`
`In the Inter Partes Review of:
`
`Trial Number: To Be Assigned
`
`
`
`U.S. Patent No. 6,407,213
`
`Filed: November 17, 1993
`
`Issued: June 18, 2002
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`Inventor(s): Paul J. Carter, Leonard G. Presta
`
`Assignee: Genentech, Inc.
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`Title: Method for making humanized antibodies Panel: To Be Assigned
`
`Mail Stop Inter Partes Review
`Commissioner for Patents
`P.O. Box 1450
`Alexandria, VA 22313-1450
`
`
`
`
`
`PETITION FOR INTER PARTES REVIEW OF
`U.S. PATENT NO. 6,407,213
`UNDER 35 U.S.C. § 311 AND 37 C.F.R. § 42.100
`
`
`
`Petition for Inter Partes Review of U.S. Patent No. 6,407,213
`
`TABLE OF CONTENTS
`
`Page
`
`I.
`
`INTRODUCTION ........................................................................................... 1
`
`II. MANDATORY NOTICES – 37 C.F.R. § 42.8(A)(1) AND (B) .................... 2
`
`A.
`
`B.
`
`C.
`
`D.
`
`37 C.F.R. § 42.8(b)(1): Real Party-In-Interest ...................................... 2
`
`37 C.F.R. § 42.8(b)(2): Related Matters ............................................... 2
`
`37 C.F.R. § 42.8(b)(3): Lead and Back-Up Counsel ............................ 3
`
`37 C.F.R. § 42.8(b)(4): Service Information ......................................... 3
`
`III. PAYMENT OF FEES – 37 C.F.R. § 42.103 ................................................... 4
`
`IV. GROUNDS FOR STANDING – 37 C.F.R. § 42.104(a) ................................ 4
`
`V.
`
`IDENTIFICATION OF CHALLENGE – 37 C.F.R. § 42.104(b) ................... 4
`
`A.
`
`B.
`
`C.
`
`D.
`
`E.
`
`F.
`
`’213 Patent Background ........................................................................ 8
`
`Summary of the Argument .................................................................. 10
`
`Prosecution History and Related Proceedings .................................... 14
`
`Level of Ordinary Skill in the Art ....................................................... 15
`
`Claim Construction ............................................................................. 16
`
`Prior Art ............................................................................................... 19
`
`VI. THE PRIOR ART RENDERS THE CHALLENGED CLAIMS
`UNPATENTABLE ........................................................................................ 27
`
`A. Ground 1: Claims 1–2, 25, 29, 63, 66, 67, 71–72, 75–76 and
`80–81 Are Anticipated by Kurrle ........................................................ 28
`
`B. Ground 2: Claims 1, 2, 4, 29, 62–64 and 80–81 Are Anticipated
`by Queen 1990 ..................................................................................... 34
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`Petition for Inter Partes Review of U.S. Patent No. 6,407,213
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`C. Ground 3: Claims 1–2, 4, 25, 29, 62–64, 66–67, 69, 71–72, 75–
`76, 78 and 80–81 Are Unpatentable as Obvious over Queen
`1990 and Kurrle ................................................................................... 41
`
`D. Ground 4: Claim 12 Is Obvious over Queen 1990, Kurrle, and
`Furey .................................................................................................... 51
`
`E.
`
`F.
`
`Ground 5: Claims 73 and 77 Are Obvious over Queen 1990,
`Kurrle and Chothia & Lesk ................................................................. 52
`
`Ground 6: Claim 74 Is Obvious over Queen 1990, Kurrle and
`Chothia 1985 ....................................................................................... 54
`
`G. Ground 7: Claims 79 and 65 Are Obvious over Queen 1990,
`Kurrle, Chothia & Lesk and Chothia 1985 ......................................... 54
`
`H. Ground 8: Claims 30–31, 33 and 42 Are Obvious over Queen
`1990 in View of Hudziak .................................................................... 56
`
`I.
`
`J.
`
`Ground 9: Claim 42 Is Obvious over Queen 1990, Hudziak and
`Furey .................................................................................................... 61
`
`Ground 10: Claim 60 Is Obvious over Queen 1990, Hudziak
`and Chothia & Lesk ............................................................................. 62
`
`K.
