. 142,
`pp. 135-154 (2002).
`Jean F. Le Bigot et al., Metabolism of Ketotifen by Human Liver
`Microsomes, DRUG METAB. DISPOS., Vol. 11, pp. 585-589
`(1983).
`Press Release, Aegerion Pharmaceuticals, FDA Advisory
`Committee Recommends Approval of Lomitapide for
`Treatment of Homozygous Familial Hypercholesterolemia
`(HoFH) (Oct. 17, 2012).
`Pharmaceutical Product Development, Inc., Annual Report
`(Form 10-K) (Dec. 31, 2005).
`Frank M. Sacks et al., Severe Hypertriglyceridemia With
`Pancreatitis: Thirteen Years’ Treatment With Lomitapide, JAMA
`INTERN. MED., Vol. 174, No. 3 (Mar. 2014).
`Internet Archive WayBack, Machine Error Message (June 6,
`2016).
`Internet Archive WayBack Machine, PPD Analyst/Investor
`Day: Dapoxetine
`
`Internet Archive WayBack Machine, PPD Analyst/Investor
`Day: DP4 Inhibitor
`U.S. Patent No. 5,739,135
`U.S. Patent No. 5,883,109
`U.S. Patent No. 6,582,698
`Patent Owner’s Motion to Amend Under 37 C.F.R. § 42.121
`Marjel van Dam et al., Efficacy and Safety of Implitapide (Bay
`13-9952), a Microsomal Triglyceride Transfer Protein
`Inhibitor, in Patients with Primary Hypercholesterlemia, Stein
`Phase I Study (2001).
`
`5
`
`
`
`
`
`
`
`Ex. 2052
`
`Ex. 2053
`
`Ex. 2054
`
`Ex. 2055
`
`Ex. 2056
`
`Ex. 2057
`
`Ex. 2058
`
`Ex. 2059
`
`Ex. 2060
`
`Ex. 2061
`
`Ex. 2062
`
`Ex. 2063
`
`Daru Sharp et al., Cloning and gene defects in microsomal
`triglyceride transfer protein associated with
`abetalipoproteinaemia, NATURE 365, 65 - 69 (Sept. 2, 1993).
`Marc A. Pfeffer et al., Safety and tolerability of pravastatin in
`long-term clinical trials. Prospective Pravastatin Pooling
`(PPP) Project, CIRC. (May 21, 2002).
`J. D. Adams et al., Studies on the biotransformation of
`ketamine. I - Identification of metabolites produced in vitro
`from rat liver microsomal preparations, BIO. MASS SPECTROM.,
`Vol. 8, No. 8 (Aug. 1981).
`Richard E. Gregg, M.D., curriculam vitae
`John R. Wetterau et al., Absence of Microsomal Triglyceride
`Transfer Protein in Individuals with Abetalipoproteinemia,
`SCIENCE, Vol. 258 (Nov. 6, 1992).
`Bristol Meyers Squibb, Clinical Study Report, The Effects of
`Chronic Dosing of BMS-201038 on Hepatic Fat Accumulation
`and Reversibility as Assessed by Nuclear Magnetic Resonance
`Spectroscopy (NMRS), (Jan. 2002) (filed under seal)
`Bristol Meyers Squibb, BMS-201038 Investigator Brochure
`General Addendum (Oct. 1997).
`Adrien Albert, Xenobiosis: Food, Drugs and Poisons in the
`Human Body, Chapman & Hall (1987).
`Goodman, et. al., Goodman & Gilman’s The Pharmacological
`Basis of Therapeutics, (Macmillan Publishing Compnay) (1985).
`Han van de Waterbeemd et al., ADMET in Silico Modelling:
`Towards Prediction Paradise?, NAT. REV. DRUG. DISCOV., Vol.
`2, No. 3, pp. 192-204 (2003).
`35 FDA-Approved Prescription Drugs Later Pulled from the
`Market (Jan. 30, 2014, 1:09 PM),
`http://prescriptiondrugs.procon.org/view.resource.php?resourceID
`=005528.
`William H. Halliwell, Cationic Amphiphilic Drug-Induced
`Phospholipidosis, TOXICOL. PATHOL., Vol. 25, pp. 53-60 (1997).
