Paper No. 1
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`UNITED STATES PATENT AND TRADEMARK OFFICE
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`BEFORE THE PATENT TRIAL AND APPEAL BOARD
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`COALITION FOR AFFORDABLE DRUGS IX LLC,
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`Petitioner
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`v.
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`BRISTOL-MYERS SQUIBB PHARMA COMPANY
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`Patent Owner
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` IPR2015-___________
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`Title: LACTAM-CONTAINING COMPOUNDS AND DERIVATIVES
`THEREOF AS FACTOR XA
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`
`PETITION FOR INTER PARTES REVIEW OF
`U.S. PATENT NO. 6,967,208
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`TABLE OF CONTENTS
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`TABLE OF AUTHORITIES ................................................................................... iv  
`LIST OF EXHIBITS ................................................................................................. v  
`I.  
`Introduction ................................................................................................... 1  
`II.   Grounds for Standing .................................................................................... 1  
`III.  Mandatory Notices ....................................................................................... 1  
`A.   Real Party-In-Interest ............................................................................. 1  
`B.   Related Matters ...................................................................................... 2  
`C.   Lead and Back-Up Counsel, and Service Information ........................... 3  
`IV.  Payment of Fees ........................................................................................... 3  
`V.   Identification of Challenge ........................................................................... 3  
`A.   Overview of the ’208 Patent ................................................................... 3  
`1.
`   The ’208 Specification ..................................................................... 3  
`   The ’208 Claims ............................................................................... 5  
`2.
`   The ‘208 Prosecution History ........................................................ 10  
`3.
`   The Certificate of Correction ......................................................... 12  
`4.
`B.   Claim Construction of Challenged Claims ........................................... 13  
`1.   “1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxo-1-
`piperidinyl)phenyl-4,5,6,7-tetrahydro-1Hpyrazolo-[3,4-
`c]pyridine-3-carboxamide” ............................................................ 14  
`2.   “Pharmaceutically acceptable salt” ................................................ 14  
`3.   Claims for Which Review Is Requested ........................................ 15  
`4.   Statutory Grounds of Challenge ..................................................... 15  
`C.   Overview of the Cited Art .................................................................... 15  
`1. PCT Publication No. WO 00/39131 (Ex. 1003) .............................. 16  
`2.   U. S. Patent 6,413,980 (Ex. 1004) ................................................. 17  
`D.   Level of Skill in the Art ........................................................................ 19  
`VI.  Detailed Explanation of the Challenge ...................................................... 20  
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`A.   Ground 1: PCT Published Application WO 00/39131 to Fevig et
`al. (“Fevig I”) (Ex. 1003) anticipates claims 1-13, 20-27, and
`34-61 of US 6,967,208 under 35 U.S.C. § 102(b). ............................... 20  
`1.   Anticipation of Claim 13 by Fevig I. ............................................. 22  
`2.   Anticipation of Claim 8 by Fevig I. ............................................... 27  
`3.   Anticipation of Claim 1 by Fevig I. ............................................... 28  
`4.   Anticipation of Claim 2 by Fevig I. ............................................... 34  
`5.   Anticipation of Claim 3 by Fevig I. ............................................... 35  
`6.   Anticipation of Claim 4 by Fevig I. ............................................... 35  
`7.   Anticipation of Claim 5 by Fevig I. ............................................... 36  
`8.   Anticipation of claim 6 by Fevig I. ................................................ 36  
`9.   Anticipation of Claim 7 by Fevig I. ............................................... 37  
`10.   Anticipation of claims 9-12, 20-27, and 34-61 by Fevig I. ........... 38  
`B.   Ground 2: U.S. Patent 6,413,980 to Fevig et. al (“Fevig II”) (Ex.
`1004) anticipates claims 1-13, 20-27, and 34-61 of U.S.