`
`Secondary Considerations Cannot Overcome Obviousness ............... 62
`
`VII. CONCLUSION .............................................................................................. 68
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`Petition for Inter Partes Review of U.S. Patent No. 6,407,213
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`TABLE OF AUTHORITIES
`
` Page(s)
`
`Cases
`Adair v. Carter,
`101 U.S.P.Q.2d 1625 (Fed. Cir. 2012) ......................................................... 15, 16
`
`Atlas Powder Co. v. Ireco Inc.,
`190 F.3d 1342 (Fed. Cir. 1999) ........................................................ 31, 34, 38, 51
`
`Ecolochem, Inc. v. Southern California Edison Co.,
`91 F.3d 169 (Fed. Cir. 1996) .............................................................................. 17
`
`Ex Parte Takeshi Shimono,
`2015 WL 1952506, Appeal 2013–003410 (PTAB Apr. 29, 2015) .............. 63, 64
`
`In re Cuozzo Speed Techs., LLC,
`793 F.3d 1268 (Fed. Cir. 2015) .............................................................. 16, 17, 18
`
`In re Huai-Hung Kao,
`639 F.3d 1057 (Fed. Cir. 2011) .......................................................................... 64
`
`In re Kubin,
`561 F.3d 1351 (Fed. Cir. 2009) .......................................................................... 65
`
`In re Peterson,
`315 F.3d 1325 (Fed. Cir. 2003) .......................................................................... 56
`
`In re Skoll,
`523 F.2d 1392 (C.C.P.A. 1975) .......................................................................... 17
`
`Merck & Co. v. Teva Pharms. USA,
`395 F.3d 1364 (Fed. Cir. 2005) .......................................................................... 63
`
`Norgren Inc. v. ITC,
`699 F.3d 1317 (Fed. Cir. 2012) .......................................................................... 66
`
`Ormco Corp. v. Align Tech., Inc.,
`463 F.3d 1299 (Fed. Cir. 2006) .......................................................................... 67
`
`Pfizer, Inc. v. Apotex, Inc.,
`480 F.3d 1348 (Fed. Cir. 2007) .......................................................................... 63
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`Petition for Inter Partes Review of U.S. Patent No. 6,407,213
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`Tokai Corp. v. Easton Enters, Inc.,
`632 F.3d 1358 (Fed. Cir. 2011) .......................................................................... 63
`
`Torrent Pharms. Ltd. v. Novartis AG,
`2015 WL 5719630 (PTAB Sep. 24, 2015) ......................................................... 63
`
`Statutes
`
`35 U.S.C. §§ 102 and 103 .......................................................................................... 4
`
`35 U.S.C. § 102(a) ..................................................................................................... 7
`
`35 U.S.C. § 103(a) ..................................................................................................... 7
`
`35 U.S.C. § 135(b)(1)............................................................................................... 15
`
`35 U.S.C. § 311 .......................................................................................................... 1
`
`35 U.S.C. § 314(a) ..................................................................................................... 7
`
`35 U.S.C. § 315 .......................................................................................................... 4
`
`Other Authorities
`
`37 C.F.R. § 42.8(a)(1) and (b) ................................................................................... 2
`
`37 C.F.R. § 42.8(b)(1) ................................................................................................ 2
`
`37 C.F.R. § 42.8(b)(2) ................................................................................................ 2
`
`37 C.F.R. § 42.8(b)(3) ................................................................................................ 3
`
`37 C.F.R. § 42.8(b)(4) ................................................................................................ 4
`
`37 C.F.R. § 42.10(b) .............................................................................................. 1, 4
`
`37 C.F.R. § 42.15(a) ............................................................................................... 1, 4
`
`37 C.F.R. § 42.100 ..................................................................................................... 1
`
`37 C.F.R. § 42.100(b) .............................................................................................. 16
`
`37 C.F.R. § 42.103 ................................................................................................. 1, 4
`
`37 C.F.R. § 42.104(a) ................................................................................................. 4
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`Petition for Inter Partes Review of U.S. Patent No. 6,407,213
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`37 C.F.R. § 42.104(b) ................................................................................................ 4
`
`MPEP § 2144.05 ...................................................................................................... 56
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`Petition for Inter Partes Review of U.S. Patent No. 6,407,213
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`Exhibit No.
`1001
`
`1002 Vols.
`1–10
`1003
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`1003A
`1003B
`1003C–Q
`1004
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`1004A
`1004B
`1005
`1006
`1007
`1008
`1009
`1010
`1011
`1012
`1013
`1014
`1015
`1016
`1017
`1018
`1019
`1020
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`PETITIONER’S EXHIBIT LIST
`Description
`U.S. Patent No. 6,407,213, Method for making humanized
`antibodies (filed July 17, 1993) (issued June 18, 2002)
`File History for U.S. Patent No. 6,407,213
`
`Declaration of Dr. Foote in Support of Petition for Inter Partes
`Review of Patent No. 6,407,213
`Curriculum Vitae of Dr. Foote
`Materials Reviewed by Dr. Foote
`Exhibits C–Q of Dr. Foote’s Declaration
`Declaration of Mr. Buss in Support of Petition for Inter Partes
`Review of Patent No. 6,407,213
`Curriculum Vitae of Mr. Buss
`Materials Reviewed by Mr. Buss
`Reserved
`Reserved
`Reserved
`Reserved
`Reserved
`Reserved
`Reserved
`Reserved
`Reserved
`Reserved
`Reserved
`Reserved
`Reserved
`Reserved
`Reserved
`Reserved
`
`i
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`Petition for Inter Partes Review of U.S. Patent No. 6,407,213
`
`Exhibit No.
