`Paper No. 14
`Filed: March 20, 2019
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`UNITED STATES PATENT AND TRADEMARK OFFICE
`____________________
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`___________________
`
`NEPTUNE GENERICS, LLC
`
`PETITIONER
`
`V.
`
`AVENTIS PHARMA S.A.
`
`PATENT OWNER
`
`___________________
`
`CASE NO.: IPR2019-00136
`PATENT NO. 5,847,170
`FILED: MARCH 26, 1996
`ISSUED: DECEMBER 8, 1998
`INVENTORS: HERVÉ BOUCHARD,
`JEAN-DOMINIQUE BOURZAT, ALAIN COMMERÇON
`
`
`TITLE: TAXOIDS, THEIR PREPARATION, AND PHARMACEUTICAL
`COMPOSITIONS CONTAINING THEM
`___________________
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`PETITIONER’S UPDATED EXHIBIT LIST
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`PETITIONER’S UPDATED EXHIBIT LIST
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`Petitioner Neptune Generics, LLC hereby submits its updated exhibit list to
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`accompany the submission of Exhibit 1056:
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`Description
`Exhibit No.
`Exhibit 1001 U.S. Patent No. 5,847,170 to Hervé Bouchard, Jean-Dominique
`Bourzat, and Alain Commerçon (“’170 patent”)
`Exhibit 1002 Expert Declaration of Dr. John L. Wood, Ph.D.
`Exhibit 1003 C.V. of Dr. John L. Wood
`Exhibit 1004 Prosecution file history to U.S. Patent No. 5,847,170 (“FH”)
`Exhibit 1005 P. Potier et al., Chemical Studies of 10-Deacetyl Baccatin III:
`Hemisynthesis of Taxol Derivatives 42 TETRAHEDRON 4451-
`4460 (1986)
`Exhibit 1006 L. Kelland et al., Comparative In Vitro Cytotoxicity of Taxol and
`Taxotere against Cisplatin- Sensitive and Resistant Human
`Ovarian Carcinoma Cell Lines, 30 CANCER CHEMOTHER.
`PHARMACOL. 444 (1992)
`Exhibit 1007 J. Verweij et al., Paclitaxel (Taxol) and Docetaxel (Taxotere): Not
`Simply Two of a Kind, 5 ANN. ONCOL. 495 (1994)
`Exhibit 1008 J. S. Abrams et al., New Chemotherapeutic Agents for Breast
`Cancer, 74 CANCER SUPP. 1164 (1994)
`Exhibit 1009 Commerçon et al., Practical Semisynthesis and Antimitotic Activity
`of Docetaxel and Side-Chain Analogues, in TAXANE ANTICANCER
`AGENTS (Chapter 17), pp. 233-246 (Georg, G. et al. ed., American
`Chemical Society Symposium Series, 1994) (“Commerçon”)
`Exhibit 1010 J. Kant et al, A Chemoselective Approach to Functionalize the C-
`10 Position of 10- Deacetylbaccatin III Synthesis and Biological
`Properties of Novel C-10 Taxol Analogues, 35 TETRAHEDRON
`LETTERS No. 31, pp. 5543-5546 (1994) (“Kant”)
`Exhibit 1011 U.S. Patent No. 6,201,140 to Henry Wong and Mark. D. Wittman
`(“Wong”)
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`Description
`Exhibit No.
`Exhibit 1012 Y. Ueda et al., Synthesis and Antitumor Evaluation of 2’-
`Oxycarbonylpaclitaxels (Paclitaxel-2’-Carbonates), 4
`BIOORGANIC & MEDICINAL CHEMISTRY LETTERS No. 15, pp. 1861-
`1864 (1994)
`Exhibit 1013 Y. Ueda et al., Novel Water Soluble Phosphate Prodrugs of
`Taxol® Possessing In Vivo Antitumor Activity, 3 BIOORGANIC &
`MEDICINAL CHEMISTRY LETTERS No. 8, pp. 1761-1766 (1993)
`Exhibit 1014 U.S. Patent No. 5,587,493 to Hervé Bouchard, Jean-Dominique
`Bourzat, and Alain Commerçon (“Bouchard”)
`Exhibit 1015 Volume 7, September 28, 2017 Trial Testimony from Sanofi-
`Aventis U.S. LLC v. Fresenius Kabi USA, LLC, Civil Action
`Number 3:14-cv-07869-MAS-LHG (D.N.J.).
