`
`
`
`
`IN THE UNITED STATES PATENT AND TRADEMARK OFFICE
`_____________________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`_____________________
`
`
`ELI LILLY AND COMPANY
`Petitioner,
`
`v.
`
`TEVA PHARMACEUTICALS INTERNATIONAL GMBH
`Patent Owner.
`
`_____________________
`
`Case IPR2018-01710
`U.S. Patent No. 8,586,045
`_____________________
`
`TEVA PHARMACEUTICALS INTERNATIONAL GMBH’S
`EXHIBIT LIST
`
`
`
`
`
`
`Mail Stop “PATENT BOARD”
`Patent Trial and Appeal Board
`U.S. Patent and Trademark Office
`P.O. Box 1450
`Alexandria, VA 22313-1450
`
`
`
`
`
`
`
`Case IPR2018-01710
`Patent No. 8,586,045
`
`
`Exhibit #
`
`2001
`
`2002
`
`2003
`
`2004
`
`2005
`
`2006
`
`2007
`
`2008
`
`2009
`
`2010
`
`2011
`
`Description
`Edvinsson, L., “Calcitonin Gene-Related Peptide (CGRP) in
`Cerebrovascular Disease,” TheScientificWorldJOURNAL, 2:1484-90
`(2002)
`Hasbak, P., et al., “Investigation of CGRP Receptors and Peptide
`Pharmacology in Human Coronary Arteries. Characterization with a
`Nonpeptide Antagonist,” The Journal of Pharmacology and
`Experimental Therapeutics, 304:326-33 (2003)
`Brain, S. and Grant, A., “Vascular Actions of Calcitonin
`Gene-Related Peptide and Adrenomedullin,” Physiol Rev., 84:903-34
`(2004)
`Chiba, T., et al., “Calcitonin gene-related peptide receptor antagonist
`human CGRP-(8-37),” Am. J. Physiol.:Endocrin. & Metab.,
`19:E331-35 (1989)
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`Gegg, Jr., C., et al., “CGRP Peptide Antagonists And
`Conjugates,” U.S. Patent No. 8,168,592 B2 (filed October 19, 2006;
`issued May 1, 2012)
`Escott, K. and Brain, S., “Effect of a calcitonin gene-related peptide
`antagonist (CGRP8-37) on skin vasodilatation and oedema induced by
`stimulation of the rat saphenous nerve,” Br. J. Pharmacol.
`110:772-76 (1993)
`Rist, B., et al., “CGRP 27-37 analogues with high affinity to the
`CGRP1 receptor show antagonistic properties in a rat blood flow
`assay,” Regul. Pept. 79:153-58 (1999)
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`vasculature: a new target in the treatment of headache," Cephalalgia,
`24:611-22 (2004)
`Goadsby, P., “Calcitonin Gene-Related Peptide Antagonists as
`Treatments of Migraine and Other Primary Headaches,” Drugs,
`65:2557-67 (2005)
`Supowit, S., et al., “Calcitonin Gene-Related Peptide Protects
`Against Hypertension-Induced Heart and Kidney Damage,”
`Hypertension, 45:109-14 (2005)
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`Case IPR2018-01710
`Patent No. 8,586,045
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`
`Exhibit #
`
`2012
`
`2013
`
`2014
`
`2015
`
`2016
`
`2017
`
`2018
`
`2019
`
`2020
`
`2021
`
`Description
`Aiyar, N., et al., “Pharmacology of SB-273779, a Nonpeptide
`Calcitonin Gene-Related Peptide 1 Receptor Antagonist,” The
`Journal of Pharmacology and Experimental Therapeutics,
`296:768-75 (2001)
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`Containing These Compounds and Method for Their Production,”
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`Chaturvedula, P., et al., “Constrained Compounds as
`CGRP-Receptor Antagonists,” U.S. Patent No. 7,384,930 B2 (filed
`October 11, 2005; issued June 10, 2008)
`Rudolf, K., et al., “Modified Aminoacids, Pharmaceuticals
`Containing These Compounds and Method for Their Production,”
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`February 5, 2002)
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`7,772,224 B2 (filed April 3, 2009; issued August 10, 2010)
`Petersen, K., et al., “The CGRP-antagonist, BIBN4096BS does not
`affect cerebral or systemic haemodynamics in healthy volunteers,”
`Cephalalgia, 25:139-47 (2004)
`Leahy, D., et al., “Process For The Preparation of
`Cycloheptapyridine CGRP Receptor Antagonists,” U.S. Patent No.