`
`6
`
`
`
`
`
`
`
`Ex. 2064
`
`Ex. 2065
`
`Ex. 2066
`
`Ex. 2067
`
`Ex. 2068
`
`Ex. 2069
`
`Ex. 2070
`
`Ex. 2071
`
`Ex. 2072
`
`Ex. 2073
`
`Ex. 2074
`
`Ex. 2075
`
`Holger Fischer et. al, CAFCA: A Novel Tool for the Calculation
`of Amphiphilic Properties of Charged Drug Molecules, CHIMIA,
`Vol. 54, No. 11, pp. 640-645 (2000).
`R. Preston Mason, et. al., Reevaluating Equilibrium and Kinetic
`Binding Parameters for Lipophilic Drugs Based on a Structural
`Model for Drug Interaction with Biological Membranes, J. MED.
`CHEM., Vol. 34, No. 2, pp. 869-77 (Mar. 1991).
`Martin Tristani-Firouzi, et. al., Molecular Biology of K+
`Channels and Their Role in Cardiac Arrhythmias, AM. J. MED.,
`Vol. 110, pp. 50-59 (2001).
`Mark E. Curran, et. al, A Molecular Basis for Cardiac
`Arrhythmia: HERG Mutations Cause Long QT Syndrome, CELL,
`Vol. 80, pp. 795-803 (1995).
`Bernadr Fermini et al., Pre-Clinical Assessment of Drug-Induced
`QT Interval Prolongation, Current Issues and Impact on Drug
`Discovery, ANNU. REP. MED. CHEM., Vol. 39, pp. 323-33 (2004).
`William Crumb et al., QT Interval Prolongation by Non-
`cardiovascular Drugs: Issues and Solutions for Novel Drug
`Development, PHARM. SCI. TECHNOL. TODAY, Vol. 2, No. 7, pp.
`270-280 (1999).
`Man-Wai Lo, et. al., Pharmacokinetics of losartan, an angiotensin
`II receptor antagonist, and its active metabolite EXP3174 in
`humans, CLIN. PHARMACOL. THER., Vol. 58, No. 6, pp. 641-49
`(1995).
`Stephen J. Cutler et al., Wilson and Grisvold’s Textbook of
`Organic Medicinal and Pharmaceutical Chemistry, 65-66 (11th ed.
`2004).
`Christopher P. Cannon et al., Intensive versus Moderate Lipid
`Lowering with Statins after Acute Coronary Syndromes, N. ENG.
`J. MED., Vol. 350, No. 15 (Apr. 8, 2004).
`List of Prior Art Reviewed by Frank Sacks, M.D. for Motion to
`Amend
`H. Mabuchi et al., Causes of death in patients with familial
`hypercholesterolemia, ATHEROSCLEROSIS, Vol. 61, No. 1, pp. 1-6
`(1986).
`Aegerion Pharmaceuticals, Inc., U.S. Securities and Exchange
`Commission (Form 10-K) (March 15, 2016).
`7
`
`
`
`
`
`
`
`Ex. 2076
`
`Ex. 2077
`
`Ex. 2078
`
`Ex. 2079
`Ex. 2080
`
`Ex. 2081
`
`Ex. 2082
`
`Ex. 2083
`Ex. 2084
`
`Ex. 2085
`
`Ex. 2086
`
`Ex. 2087
`
`Ex. 2088
`
`Ex. 2089
`
`Aegerion Pharmaceuticals, Inc., U.S. Securities and Exchange
`Commission (Form 10-Q) (May 16,2016).
`December 2002 Final Clinical Trial Protocol Submitted to
`Institutional Review Board
`BMS-201038 Investigator Brochure General Addendum CV145-
`002, Multiple Dose PO (Oct. 1, 1997).
`Clinical Study Approval (Mar. 20, 2003).
`Abbreviated Clinical Study Report for CV145-009 (Jan. 7, 2002).
`Interim Clinical Study Summary Submitted to the Dorris Duke
`Charitable Foundation (Oct. 2003) (filed under seal)
`Memorandum Summarizing Results of Clinical Trial (Feb. 9,
`2004) (filed under seal)
`Declaration of Richard E. Gregg
`Aegerion Pharmaceuticals 2013 Annual Report
`Marina Cuchel et al., Homozygous familial
`hypercholesterolaemia: new insights and guidance for clinicians
`to improve detection and clinicalmanagement. A position paper
`fromthe Consensus Panel on Familial Hypercholesterolaemia of
`the European Atherosclerosis Society, EUR. HEART J., 35, at
`2146-2157 (2014).
