UNITED STATES PATENT AND TRADEMARK OFFICE
`
`_____________________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`
`_____________________
`
`APOTEX INC.,
`Petitioner,
`
`v.
`
`PFIZER INC.,
`Patent Owner.
`
`_____________________
`
`Inter Partes Review No.: IPR2021-01132
`_____________________
`
`U.S. Patent No. 6,890,927 to Bogle et al.
`Issued: May 10, 2005
`
`Title: TARTRATE SALTS OF 5,8, 14-TRIAZATERACYCLO[10.3.1.02,11
`04.9]-HEXADECA-2(11),3,5,7,9-PENTAENE AND
`PHARMACEUTICAL COMPOSITIONS THEREOF
`_____________________
`
`PETITION FOR INTER PARTES REVIEW OF U.S. PATENT NO. 6,890,927
`UNDER 35 U.S.C. §§ 311–319 AND 37 C.F.R. §§ 42.1–.80, 21.100–.123
`
`
`
`Mail Stop “PATENT BOARD”
`Patent Trial and Appeal Board
`U.S. Patent and Trademark Office
`P.O. Box 1450
`Alexandria, VA 22313-1450
`
`

`

`TABLE OF CONTENTS
`
`
`
`TABLE OF AUTHORITIES ..................................................................................... v
`LIST OF EXHIBITS AND ABBREVIATIONS ...................................................... ix
`I.
`INTRODUCTION ........................................................................................... 1
`II.
`OVERVIEW .................................................................................................... 1
`III. MANDATORY NOTICES (37 C.F.R. § 42.8) ............................................... 3
`REAL PARTIES-IN-INTEREST (37 C.F.R. § 42.8(B)(1)) ............................ 4
`RELATED MATTERS (37 C.F.R. § 42.8(B)(2)) ......................................... 4
`LEAD AND BACK-UP COUNSEL AND SERVICE INFORMATION (37
`C.F.R. § 42.8(B)(3), (4)) ......................................................................... 4
`IV. FEE PAYMENT UNDER 37 C.F.R. § 42.15(a) AND § 42.103 .................... 5
`V.
`STANDING GROUNDS (37 C.F.R. § 42.104(a)) .......................................... 6
`VI. THRESHOLD REQUIREMENT FOR INTER PARTES REVIEW ............... 6
`VII. CHALLENGE OVERVIEW AND PRECISE RELIEF REQUESTED ......... 6
`CLAIMS FOR WHICH REVIEW IS REQUESTED .......................................... 6
`STATUTORY GROUNDS OF CHALLENGE (37 C.F.R. § 42.104(B)) ........... 7
`VIII. OVERVIEW OF THE ‘927 PATENT, PROSECUTION HISTORY ............ 8
`THE ‘927 PATENT ................................................................................... 8
`PROSECUTION HISTORY .......................................................................... 9
`IX. CLAIM CONSTRUCTION .......................................................................... 13
`5,8,14-TRIAZATETRACYCLO[10.3.1.02,11.04,9]-HEXADECA-
`2(11),3,5,7,9-PENTAENE ....................................................................... 14
`“THE TARTRATE SALT OF” VARENICLINE ............................................ 14
`1.
`Tartrate Salt—Generally ........................................................... 14
`
`
`
`
`
`ii
`
`
`
`
`
`
`
`
`
`
`
`
`
`

`

`
`
`
`
`
`
`
`
`
`
`
`
`2.
`Tartrate salt—the Intrinsic Record............................................ 15
`PERSON OF ORDINARY SKILL IN THE ART ........................................ 18
`X.
`XI. THE SCOPE AND CONTENT OF THE PRIOR ART ................................ 18
`PETITIONER’S PRIOR ART TO VARENICLINE: US ‘550 (EX1006)
`AND COE (EX1005) .............................................................................. 19
`SALT SELECTION AS PART OF PHARMACEUTICAL DEVELOPMENT
`WAS WELL KNOWN ............................................................................. 24
`1.
`Berge (EX1009) ........................................................................ 25
`2.
`Gould (EX1010) ........................................................................ 26
`FURTHER TARTRATE SALT EXPECTATIONS .......................................... 28
`XII. GROUNDS FOR UNPATENTABILITY—DETAILED ANALYSIS ........ 31
`LEGAL STANDARDS .............................................................................. 31
`ANTICIPATION ...................................................................................... 33
`1.
`Ground 1: US ‘550 Alone Invalidates the Challenged
`Claims for Anticipation ............................................................. 37
`Ground 2: Coe Alone Invalidates the Challenged Claims
`for Anticipation ......................................................................... 39
`OBVIOUSNESS ....................................................................................... 41
`1.
`Ground 3: The Challenged Claims Are Obvious Over
`Coe in View of Berge ............................................................... 41
`Ground 4: The Challenged Claims Are Obvious Over
`Coe in View of Gould ............................................................... 51
`Ground 5: The Challenged Claims Are Obvious Over
`Coe in View of Gould or Berge in Further View of
`Tartrate Salt Disclosures (Exemplified by Nyqvist) ................. 56
`There Is a Clear Motivation to Combine Coe With Berge
`and/or Gould and Further With the Tartrate Salt
`
`4.
`
`2.
`
`2.
`
`3.
`
`iii
`
`