`1021
`
`1022
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`1023
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`1024
`
`1025
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`1026
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`1027
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`1028
`
`1029
`
`1030
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`
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`PETITIONER’S EXHIBIT LIST
`Description
`Hudziak et al., p185HER2 Monoclonal Antibody Has Antiproliferative
`Effects In Vitro and Sensitizes Human Breast Tumor Cells to Tumor
`Necrosis Factor, 9(3) MOLECULAR CELLULAR BIOLOLGY 1165–72
`(1989) (“Hudziak”)
`Köhler et al., Continuous Cultures of Fused Cells Secreting
`Antibody of Predefined Specificity, 256(5517) NATURE 495–97
`(1975)
`Prabakaran, The Quest for a Magic Bullet, 349(6246) SCIENCE 389
`(2015)
`Marks, The Story of Cesar Milstein and Monoclonal Antibodies: A
`Healthcare Revolution in the Making,
`http://www.whatisbiotechnology.org/exhibitions/milstein (last
`accessed March 23, 2017)
`Cosimi et al., Treatment of Acute Renal Allograft Rejection with
`OKT3 Monoclonal Antibody, 32(6) TRANSPLANTATION 535−39
`(1981) (“Cosimi ‘81”)
`Ortho Multicenter Transplant Study Group, A Randomized Clinical
`Trial of OKT3 Monoclonal Antibody for Acute Rejection of
`Cadveric Renal Transplants, 313(6) NEW ENG. J. MED. 337–42
`(1985) (“OMTSG ‘85”)
`Jaffers et al., Monoclonal Antibody Therapy: Anti-Idiotypic and
`Non-Anti-Idiotypic Antibodies to OKT3 Arising Despite Intense
`Immunosuppression, 41(5) TRANSPLANTATION 572–78 (1986)
`(“Jaffers ‘86”)
`Sears et al., Phase-I Clinical Trial of Monoclonal Antibody in
`Treatment of Gastrointestinal Tumours, 1 LANCET 762–65 (1982)
`Sikora, Monoclonal Antibodies in Oncology, 35(4) J. CLINICAL
`PATHOLOGY 369–75 (1982)
`Protein Data Bank - Chronology, National Science Foundation,
`https://www.nsf.gov/news/news_summ.jsp?cntn_id=100689 (last
`accessed April 12, 2017)
`
`ii
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`Petition for Inter Partes Review of U.S. Patent No. 6,407,213
`
`Exhibit No.
`1031
`
`1032
`
`1033
`
`1034
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`1035
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`1036
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`1037
`
`1038
`
`1039
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`1040
`
`1041
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`
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`PETITIONER’S EXHIBIT LIST
`Description
`Morrison et al., Chimeric Human Antibody Molecules: Mouse
`Antigen-Binding Domains With Human Constant Region Domains,
`81(21) PROC. NAT’L ACAD. SCI. USA 6851–55 (1984) (“Morrison
`‘84”)
`Liu et al., Chimeric Mouse-Human IgG1 Antibody that can Mediate
`Lysis of Cancer Cells, 84(10) PROC. NAT’L ACAD. SCI. USA 3439–
`43 (1987) (“Liu ‘87”)
`Jones et al., Replacing the Complementarity-Determining Regions
`in a Human Antibody With Those From a Mouse, 321(6069)
`NATURE 522–25 (1986) (“Jones ‘86”)
`Queen et al., A Humanized Antibody That Binds to the Interleukin 2
`Receptor, 86(24) PROC. NAT’L ACAD. SCI. USA 10029–33 (1989)
`(“Queen 1989”)
`Kirkman et al., Early Experience with Anti-Tac in Clinical Renal
`Transplantation, 21(1) TRANSPLANTATION PROC. 1766–68 (1989)
`(“Kirkman ‘89”)
`Waldmann et al., The Interleukin-2 Receptor: A Target for
`Monoclonal Antibody Treatment of Human T-Cell Lymphotrophic
`Virus I-Induced Adult T-Cell Leukemia, 82(6) BLOOD 1701–12
`(1993) (“Waldman ‘93”)
`Hakimi et al., Reduced Immunogenicity and Improved
`Pharmacokinetics of Humanized ANTI-Tac in Cynomolgus
`Monkeys, 147(4) J. IMMUNOLOGY 1352–59 (1991) (“Hakimi ‘91”)
`Vincenti et al., Interleukin 2-Receptor Blockade with Daclizumab to
`Prevent Acute Rejection in Renal Transplantation, 338(3) NEW ENG.
`J. MED. 161–65 (1998) (“Vincenti ‘98”)
`SEER Stat Fact Sheets: Breast Cancer, National Cancer Institute,
`http://seer.cancer.gov/statfacts/html/breast.html (last accessed
`March 17, 2017)
`Harris et al., Medical Progress: Breast Cancer, 327(5) NEW ENG. J.
`MED. 319–28 (1992) (“Harris ‘92”)
`King et al., Amplification of a Novel v-erbB-Related Gene in a
`Human Mammary Carcinoma, 229(4717) SCIENCE 974–76 (1985)
`(“King ‘85”)
`
`iii
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`Petition for Inter Partes Review of U.S. Patent No. 6,407,213
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`Exhibit No.