`Visioli, F., “Microsomoal triglyceride transfer protein
`inhibitors,” Current Opinion in Cardiovascular, Pulmonary &
`Renal Investigational Drugs 2000 2(3):292-293
`Williams, S. et al., “Novel microsomal triglyceride transfer
`protein inhibitors,” Expert Opin. Ther. Patents (2003) 13(4):
`479-488
`Funatsu, T. et al. “Atorvastatin Increases Hepatic Fatty Acid
`Beta- Oxidation in Sucrose-Fed Rats: Comparison with an MTP
`Inhibitor” European Journal of Pharmacology 455 (2002) 161-
`167
`Barclay, L., “Hyperlipidemia”, NMT Briefs, 2003, 1-4
`
`8
`
`
`
`
`
`
`
`Evans, M., et al., “Medical Lipid-Regulating Therapy: Current
`Evidence, Ongoing Trials and Future Developments,” Drugs
`2004: 64 (11): 1181-1196
`
`US5760246A Biller S. et al., 1998
`
`Intentionally left blank
`
`WO 98/03069, Gregg R. et al.
`
`Ex. 2090
`
`Ex. 2091
`
`Ex. 2092
`
`Ex. 2093
`
`US6057339A, Gregg R., 2000
`Ex. 2094
`US6066653A, Gregg R. et al., 2000
`Ex. 2095
`Ex. 2096 WO1998031367, Gregg R. et al.
`US6620821B2, Robl J., 2003
`Ex. 2097
`US6627636B2 –Robl, J. 2003
`Ex. 2098
`US6812345B2 – Robl, J. et al. 2004
`Ex. 2099
`US7358254B2 – Robl, J. et al., 2008
`Ex. 2100
`US5990110A, Firestone R., 1999
`Ex. 2101
`Ex. 2102 WO 2005/097131, Engelen, M. et al.
`van Dam, M.J., Dyslipidemia; diagnosis and treatment,
`Dissertation, UvA-DARE, 2001, 147-157
`U.S. National Institutes of Health, Implitapide in Patients With
`Hypertriglyceridemia on Maximal, Concurrent Triglyceride-
`Lowering Therapy, NIH Clinical Trials.gov, NT0008013, 2004,
`1-3
`U.S. National Institutes of Health, Implitapide in Patients
`With Homozygous Familial Hypercholesterolemia on
`Maximal Concurrent Lipid-Lowering Therapy, NIH
`Clinical Trials.gov, NCT00079846, 2003, 1-3
`Baddour, L. et al., PPD to Hold Analyst Day on February 5, 2004
`(Jan. 15, 2004)
`
`Ex. 2103
`
`Ex. 2104
`
`Ex. 2105
`
`Ex. 2106
`
`9
`
`
`
`
`
`
`
`Ex. 2107
`
`Ex. 2108
`
`Ex. 2109
`
`Ex. 2110
`
`Gruetzmann R., et al., “Impiltapide inhibits secretation of
`apoB- associated lipoproteins by inhibition of the MTP,”
`Eur. Heart J. 2000, 21 (Suppl), Abst 3271, p. 600.
`Bischoff, H.,
`et
`al., Bay
`13-9952
`(implitapide):
`pharmacodynamic effects of a new MTP inhibitor on plasma
`lipids and adipose tissue in animals, Eur. Heart J. 2000, 21
`(Suppl), Abst P3501, p. 636
`Zaiss, S., et al., 194, Bay 13-9952 (Implitapide), an inhibitor of
`the MTP, inhibits atherosclerosis and prolongs lifetime in apo-
`E knockout mice, Eur. Hert J. 2000, 21 (Suppl), Abst 194, p. 16
`Bayes, M., et al., Gateways to Clinical Trials, Methods Find
`Exp Clin Pharmacol 2002, 24(1): 37-55
`
`Ex. 2111
`
`Sorbera, L.A., et al., Implitapide, Drugs of the Future, 2000,
`25(11): 1138-1144
`US20060135460A1, Widder K. et al., 2006
`Ex. 2112
`Ex. 2113 WO 2006/063128, Widder K. et al.
`US20060153913A1, Yamane S. et al., 2006
`Ex. 2114
`Ex. 2115 WO 2006/046623, Yamane S. et al.
`US20060211762A1, Rongen, R. et al., 2006
`Ex. 2116
`Ex. 2117 WO 2006/062748, Rongen, R. et al.
