`
`Filed on behalf of Apotex Inc.
`By: Kenneth J. Burchfiel
`
`Grant S. Shackelford
`
`Sughrue Mion, PLLC
`
`2100 Pennsylvania Ave., NW
`
`Washington, DC 20037
`
`Telephone: 202-293-7060
`
`Facsimile: 202-293-7860
`
`email:
`kburchfiel@sughrue.com
`gshackelford@sughrue.com
`
`
`
`
`
`IN THE UNITED STATES PATENT AND TRADEMARK OFFICE
`__________________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`__________________
`
`APOTEX INC.
`Petitioner
`
`v.
`
`MERCK & CO., INC.
`Patent Owner
`__________________
`
`Patent No. 5,691,336
`__________________
`
`
`
`APOTEX INC.’S EXHIBIT LIST
`
`(Inter Partes Review of U.S. Patent No. 5,691,336)
`
`
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`
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`Apotex
`Exhibit
`#
`
`APOTEX INC. Exhibit List for
`Inter Partes Review of U.S. Patent No. 5,691,336
`
`Description
`
`Ex. 1001 U.S. Patent No. 5,691,336 to Dorn et al.
`
`Ex. 1002 Declaration of Longqin Hu, Ph. D. ("Hu Decl.")
`
`Ex. 1003 U.S. Patent No. 5,637,699 to Dorn et al.
`
`Ex. 1004 U.S. Patent No. 5,070,082 to Murdock et al.
`
`Ex. 1005 Murdock, K.C., et al., N-Phosphoryl Derivatives of Bisantrene.
`Antitumor Prodrugs with Enhanced Solubility and Reduced Potential
`for Toxicity, J. MED. CHEM., 36, 2098-2101 (July 23, 1993)
`
`Ex. 1006 U.S. Patent No. 3,661,926 to Van Den Bos et al.
`
`Ex. 1007 Atanassova, T. et al., Synthesis of N-substituted 2-imidazolidinone,”
`PHARMAZIE, 42(9), 670-671 (1991)
`
`Ex. 1008 Bundgaard, H. et al., Prodrugs as drug delivery systems IV: N-mannich
`bases as potential novel prodrugs for amides, ureides, amines, and
`other NH-acidic compounds, J. PHARM. SCI., 69, 44-46 (1980)
`
`Ex. 1009 Bundgaard, H. (ed.), Design of Prodrugs, Chapter 1: “Design of
`prodrugs: Bioreversible derivatives for various functional groups and
`chemical entities,” Preface and 1-92 (1985)
`
`Ex. 1010 Bundgaard, H. (ed.), Design of Prodrugs, Chapter 7: “Prodrugs for
`improved formulation properties,” 243-269 (1985)
`
`Ex. 1011 Bundgaard, H., Formation of Prodrugs of Amines, Amides, Ureides,
`and Imides, METHODS IN ENZYMOLOGY, 112, 347-359 (1985)
`
`Ex. 1012 Balant, L.P. et al., Prodrugs for the improvement of drug absorption via
`different routes of administration, EUR. J. DRUG METABOL.
`PHARMACOKIN., 15(2), 143-153 (1990)
`
`Ex. 1013 Avis, K.E. et al. (eds.), Pharmaceutical Dosage Forms: Parenteral
`Medications Volume 1, Chapter 2: Duma, R.J. et al. Parenteral Drug
`1
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`
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`
`Apotex
`Exhibit
`#
`
`APOTEX INC. Exhibit List for
`Inter Partes Review of U.S. Patent No. 5,691,336
`
`Description
`
`Administration: Routes, Precautions, Problems, Complications and
`Drug Delivery Systems,” 17-58 (1992)
`
`Ex. 1014 Varia, S.A. et al., Phenytoin Prodrugs III: Water-Soluble Prodrugs for
`Oral and/or Parenteral Use, J. PHARM. SC. 73(8) 1068-1073 (1984)
`
`Ex. 1015 Fischer, J.H., et al., Fosphenytoin Clinical Pharmacokinetics and
`Comparative Advantages in the Acute Treatment of Seizures, CLIN.