`6,967,208 under 35 U.S.C. § 102(e). .................................................... 38  
`1. Anticipation of Claim 13 by Fevig II. ............................................. 39  
`2. Anticipation of Claim 8 Fevig II. .................................................... 43  
`3. Anticipation of Claim 1-7 Fevig II. ................................................. 44  
`4. Anticipation of claims 9-12, 20-27 and 34-61. ............................... 51  
`C.   Grounds 3 and 4: Fevig I and Fevig II, each in its own right,
`renders the challenged claims of the ‘208 Patent obvious under
`35 U.S.C. 103(a). .................................................................................. 54  
`D.   Secondary Considerations of Non-Obviousness Do Not Rebut
`the Prima Facie Case of Obviousness .................................................. 58  
`VII.   Conclusion .............................................................................................. 60  
`CERTIFICATE OF SERVICE ................................................................................ 61  
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`TABLE OF AUTHORITIES
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`Cases  
`App. of Susi
`440 F.2d 442; 169 U.S.P.Q. 423 (CCPA, 1971) ......................................... 21, 57
`Application of Ruff
`256 F.2d 590 (CCPA 1958) ............................................................ 21, 27, 34, 44
`Atlas Powder Co. v. Ireco, Inc.
`190 F.3d 1342, 51 U.S.P.Q.2d (BNA) 1943 (Fed. Cir. 1999) ........ 21, 27, 34, 44
`Calloway Golf Company v. Acushnet Company
`576 F.3d 1331 (Fed. Cir. 2009) ........................................................................... 6
`In re Swanson
`540 F.3d 1368 (Fed. Cir. 2008) ........................................................................ 19
`Merck v Biocraft Labs.
`874 F2d 804; 10 U.S.P.Q. 2d 1843 (Fed. Cir. 1989) ........................................ 57
`Ruiz v. A.B. Chance Co.
`234 F.3d 654 (Fed. Cir. 2000) ........................................................................... 59
`Upsher-Smith Labs., Inc. v. Pamlab, L.L.C. 412 F.3d 1319 (Fed. Cir. 2005) ......... 30
`Verdegaal Bros. v. Union Oil Co. of California
`814 F.2d 628 (Fed. Cir. 1987) ........................................................................... 20
`Statutes  
`35 U.S.C. 102(e)(2) ................................................................................................ 18
`35 U.S.C. 303(a) ..................................................................................................... 19
`Regulations  
`37 C.F.R. § 42.100(b) ............................................................................................. 14
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`LIST OF EXHIBITS
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`Exhibit 1001 U.S. 6,967,208 to Pinto et. al, titled, “Lactam Containing
`Compounds and Derivatives Thereof as Factor Xa Inhibitors,”
`filed on September 17, 2002, and issued on November 22, 2005
`(“the ’208 Patent”).
`Exhibit 1002 Excerpts from the File History of U.S. Patent No. 6,967,208.
`Exhibit 1003 Published PCT Application WO 00/39131 titled Nitrogen
`Containing Heterobicycles as Factor Xa Inhibitors, published on
`July 6, 2000 (“Fevig I”).
`Exhibit 1004 U.S. Patent 6,413,980 to Fevig et. al, titled Nitrogen Containing
`Heterobicycles as Factor Xa Inhibitors, filed on December 22,
`1999. (“Fevig II”)
`Exhibit 1005 Excerpts from the File History of U.S. Patent 6,413,980
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`Exhibit 1006 Published PCT Application WO 95/01980 titled Bicyclic
`Tetrahydro Pyrazolopyridines, filed July 3, 1993. (Duplantier)
`Exhibit 1007 Reserved
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`Exhibit 1008 Expert Declaration of George Burton
`Exhibit 1009 Prescribing Information– Eliquis FDA Label
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`I.
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`Introduction
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`Petitioner Coalition For Affordable Drugs IX LLC (“CFAD”), requests an
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`Inter Partes Review (“IPR”) of Claims 1-13, 20-27, and 34-61 (collectively, the
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`“Challenged Claims”) of U.S. Patent No. 6,967,208 (the “’208 Patent”) (Ex. 1001)
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`in accordance with 35 U.S.C.§§ 311–19 and 37 C.F.R. §§ 42.100 et seq.
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`II. Grounds for Standing
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`Petitioner certifies that the ’208 Patent is available for IPR and that the
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`Petitioner is not barred or estopped from requesting IPR challenging the claims of
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`the ’208 Patent on the grounds identified in this petition.
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`III. Mandatory Notices
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`A. Real Party-In-Interest
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`Pursuant to 37 C.F.R. § 42.8(b)(1), Petitioner certifies that Coalition For
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`Affordable Drugs IX LLC (“CFAD IX ”), Hayman Credes Master Fund, L.P.
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`(“Credes”), Hayman Orange Fund SPC – Portfolio A (“HOF”), Hayman Capital
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`Master Fund, L.P. (“HCMF”), Hayman Capital Management, L.P. (“HCM”),
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`Hayman Offshore Management, Inc. (“HOM”), Hayman Investments, L.L.C.