`1042
`
`1043
`
`1044
`
`1045
`
`1046
`
`1047
`
`1048
`
`1049
`
`1050
`
`1051
`
`
`
`PETITIONER’S EXHIBIT LIST
`Description
`Semba et al., A v-erbB-Related Protooncogene, c-erbB-2, is Distinct
`from the c-erbB-1 / Epidermal Growth Factor-Receptor Gene and is
`Amplified in a Human Salivary Gland Adenocarcinoma, 82(19)
`PROC. NAT’L ACAD. SCI. USA 6497–01 (1985) (“Semba ‘85”)
`Coussens et al., Tyrosine Kinase Receptor with Extensive Homology
`to EGF Receptor Shares Chromosomal Location with neu
`Oncogene, 230(4730) SCIENCE 1132–39 (1985) (“Coussens ‘85”)
`Fukushige et al., Localization of a Novel v-erbB-Related Gene, c-
`erbB-2, on Human Chromosome 17 and its Amplification in a
`Gastric Cancer Cell Line, 6(3) MOLECULAR CELLULAR BIOLOGY
`955–58 (1986)
`Slamon et al., Human Breast Cancer: Correlation of Relapse and
`Survival with Amplification of the HER-2/neu Oncogene, 235(4785)
`SCIENCE 177–82 (1987) (“Slamon ‘87”)
`Kraus et al., Overexpression of the EGF Receptor-Related Proto-
`Oncogene erbB-2 in Human Mammary Tumor Cell Lines by
`Different Molecular Mechanisms, 6(3) The EMBO J. 605– 10
`(1987)
`Hudziak et al., Increased Expression of the Putative Growth Factor
`Receptor p185HER2 Causes Transformation and Tumorigenesis of
`NIH 3T3 Cells., 84(20) PROC. NAT’L ACAD. SCI. USA 7159–163
`(1987) (“Hudziak ‘87”)
`Shepard et al., Monoclonal Antibody Therapy of Human Cancer:
`Taking the HER2 Protooncogene to the Clinic, 11(3) J. CLINICAL
`IMMUNOLOGY, 117–27 (1991)
`Chothia et al., Conformations of Immunoglobulin Hypervariable
`Regions, 342(21) NATURE 877–83 (1989) (“Chothia ‘89”)
`Queen, International Publication No. WO 1990/07861 (published
`July 26, 1990) (“Queen 1990”)
`Tramontano et al., Framework Residue 71 is a Major Determinant
`of the Position and Conformation of the Second Hypervariable
`Region in the VH Domains of Immunoglobulins, 215(1) J.
`MOLECULAR BIOLOGY 175–82 (1990) (“Tramontano”)
`
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`Petition for Inter Partes Review of U.S. Patent No. 6,407,213
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`Exhibit No.
`1052
`
`1053
`1054
`1055
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`1056
`1057
`1058
`
`1059
`
`1060
`1061
`1062
`
`1063
`
`
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`PETITIONER’S EXHIBIT LIST
`Description
`Kabat et al., SEQUENCES OF PROTEINS OF IMMUNOLOGICAL
`INTEREST: TABULATION AND ANALYSIS OF AMINO ACID AND
`NUCLEIC ACID SEQUENCES OF PRECURSORS, V-REGIONS, C-REGIONS,
`J-CHAIN, T-CELL RECEPTOR FOR ANTIGEN, T-CELL SURFACE
`ANTIGENS, β2-MICROGLUBINS, MAJOR HISTOCOMPATIBILITY
`ANTIGENS, THY-1 COMPLEMENT, C-REACTIVE PROTEIN,
`THYMOPOIETIN, POST-GAMMA GLOBULIN, AND α2-MACROGLOBULIN
`41–175 (4th ed. 1987) (“Kabat 1987”)
`Reserved
`Reserved
`Kabat et al., 1 SEQUENCES OF PROTEINS OF IMMUNOLOGICAL
`INTEREST: TABULATION AND ANALYSIS OF AMINO ACID AND
`NUCLEIC ACID SEQUENCES OF PRECURSORS, V-REGIONS, C-REGIONS,
`J-CHAIN, T-CELL RECEPTOR FOR ANTIGEN, T-CELL SURFACE
`ANTIGENS, β2-MICROGLUBINS, MAJOR HISTOCOMPATIBILITY
`ANTIGENS, THY-1 COMPLEMENT, C-REACTIVE PROTEIN,
`THYMOPOIETIN, POST-GAMMA GLOBULIN, α2-MACROGLOBULINS,
`AND OTHER RELATED PROTEINS 103–338 (5th ed. 1991) (“Kabat
`1991”)
`Reserved
`Reserved
`Davies & Metzger, Structural Basics of Antibody Function, 1 ANN.
`REV. IMMUNOLOGY 87–117 (1983) (“Davies & Metzger”)
`Amit et al., Three-Dimensional Structure of an Antigen-Antibody
`Complex at 2.8 Å Resolution, 233(4765) SCIENCE 747–53 (1986)
`(“Amit ‘86”)
`Reserved
`Reserved
`Chothia & Lesk, Canonical Structures for the Hypervariable
`Regions of Immunoglobulins, 196(4) J. MOLECULAR BIOLOGY 901–
`17 (1987) (“Chothia & Lesk”)
`Chothia et al., Domain Association in Immunoglobulin Molecules:
`The Packing of Variable Domains, 186 J. MOLECULAR BIOLOGY
`651–63 (1985)
`
`v
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`Petition for Inter Partes Review of U.S. Patent No. 6,407,213
`
`Exhibit No.