`US20070098778A1, Borsadia S., 2007
`Ex. 2118
`Ex. 2119 WO 2005/084666, Borsadia S.
`Ex. 2120 WO 96/26205, Wetterau, J. et al.
`Ex. 2121 WO 98/03174, Firestone, R.
`Ex. 2122 WO 98/27979, Tino, J.
`Aguilar-Salinas, C., et al., Efficacy and safety of atorvastatin
`in hyperlipidemic, type 2 diabetic patients. A 34-week,
`multicenter, open-label study, Eslevier, Atheroslerosis, 2000,
`489-496
`
`Ex. 2123
`
`10
`
`
`
`
`
`
`
`Ex. 2124
`
`Ex. 2125
`
`Ex. 2126
`
`Ex. 2127
`
`Capuzzi, D., et al., Niacin Dosing: Relationship to Benefits
`and Adverse Effect, Current Atherosclerosis Reports, 2000,
`2, 64-71
`Teramoto T. et al.; Effect of large dose of niceritrol (Perycit)
`on hypercholesterolemia –by administering Gradually
`Increasing Doses, Hardening of the arteries (1991), 199-208
`Reference 4 cited in JPA No. 2007-502093, Vol. 40, 3389-3397.
`Knopp R., Treatment of Lipid Disorders, New England Journal
`of Medicine, August, 1999,Vol. 341:498-511
`Bays, H. et al., Pharmacotherapy for dyslipidaemia - current
`therapies and future agents, Expert Opin. Pharmacother.
`(2003) 4(11), 1901-38
`Bruckert, E., New lipid-modifying therapies, Expert Opin.
`lnvescig. Drugs (2003) 12(3): 325-335
`Kastelein, J., What future for combination therapies? Int. J.
`Clin. Pract. Suppl. Mar. 2003, (134), 45-50
`US4686237A, Anderson, P., 1987
`Ex. 2131
`Ex. 2132 WO 98 31366, Behounek, E. et al.
`US6194454B1, Dow, R., 2001
`Ex. 2133
`US20020035064A1, Robl, J. et al, 2002
`Ex. 2134
`US20080248070A1, Tunac J, 2008
`Ex. 2135
`US20050101561A, Tunac J., 2005
`Ex. 2136
`Ex. 2137 WO 98/31225, Gregg, R.
`Ex. 2138 WO 98/50028, Gregg, R. et al.
`US6875782B2, Cheng, P. et al., 2005
`Ex. 2139
`US20030109543A1, Ogletree, M., 2003
`Ex. 2140
`US20040058908A1, Keller, B, et al., 2004
`Ex. 2141
`Ex. 2142 WO 00/38725, Keller, B, et al.
`
`Ex. 2128
`
`Ex. 2129
`
`Ex. 2130
`
`11
`
`
`
`
`
`
`
`Ex. 2147
`
`Ex. 2148
`
`Ex. 2149
`
`Ex. 2150
`
`Ex. 2151
`
`Ex. 2152
`
`US20070099884A1, Erondu, N, et al., 2007
`Ex. 2143
`Ex. 2144 WO 2004/110375, Erondu, N, et al.
`Ex. 2145 WO 2005/000217, Erondu, N, et al.
`Ex. 2146 Microsomal Triglyceride Transfer Protein, 1-6
`Wetterau, J., et al., Microsomal triglyceride transfer protein,
`Biochimica et Biophysica Acta 1345 (1997) 136-150
`Thomas, L., Alleviation of MTP inhibitor-induced hepatic
`steatosis in hyperlipidemic fa/fa rats by fenofibrate, Department
`of Metabolic Diseases and Dept. of Chemical Research,
`Boehringer Ingelheim, 1 page
`Wierzbicki, A., New lipid-lowering agents, Expert Opin.
`Emerging Drugs (2003) 8(2): 365-376
`Atzel, A., et al., Mechanism of Microsomal Triglyceride
`Transfer Protein Catalyzed Lipid Transport, Biochemistry
`1993, 32, 10444-10450
`Bakillah, A., et al., Decreased Secretion of ApoB Follows
`Inhibition of ApoB-MTP Binding by a Novel Antagonist,
`Biochemistry 2000, 39, 4892-4899
`Jamil, H., et al., An inhibitor of the microsomal triglyceride
`transfer protein inhibits apoB secretion from HepG2 cells, Proc.