`

`5.
`
`Disclosures as in Nyqvist .......................................................... 64
`There Was a Reasonable Expectation of Success
`Combining a Known Compound with a Common Salt ............ 67
`Lack of Secondary Considerations ........................................... 68
`6.
`XIII. THE BOARD SHOULD INSTITUTE TRIAL BASED ON
`APOTEX’S PETITION (35 U.S.C. § 325(D)) .............................................. 69
`XIV. CONCLUSION .............................................................................................. 71
`
`
`
`iv
`
`

`

`TABLE OF AUTHORITIES
`Cases
`
`10X Genomics, Inc. v. Bio-Rad Lab’ys., Inc.,
`IPR2021-00133, Paper 11 at 15 (P.T.A.B. May 14, 2021) ..................................70
`Abbott Lab’ys. v. Sandoz, Inc.,
`566 F.3d 1282 (Fed. Cir. 2009) ..................................................................... 13, 16
`Amneal Pharm., LLC v. Supernus Pharm., Inc.,
`IPR2013-00368, Paper 8 at 12 (P.T.A.B. Dec. 17, 2013) ....................................69
`Ariosa Diagnostics v. Verinata Health, Inc.,
`805 F.3d 1359 (Fed. Cir. 2015) ............................................................................18
`Becton, Dickinson and Co. v. B. Braun Melsungen AG,
`IPR2017-01586, Paper 8 at 17 (P.T.A.B. Dec. 15, 2017) .....................................69
`Bristol-Myers Squibb Co. v. Ben Venue Lab’ys, Inc.,
`246 F.3d 1368 (Fed. Cir. 2001) ............................................................................32
`Custom Accessories, Inc. v. Jeffrey-Allan Indus., Inc.,
`807 F.2d 955 (Fed. Cir. 1986) ..............................................................................18
`Eli Lilly & Co. v. Trs. of the Univ. of Pa.,
`IPR2016-00458, Paper 7 at 21 (P.T.A.B. July 14, 2016) .....................................49
`Fantasia Trading LLC v. CogniPower, LLC,
`IPR2021-00067, Paper 21 at 38 (P.T.A.B. May 12, 2021) ...................................71
`Galderma Lab’ys, L.P. v. Tolmar, Inc.,
`737 F.3d 731 (Fed. Cir. 2013) ..............................................................................47
`Hamilton Techs. LLC v. Fleur Tehrani,
`IPR2020-01199, Paper 6 at 21 (P.T.A.B. Jan. 6, 2021) ........................................71
`Hoffmann-La Roche Inc. v. Apotex Inc.,
`748 F.3d 1326 (Fed. Cir. 2014) ............................................................................68
`In re Cruciferous Sprout Litig.,
`301 F.3d 1343 (Fed. Cir. 2002) ............................................................................31
`
`v
`
`

`

`In re Kao,
`639 F.3d 1057 (Fed. Cir. 2011) ............................................................................33
`In re Omeprazole Patent Litig.,
`483 F.3d 1364 (Fed. Cir. 2007) ............................................................................32
`In re Packard,
`751 F.3d 1307 (Fed. Cir. 2014) ............................................................................15
`In re Petering,
`301 F.2d 676 (C.C.P.A. 1962) ..............................................................................35
`In re Preda,
`401 F.2d 825 (C.C.P.A. 1968) ..............................................................................31
`King Pharm., Inc. v. Eon Labs., Inc.,
`616 F.3d 1267 (Fed. Cir. 2010) ............................................................................32
`KSR Int’l Co. v. Teleflex Inc.,
`550 U.S. 398 (2007) ..................................................................................... passim
`Mintz v. Dietz & Watson, Inc.,
`679 F.3d 1372 (Fed. Cir. 2012) ............................................................................33
`Motorola Mobility LLC v. Arnouse,
`IPR2013-00010 (MT), Paper 20 at 6 (P.T.A.B. Jan. 30, 2013) ............................. 6
`Mylan Pharm., Inc. v. Allergan, Inc.,
`IPR2016-01129, Paper 8 at 21 (P.T.A.B. Dec. 8, 2016) ......................................49
`Mylan Pharmaceuticals Inc. v. Merck Sharp & Dohme Corp.,
`IPR2020-00040, Paper 91 (P.T.A.B. May 7, 2021) ...................................... 42, 43
`Newell Cos., Inc. v. Kenney Mfg. Co.,
`864 F.2d 757 (Fed. Cir. 1988) ..............................................................................68
`Novo Nordisk A/S v. Caraco Pharm. Lab’ys, Ltd.,
`719 F.3d 1346 (Fed. Cir. 2013) ............................................................................47
`On Demand Mach. Corp. v. Ingram Indus.,
`442 F.3d 1331 (Fed. Cir. 2006) ............................................................................16
`
`vi
`
`