`1064
`1065
`1066
`1067
`1068
`
`1069
`
`1070
`1071
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`1072
`1073
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`1074
`1075
`1076
`1077
`1078
`1079
`
`1080
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`
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`PETITIONER’S EXHIBIT LIST
`Description
`
`Reserved
`Reserved
`Reserved
`Reserved
`Verhoeyen et al., Reshaping Human Antibodies: Grafting an
`Antilysozyme Activity, 239(4847) SCIENCE 1534–36 (1988)
`(“Verhoeyen ‘88”)
`Riechmann et al., Reshaping Human Antibodies for Therapy,
`332(6162) NATURE 323–27 (1988) (“Riechmann ‘88”)
`Reserved
`Kurrle et al., EP Publication Number 0403156, Improved
`Monoclonal Antibodies Against the Human Alphabeta T-Cell
`Receptor, Their Production and Use (published December 19, 1990)
`(“Kurrle”)
`Reserved
`Winter et al., EP Publication Number 0239400, Recombinant
`Antibodies and Methods for Their Productions (published
`September 30, 1987)
`Reserved
`Reserved
`Reserved
`Reserved
`Reserved
`Kabat et al., SEQUENCES OF PROTEINS OF IMMUNOLOGICAL
`INTEREST: TABULATION AND ANALYSIS OF AMINO ACID AND
`NUCLEIC ACID SEQUENCES OF PRECURSORS, V-REGIONS, C-REGIONS,
`J-CHAIN, β2 MICROGLOBULINS, MAJOR HISTOCOMPATIBILITY
`ANTIGENS, THY-1, COMPLEMENT, C-REACTIVE PROTEIN,
`THYMOPOIETIN, POST-GAMMA GLOBULIN, AND α2-MACROGLOBULIN
`(1983)
`Bernstein et al., The Protein Data Bank: A Computer-based
`Archival File for Macromolecular Structures, 112(3) J. MOLECULAR
`BIOLOGY 535–42 (1977)
`
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`Petition for Inter Partes Review of U.S. Patent No. 6,407,213
`
`Exhibit No.
`1081
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`1082
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`1083
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`1084
`1085
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`1086
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`1087
`
`1088
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`1089
`
`1090
`
`1091
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`
`
`PETITIONER’S EXHIBIT LIST
`Description
`Sheriff et al., Three-Dimensional Structure of an Antibody- Antigen
`Complex, 84(22) PROC. NAT’L ACAD. SCI. USA. 8075–79 (1987)
`(“Sheriff ‘87”)
`Marquart et al., The Three-Dimensional Structure of Antibodies,
`3(6) IMMUNOLOGY TODAY 160–66 (1982)
`Saul et al., Preliminary Refinement and Structural Analysis of the
`Fab Fragment from Human Immunoglobulin New at 2.0 Å
`Resolution*, 253(2) J. BIOLOGICAL CHEMISTRY 585–95 (1978)
`(“Saul ‘78”)
`Reserved
`Satow et al., Phosphocholine Binding Immunogloubulin Fab
`McPC306 An X-ray Diffraction Study at 2•7 Å, 190(4) J.
`MOLECULAR BIOLOGY 593–604 (1986)
`Herron et al., Three-Dimensional Structure of a Fluorescein-Fab
`Complex Crystallized in 2-Methyl-2,4-Pentanediol, 5(4) PROTEINS
`271–80 (1989)
`Padlan et al., Structure of an Antibody-Antigen Complex: Crystal
`Structure of the HyHEL-10 Fab-Lysozyme Complex, 86(15) PROC.
`NAT’L ACAD. SCI. USA 5938–42 (1989) (“Padlan ‘89”)
`Kumar et al., Regulation of Phosphorylation of the c-erbB-2/HER2
`Gene Product by Monoclonal Antibody and Serum Growth
`Factor(s) in Human Mammary Carcinoma Cells, 11(2) MOLECULAR
`CELLULAR BIOLOGY 979–86 (1991)
`Soomro et al., C-erbB-2 Expression in Different Histological Types
`of Invasive Breast Carcinoma, 44(3) J. CLINICAL PATHOLOGY 211–
`14 (1991)
`Wilson & Goulding, A BIOLOGIST‘S GUIDE TO PRINCIPLES AND
`TECHNIQUES OF PRACTICAL BIOCHEMISTRY, §Protein Sequencing,
`170–73 (3d ed. 1986)
`Edelman et al., The Covalent Structure of an Entire γG
`Immunoglobulin Molecule*, 63(1) PROC. NAT’L ACAD. SCI. USA
`78–85 (1969)
`
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`Petition for Inter Partes Review of U.S. Patent No. 6,407,213
`
`Exhibit No.
`1092
`
`1093
`
`1094
`1095 Vols.
`1–15
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`1096
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`1097
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`1098
`1099
`1100
`
`1101
`1102
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`1103
`
`1104
`
`
`
`PETITIONER’S EXHIBIT LIST
`Description
`Capra & Kehoe, Variable Region Sequences of Five Human
`Immunoglobulin Heavy Chains of the VHIII Subgroup: Definitive
`Identification of Four Heavy Chain Hypervariable Regions, 71(3)
`PROC. NAT’L ACAD. SCI. USA 845–48 (1974)
`Morin, From Oncogene to Drug: Development of Small Molecule
`Tyrosine Kinase Inhibitors as Anti-Tumor and Anti-Angiogenic
`Agents, 19(56) ONCOGENE 6574– 83 (2000)
`Reserved
`Patent Interference No. 105,744 (Senior party Application No.