`Natl. Acad. Sci. USA, Vol. 93, 1996. 11991-11995
`Liao, W., et al., Blocking microsomal triglyceride transfer
`protein interferes with apoB secretion without causing retention
`or stress in the ER, Journal of Lipid Research, Volume 44,
`2003, 978-985
`US5789197A, Wetterau II, J. et al., 1998
`US6492365B1, Wetterau II, J. et al., 2002
`US6720351B2, Bertinato, P, et al., 2004
`US20030187053, Bertinato, P, et al.
`US6979692B2, Bertinato, P, et al., 2005
`US20020045271A1, Hussain M. et al., 2002
`
`Ex. 2153
`
`Ex. 2154
`Ex. 2155
`Ex. 2156
`Ex. 2157
`Ex. 2158
`Ex. 2159
`
`12
`
`
`
`
`
`
`
`US20040014748A1, Grutzmann R. et al., 2004
`Ex. 2160
`US20060166999A1 - Grutzmann R. et al., 2006
`Ex. 2161
`US20050090426A1, Blumberg R., 2005
`Ex. 2162
`US20060205726A1, Hagiwara, A., 2006
`Ex. 2163
`EP 1 181 954, Chang, G., et al.
`Ex. 2164
`EP 1 099 442, Chang, G., et al.
`Ex. 2165
`DE19951022, Chang, G., et al.
`Ex. 2166
`CA 2,091,102, Wetterau II, J. et al.
`Ex. 2167
`CA 2291471, Chang, G., et al.
`Ex. 2168
`Ex. 2169 WO 96/40640, Chang, G., et al.
`JP2002220345, Takeshi, N., et al.
`Ex. 2170
`Ex. 2171 WO 97/41111, Urban, F.
`Ex. 2172 WO 2005/051382, Moritani, H., et al.
`Ex. 2173 WO 2005/094864, Eaton, S., et al.
`Parsons, C.G., et al., Memantine is a clinically well
`tolerated NMDA receptor antagonist - a review of
`preclinical data, Neuropharmacology 38 (1999) 735-767
`Catapano, A.L., Ezetimibe: a selective inhibitor of
`cholesterol absorption, European Heart Journal
`Supplements (2001) 3 (Supplement E), E6-E10
`Capson, T., Synthesis and Evaluation of Ammonium Analogs of
`Carbocationic Intermediates in Squalene Biosynthesis,
`Dissertation, Department of Med. Chem., The University of
`Utah, Vol. 4803B of Dissertations Abstracts International,
`1987, Abstract
`
`Ex. 2176
`
`Ex. 2174
`
`Ex. 2175
`
`13
`
`
`
`
`
`
`
`Ex. 2177
`
`Ex. 2178
`
`Ex. 2179
`
`Ex. 2180
`
`Ex. 2181
`
`Ex. 2182
`
`Ex. 2183
`
`Ex. 2184
`
`Ex. 2185
`
`Ex. 2186
`
`Ex. 2187
`Ex. 2188
`Ex. 2189
`Ex. 2190
`Ex. 2191
`
`Corey, E.J., et al. Application of Unreactive Analogs of
`Terpenoid Pyrophsphates to Studies of Multistep Biosynthesis,
`Demonstration That “Presqualene Pyrophosphate” is an
`Essential Intermediate on the Path to Squalene, Journal. Of the
`American Chemical Society, 98:5, 1976, 1291-93
`De Montellano, P., et al., Inhibition of Squalene Synthetase
`by Farnesyl Pyrophosphate Analogues, Journal of
`Medicinal Chemistry, 1977, Vol. 20, 243-49
`Earl, J., et al., Ezetimbe, Nature Reviews, Vol. 2, 2003, 97
`National Cholesterol Education Program, Adult Treatment Panel
`III Report, 2001, 373 pages
`Farrell, G., Drugs and Steatohepatitis, Seminars in Liver
`Disease, Vol. 22, No. 2, 2002, 185-194
`Gagne, C., et al., Efficacy and Safety of Ezetimibe
`Coadministered With Atorvastatin or Simvastatin in Patients
`with Homozygous Familial Hypercholesterolemia, Circulation,
`2002; 105:2469-2475
`Kirkpatrick, P., et al., Market Indicators, Nature, Vol. 2, 2003, 98
`McClard, R., Novel Phosphonylphosphinyl Analogues of
`Biochemically Interesting Diphosphates, Syntheses and Properties
`of P-C-P-C Analogues of Isopentenyl Diphosphate and
`Dimethylally Diphosphate, J. Am. Chem. Soc., 1987, 109, 5544-5
`Ritter, T., et al., Heterocyclic ring scaffolds as small-
`molecule cholesterol absorption inhibitors, Org. Biomol.