`

`Ormco Corp. v. Align Tech., Inc.,
`463 F.3d 1299 (Fed. Cir. 2006) ............................................................................33
`Perricone v. Medicis Pharm. Corp.,
`432 F.3d 1368 (Fed. Cir. 2005) ............................................................................35
`Pfizer Inc. v. Apotex Inc.,
`Case No. 10-cv-06464 (S.D.N.Y.) ......................................................................... 6
`Pfizer, Inc. v. Apotex, Inc.,
`480 F.3d 1348 (Fed. Cir. 2007) .................................................................... passim
`PharmaStem Therapeutics, Inc. v. ViaCell, Inc.,
`491 F.3d 1342 (Fed. Cir. 2007) ................................................................. 2, 21, 23
`Phillips v. AWH Corp.,
`415 F.3d 1303 (Fed. Cir. 2005) ..................................................................... 13, 16
`Randall Mfg. v. Rea,
`733 F.3d 1355 (Fed. Cir. 2013) ............................................................................18
`Rasmusson v. SmithKline Beecham Corp.,
`413 F.3d 1318 (Fed. Cir. 2005) ............................................................................32
`Spansion, Inc. v. Int’l Trade Comm’n,
`629.F.3d 1331 (Fed. Cir. 2010) ............................................................................41
`Umicore AG & Co. KG v. Basf Corp.,
`IPR2015-01124, Paper 8 at 22 (P.T.A.B. Nov. 2, 2015) .....................................49
`Valeant Pharm. Int’l, Inc. v. Mylan Pharm. Inc.,
`955 F.3d 25 (Fed. Cir. 2020) ................................................................................67
`Wyers v. Master Lock Co.,
`616 F.3d 1231 (Fed. Cir. 2010) ..................................................................... 50, 69
`
`Statutes
`
`35 U.S.C. § 102(b) ...............................................................................................9, 20
`35 U.S.C. § 102(e) ...............................................................................................9, 19
`
`vii
`
`

`

`35 U.S.C. § 103(a) ...................................................................................................32
`35 U.S.C. § 314(a) ..................................................................................................... 6
`35 U.S.C. § 325(d) ...................................................................................................69
`35 U.S.C. §§ 311–19 .................................................................................................. 1
`37 C.F.R. §§ 42 et seq. ............................................................................................... 1
`
`Other Authorities
`
`MPEP § 2173.05(e) (7th ed. Feb. 2000) ..................................................................15
`MPEP § 2173.05(e) (9th ed. Jan. 2018) ...................................................................15
`Trial Practice Guide,
`77 Fed. Reg. 48,759-60 .......................................................................................... 4
`
`Regulations
`
`37 C.F.R. § 42.10(b) .................................................................................................. 4
`37 C.F.R. § 42.100(b) ..............................................................................................13
`37 C.F.R. § 42.6(c) ..................................................................................................... 7
`37 C.F.R. § 42.8(a)(1) ................................................................................................ 3
`37 C.F.R. § 42.8(b) .................................................................................................... 3
`37 C.F.R. § 42.8(b)(1) ................................................................................................ 4
`37 C.F.R. § 42.8(b)(2) ................................................................................................ 4
`37 C.F.R. § 42.8(b)(3) ................................................................................................ 4
`37 C.F.R. § 42.8(b)(4) ................................................................................................ 4
`
`
`
`viii
`
`