`11/284,261, Inventors John Robert Adair et al., Junior Party, U.S.
`Patent 6,407,213, Inventors Paul J. Carter and Leonard G. Presta)
`(“Adair”)
`U.S. Patent No. 5,677,171, Monoclonal Antibodies Directed to the
`HER2 Receptor (filed August 5, 1994) (issued October 14, 1997)
`Sambrook et al., MOLECULAR CLONING: A LABORATORY MANUAL
`(Cold Spring Harbor Laboratory Press, 2d ed. 1989)
`Reserved
`Reserved
`Colman et al., Three-Dimensional Structure of a Complex of
`Antibody with Influenza Virus Neuraminidase, 326(6111) NATURE
`358–63 (1987) (“Colman ‘87”)
`Reserved
`Bender et al., Immunogenicity, Efficacy and Adverse Events of
`Adalimumab in RA Patients, 27(3) RHEUMATOLOGY INT’L 269–74
`(2007)
`Brient & Nisonoff, Quantitative Investigations of Idiotypic
`Antibodies. IV. Inhibition by Specific Haptens of the Reaction of
`Anti-Hapten Antibody with Its Anti-Idiotypic Antibody, 132 J.
`EXPERIMENTAL MED. 951–61 (1970)
`Koprowski et al., Human Anti-Idiotype Antibodies in Cancer
`Patients: Is the Modulation of the Immune Response Beneficial for
`the Patient?, 81(1) PROC. NAT’L. ACAD. SCI. USA 216–19 (1984)
`(“Koprowski ‘84”)
`
`viii
`
`
`
`Petition for Inter Partes Review of U.S. Patent No. 6,407,213
`
`Exhibit No.
`1105
`
`1106
`
`1107
`
`1108
`1109
`1110
`1111
`1112
`1113
`
`1114
`
`1115
`
`1116
`
`1117
`1118
`1119
`1120
`1121
`
`
`
`PETITIONER’S EXHIBIT LIST
`Description
`Chanh et al., Monoclonal Anti-Idiotypic Antibody Mimics the CD4
`Receptor and Binds Human Immunodeficiency Virus, 84 PROC.
`NAT’L. ACAD. SCI. USA 3891–95 (1987) (“Chanh ‘87”)
`Schroff et al., Human Anti-Murine Immunoglobulin Responses in
`Patients Receiving Monoclonal Antibody Therapy, 45(2) CANCER
`RES. 879–85 (1985) (“Schroff ‘85”)
`Abdou et al., Network Theory in Autoimmunity. In Vitro
`Suppression of Serum Anti-DNA by Anti-idiotypic Antibody in
`Systemic Lupus Erythematosus, 67(5) J. CLINICAL INVESTIGATION
`1297–1304 (1981)
`Reserved
`Reserved
`Reserved
`Reserved
`Reserved
`Epp et al., The Molecular Structure of a Dimer Composed of the
`Variable Portions of the Bence-Jones Protein REI Refined at 2.0-Å
`Resolution, 14(22) BIOCHEMISTRY 4943–52 (1975)
`Mian, Structure, Function and Properties of Antibody Binding Sites,
`217(1) J. MOLECULAR BIOLOGY 133–51 (1991)
`Poljak et al., The Three-Dimensional Structure of the Fab Fragment
`of A Human Myeloma Immunoglobulin at 2.0-Å Resolution, 71(9)
`PROC. NAT’L ACAD. SCI. USA. 3440–44 (1974)
`Padlan et al., Model Building Studies of Antigen-binding Sites: the
`Hapten Binding Site of MOPC-315, 41 COLD SPRING HARBOR SYMP.
`QUANTITATIVE BIOLOGY 627–37 (1977)
`Reserved
`Reserved
`Reserved
`Reserved
`Suh et al., The Galactan-Binding Immunoglobulin Fab J539: An X-
`Ray Diffraction Study at 2.6-Å Resolution, 1(1) PROTEINS 74–80
`(1986) (“Suh ‘86”)
`
`ix
`
`
`
`Petition for Inter Partes Review of U.S. Patent No. 6,407,213
`
`Exhibit No.
`1122
`1123
`1124
`1125
`
`1126
`
`1127
`
`1128
`
`1129
`
`1130
`
`1131
`
`1132
`1133
`1134
`1135
`1136
`1137
`1138
`1139
`
`
`
`PETITIONER’S EXHIBIT LIST
`Description
`
`Reserved
`Reserved
`Reserved
`Furey et al., Structure of A Novel Bence-Jones Protein (Rhe)
`Fragment at 1.6Å Resolution, 167(3) J. MOLECULAR BIOLOGY 661–
`92 (1983) (“Furey”)
`Segal et al., The Three-Dimensional Structure of a
`Phosphorylcholine-Binding Mouse Immunoglobulin Fab and the
`Nature of the Antigen Binding Site, 71(11) PROC. NAT’L ACAD. SCI.
`USA 4298 (1974)
`Jones, Diffraction Methods for Biological Macromolecules.