`8,669,368 B2 (filed September 19, 2011; issued March 11, 2014)
`Clinical Trials for BIBN4096BS, downloaded from
`https://clinicaltrials.gov/ct2/results?cond=&term=bibn4096bs&cntry
`=&state=&city=&dist (last accessed November 5, 2018)
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`Case IPR2018-01710
`Patent No. 8,586,045
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`
`Exhibit #
`
`2022
`
`2023
`
`2024
`
`2025
`
`2026
`
`2027
`
`2028
`
`2029
`
`2030
`
`2031
`
`Description
`Clinical Trials for MK-0974, downloaded from
`https://clinicaltrials.gov/ct2/results?cond=&term=mk-0974&cntry=
`&state=&city=&dist (last accessed on November 15, 2018)
`Clinical Trials for BMS-927711, downloaded from
`https://clinicaltrials.gov/ct2/results?cond=&term=BMS-927711&cnt
`ry=&state=&city=&dist (last accessed on November 5, 2018)
`Zeller, J., et al., “Antagonist Antibodies Directed Against Calcitonin
`Gene-Related Peptide and Methods Using Same,” U.S. Patent No.
`8,007,794 B2 (filed November 2, 2006; issued August 30, 2011)
`Zeller, J., et al., “Antagonist Antibodies Directed Against Calcitonin
`Gene-Related Peptide and Methods Using Same,” U.S. Patent No.
`8,597,649 B2 (filed April 25, 2013; issued December 3, 2013)
`Zeller, J., et al., "Antagonist Antibodies Directed Against Calcitonin
`Gene-Related Peptide and Methods Using Same," U.S. Patent No.
`9,340,614 B2 (filed August 31, 2015; issued May 17, 2016)
`Zeller, J., et al., "Antagonist Antibodies Directed Against Calcitonin
`Gene-Related Peptide and Methods Using Same," U.S. Patent No.
`9,266,951 B2 (filed August 31, 2015; issued February 23, 2016)
`Zeller, J., et al., "Antagonist Antibodies Directed Against Calcitonin
`Gene-Related Peptide and Methods Using Same," U.S. Patent No.
`9,346,881 B2 (filed August 31, 2015; issued May 24, 2016)
`Zeller, J., et al., "Antagonist Antibodies Directed Against Calcitonin
`Gene-Related Peptide," U.S. Patent No. 9,890,210 B2 (filed May 5,
`2017; issued February 13, 2018)
`Zeller, J., et al., "Antagonist Antibodies Directed Against Calcitonin
`Gene-Related Peptide," U.S. Patent No. 9,890,211 B2 (filed May 5,
`2017; issued February 13, 2018)
`Zeller, J., et al., "Methods for Treating Headache Using Antagonist
`Antibodies Directed Against Calcitonin Gene-Related Peptide," U.S.
`Patent No. 9,884,907 B2 (filed May 5, 2017; issued February 6,
`2018)
`
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`Case IPR2018-01710
`Patent No. 8,586,045
`
`
`Exhibit #
`
`2032
`
`2033
`2034
`2035
`2036
`2037
`2038
`2039
`2040
`2041
`2042
`2043
`2044
`2045
`
`2046
`
`2047
`
`2048
`
`2049
`2050
`2051
`
`2052
`
`Description
`Zeller, J., et al., "Methods for Treating Headache Using Antagonist
`Antibodies Directed Against Calcitonin Gene-Related Peptide," U.S.