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`(“HI”), nXn Partners, LLC (“nXnP”), IP Navigation Group, LLC (“IPNav”), J.
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`Kyle Bass, and Erich Spangenberg are the real parties in interest (collectively,
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`“RPI”). The RPI hereby certify the following information: CFAD IX is a wholly
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`owned subsidiary of Credes. Credes is a limited partnership. HOF is a segregated
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`portfolio company. HCMF is a limited partnership. HCM is the general partner and
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`investment manager of Credes and HCMF. HCM is the investment manager of
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`HOF. HOM is the administrative general partner of Credes and HCMF. HI is the
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`general partner of HCM. J. Kyle Bass is the sole member of HI and sole
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`shareholder of HOM. CFAD IX, Credes, HOF and HCMF act, directly or
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`indirectly, through HCM as the general partner and/or investment manager of
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`Credes, HOF and HCMF. nXnP is a paid consultant to HCM. Erich Spangenberg is
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`the Manager and majority member of nXnP. IPNav is a paid consultant to nXnP.
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`Erich Spangenberg is the Manager and majority member of IPNav. Other than
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`HCM and J. Kyle Bass in his capacity as the Chief Investment Officer of HCM and
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`nXnP and Erich Spangenberg in his capacity as the Manager/CEO of nXnP, no
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`other person (including any investor, limited partner, or member or any other
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`person in any of CFAD IX, Credes, HOF, HCMF, HCM, HOM, HI, nXnP or
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`IPNav) has authority to direct or control (i) the timing of, filing of, content of, or
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`any decisions or other activities relating to this Petition or (ii) any timing, future
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`filings, content of, or any decisions or other activities relating to the future
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`proceedings related to this Petition. All of the costs associated with this Petition
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`will be borne by HCM, CFAD IX, Credes, HOF and/or HCMF.
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`B. Related Matters
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`The Petitioner has found no record of the ’208 Patent having been
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`involved in any related matters in any United States District Court or in the U.S.
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`Patent and Trademark Office.
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`C. Lead and Back-Up Counsel, and Service Information
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`Lead counsel is Thomas C. Wright, Reg. No. 47189, of CUNNINGHAM
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`SWAIM LLP, 7557 Rambler Road, Suite 440, Dallas, TX 75231, P:
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`469.729.7010/F: 214.613.1163 twright@cunninghamswaim.com. Back-up counsel
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`is Lekha Gopalakrishnan, Reg. No. 46,733, of Winstead P.C., 500 Winstead Bldg.,
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`2728 Harwood Street, Dallas, TX 75201, P: 214.745.5356/F: 214.745.5390
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`lgopalakrishnan@winstead.com. Petitioner consents to electronic service.
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`IV. Payment of Fees
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`The required fees are submitted herewith in accordance with 37 C.F.R. §§
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`42.103(a) and 42.15(a). If any additional fees are due during this proceeding, the
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`Office is authorized to charge such fees to Deposit Account No. 506787.
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`V.
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`Identification of Challenge
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`A. Overview of the ’208 Patent
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`1.
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`The ’208 Specification
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`The ’208 Patent was filed on September 17, 2002 and claims benefit of
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`provisional applications Nos. 60/324,165 and 60/402,317, for which the earliest
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`filing date is September 21, 2001. (Ex. 1001 Front Cover.)
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`The ‘208 Patent is titled “Lactam Containing Compounds and Derivatives
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`thereof as Factor Xa Inhibitors,” and it describes and claims compositions “which
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`are inhibitors of trypsin-like serine protease enzymes, especially factor Xa,
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`pharmaceutical compositions containing the same and methods of using the same
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`as anticoagulant agents for treatment of thromboembolic disorders.” Id. at 1: 21-
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`25. The ‘208 specification acknowledges that Factor Xa inhibitors containing
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`moieties closely related to those claimed in the ‘208 were known in the art at the
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`time of filing. Id. at 1:27-5:22. Thus the only alleged improvement of the ‘208
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`Patent is the preparation and use of “efficacious and specific inhibitors of factor
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`Xa.” Ex. 1008 at 24. But while the patent does describe the synthesis of
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`numerous alleged factor Xa inhibitors, there is not a single working example
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`showing administration of any of the disclosed compounds to a patient, or any in
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`vitro or in vivo testing to prove efficacy, pharmacokinectics, and the like. Id.