`Chem., 2005, 3, 3514-3523
`Sudhop, T., et al., Cholesterol Absorption Inhibitors for the
`Treatment of Hypercholesterolaaemia, Drugs, 2002; 62(16),
`2333-2347
`US3983140A, Endo, A. et al., 1976
`US4231938A, Monaghan, R., et al., 1980
`US4346227A, Terahara, A., 1982
`US4448784A, Glamkowski E., et al., 1984
`US4450171A, Hoffman, W., et al., 1984
`
`14
`
`
`
`
`
`
`
`Ex. 2192
`Ex. 2193
`Ex. 2194
`Ex. 2195
`Ex. 2196
`Ex. 2197
`Ex. 2198
`Ex. 2199
`Ex. 2200
`Ex. 2201
`Ex. 2202
`Ex. 2203
`EX.
`Ex. 2204
`EX‘
`Ex. 2205
`EX.
`Ex. 2206
`EX 2206
`Ex. 2207
`EX 2207
`Ex. 2208
`Ex. 2209
`Ex. 2210
`Ex. 2211
`Ex. 2212
`Ex. 2213
`Ex. 2214
`
`US4499289A, Baran, J., 1985
`US4499289A, Baran, J., 1985
`US4613610A, Waring, J., 1986
`US461361OA, Waring, J., 1986
`US4647576A, Hoefle, M., et al., 1987
`US4647576A, Hoefle, M., et a1., 1987
`US4716175B1, Hoefle, M., et al., 1987
`US4716175B1, Hoefle, M., et a1., 1987
`US4871721A, Biller, S., 1989
`US4924024A, Biller, S., 1990
`US5015644A, Roth, B. et al., 1991
`US5026554A, Bartizal, K., et al., 1991
`US5117080A, Lee, K., 1992
`US5510379A, Lee, H., et al., 1996
`US5595872A, Wetterau II, J., et al., 1997
`US5684014A, Muller, U. et al., 1997
`M1111C1',
`Ct 211.,
`EP0705831, Muller, U. et al.
`MUHCT,
`Ct al.
`US5712396A, Magnin D., et al., 1998
`Magnin 1)., Ct 211.,
`US5767115A, Rosenblum, S., et al., 1998
`US5767115A, Rosenblum, s., et a1., 1998
`US5786361A, Muller, U., et al., 1998
`US5786361A, Muller, U., et a1., 1998
`EP 0 802 198, Muller, U., et al.
`US5811429A, Connell, R., et al., 1998
`EP0779279, Connell, R., et al.
`US5827875A, Dickson, J., 1998
`US5885983A, Biller S., et al., 1999
`US5952498A, Lenfers, J., et al., 1999
`US6034115A, Connell, R., et al., 2000
`
`15
`
`
`
`
`
`
`
`EP 0 779 276, Connell, R., et al.
`Ex. 2215
`US6066650A, Biller, S., et al., 2000
`Ex. 2216
`US6114341A, Muller, U., et al., 2000
`Ex. 2217
`EP0799828, Muller, U., et al.
`Ex. 2218
`US6121283A, Chang, G., et al., 2000
`Ex. 2219
`Ex. 2220 WO 98/23593, Chang, G., et al.
`US6140343A, DeNinno, M., et al., 2000
`Ex. 2221
`US6245775B1, Muller, U., et al., 2001
`Ex. 2222
`US6265431B1, Muller, U., et al., 2001
`Ex. 2223
`US6297233B1, Stein, P., et al., 2001
`Ex. 2224
`US6344450B1, Bisacchi, G., et al., 2002
`Ex. 2225
`US6479503B2, Muller, U., et al., 2002
`Ex. 2226
`US6858622B2, Muller, U., et al., 2005
`Ex. 2227
`US6498156B2, Glombik, H., et al., 2002
`Ex. 2228
`US6774236B1, Lenfers, J., 2004
`Ex. 2229
`US6846836B2, Hamann, L., et al., 2005
`Ex. 2230
`US6884812B2, Glombik, H., et al., 2005
`Ex. 2231
`US6916809B2, Chen, P., et al., 2005
`Ex. 2232
`US6916813B2, Atwal, K., et al., 2005
`Ex. 2233
`US7053080B2, Davis, H., et al., 2006
`Ex. 2234
`US7056906B2, Strony J., 2006
`Ex. 2235
`US7394501B2, Iwata, T., 2008
`Ex. 2236
`US20030069221A1, Kosoglou, T., et al., 2003
`Ex. 2237
`
`16
`
`
`
`
`
`
`
`US20030153541A1, Dudley, R., et al., 2003
`Ex. 2238
`US20030162788A1, Thomas, L., et al., 2003
`Ex. 2239
`US20050075367A1, Hagiwara, A., et al., 2005
`Ex. 2240
`US20060069161A1, Lee, M., et al., 2006
`Ex. 2241
`US20060160834A1, Fong, T., et al., 2006
`Ex. 2242
`Ex. 2243 WO 2004/110368, Fong, T., et al.