`

`LIST OF EXHIBITS AND ABBREVIATIONS
`
`Exhibit Abbreviation
`1001
`‘927 patent
`
`Description
`U.S. Patent No. 6,890,927 B2
`
`1002
`
`Gould Decl.
`
`Expert Declaration of Dr. Philip Gould in Support of
`Petition for Inter Partes Review of U.S. Patent
`No. 6,890,927
`
`1003
`
`Gould CV
`
`Dr. Philip Gould Curriculum Vitae
`
`1004
`
`‘927 patent PH
`
`File History for U.S. Patent Application No.
`10/139,730, issued as the ‘927 patent
`
`1005
`
`Coe
`
`International Patent Application No.
`WO 1999/035131, to Coe et al.
`
`1006
`
`US ‘550
`
`U.S. Patent No. 6,410,550
`
`1007
`
`US ‘550 PH
`
`File History for U.S. Patent Application No.
`09/402,010, issued as US ‘550
`
`1008
`
`CA ‘490
`
`Canadian Patent Application No. 2,467,490
`
`1009
`
`Berge
`
`1010
`
`Gould
`
`1011 Wells
`
`1012
`
`Bighley
`
`Stephen M. Berge et al., Pharmaceutical Salts, 66 J.
`PHARM. SCIS. 1 (1977)
`
`Philip L. Gould, Salt Selection for Basic Drugs, 33
`INT’L J. PHARM. 201 (1986)
`
`JAMES I. WELLS, PHARMACEUTICAL
`PREFORMULATION: THE PHYSICOCHEMICAL
`PROPERTIES OF DRUG SUBSTANCES 21 (1988)
`
`Lyle D. Bighley et al., Salt Forms of Drugs and
`Absorption, in 13 ENCYCLOPEDIA OF
`PHARMACEUTICAL TECHNOLOGY 453 (James
`Swarbrick & James C. Boylan eds., 1996)
`
`ix
`
`

`

`1013
`
`Paulekuhn
`
`1014 Morris
`
`1015
`
`Bastin
`
`1016
`
`Nyqvist
`
`1017
`
`Jessen
`
`1018
`1019
`1020
`1021
`
`US ‘495
`
`US ‘376
`
`US ‘198
`
`US ‘388
`
`1022
`
`Stahl
`
`1023
`
`Pharmeuropa 2000
`
`G. Steffen Paulekuhn et al., Trends in Active
`Pharmaceutical Ingredient Salt Selection Based on
`Analysis of the Orange Book Database, 50 J.
`MEDICINAL CHEMISTRY 6665 (2007)
`
`Kenneth R. Morris et al., An Integrated Approach to
`the Selection of Optimal Salt Form for a New Drug
`Candidate, 105 INT’L J. PHARM. 209 (1994)
`
`Richard J. Bastin et al., Salt Selection and
`Optimisation Procedures for Pharmaceutical New
`Chemical Entities, 4 ORGANIC PROCESS RSCH. &
`DEV. 427 (2000)
`
`International Patent Application No.
`WO 1998/054166, to Nyqvist et al.
`
`International Patent Application No.
`WO 2000/055131, to Jessen et al.
`
`U.S. Patent No. 5,834,495
`
`U.S. Patent No. 5,073,376
`
`U.S. Patent No. 2,870,198
`
`U.S. Patent No. 6,794,388
`
`HANDBOOK OF PHARMACEUTICAL SALTS 329 (P.
`Heinrich Stahl & Camille G. Wermuth eds., 1st ed.
`2002)
`
`European Directorate for the Quality of Medicines
`and Healthcare, Enquiry: Alkyl Mesilate
`(Methanesulphonate) Impurities in Mesilate Salts, 12
`PHARMEUROPA 27 (2000)
`
`x
`
`

`

`1024
`
`Aakeroy
`
`Christer B. Aakeroy & Peter B. Hitchcock;
`Hydrogen-bonded Layers of Hydrogentartrate
`Anions: Two-dimensional Building Blocks for Crystal
`Engineering, 3 J. MATERIAL CHEMISTRY 1129
`(1993).
`
`
`
`xi
`
`

`

`I.
`
`INTRODUCTION
`Apotex Inc. (“Apotex”/“Petitioner”) petitions for Inter Partes Review (“IPR”)
`
`under 35 U.S.C. §§ 311–19 and 37 C.F.R. §§ 42 et seq., seeking cancellation of
`
`claims 1-2 (the “Challenged Claims”) of U.S. Patent No. 6,890,927 to Bogle et al.
`
`(“the ‘927 patent”) (EX1001), owned by Pfizer Inc. (“Patentee”/“Pfizer”).
`
`II. OVERVIEW
`The Challenged Claims involve an admitted prior art compound, 5,8,14-
`
`triazatetracyclo[10.3.1.02,11.04,9]-hexadeca-2(11),3,5,7,9-pentaene—colloquially,
`
`“varenicline.” Facially, the ‘927 patent claims involve varenicline tartrate salts;
`
`crystals; and particular solid-state crystalline forms. The Challenged Claims
`
`purportedly involve tartrate (including L-tartrate) salts. During prosecution, Pfizer
`
`argued the claims involved particular crystalline varenicline tartrate polymorphs.
`
`(See Sect. VIII.B).
`
`Petitioner files this Petition, supported by an expert declaration from Dr.
`
`Philip Gould (EX1002), to apprise the Board of invalidating prior art—known to the
`
`Patentee, but not before the examiner—when issuing the ‘927 patent.
`
`The ‘927 patent concedes that varenicline “and its hydrochloride salt” were
`
`“referred to in WO 99/35131 [Coe],” and that Coe (EX1005) “generically recite[s]
`
`pharmaceutically acceptable acid addition salts for the compounds referred to
`
`therein.” (EX1001, 2:13-22). See PharmaStem Therapeutics, Inc. v. ViaCell, Inc.,
`
`