`Interactive Computer Graphics: FRODO, 115 METHODS
`ENZYMOLOGY 157–71 (1985) (“Jones ‘85”)
`Co et al., Humanized Antibodies for Antiviral Therapy, 88(7) PROC.
`NAT’L ACAD. SCI. USA 2869–73 (1991) (“Co ‘91”)
`Excel Trick, History of Microsoft Excel 1978–2013,
`http://www.exceltrick.com/others/history-of-excel/ (last accessed
`April 13, 2017)
`U.S. Patent No. 4,891,762, Method and Apparatus for Tracking,
`Mapping and Recognition of Spatial Patterns (filed February 9,
`1988) (issued January 2, 1990)
`Wallick et al., Glycosylation of A VH Residue of a Monoclonal
`Antibody Against α(L-6) Dextran Increases its Affinity for Antigen,
`168(3) J. EXPERIMENTAL MED. 1099–109 (1988) (“Wallick ‘88”)
`Reserved
`Reserved
`Reserved
`Reserved
`Reserved
`Reserved
`Reserved
`Reserved
`
`x
`
`
`
`Petition for Inter Partes Review of U.S. Patent No. 6,407,213
`
`Exhibit No.
`1140
`1141
`1142
`1143
`1144
`1145
`1146
`1147
`1148
`1149
`1150
`1151
`1152
`1153
`1154
`1155
`1156
`1157
`1158
`1159
`1160
`1161
`1162
`1163
`1164
`1165
`1166
`1167
`1168
`1169
`
`
`
`PETITIONER’S EXHIBIT LIST
`Description
`
`Reserved
`Library of Congress Copyright Record for Cosimi ‘81
`Library of Congress Copyright Record for OMTSG ‘85
`Library of Congress Copyright Record for Jaffers ‘86
`Library of Congress Copyright Record for Morrison ‘84
`Library of Congress Copyright Record for Liu ‘87
`Library of Congress Copyright Record for Jones ‘86
`Library of Congress Copyright Record for Queen 1989
`Library of Congress Copyright Record for Kirkman ‘89
`Library of Congress Copyright Record for Waldamnn ‘93
`Library of Congress Copyright Record for Hakimi ‘91
`Library of Congress Copyright Record for Vincenti ‘98
`Library of Congress Copyright Record for Harris ‘92
`Library of Congress Copyright Record for King ‘85
`Library of Congress Copyright Record for Semba ‘85
`Library of Congress Copyright Record for Coussens ‘85
`Library of Congress Copyright Record for Slamon ‘87
`Library of Congress Copyright Record for Hudziak ‘87
`Library of Congress Copyright Record for Chothia ‘89
`Library of Congress Copyright Record for Davies & Metzger
`Library of Congress Copyright Record for Amit ‘86
`Reserved
`Reserved
`Library of Congress Copyright Record for Verhoeyen ‘88
`Library of Congress Copyright Record for Riechmann ‘88
`Reserved
`Reserved
`Library of Congress Copyright Record for Sheriff ‘87
`Library of Congress Copyright Record for Saul ‘78
`Reserved
`
`xi
`
`
`
`Petition for Inter Partes Review of U.S. Patent No. 6,407,213
`
`Exhibit No.
`1170
`1171
`1172
`1173
`1174
`1175
`1176
`1177
`1178
`1179
`1180
`1181
`1182
`
`1183
`
`1184
`1184A
`
`1184B
`
`1184C
`
`PETITIONER’S EXHIBIT LIST
`Description
`Library of Congress Copyright Record for Padlan ‘89
`Library of Congress Copyright Record for Colman ‘87
`Library of Congress Copyright Record for Koprowski ‘84
`Library of Congress Copyright Record for Chanh ‘87
`Library of Congress Copyright Record for Schroff ‘85
`Reserved
`Reserved
`Reserved
`Library of Congress Copyright Record for Suh ‘86
`Library of Congress Copyright Record for Jones ‘85
`Library of Congress Copyright Record for Co ‘91
`Library of Congress Copyright Record for Wallick ‘88
`Bodmer, International Publication No. WO 1989/01783 (published
`March 9, 1989)
`Gorman, International Publication No. WO 1992/05274 (published
`April 2, 1992)
`Declaration of Karen Younkins
`Three-Dimensional Structure of an Antibody-Antigen Complex,
`RCSB Protein Data Bank,
`http://www.rcsb.org/pdb/explore/obsolete.do?obsoleteId=2HFL&evt
`c=Suggest&evta=PDBID&evtl=autosearch_SearchBar_querySugge
`st (last accessed April 25, 2017)
`The Three-Dimensional Structure of Antibodies, RCSB Protein Data
`Bank,
`http://www.rcsb.org/pdb/explore/obsolete.do?obsoleteId=1FB4 (last
`accessed April 25, 2017)
`Preliminary Refinement and Structural Analysis of the FAB
`Fragment from Human Immunoglobulin New at 2.0 Angstroms
`Resolution, RCSB Protein Data Bank,
`http://www.rcsb.org/pdb/explore/obsolete.do?obsoleteId=3FAB
`(last accessed April 25, 2017)
`
`
`
`xii
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`Petition for Inter Partes Review of U.S. Patent No. 6,407,213
`
`Exhibit No.