`Exhibit 1016 Klein et al., Chemistry and Antitumor Activity on 9(R)-
`Dihydrotaxanes, in TAXANE ANTICANCER AGENTS (Chapter 20),
`pp. 276-287 (Georg, G. et al. ed., American Chemical Society
`Symposium Series, 1994) (“Klein”)
`Exhibit 1017 M. Inaba et al., Evaluation of Antitumor Activity in a Human
`Breast Tumor/Nude Mouse Model with a Special Emphasis on
`Treatment Dose, 64 Cancer pp. 1577-1582 (1989)
`Exhibit 1018 Margraff, Bézard, Bourzat, and Commerçon, Synthesis of 19-
`Hydroxy Docetaxel from a Novel Baccatin, 4 BIOORGANIC &
`MEDICINAL CHEMISTRY LETTERS, No. 2, pp. 233-236 (1994)
`Exhibit 1019 Untch et al, Comparison of paclitaxel and docetaxel (Taxotere) in
`gynecologic and breast cancer cell lines with the ATP-cell viability
`assay, 5 ANTI-CANCER DRUGS, pp. 24-30 (1994)
`Exhibit 1020 A. Joshi et al., Results of a phase II randomized controlled clinical
`trial comparing efficacy of Cabazitaxel versus Docetaxel as
`second line or above therapy in recurrent head and neck cancer,
`75 ORAL ONCOLOGY pp. 54-60 (2017)
`Exhibit 1021 P. Vrignaud et al, Preclinical Antitumor Activity of Cabazitaxel, a
`Semisynthetic Taxane Active in Taxane-Resistant Tumors, 19 Clin
`Cancer Res No. 11 pp. 2973-2983 (2013)
`Exhibit 1022 U.S. Patent No. 5,489,601 to Robert Holton and Kasthuri Rengan
`Exhibit 1023 Publication information regarding Kant, Ex.1010.
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`Exhibit 1026
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`Description
`Exhibit No.
`Exhibit 1024 National Cancer Institute Division of Cancer Treatment and
`Diagnosis, Developmental Therapeutics Program (DTP) website
`and timeline entitled: “Success Story Taxol® (NSC 125973)” at
`https://dtp.cancer.gov/timeline/flash/success_stories/s2_taxol.htm
`Exhibit 1025 U.S. Food & Drug Administration website printout New Drug
`Application 020262 (Taxol) with Original Approval and
`Supplements shown, from:
`https://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=
`overview.process&ApplNo=020262
`I. Ojima et al, Structure-Activity Relationships of New Taxoids
`Derived from 14β-Hydroxy-10-Deacetylbaccatin III, 37 J. MED.
`CHEM. No. 10 pp. 1408-1410 (1994)
`Exhibit 1027 Abstract to E.K. Rowinsky et al., Clinical toxicities encountered
`with paclitaxel (Taxol), SEMIN. ONCOLO. 20 (4 Suppl. 3), pp. 1-15
`(Aug. 1993)
`Exhibit 1028 E.A. Eisenhauer et al., European-Canadian Randomized Trial of
`Paclitaxel in Relapsed Ovarian Cancer: High-Dose Versus Low-
`Dose and Long Versus Short Infusion, 12 J. CLINICAL ONCOLOGY,
`PP. 2654-2666 (Aug. 1993)
`Exhibit 1029 K. Diergarten et al., Taxol: A New Antineoplastic Agent, 16
`ONKOLOGIE, pp. 329-337 (1993)
`Exhibit 1030 J. D. Hainsworth et al., Paclitaxel Administered by 1-Hour
`Infusion—Preliminary Results of a Phase I/II Trial Comparing
`Two Schedules, 74 CANCER No. 4, pp. 1377-1382 (Aug. 15, 1994)
`Exhibit 1031 R.S. Finley et al., Patient Care Issues: The Management of
`Paclitaxel-Related Toxicities, 28 THE ANNALS OF
`PHARMACOTHERAPY, pp. S27-S30 (May 1994)
`Exhibit 1032 “Taxol Approved for Breast Cancer,” THEPHARMALETTER—UP TO
`DATE NEWS FOR THE PHARMACEUTICAL AND BIOTECHNOLOGY
`INDUSTRIES-- https://www.thepharmaletter.com/article/taxol-
`approved-for-breast-cancer (April 25, 1994) (visited July 2, 2018)
`Exhibit 1033 L. Webster et al., Measurement of Cremophor EL Following
`Taxol: Plasma Levels Sufficient to Reverse Drug Exclusion
`Mediated by the Multidrug Resistant Phenotype, 85 J. NATL.