`

`491 F.3d 1342, 1362 (Fed. Cir. 2007) (specification statements regarding prior art
`
`bind patentees). Though the examiner rejected the claims over Coe, Pfizer argued
`
`the “specific tartrate salt of [varenicline]” was insufficiently taught. (See Sect.
`
`VIII.B).
`
`Anticipation. The examiner lacked U.S. Patent No. 6,410,550 (“US ‘550”)
`
`(EX1006), a U.S. national stage entry to Coe (EX1005). Before the May 2001
`
`priority date, US ‘550 claimed varenicline as a species, plus pharmaceutically
`
`acceptable salts. (EX1007.417, 01/03/2001 Response and Amendment). US ‘550
`
`(like Coe) taught tartaric acid as one of only 14 “pharmaceutically acceptable acid
`
`addition salts.” (EX1006, 8:44-49; EX1005, 10:12-16). During prosecution of US
`
`‘550, Pfizer insisted this disclosure, plus US ‘550/Coe’s Example 26 preparing
`
`varenicline, justified written description support. (EX1007.417-418, 01/03/2001
`
`Response and Amendment).
`
`The examiner lacked Pfizer’s separate patent admissions that practicing
`
`Example 26 of Coe/US ‘550 with tartaric acid yields crystalline varenicline tartrate.
`
`(See Sect. XI.A; EX1008.004, 012, 021).
`
`Either admission confirms Coe and/or US ‘550 anticipate the Challenged
`
`Claims.
`
`Obviousness. It was obvious for ordinarily-skilled chemists to reach
`
`varenicline tartrate from Coe alone. But the examiner lacked art describing drug salt
`
`2
`
`

`

`selections—Berge (EX1009) and Gould (EX1010)—showing
`
`tartrate salts
`
`(including stereoisomers) were known; and taught the routine salt-selection
`
`rationales, including reduced hygroscopicity and improved stability. Coe plus Berge
`
`and/or Gould independently ground obviousness findings. (See Sect. XII.C.1-2).
`
`Pfizer told the examiner that two varenicline tartrate crystals showed
`
`unexpected results. The ‘927 patent states previously-prepared varenicline salts
`
`(hydrochloride) were “significantly hygroscopic,” while tartrate salts exerted more
`
`“favorable characteristics.” (EX1001, 9:19-32). Prior art the examiner lacked,
`
`including Gould, taught the hygroscopic hydrochloride salt problem; Nyqvist and
`
`others used tartrate salts to successfully solve it. (EX1016.003-004, Nyqvist;
`
`EX1002, Gould Decl. ¶¶ 131-148 (collecting multiple similar citations)). Coe plus
`
`Berge/Gould, plus Nyqvist, is an independent obviousness ground. (See Sect.
`
`XII.C.3).
`
`Petitioner respectfully submits that the person of ordinary skill in the art
`
`(“POSA”) possessed varenicline tartrate salts as known and obvious given the prior
`
`art.
`
`III. MANDATORY NOTICES (37 C.F.R. § 42.8)
`Under 37 C.F.R. §§ 42.8(a)(1) and 42.8(b), Apotex provides its mandatory
`
`Petition notices.
`
`3
`
`