`PHARMACOKINET., 42(1), 33-58 (2003)
`
`Ex. 1016 Kearney, et al., The in Vitro Enzymic Labilities of Chemically Distinct
`Phosphomonoester Prodrugs, PHARM. RES., 9(4), 497-503 (1992)
`
`Ex. 1017 Sommer, F.G., et al., Pain Accompanying Leg Venography: A
`Comparison of Sodium and Methylglucamine Diatrizoates, RADIOLOGY,
`133, 790-791 (1979)
`
`Ex. 1018 Chromy, V., et al., D(-)-N-Methylglucamine Buffer for pH 8.5 to 10.5,
`CLIN. CHEM., 24(2), 379-381 (1978)
`
`Ex. 1019 U.S. Patent No. 3,981,994 to Hoffmann et al.
`
`Ex. 1020 U.S. Patent No. 3,867,397 to Bohner et al.
`
`Ex. 1021 Berge, S.M. et al., Pharmaceutical Salts, J. PHARM. SCI., 66(1), 1-19
`(1977)
`
`Ex. 1022 U.S. Patent No. 4,748,174 to Veronesi
`
`Ex. 1023 Merck & Co. Emend® (aprepitant) Drug Information Label
`
`Ex. 1024 Merck & Co. Emend® (fosaprepitant dimeglumine) Drug Information
`Label
`
`Ex. 1025 U.S. Patent Application Serial No. 08/169,889, filed December 17,
`1993, abandoned
`
`
`
`2
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`Apotex
`Exhibit
`#
`
`APOTEX INC. Exhibit List for
`Inter Partes Review of U.S. Patent No. 5,691,336
`
`Description
`
`Ex. 1026 Ex parte Dong, Appeal No. 2011-010047 (P.T.A.B. Jan. 28, 2013)
`
`Ex. 1027 Ex parte Cao, Appeal No. 2010-004081 (B.P.A.I. Sept. 19, 2011)
`
`Ex. 1028 Hale, J.J. et al., Structural Optimization Affording 2-(R)-(l-(R)-3,5-
`Bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-oxo-
`l,2,4-triazol-5-yl)methylmorpholine, a Potent, Orally Active, Long-
`Acting Morpholine Acetal Human NK-1 Receptor Antagonist, J. MED.
`CHEM., 41, 4607-4614 (1998)
`
`Ex. 1029 Hale, J.J., et. al., Phosphorylated Morpholine Acetal Human
`Neurokinin-1 Receptor Antagonists as Water-Soluble Prodrugs, J. MED.
`CHEM., 43, 1234-1241 (2000)
`
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`3
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`APOTEX INC. Exhibit List for
`Inter Partes Review of U.S. Patent No. 5,691,336
`
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`Respectfully submitted,
`
`/Grant Shackelford/
`Grant S. Shackelford
`Reg. No. 70,504
`SUGHRUE MION, PLLC
`2100 Pennsylvania Ave, NW
`Washington, DC 20037
`Telephone: (202) 293-7060
`Facsimile: (202) 293-7860
`
`4
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`CERTIFICATE OF SERVICE
`(37 C.F.R. §§ 42.6(e) and 42.105(a))
`
`The undersigned hereby certifies that the above-captioned APOTEX INC.’S
`
`EXHIBIT LIST and Exhibits 1026-1029 were served on July 24, 2015 by filing
`
`these documents through the Patent Review Processing System as well as
`
`delivering copies via electronic mail upon the following attorneys of record for the
`
`Patent Owner:
`
`Bruce M. Wexler (brucewexler@paulhastings.com)
`Preston K. Ratliff, II (prestonratliff@paulhastings.com)
`Gregory A. Morris (gregorymorris@paulhastings.com)
`Naveen Modi (naveenmodi@paulhastings.com)
`Richard C. Billups (richard_billups@merck.com)
`Gerard M. Devlin, Jr. (gerard_devlin@merck.com)
`
`
`
`DATE: July 24, 2015
`
`
`/Grant Shackelford/
`Grant S. Shackelford
`Reg. No. 70,504
`SUGHRUE MION, PLLC
`2100 Pennsylvania Ave, NW
`Washington, DC 20037
`Telephone: (202) 293-7060
`Facsimile: (202) 293-7860