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`Thus there is no disclosure that any of the compounds described in the ‘208 Patent
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`is an actual Xa inhibitor, much less an “efficacious” one. Id.
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`The ‘208 Patent is an extreme example of the abuse of the use of Markush
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`groups in claims drafting. The ‘208, with its sprawling and outlandish claims,
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`teaches absolutely nothing with specificity with respect to any particular
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`compound. Therefore any and all possibilities for any and all structures are as
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`equally likely to be chosen by a person of ordinary skill, as not, from the starting
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`Markush group in the single, independent claim 1 since nothing is claimed with
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`any specificity or with any certainty.
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`Further, since there is no pharmacological data presented in the
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`specification, there is no information that establishes the inhibiting properties of
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`any of the enormous number of claimed compounds, or whether any of them are
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`more effective inhibitors than any of the others. In other words, there are no
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`distinguishing characteristics that would lead one of ordinary skill in the art to
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`choose any particular combination of moiety/moieties to form any one of the
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`specific compound(s) as claimed for any reason. Rather a person of ordinary skill
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`would recognize all of the disclosed compounds as reasonable candidates for the
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`stated purpose of being Factor Xa inhibitors absent further guidance and
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`disclosure. Id.
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`2.
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`The ’208 Claims
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`The claims at issue here can be summarized as a typical funnel that begins
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`with an enormous number of alternatives in the only independent claim (claim
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`1) of 103 claims, composed of Markush group alternatives for different sub-
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`units of the overall molecular structure that is claimed. As with any claim-
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`funnel, the scope of the independent claim is further limited through a chain of
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`dependent claims. In this case, the total number of claimed variations or
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`alternatives is decreased until a single molecular formula is claimed, inter alia,
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`in claim 13. The reduction in claim scope is accomplished not through the
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`addition of new claim elements, but through the successive reduction in the
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`number of alternative formulations possible under each dependent claim. Id. at
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`26.
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`Claim 13 depends, ultimately from claim 1. Due to the chain of claim
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`dependency (i.e., claim 13 depends from claim 8 and claim 8 depends from
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`claim 1) the patent owner cannot deny that the single compound of claim 13 is
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`claimed in each of the earlier claims in that chain since a dependent claim must
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`contain all of the elements of any claim from which it depends. Id. at 27. MPEP
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`608.01(i)(c) (“Claims in dependent form shall be construed to include all the
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`limitations of the claim incorporated by reference into the dependent claim”).
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`The claims at issue here do nothing more than progressively restrict the
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`large number of alternative compounds claimed in claim 1 until they are reduced
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`to a few (claims 2-8) or a single molecule (e.g. claim 13). Ex. 1008 at 28.
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`Further, if claim 13 is determined to have been taught in the prior art, no
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`antecedent claims can be found nonobvious. Calloway Golf Company v.
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`Acushnet Company, 576 F.3d 1331, 1344 (Fed. Cir. 2009) (“A broader
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`independent claim cannot be nonobvious where a dependent claim stemming
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`from that independent claim is invalid for obviousness”).
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`What follows is a general description of the claims that are at issue in this
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`IPR petition:
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`Claim 1, the only independent claim in the ‘208 Patent, recites a generic
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`claim for a compound of the formula:
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`wherein P4 is further defined as -G1-G and M4 is –A-B1 . Ex. 1001 237: 3-10 and
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`1 When the “P” and “M” rings defined in the amendment are fused via the
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`dangling bonds of the individual rings (represented by the zig-zagging lines,
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`above in “P and “M” separately), the result is a fused two-ring system of
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`Structure 1, below.
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` Structure 1
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`Where P4 is replaced by “G1-G” as defined in claim 1 of the ‘208 Patent. “M4”
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`was further defined in the Certificate of Correction for claim 1 to be the “A-B” unit
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`which results in the structure of the ring system being:
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`Cert. of Cor. pg 2 correcting line 34. The components of this generic formula are
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`set forth as a massive listing of nested chemical moieties in the form of multiple
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`Markush groups that take up over five columns of the patent consisting of
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`inestimable combinations. The claim concludes with “or a pharmaceutically
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`acceptable salt thereof.” Ex. 1001 at 237:1-242:23 and Cert. of Cor. pg 1-2
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`correcting multiple entries in all of columns 237-242; Ex. 1008 at 30.