`

` REAL PARTIES-IN-INTEREST (37 C.F.R. § 42.8(B)(1))
`Petitioner Apotex Inc., Apotex Corp., Apotex Holdings Inc., and Apotex
`
`Pharmaceuticals Holdings Inc. are the real parties-in-interest (“RPI”) here. No other
`
`parties exercised or could have exercised control over this petition; or funded or
`
`directed this petition. See Trial Practice Guide, 77 Fed. Reg. 48,759-60.
`
` RELATED MATTERS (37 C.F.R. § 42.8(B)(2))
`To the best of Petitioner’s knowledge, no other judicial or administrative
`
`matters would affect, or be affected by, a decision in this proceeding.
`
`The Public Patent Application Retrieval (PAIR) website reports U.S. Patent
`
`Application No. 11/069,724 issued as U.S. Patent No. 7,265,119 on September 4,
`
`2007, as a continuation of the ‘927 patent. There are no related United States
`
`pending patent applications.
`
` LEAD AND BACK-UP COUNSEL AND SERVICE INFORMATION (37
`C.F.R. § 42.8(B)(3), (4))
`Petitioner identifies its lead and backup counsel below. A Power of Attorney
`
`is filed concurrently herewith under 37 C.F.R. § 42.10(b).
`
`4
`
`

`

`Lead
`
`Back-Up
`
`Deanne M. Mazzochi (Reg. No. 50,158)
`dmazzochi@rmmslegal.com)
`
`Postal and Hand Delivery Address
`Rakoczy Molino Mazzochi Siwik LLP
`6 West Hubbard Street, Suite 500
`Chicago, IL 60654
`Telephone: (312) 222-6305
`Facsimile: (312) 222-6325
`
`Petitioner consents to email service at:
`APO_VAR_IPR@rmmslegal.com
`
`William A. Rakoczy
`(pro hac vice to be filed)
`wrakoczy@rmmslegal.com
`
`Paul J. Molino (Reg. No. 45,350)
`paul@rmmslegal.com
`
`Jeffrey A. Marx (Reg. No. 56,977)
`jmarx@rmmslegal.com
`
`Postal and Hand Delivery Address
`Rakoczy Molino Mazzochi Siwik LLP
`6 West Hubbard Street, Suite 500
`Chicago, IL 60654
`Telephone: (312) 222-5127
`Facsimile: (312) 843-6260
`
`
`
`
`Please direct all correspondence to lead and back-up counsel at the contact
`
`information
`
`above.
`
` Petitioner
`
`consents
`
`to
`
`service by
`
`email
`
`at:
`
`dmazzochi@rmmslegal.com, wrakoczy@rmmslegal.com, paul@rmmslegal.com,
`
`and jmarx@rmmslegal.com. Petitioner will file a pro hac vice admission motion for
`
`William A. Rakoczy upon authorization.
`
`IV. FEE PAYMENT UNDER 37 C.F.R. § 42.15(a) AND § 42.103
`The required fees are submitted herewith. The undersigned representative of
`
`Petitioner hereby authorizes the Patent Office to charge any additional fees or credit
`
`any overpayment to Deposit Account 503626.
`
`5
`
`

`

`V.
`
`STANDING GROUNDS (37 C.F.R. § 42.104(a))
`Petitioner certifies that the ‘927 patent is available for IPR and that Petitioner
`
`is not barred or estopped from requesting an IPR challenging any claim of the ‘927
`
`patent on the grounds identified in this Petition. See Motorola Mobility LLC v.
`
`Arnouse, IPR2013-00010 (MT), Paper 20 at 6 (P.T.A.B. Jan. 30, 2013). Petitioner
`
`and the RPIs have not filed a civil action challenging the validity of the ‘927 patent.
`
`Nor was Petitioner or any other RPI served with a complaint alleging ‘927 patent
`
`infringement more than one year before filing this Petition. On August 30, 2010,
`
`Pfizer sued Apotex alleging ‘927 patent infringement; but never served its
`
`complaint; Pfizer voluntarily dismissed suit on December 21, 2010. See Pfizer Inc.
`
`v. Apotex Inc., Case No. 10-cv-06464 (S.D.N.Y.).
`
`VI. THRESHOLD REQUIREMENT FOR INTER PARTES REVIEW
`IPR petitions must demonstrate “a reasonable likelihood that the petitioner
`
`would prevail with respect to at least [one] of the claims challenged in the petition.”
`
`35 U.S.C. § 314(a). This Petition satisfies the standard. As explained below, for
`
`each ground, there is a reasonable likelihood that Petitioner will prevail with respect
`
`to at least one of the Challenged Claims.
`
`VII. CHALLENGE OVERVIEW AND PRECISE RELIEF REQUESTED
` CLAIMS FOR WHICH REVIEW IS REQUESTED
`Petitioner requests IPR of claims 1-2 of the ‘927 patent, and cancellation of
`
`these claims as unpatentable.
`
`6
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`