`1184D
`
`1184E
`
`1184F
`
`1184G
`
`1184H
`
`1184I
`
`1185
`
`1186
`1187
`1188
`
`PETITIONER’S EXHIBIT LIST
`Description
`Refined Crystal Structure of the Galactan-Binding Immunoglobulin
`Fab J539 at 1.95-Angstroms Resolution, RCSB Protein Data Bank,
`http://www.rcsb.org/pdb/explore/explore.do?structureId=2FBJ (last
`accessed May 4, 2017)
`Phosphocholine Binding Immunoglobulin Fab McPC603. An X-ray
`Diffraction Study at 2.7 A, RCSB Protein Data Bank,
`http://www.rcsb.org/pdb/explore/explore.do?structureId=1MCP
`(last accessed May 4, 2017)
`Three-dimensional Structure of a Fluorescein-Fab Complex
`Crystallized in 2-methyl-2,4-pentanediol, RCSB Protein Data Bank,
`http://www.rcsb.org/pdb/explore/explore.do?structureId=4FAB (last
`accessed May 4, 2017)
`Structure of an Antibody-Antigen Complex: Crystal Structure of the
`HyHEL-10 Fab-lysozyme Complex, RCSB Protein Data Bank,
`http://www.rcsb.org/pdb/explore/explore.do?structureId=3HFM
`(last accessed May 4, 2017)
`The Molecular Structure of a Dimer Composed of the Variable
`Portions of the Bence-Jones Protein REI Refined at 2.0-A
`Resolution, RCSB Protein Data Bank,
`http://www.rcsb.org/pdb/explore/explore.do?structureId=1REI (last
`accessed May 4, 2017)
`Structure of a Novel Bence-Jones Protein (Rhe) Fragment at 1.6 A
`Resolution, RCSB Protein Data Bank,
`http://www.rcsb.org/pdb/explore/explore.do?structureId=2RHE (last
`accessed May 4, 2017)
`Miller, To Build a Better Mousetrap, Use Human Parts, 90(1) J.
`NAT’L CANCER INST. 1416 (1998) (“Miller ‘98”)
`Library of Congress Copyright Record for Miller ‘98
`Declaration of Amanda Hollis
`Declaration of Christopher Lowden
`
`
`
`xiii
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`
`
`Petition for Inter Partes Review of U.S. Patent No. 6,407,213
`
`I.
`
`INTRODUCTION
`
`Pursuant to 35 U.S.C. § 311 and 37 C.F.R. § 42.100, Petitioner Pfizer, Inc.
`
`petitions for Inter Partes Review (“IPR”) of claims 1, 2, 4, 12, 25, 29–31, 33, 42,
`
`60, 62–67, 69 and 71–81 (“Challenged Claims”) of U.S. Patent No. 6,407,213
`
`(“’213 patent,” Ex. 1001). With this Petition is a Power of Attorney pursuant to 37
`
`C.F.R. § 42.10(b); and pursuant to 37 C.F.R. § 42.103, the fee set forth in
`
`§ 42.15(a).
`
`By a preponderance of the evidence, this Petition proves the prior art renders
`
`the Challenged Claims unpatentable. Prior art disclosing methods of making
`
`humanized antibodies—including the detailed roadmaps taught in Kurrle1 and
`
`Queen 19902—anticipate and render obvious the Challenged Claims to a person of
`
`
`1 Kurrle et al., EP Publication Number 0403156, Improved monoclonal
`
`antibodies against the human alphabeta T-Cell receptor, their production and
`
`use (published December 19, 1990) (“Kurrle”) (Ex. 1071).
`
`2 Queen, International Publication No. WO 1990/07861 (published July 26,
`
`1990) (“Queen 1990”) (Ex. 1050).
`
`
`
`1
`
`
`
`Petition for Inter Partes Review of U.S. Patent No. 6,407,213
`
`ordinary skill in the art (“POSITA”) as of the priority date of the ’213 patent.3
`
`II. MANDATORY NOTICES – 37 C.F.R. § 42.8(A)(1) AND (B)
`A.
`37 C.F.R. § 42.8(b)(1): Real Party-In-Interest
`Pfizer, Inc. (“Pfizer” or “Petitioner”) is the real party-in-interest for
`
`Petitioner.
`
`37 C.F.R. § 42.8(b)(2): Related Matters
`
`B.
`Petitioner concurrently files two IPR petitions for claims of the ’213 patent.
`
`Petitioner is aware of two earlier IPR proceedings for the ’213 patent, both filed by
`
`third-party Mylan Pharmaceuticals Inc.: IPR2016–01693 and IPR2016–01694.
`
`These proceedings were terminated by the Board on March 10, 2017 after the
`
`parties filed a Joint Motion to Terminate. Paper No. 24, IPR2016–01693; Paper
`
`No. 23, IPR2016–01694 (March 10, 2017). Petitioner is also aware of two current
`
`IPR proceedings for the ’213 patent, both filed by third-party Celltrion, Inc.:
`
`IPR2017-01373 and IPR2017-01374. Petitioner is not aware of any other judicial
`
`or administrative matters that would affect,