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`Claim 2 depends from claim 1 and recites a subset of the enormous range
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`of compounds in claim 1 by listing alternatives for a subunit (labeled G) of the
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`P4 moiety and a subunit (labeled A) of the M4 moiety of the formula provided
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`above. Id. at 242:24-245:29 and Cert. of Cor. pg 2-3 correcting columns 243
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`and 244. Even this “narrowing” would results in, still, millions of potential
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`combinations. Ex. 1008 at 31.
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`Claim 3 depends from claim 2 and defines a list of 168 alternatives for
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`moiety G in the form of structural formulae. In the addition it provides that “G1
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`is absent or selected from” a list of generic formulae, each with multiple
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`variations and further limits moiety “A”. Ex. 1001 at 245:30-254:41 and Cert.
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`Structure 2
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`Structure 2 appears in the ‘208 Patent at 134:60 (where R1a = H). Ex. 1008 at 45  
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`of Corr. pg 3-5 correcting columns 246, 248, 249, 251-254; Ex. 1008 at 32.
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`Claim 4 depends from claim 3 and narrates 96 alternative structural
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`variations for the “G” moiety, a subset of the 168 in claim 3. Claim 4 also
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`includes the alternative that “G1” is absent or chosen form another list of
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`alternatives that themselves include variations chosen from one or more of 12
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`groups of additional variables. Id. at 254:42-259:67 and Cert. of Corr. pg 5-6
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`correcting columns 255, 256, 258 and 259; Ex. 1008 at 33.
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`Claim 5 depends from claim 4, and continuing with the theme of claims 3
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`and 4, recites 58 alternatives for the “G” moiety as structural formulae (a subset
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`of the 96 listed in claim 4) and number of additional alternatives including the
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`“A” and “B” moieties. Id. at 260:1 -263:44 and Cert. of Corr. pg 6-7 correcting
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`columns 261-263; Ex. 1008 at 34.
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`Claim 6 depends from claim 5, and, again recites a vast subset of
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`structural alternatives in which G1 is absent with 27 alternatives for moiety G
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`and two alternatives for –A-B. Id. at 263:45-265:28 and Cert. of Corr. pg 7
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`correcting col 265 lines 20-25; Ex. 1008 at 35.
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`Claim 7 depends from claim 6 and defines a single alternative for the
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`moiety labeled “-A-B.” The “-A-B” structural unit is included in all of the
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`claims that are at issue in this IPR, but is never shown in any of the structural
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`diagrams or demonstrated in the specifications with particularity. It is merely
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`defined in the claims. Id. at 265:29-39 and Cert. of Cor. pg 7 correcting line 35
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`by deleting the second structure; Ex. 1008 at 36.
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`Claim 8 depends from claim 1, and claims “a compound according to
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`claim 1 wherein the compound is selected from” a group of 65 specific
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`compounds “or a pharmaceutically acceptable salt form thereof” admitted to
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`being covered by the generic formula of claim 1. Ex. 1001 at 265:39-268:41 and
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`see also Cert. of Corr pg 7 correcting col 655 line 66 from “…pyrazole-…” to
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`“…pyrazolo-…” as well as other numerous corrections; Ex. 1008 at 37.
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`Claim 13 depends from claim 8, and recites a single compound, 1-(4-
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`methoxyphenyl)-7-oxo-6-4[4-(2-oxo-1-piperidinyl)phenyl-4,5,6,7-tetrahydro-
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`1Hpyrazolo-[3,4-c]pyridine-3-carboxamide or a pharmaceutically acceptable
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`salt form thereof, which is the ninth compound of the 65 compounds listed in
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`claim 8. Id. at 269:1-6 and see also Cert. of Corr. page 10 correcting col 269
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`line 4 from “…pyrazole-…” to “…pyrazolo-…” as well as other corrections;
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`Ex. 1008 at 38.
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`Claims 9-12, 20-27, and 34-61 all depend from one of the above-
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`described claims and add nothing of patentable distinction, but rather simply
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`recite, for example, a specific condition for which the compounds claimed in the
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`claims above may be administered Ex. 1001 passim; Ex. 1008 at 39.
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`3.
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`The ‘208 Prosecution History
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`The application that led to the ‘208 Patent was filed on September 17,
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`2002 and contained 30 claims. A restriction requirement was issued on
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`September 29, 2003. In issuing the restriction requirement the examiner stated
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`that all 30 claims were generic and that an election of a single species for
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`examination was required. In response the applicant elected 2(1-(4-
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`methoxyphenyl)-3-[(methylamino)methyl]-6-[-4-(2-oxo-1-piperdinyl)phenyl]-
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`1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridine-7-one.