`US20060211020A1, Farrer, L., et al., 2006
`Ex. 2244
`US20070027093A1, Ogawa, N., et al., 2007
`Ex. 2245
`Ex. 2246 WO 2005/072740, Ogawa, N., et al.
`US20070032404A1, Sweet, L., 2007
`Ex. 2247
`US20080016127A1, Field, S., 2007
`Ex. 2248
`EP0142146, Hoffman W., et al.
`Ex. 2249
`GB 2205837, Karanewsky, D., et al.
`Ex. 2250
`FR2596393, Jean, C., et al.,
`Ex. 2251
`Ex. 2252 WO 0108679, Verkade, H.
`Ex. 2253 WO 2004/028544, Grondahl, C., et al.
`Ex. 2254 WO 86/03488, Kathawala, F., et al.
`Ex. 2255 WO 86/07054, Wareing, J.
`EP0221025, Wareing, J., et al.,
`Ex. 2256
`EP0325130, Rolf, A., et al.
`Ex. 2257
`Ex. 2258 WO 96/26948, Fancelli, D., et al.
`Ex. 2259 WO 2005/033100, Carreira, E., et al.
`JP 2003-321424, Hagiwara, A., et al.
`Ex. 2260
`
`17
`
`
`
`
`
`
`
`Ex. 2261
`
`Ex. 2262
`
`Ex. 2263
`
`Ex. 2264
`
`Ex. 2265
`
`Ex. 2266
`Ex. 2267
`Ex. 2268
`Ex. 2269
`Ex. 2270
`Ex. 2271
`Ex. 2272
`Ex. 2273
`Ex. 2274
`Ex. 2275
`Ex. 2276
`
`Hussain, M., et al., Multiple functions of microsomal
`triglyceride transfer protein, Nutrition & Metabolism, 2012,
`9:14, 1-16
`Li. J., et al., Bioorganic & Medicinal Chemistry Letters 16
`(2006) 3039-3042
`Looije, N., et al., Disodium Ascorbyl Phytostanyl Phosphates
`reduces plasma cholesterol concentration, body weight and
`abdominal fat gain within a dietary-induced obese mouse
`model, J Pharm Pharmaceut Sci 8 (3):400-408, 2005
`
`Aggarwal, D., et al., JTT-130, a microsomal triglyceride
`transfer protein inhibitor lowers plasma triglycerides and LDL
`cholesterol concentrations without increasing hepatic
`triglycerides in guinea pigs, BMC Cardiovascular Disorders
`2005, 5:30, 1-8
`Samaha, F., et al., Inhibition of microsomal triglyceride
`transfer protein alone or with ezetimibe in patients with
`moderate hypercholesterolemia, Nature Clinical Practice,
`Cardiovascular Medicine, August 2008, Vol. 5 No. 8, 497-
`505
`US7645732B2, Ye, J., et al., 2010
`US20060252733A1, Jansen, B., 2006
`US20060270655A1, Swick, A., et al., 2006
`US20070088089A1, Wisler, G., 2007
`US20070093468A1, Wisler, G., 2007
`US20070093527A1, Wisler, G., 2007
`US20080033019A1, Stamler, J., 2008
`US20080051427A1, Shuckler, F., 2008
`US20080103122A1, Veltri, E., 2008
`US20080161279A1, Wisler, G., 2008
`US20080175864A1, Ye J., et al., 2008
`
`18
`
`
`
`
`
`
`
`US20080241869A1, Davis, R., 2008
`Ex. 2277
`US20080253985A1, Wisler, G., 2008
`Ex. 2278
`US20080255084A1, Webb, R., 2008
`Ex. 2279
`US20080280992A1, Kunz, K., et al., 2008
`Ex. 2280
`US20090042835A1, Davis, R., 2009
`Ex. 2281
`US20090054393A1, Wisler, G., 2009
`Ex. 2282
`US20090093527A1, Li, C., et al., 2009
`Ex. 2283
`US20100273829A1, Wisler, G., 2010
`Ex. 2284
`Ex. 2285 WO 2006/108666, Schrattenholz, A.