`

`STATUTORY GROUNDS OF CHALLENGE (37 C.F.R. § 42.104(B))
`
`Petitioner respectfully requests IPR of claims 1-2 of the ‘927 patent on each
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`specific ground of unpatentability outlined below. Per 37 C.F.R. § 42.6(c), copies
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`of the references are filed herewith. In support of the proposed grounds, this Petition
`
`includes the declaration of a technical expert, Dr. Philip Gould (EX1002), explaining
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`what the art would have conveyed to a POSA. Dr. Gould is an expert in the relevant
`
`field. (EX1003).
`
`Ground
`1
`2
`3
`4
`
`5
`
`35 U.S.C.
`§102
`
`§102
`
`§103
`
`§103
`
`§103
`
`Reference(s)
`US ‘550
`Coe
`
`Coe + Berge
`
`Coe + Gould
`
`Coe + Berge or Gould, +
`Nyqvist
`
`‘927 patent Claims
`1-2
`
`1-2
`
`1-2
`
`1-2
`
`1-2
`
`Each of the above prior art references and/or combinations renders the
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`Challenged Claims invalid. The above-mentioned and other prior art references
`
`cited herein and by Dr. Gould provide further background on the art, motivation to
`
`combine the references, and/or show reasonable expectations of success in
`
`combining the references’ teachings to arrive at the claimed invention. Petitioner’s
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`full statement of the reasons for the relief requested is set forth in detail in Section
`
`XII and in the supporting Gould Declaration.
`
`7
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`

`

`VIII. OVERVIEW OF THE ‘927 PATENT, PROSECUTION HISTORY
` THE ‘927 PATENT
`The ‘927 patent issued on May 10, 2005, from U.S. Patent Application No.
`
`10/139,730, filed May 6, 2002 (“the ‘730 application”), claiming benefit to U.S.
`
`Provisional Patent Application No. 60/290,861, filed May 14, 2001.1
`
`The ‘927 patent’s specification primarily involves crystalline polymorphs of
`
`varenicline tartrate salts. (EX1001, Abstract). The Detailed Description Section
`
`devotes pages to solid-state forms (e.g., Forms A, B, C, X and Y) of varenicline
`
`tartrate, as do the Figures. (Ex. 1001, 2:32-3:35). Each Example (1-4) involves
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`crystalline tartrate salts. (EX1002, ¶ 98).
`
`The ‘927 specification asserts varenicline “binds to neuronal nicotinic
`
`acetylcholine specific receptor sites and is useful in modulating cholinergic
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`function,” (EX1001, 1:29-32), rendering it “useful in the treatment of [a number of
`
`diseases], particularly, nicotine dependency, addiction and withdrawal; including
`
`use in smoking cessation therapy.” (Id., 1:32-60).
`
`The ‘927 patent admits that the prior art knowledge included varenicline and
`
`its hydrochloride salts; and that varenicline binds to neuronal nicotinic receptor sites:
`
`
`
`1 Solely for this IPR, Petitioner assumes a May 14, 2001 priority date.
`
`8
`
`

`

`
`
`(Id., 2:13-22). The referenced WO 99/35131 (“Coe,” EX1005) is prior art under 35
`
`U.S.C. § 102(b) (2001). As discussed in Section XI.A, during US ‘550’s
`
`prosecution, Pfizer admitted the US ‘550 specification (identical in all relevant
`
`material respects to Coe) contained written description support for the varenicline
`
`species and its salts, a critical admission for purposes of pre-AIA 35 U.S.C. § 102(e),
`
`as later discussed. (See EX1007.417-418, 01/03/2001 Response and Amendment
`
`(Claim 8 (as new claim 21) to varenicline species and its salts “add[ed] no new
`
`matter” and was “supported” by Example 26)).
`
`PROSECUTION HISTORY
`
`Originally-filed claims 1-2 match Challenged Claims 1-2. (See EX1004.044-
`
`050, 05/06/2002 Claims). Originally-filed independent claim 1 of the ‘730
`
`application stated:
`
`
`
`9
`
`

`

`(EX1004.044; EX1002, ¶ 83).
`
`In the February 5, 2003, office action, the Examiner rejected claims 1-2 as
`
`anticipated and obvious. (EX1004.197-203, 02/05/2003 Non-Final Action;
`
`EX1002, ¶ 85). In response, Pfizer cancelled claims 1-2:
`
`
`
`(EX1004.209, 07/07/2003 Amendment; EX1002, ¶ 86). Pfizer also deleted
`
`reference to those claims in its pharmaceutical composition, method of use, and
`
`method of treatment claims. (EX1004.213, 07/07/2003 Amendment). Pfizer
`
`represented that the remaining claims were not anticipated or obvious because the
`
`prior art did not teach the particular crystalline polymorphs: “the specific anhydrous
`
`tartrate salt having the x-ray diffraction features” listed in the claims, or “a hydrate
`
`tartrate” with salt isomers. (EX1004.216, 07/07/2003 Remarks; EX1002, ¶ 87).
`
`Pfizer insisted the prior art lacked a “suggestion” to prepare either the “anhydrous”
`
`or “hydrate” crystalline forms. (EX1004.216, 07/07/2003 Remarks; EX1002, ¶ 87).
`
`The examiner rejected the broader claims (EX1004.225-229, 09/24/2003
`
`Non-Final Action) as substantial duplicates of the four specifically-claimed
`
`polymorphs: anhydrous varenicline L-tartrate; the L-tartrate salt of varenicline as a
`
`hydrate; the anhydrous D,L-tartrate salt of varenicline; and the hydrate of varenicline
`
`D,L-tartrate salt. (EX1004.227 (pending claims “are all drawn to one compound
`
`10
`
`