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`The first, and only, substantive office action on the merits was issued on
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`October 23, 2003. In the action claims 1-21 were rejected and claims 22-30
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`were withdrawn for being drawn to non-elected subject matter. The rejected
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`claims were characterized as constituting an improper Markush group. The
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`variables “P” and “M” that made up the two core rings of the generic formula
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`were originally submitted as follows:
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`P4-P-M-M4
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`The examiner then requested changes “in the core of the compound that
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`determines classification” for the purposes of examination. Ex. 1002 at 4.
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`A response was filed on November 19, 2003 that cancelled claims 9-15
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`and 2-30 that left claims 1-8 and 16-19 pending. Claims 31-121 were then
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`added. Claim 1 was amended such that the generic formula above was replaced
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`with the formula illustrated here
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`with rings P and M defined as two specific systems:
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` “P” “M”
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`Ex. 1002 at 7-8
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`The amendment of claim 1 resulted in the issuance of a Notice of Allowance
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`on March 11, 2004. No reason for allowance was given. An Amendment and
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`Request for Continued Examination was filed on September 16, 2004 and
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`September 22, 2004 that added claims 122-133. A second Notice of Allowance
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`was issued on October 13, 2004 for the amendments. Another RCE was filed
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`November 3, 2004 with a third Notice of Allowance issued December 8, 2004.
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`4.
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`The Certificate of Correction
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`Perhaps the most significant event in the prosecution of the ‘208 was the 13
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`page Certificate of Correction that was filed by the patent owner. The corrections
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`resulted in numerous changes to the claims Ex. 1001 Cert. of Corr. pg 1-13. In
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`addition to the above-mentioned definition of “M4” as “A-B,”(Cert. of Corr. pg 2)
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`the other changes specifically relevant to this IPR are correction of the spelling of
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`the name of the compound in claim 13, and the correction of that same compound
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`name in the list of those in claim 8 by replacing “pyrazole” with “pyrazolo”. Ex
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`1001, Cert. of Corr. at pg 7 and 10; Ex. 1008 at 46. It should be noted that while
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`this request for an IPR is limited to validity challenges for anticipation and
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`obviousness, the Certificate of Correction for the ‘208 Patent raises serious
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`questions about the validity of the ‘208 claims under 35 U.S.C. §112. The
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`“corrections” go well beyond fixing typographical errors and the like, as is
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`appropriate in a Certificate of Correction. MPEP 1481 (“the Director may…issue
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`a certificate of correction, if the correction does not involve such changes in the
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`patent as would constitute new matter or would require examination”) These
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`changes did indeed add new matter and substantive language to the claims that was
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`never considered by any examiner. Further, many of the corrections go to
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`renaming previously “examined” compounds. For example, the Certificate reads,
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`“’P4 is –G1-G;’ should read –M4 is –A-B; P4 is G1-G; “Ex1001 Cert. of Corr. at 2.
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`As set forth below, the “A-B” units added as a “correction” do appear in the Patent
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`Owner’s own prior art relied upon in this request. The corrections improperly
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`added new, unexamined, chemical structures into the patent without the benefit of
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`any prior art analysis. Id.
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`B. Claim Construction of Challenged Claims
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`A claim subject to IPR receives the “broadest reasonable construction in
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`light of the specification of the patent in which it appears.” 37 C.F.R. §
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`42.100(b). Unless otherwise noted below, Petitioner accepts, for purposes of
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`IPR only, that the claim terms of the ‘208 Patent are presumed to take on their
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`ordinary and customary meaning that they would have to one of ordinary skill
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`in the art.
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`1. “1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxo-1-
`piperidinyl)phenyl-4,5,6,7-tetrahydro-1Hpyrazolo-[3,4-
`c]pyridine-3-carboxamide”
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`The term 1-( 4-methoxyphenyl)-7-oxo-6-[ 4-(2-oxo-1-
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`piperaziny l)pheny 1 ]-4,5,6, 7-tetrahydro-1H -pyrazolo
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`[3,4-c ]pyridine-3-carboxamide (Ex. 1001 Example 97 - col 208:51-55)
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`corresponds to the structure:
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`O
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`H2N
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`N
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`N
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`N
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`O
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`N
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`O
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`O
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`Structure 3
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`which is also known as apixaban or by the commercial brand of Eliquis. Ex.