`Ex. 2286 WO 2006/111238, Chevreuil, O., et al.
`Ex. 2287 WO 2007/047880, Wisler, G.
`Ex. 2288 WO 2007/047724, Wisler, G.
`Ex. 2289 WO 2008/012056, Pacholik, J., et al.
`Ex. 2290 WO 2008/021353, Luo, G.
`Ex. 2291 WO 2008/030382, Veltri, E.
`Ex. 2292 WO 2008/072061, Gossellin, J., et al.
`Ex. 2293 WO 2008/075949, Troost, F., et al.
`Ex. 2294 WO 2008/079398, Wisler, G.
`Ex. 2295 WO 2008/090198, King, P., et al.
`Ex. 2296 WO 2008/115574, Bobotas, G., et al.
`US 7932268 Rader et al.
`Ex. 2297
`US 6949572 Bertinato et al.
`Ex. 2298
`US 20090042941 Rader et al.
`Ex. 2299
`
`19
`
`
`
`
`
`
`
`
`
`Ex. 2300
`
`Ex. 2301
`
`Ex. 2302
`Ex. 2303
`
`Aegerion Pharmaceuticals, Starting Juxtapid (Accessed June 7,
`2016) http://www.juxtapid.com/starting-juxtapid
`Aegerion Pharmaceuticals, Dosing and Administration (Accessed
`June 7, 2016) http://www.juxtapid.com/healthcare-
`professionals/dosing-and-administration.
`U.S. Patent No. 5,739,135 to Biller et al.
`U.S. Patent No. 6,582,698 to Dedrick et al
`
`20
`
`
`
`
`
`CERTIFICATION OF SERVICE
`
`The undersigned hereby certifies that the foregoing “UPDATED LIST OF
`
`PATENT OWNER’S EXHIBITS” was served electronically via e-mail on June 7,
`
`2016 on the following:
`
`
`Dr. Gregory Gonsalves
`2216 Beacon Lane
`Falls Church, Virginia 22043
`(571) 419-7252
`gonsalves@gonsalveslawfirm.com
`
`Christopher Casieri
`McNeely, Hare & War LLP
`12 Roszel Road, Suite C104
`Princeton, NJ 08540
`(609) 731-3668
`chris@miplaw.com
`
`Counsel for Petitioner Coalition
`for Affordable Drugs VIII, LLC
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`/Russell W. Warnick/
`Russell W. Warnick
`
`Dated: June 7, 2016
Accessing this document will incur an additional charge of $.
After purchase, you can access this document again without charge.
Accept $ Charge
Still Working On It
This document is taking longer than usual to download. This can happen if we need to contact the court directly to obtain the document and their servers are running slowly.
Give it another minute or two to complete, and then try the refresh button.
A few More Minutes ... Still Working
It can take up to 5 minutes for us to download a document if the court servers are running slowly.
Thank you for your continued patience.
This document could not be displayed.
We could not find this document within its docket. Please go back to the docket page and check the link. If that does not work, go back to the docket and refresh it to pull the newest information.
Your account does not support viewing this document.
You need a Paid Account to view this document. Click here to change your account type.
Your account does not support viewing this document.
Set your membership
status to view this document.
With a Docket Alarm membership, you'll
get a whole lot more, including:
- Up-to-date information for this case.
- Email alerts whenever there is an update.
- Full text search for other cases.
- Get email alerts whenever a new case matches your search.
One Moment Please
The filing “” is large (MB) and is being downloaded.
Please refresh this page in a few minutes to see if the filing has been downloaded. The filing will also be emailed to you when the download completes.
Your document is on its way!
If you do not receive the document in five minutes, contact support at support@docketalarm.com.
Sealed Document
We are unable to display this document, it may be under a court ordered seal.
If you have proper credentials to access the file, you may proceed directly to the court's system using your government issued username and password.
Access Government Site