`

`each …. These claims cannot be narrowed because the same compound is being
`
`claimed different ways.” (emphasis original)); EX1002, ¶ 88).
`
`Pfizer next “reinstated” the originally-cancelled claims 1 (to the “tartrate salt”
`
`of varenicline) and 2 (the L-tartrate salt):
`
`(EX1004.232, 03/25/2004 Amendment).
`
`After several rounds of amendments, Pfizer again cancelled claims 1-2, but
`
`added new claims 67-68:
`
`
`
`
`
`(EX1004.261, 04/28/2004 Amendment).
`
`Unsurprisingly, in the Final Rejection, the examiner objected that the
`
`“presentation of the instant claims is confusing.” (EX1004.285, 08/19/2004 Final
`
`Action). Pfizer was “requested to rewrite these claims in consecutive order for ease
`
`of examination and to avoid errors ….” (Id.)
`
`11
`
`

`

`The examiner maintained the obviousness rejection because Coe disclosed
`
`varenicline and a tartaric acid salt and the proposed claims “differ from the reference
`
`by reciting a specific salt of the reference,” and thus the basis for the rejection
`
`remained the same as the previous office action. (Id.) The examiner maintained his
`
`“duplicate claims” rejection.
`
`In an amendment after final, Pfizer argued Coe did not “suggest or disclose
`
`specific tartrate salts and polymorphs” of varenicline from the “generic structures”
`
`that were “necessary to arrive at the specific tartrate salt of” varenicline.
`
`(EX1004.294-295, 11/19/2004 Response). Pfizer argued Coe did not “suggest[] or
`
`disclos[e] any specific polymorphs of tartrate salts.” (EX1004.295). And, Pfizer
`
`expressly stated (when claim 67 facially recited just a “tartrate” salt; and dependent
`
`claim 68 facially recited just a particular isomer of tartrate salt), that “Claims 67-70
`
`of the claimed invention all relate to specific polymorphs of the tartrate salt of
`
`[varenicline].” (Id. (emphasis added)).
`
`But-for the examiner’s belief that Coe lacked written description support for
`
`the varenicline tartrate species; and Pfizer’s insistence that all claims—including
`
`pending claims 67 and 68—were limited to specific polymorphs of the varenicline
`
`tartrate salt, the Challenged Claims would not have issued.
`
`Pfizer further argued “the claimed anhydrous [crystalline] and hydrate
`
`[crystalline] tartrate salts of” varenicline were “significantly and surprisingly less
`
`12
`
`

`

`hygroscopic that [sic] the corresponding hydrochloride salt,” rendering “this
`
`unexpected decrease in hygroscopicity of the claimed tartrate salts” “unobvious to
`
`the worker of skill in the art.” (EX1004.295, 11/19/2004 Response). As discussed
`
`in Section XIII, below, the examiner lacked prior art showing hydrochloride salt
`
`hygroscopicity was known, and that a salt switch—including to tartrate salts—
`
`solved the problem. The examiner thus lacked art confirming the POSA could
`
`reasonably expect Pfizer’s results.
`
`A Notice of Allowance issued thereafter. (EX1004.304, 12/03/2004 Notice
`
`of Allowability; EX1004.307, 12/03/2004 Interview Summary).
`
`IX. CLAIM CONSTRUCTION
`Under 37 C.F.R. § 42.100(b), the Challenged Claims have their “ordinary and
`
`customary meaning” as “understood by one of ordinary skill in the art and the
`
`prosecution history pertaining to the patent.” Id.; see Phillips v. AWH Corp., 415
`
`F.3d 1303, 1315-18 (Fed. Cir. 2005) (en banc). Under Phillips, a claim term is given
`
`“the meaning that the term would have to a person of ordinary skill in the art in
`
`question at the time of the invention.” 415 F.3d at 1313. The specification and
`
`prosecution history may su