`1009 pg. 12 section 11 “Description” and Ex. 1008 at 51-52.
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`2. “Pharmaceutically acceptable salt”
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`The term “pharmaceutically acceptable salt” means: those compounds,
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`materials, compositions, and/or dosage forms which are, within the scope of
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`sound medical judgment, suitable for use in contact with the tissues of human
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`beings and animals without excessive toxicity irritation, allergic response, or
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`other problem or complication, commensurate with a reasonable benefit/risk
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`ratio” Ex. 1001 116:40-47, Ex.1008 at 53.
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` Statement of Precise Relief Requested for Each Claim Challenged
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`3. Claims for Which Review Is Requested
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`Petitioners request IPR under 35 U.S.C. § 311 of claims 1-13, 20-27 and
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`34-61 of the ‘208 Patent, and such cancellation of said claims as unpatentable.
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`4. Statutory Grounds of Challenge
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`Claims 1-13, 20-27, and 34-61 are unpatentable under 35 U.S.C. §§ 102
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`and/or 103 for the following reasons:
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`Ground Proposed Rejections for the ‘208 Patent
`1
`Claims 1-13, 20-27, and 34-61 are anticipated
`under 35 U.S.C. § 102(b) by the publication of
`PCT Application WO 00/39131A1 (Fevig I).
`Claims 1-13, 20-27, and 34-61 are anticipated
`under 35 U.S.C. 102(e) by United States Patent
`6,413,980 (Fevig II)
`Claims 1-13, 20-27, and 34-61 3 are obvious under 35
`U.S.C. § 103(a) in view of the publication of PCT
`application WO 00/39131A1 (Fevig I).
`Claims 1-13, 20-27, and 34-61 are obvious under 35
`U.S.C. § 103(a) in view of United States Patent
`6,413,980 (Fevig II)
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`2
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`3
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`4
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`Overview of the Cited Art
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`C.
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`Exhibit No.
`1003
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`1004
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`1003
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`1004
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`The references relied upon to establish the invalidity of the ‘208 Patent are a
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`published PCT application belonging to the Patent Owner as well as the U.S.
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`version of that PCT application filed in the U.S. without claiming priority to the
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`PCT. Both the PCT application and the U.S. Patent claim priority to the same two
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`U.S. Provisional Applications, US 60/127,633 and US 60/113,628. The published
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`application is prior art under 35 USC 102(b) and the U.S. Patent is prior art under
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`35 USC 102(e)(2).
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`
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`1. PCT Publication No. WO 00/39131 (Ex. 1003)
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`International Publication No. WO 00/39131 (here after “Fevig I”) entitled
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`“Nitrogen Containing Heterocycles of Factor Xa Inhibitors” was published on
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`July 6, 2000. It does not designate the United States and was filed before
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`November 29, 2000. Therefore, Fevig I is 102(b) prior art as of its publication
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`date. MPEP 2136.03 II(B). The publication date of the Fevig I application, July
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`6, 2000, is more than one year before September 21, 2001, the earliest priority
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`date of the ‘208 Patent. Ex 1001 Front Cover. Fevig I is over 300 pages long
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`and, like the ‘208 Patent, discloses an enormous number of compounds claimed to
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`be Factor Xa inhibitors. Ex. 1003 passim; Ex. 1008 at 55.
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`Fevig I is mentioned in the ‘208 Patent, and was submitted on an IDS
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`disclosing prior art document references during the prosecution of the application
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`leading to the ‘208 Patent but Fevig I was not substantively considered by the
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`Examiner during prosecution of the ‘208 Patent. Despite the fact that Fevig I was
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`disclosed to the examiner in an expansive dump of prior art during prosecution of
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`the ‘208 Patent, it is undeniable that the compound disclosed in claim 13 of the
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`‘208 Patent is also explicitly disclosed in Fevig I. The examiner, who was
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`undoubtedly under time constraints, would not have the time to appreciate the fact
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`that the claims of the ‘208 are covered by the disclosure of Fevig I given the
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`enormously complicated Markush structure of the both Fevig I and the ‘208
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`Patent.
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`Apparently acknowledging the substantial overlap between the disclosure
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`of Fevig I and the ‘208 Patent, the Patent Owner, in describing the scope of Fevig
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`I in the Background of the Invent