`Patent No. 9,884,908 B2 (filed May 5, 2017; issued February 6,
`2018)
`File History for U.S. Patent No. 8,007,794 B2
`File History for U.S. Patent No. 8,586,045 B2
`File History for U.S. Patent No. 8,734,802 B1
`File History for U.S. Patent No. 9,115,194 B2
`File History for U.S. Patent No. 9,328,168 B2
`File History for U.S. Patent No. 9,346,881 B2
`File History for U.S. Patent No. 9,266,951 B2
`File History for U.S. Patent No. 9,340,614 B2
`File History for U.S. Patent No. 9,365,648 B1
`File History for U.S. Patent No. 9,890,211 B2
`File History for U.S. Patent No. 9,890,210 B2
`File History for U.S. Patent No. 9,884,907 B2
`File History for U.S. Patent No. 9,884,908 B2
`Clinical Trials for BHV-3000, downloaded from
`https://clinicaltrials.gov/ct2/results?cond=&term=bhv-3000&cntry=
`&state=&city=&dist (last accessed on November 5, 2018)
`Alberts, B., et al., Molecular Biology of the Cell, p. G:34, 4th ed.,
`Garland Science, Taylor & Francis Group, New York (2002)
`John H. Byrne, Essential Medical Physiology, Chapter 6:
`Neuromuscular and Synaptic Transmission, pp. 97-122, (Leonard R.
`Johnson, ed.), 3rd Ed., Elsevier Academic Press, Amsterdam (2003)
`Intentionally left blank
`Intentionally left blank
`Intentionally left blank
`Inman, S., “Anti-CGRP Monoclonal Antibodies Transforming
`Migraine Treatment,” (Oct. 22, 2018), NeurologyLive
`https://www.neurologylive.com/conferences/ana-2018/anticgrp-mon
`oclonal-antibodies-transforming-migraine-treatment, (last visited
`May 20, 2019)
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`Case IPR2018-01710
`Patent No. 8,586,045
`
`
`Exhibit #
`2053
`2054
`2055
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`2056
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`2057
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`2058
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`2059
`
`2060
`
`2061
`
`2062
`
`2063
`
`2064
`
`2065
`
`Description
`“Pain Like No Other,” UCLA Health David Geffen School of
`Medicine 38(2): 18-25 (2018)
`Intentionally left blank
`Curriculum Vitae of Steven M. Foord, Ph.D.
`Hay, D.L., et al., “A comparison of the actions of BIBN4096BS and
`CGRP8-37 on CGRP and adrenomedullin receptors expressed on
`SK-N-MC, L6, Col 29 and Rat 2 cells,” British Journal of
`Pharmacology 137(1): 80-86 (2002)
`Hay, D.L., et al., “CL/RAMP2 and CL/RAMP3 produce
`pharmacologically distinct adrenomedullin receptors: a comparison
`of effects of adrenomedullin22–52, CGRP8–37 and BIBN4096BS,”
`British Journal of Pharmacology 140(3): 477-486 (2003)
`Uren, N.G., et al., “Effect of intravenous calcitonin gene related
`peptide on ischaemia threshold and coronary stenosis severity in
`humans,” Cardiovascular Research 27: 1477-1481 (1993)
`Geppetti, P., et al., “CGRP and migraine: neurogenic inflammation
`revisited,” Journal of Headache & Pain 6(2):61-70 (2005)
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`receptor: receptor Activity-modifying protein complexes,”
`Molecular Pharmacology 67(5): 1655-1665 (2005)
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`Gene-Related Peptide in Coronary Heart Disease,” Pharmacology
`60:1-8 (2000)
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`Receptors, 65-84, (Jack R. Cooper et al. eds., 8th ed. 2003)
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`Limited, (2003)
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`cell-surface receptors, 537-538, (Harvey Lodish et al. eds., 5th ed.