`CANCER INST., No. 20 pp. 1685-1690 (October 20, 1993)
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`Exhibit 1035
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`Description
`Exhibit No.
`Exhibit 1034 F. Gueritte-Voegelein, P. Potier et al., Relationships between the
`Structure of Taxol Analogues and Their Antimitotic Activity, 34 J.
`MED. CHEM., No. 3 pp. 992-998 (1991)
`I. Ojima et al., Syntheses and Structure-Activity Relationships of
`New Taxoids, in TAXANE ANTICANCER AGENTS (Chapter 19), pp.
`262-275 (Georg, G. et al. ed., American Chemical Society
`Symposium Series, 1994)
`Exhibit 1036 Golick J. et al., Phosphonooxymethyl ethers of taxane derivatives,
`European Patent Application Publication No. 0 604 910 A1,
`Application No. 93120801.1, filed December 23, 1993, published
`July 6, 1994.
`Exhibit 1037 H. Lataste, V. Senilh, M. Wright, D. Guenard, and P. Potier,
`Relationships between the structures of taxol and baccatine III
`derivatives and their in vitro action on the disassembly of
`mammalian brain and Physarum amoebal microtubules, in 81
`PROC. NATL. ACAD. SCI USA, pp. 4090-4094 (July 1984)
`Exhibit 1038 A. Greene, Pierre Potier et al., A Highly Efficient, Practical
`Approach to Natural Taxol, in 110 J. AM. CHEM. SOC. No. 17, pp.
`5917-5919 (1988) (“Potier 1988”)
`Exhibit 1039 Excerpt [Chapter 2] from R. SILVERMAN, THE ORGANIC
`CHEMISTRY OF DRUG DESIGN AND DRUG ACTION, pp. 4-51 (1992)
`Exhibit 1040 D. Guenard, F. Gueritte-Voegelein, and P. Potier, Taxol and
`Taxotere: Discovery, Chemistry, and Structure-Activity
`Relationships, 26 ACC. CHEM. RES. No. 4, pp. 160-167 (1993)
`(“Potier 1993”)
`Exhibit 1041 J. Pezzuto et al., A Mixed Micellar Formulation Suitable for the
`Parenteral Administration of Taxol, in 11 PHARMACEUTICAL
`RESEARCH No. 2, pp. 206-212 (1994)
`Exhibit 1042 Second Declaration of Alain Commerçon, dated April 23, 1998,
`excerpted from prosecution history (Ex.1004) of the U.S. Patent
`No. 5,847,170 (Ex.1001) (“Commerçon Declaration” or
`“Declaration”).
`Exhibit 1043 Bissery, M.C. et al., Experimental Antitumor Activity of Taxotere
`(RP 56976, NSC 628503), a Taxol Analogue, in 51 CANCER
`RESEARCH, pp. 4845-4852 (Sept. 15, 1991)
`Exhibit 1044 Riou, J.F. et al., Effects of Taxotere on Murine and Human Tumor
`Cell Lines, in 187 BIOCHEMICAL AND BIOPHYSICAL RESEARCH
`COMMUNICATIONS, No. 1, pp. 164-170 (Aug. 31, 1992)
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`Description
`Exhibit No.