`2003)
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`BIBN4096BS on CGRP-induced responses in human subcutaneous
`arteries,” British Journal of Pharmacology 143(8): 1066-1073 (2004)
`
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`Case IPR2018-01710
`Patent No. 8,586,045
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`
`Exhibit #
`
`2066
`
`2067
`
`2068
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`2069
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`2070
`
`2071
`
`2072
`
`2073
`
`2074
`2075
`2076
`
`2077
`
`2078
`
`Description
`Gallai, V., et al., “Vasoactive peptide levels in the plasma of young
`migraine patients with and without aura assessed both interictally and
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`Sarchielli, P., et al., “Nitric oxide metabolites, prostaglandins
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`Hay, D.L. and Poyner, D. “The Preclinical Pharmacology
`of BIBN4096BS, a CGRP Antagonist,” Cardiovascular Drug
`Reviews 23(1): 31-42 (2005)
`Intentionally left blank
`Wimalawansa, S.J., “Circadian variation of plasma calcitonin
`gene-related peptide in man,” Journal of Neuroendocrinology 3(3):
`319-322 (1991)
`Burgey, C., et al., “CGRP Receptor Antagonists,” PCT International
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`October 28, 2004)
`Intentionally left blank
`Hendrikse, E.R., et al., “Molecular studies of CGRP and the CGRP
`family of peptides in the central nervous system,” Cephalalgia 39(3):
`403-419 (2019)
`Intentionally left blank
`Concise Dictionary of Biomedicine and Molecular Biology, pp. 40,
`80 (Juo, P-S., ed.)
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`Jain, R., “Physiological barriers to delivery of monoclonal antibodies
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`814s-819s (1990)
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`trigemino-cerebrovascular system?,” Br. J. Neurosurgery 4: 171-180
`(1990)
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`Case IPR2018-01710
`Patent No. 8,586,045
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`
`Exhibit #
`
`2079
`
`2080
`2081
`2082
`2083
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`2084
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`2085
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`2086
`2087
`
`2088
`
`2089
`
`2090
`
`2091
`
`2092
`
`Description
`Gennari, C., et al., “Improved cardiac performance with human
`calcitonin gene related peptide in patients with congestive heart
`failure,” Cardiovascular Research 24: 239-241 (1990)
`Intentionally left blank
`Intentionally left blank
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`Intentionally left blank
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`hypoxic pulmonary hypertension,” Am. J. Physiol. 263(3):
`H681-H690 (1992)
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`Etminan, M., et al., “Risk of ischaemic stroke in people with
`migraine: systematic review and meta-analysis of observational
`studies,” Brit. Med. J. 330: 63-65 (2005)
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`ed., Garland Science, Taylor & Francis Group, New York (2002)
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`Patent No. 8,586,045
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`
`Exhibit #
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`2093
`
`2094
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`2095
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`2096
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`2097
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`2098
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`2099
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`2100
`
`2101
`
`2102
`
`2103
`
`2104
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`Description
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`secreting antibody of predefined specificity,” Nature 256(5517):
`495-497 (1975)
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`Case IPR2018-01710
`Patent No. 8,586,045
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`
`Exhibit #
`2105
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`2106
`
`2107
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`2108
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`2109
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`
`2111
`
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`
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`Patent No. 8,586,045
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`
`Exhibit #
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`2116
`
`2117
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`2118
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`2119
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`2120
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`2121
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`2122
`2123
`
`2124
`
`2125
`
`2126
`
`2127
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`2128
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`of Immunization Procedures,” ILAR Journal 46(3): 241-257 (2005)
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`Case IPR2018-01710
`Patent No. 8,586,045
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`
`Exhibit #
`
`2129
`
`2130
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`2131
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`2132
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`2133
`
`2134
`
`2135
`
`2136
`
`2137
`2138
`
`2139
`
`Description
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`Case IPR2018-01710
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`Case IPR2018-01710
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`Case IPR2018-01710
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`2164
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`Case IPR2018-01710
`Patent No. 8,586,045
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`2175
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`Case IPR2018-01710
`Patent No. 8,586,045
`
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`2183
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`- 17 -
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`
`
`Case IPR2018-01710
`Patent No. 8,586,045
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`2193
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`- 18 -
`
`
`
`Case IPR2018-01710
`Patent No. 8,586,045
`
`
`Exhibit #
`
`2202
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`2203
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`2204
`
`2205
`
`2206
`
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`
`2208
`
`2209
`
`2210
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`2213
`2214
`
`Description
`“Teva Announces U.S. Approval of
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