`Exhibit 1045 U.S. Food & Drug Administration website printout for New Drug
`Application 020449 (Taxotere/Docetaxel) with Original Approval
`and Supplements shown, from:
`https://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=
`overview.process&ApplNo=020449
`Exhibit 1046 Georg, G., et al, Preface to TAXANE ANTICANCER AGENTS (Georg,
`G. et al. ed., American Chemical Society Symposium Series, 1994)
`Exhibit 1047 Abstract of Oudard, S. et al, Cabazitaxel versus Docetaxel as First-
`Line Therapy for Patients with Metastatic Castration-Resistant
`Prostate Cancer: A Randomized Phase III Trial—FIRSTANA, 35
`J. Clinical Oncology No. 28 pp. 3189-3197 (Oct. 1, 2017)
`Exhibit 1048 U.S. Patent No. 8,927,592 to Sunil Gupta
`Exhibit 1049 Redacted Opinion, Document No. 328, from Case No. 14-7869,
`Sanofi-Aventis U.S. LLC v. Fresenius Kabi USA, LLC, (D. NJ
`December 19, 2017) (“Opinion”)
`Exhibit 1050 Nicolaou, K.C. et al., Total synthesis of taxol, in 367 NATURE pp.
`630-634 (Feb. 17, 1994)
`Exhibit 1051 Holton, R.A. et al, First Total Synthesis of Taxol. 1.
`Functionalization of the B Ring, and 2. Completion of the C and D
`Rings, in 367 J. AM. CHEM. SOC., No. 4, pp. 1597-1600 (1994)
`Exhibit 1052 Ojima, I., et al, New and Efficient Approaches to the Semisynthesis
`of Taxol and its C-13 Side Chain Analogs by Means of β-Lactam
`Synthon Method, in 48 TETRAHEDRON, No. 34, pp. 6985-7012
`(1992)
`Exhibit 1053 Suffness, Matthew, Chapter 1 Overview of Paclitaxel Research –
`Progress on Many Fronts, in TAXANE ANTICANCER AGENTS
`(Chapter 1), pp. 1-17, (Georg, G. et al. ed., American Chemical
`Society Symposium Series, 1994)
`Exhibit 1054 Excerpts from MEDICINAL CHEMISTRY: PRINCIPLES AND PRACTICE
`(King, Frank. ed., Royal Society of Chemistry, 1994)
`Exhibit 1055 Excerpts from Larock, Richard, COMPREHENSIVE ORGANIC
`TRANSFORMATIONS, VCH Publishers (1989)
`Exhibit 1056 Transcript of conference call with the Patent Trial and Appeals
`Board dated February 28, 2019
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`Dated March 20, 2019
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`Respectfully Submitted,
`
`/Alexander E. Gasser/
`Alexander E. Gasser (Reg. No. 48,760)
`SKIERMONT DERBY LLP
`1601 Elm Street, Suite 4400
`Dallas, TX 75201
`P: 214-978-6600/F: 214-978-6601
`Lead Counsel for Petitioner
`
`Sarah Spires (Reg. No. 61,501)
`Paul J. Skiermont (pro hac vice to be
`requested)
`SKIERMONT DERBY LLP
`1601 Elm Street, Suite 4400
`Dallas, TX 75201
`P: 214-978-6600/F: 214-978-6601
`
`Mieke Malmberg (pro hac vice to be
`requested)
`SKIERMONT DERBY LLP
`800 Wilshire Blvd., Suite 1450
`Los Angeles, CA 90017
`P: 213-788-4500/F: 213-788-4545.
`
`Back-Up Counsel for Petitioner
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`CERTIFICATE OF SERVICE
`
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`The undersigned hereby certifies that a copy of the foregoing Petitioner’s
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`Updated Exhibit List and Exhibit 1056 were served on March 20, 2019, by
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`delivering a copy via electronic mail to the attorneys of record for the Patent
`
`Owner as follows:
`
`Daniel J. Minion (Reg. No. 53,329)
`Dominick A. Conde (Reg. No. 33,856)
`William E. Solander (pro hac vice to be filed)
`Melinda R. Roberts (pro hac vice to be filed)
`Venable LLP
`1290 Avenue of the Americas
`New York, NY 10104-3800
`DMinion@Venable.com
`DConde@Venable.com
`WSolander@Venable.com
`MRRoberts@Venable.com
`
`
`Dated: March 20, 2019
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`
`
`/Alexander E. Gasser/
`Alexander E. Gasser (Reg. No. 48,760)
`SKIERMONT DERBY LLP
`1601 Elm Street, Suite 4400
`Dallas, TX 75201
`P: 214-978-6600/F: 214-978-6601
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