By: Matthew L. Fedowitz, Esq.
`
`Daniel R. Evans, Esq.
`
`MERCHANT & GOULD P.C.
`1900 Duke Street, Suite 600
`Alexandria, VA 22314
`Main Telephone: (703) 684-2500
`Main Facsimile: (703) 684-2501
`
`UNITED STATES PATENT AND TRADEMARK OFFICE
`_____________________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`_____________________
`
`
`BRECKENRIDGE PHARMACEUTICAL, INC.
`Petitioner
`
`v.
`
`
`RESEARCH CORPORATION TECHNOLOGIES, INC.
`Patent Owner
`
`_____________________
`
`Case No. To Be Assigned
`Patent No. RE38,551
`_____________________
`
`
`PETITION FOR INTER PARTES REVIEW
`UNDER 35 U.S.C. §§ 311-319 AND 37 C.F.R. § 42.100 ET SEQ.
`
`
`
`
`
`
`
`
`
`
`
`
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`
`

`

`
`
`
`TABLE OF CONTENTS
`
`I.  MANDATORY NOTICES UNDER 37 C.F.R. § 42.8 ....................................... 7 
`A.  Real Parties-In-Interest under 37 C.F.R. § 42.8(b)(1) ...................................... 7 
`B.  Related Matters under 37 C.F.R. § 42.8(b)(2).................................................. 7 
`C.  Lead and Backup Counsel under 37 C.F.R. § 42.8(b)(3) ............................... 10 
`D.  Service Information under 37 C.F.R. § 42.8(b)(4) ......................................... 10 
`II.  REQUIREMENTS FOR IPR UNDER 37 C.F.R. § 42.104 .............................. 11 
`A.  Grounds For Standing Under 37 C.F.R. § 42.104(a) ..................................... 11 
`B.  Identification of Challenge and Precise Relief Requested, 37 C.F.R. §
`42.104(b) ............................................................................................................... 11 
`III. SUMMARY OF THE ’551 PATENT ............................................................... 15 
`IV. PREVIOUS PETITIONS ................................................................................... 17 
`V. CLAIM CONSTRUCTION UNDER 37 C.F.R. § 42.104(b)(3) ........................ 18 
`A.  “Therapeutic Composition” in Claim 10 ........................................................ 18 
`B.  “A Compound in the R Configuration” in Claim 1 ........................................ 21 
`VI. LEVEL OF SKILL AND KNOWLEDGE IN THE ART ................................. 22 
`A.  Cortes (Ex. 1015) ............................................................................................ 24 
`B.  LeGall (1987) (Ex. 1008) ............................................................................... 24 
`C.  Kohn 1991 (Ex. 1012) .................................................................................... 26 
`D.  ’729 Patent (1991) (Ex. 1009) ........................................................................ 28 
`E.  Kohn 1993 (Ex. 1017) .................................................................................... 29 
`F.  Choi (1995) (Ex. 1010) ................................................................................... 30 
`G.  ’301 Patent (1995) (Ex. 1019) ........................................................................ 31 
`VII. CLAIM-BY-CLAIM EXPLANATION OF GROUNDS FOR
`UNPATENTABILITY............................................................................................. 33 
`A.  Ground 1A: Claims 1 and 3-8 Are Anticipated by LeGall ............................ 33 
`1.  New evidence establishes that LeGall is prior art ....................................... 33 
`2.  LeGall discloses “racemic lacosamide” and R-lacosamide and therefore
`anticipates claims 1 and 3-8 ............................................................................... 36 
`B.  Ground 1B: Claims 2 and 9-13 Are Obvious Over LeGall And The ’729
`Patent ..................................................................................................................... 37 
`
`
`
`1
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`

`

`
`
`
`1.  Claims 2 and 9 to “substantially” or “90%” pure R- enantiomer are
`obvious over LeGall and ’729 patent ................................................................ 37 
`2.  Claim 10 to a “therapeutic composition” is obvious over LeGall and the
`’729 patent ......................................................................................................... 41 
`3.  Claims 11-13 to methods of treatment are obvious over LeGall and ’729
`patent .................................................................................................................. 44 
`C.  Ground 2A: Claims 1-9 Are Obvious Over Choi and Kohn 1991 ................. 47 
`1.  Choi and Kohn 1991 are prior art ................................................................ 47 
`2.  POSA had a reason to select Compound 2d of Choi as a lead compound .. 48 
`3.  POSA had a reason to modify the hydroxymethyl compound to a
`“functionalized oxygen” group .......................................................................... 54 
`4.  POSA would have a Reasonable Expectation of Success in making
`Raceamic Lacosamide and R-Lacosamide ........................................................ 55 
`D.   Ground 2B: Claims 10-13 Are Obvious Over Choi, Kohn 1991, And ’729
`Patent ..................................................................................................................... 56 
`E.   Ground 3A: Claims 1-9 Are Obvious Over Kohn 1991 and Silverman ...... 57 
`1.  Kohn 1991 and Silverman are prior art ....................................................... 57 
`2.  Activity data and bioisosterism suggest the change from methoxyamino to
`methoxymethyl (lacosamide) ............................................................................ 57 
`F.  Ground 3B: Claims 10-13 Are Obvious Over Kohn 1991, Silverman, and
`’729 Patent ............................................................................................................ 61 
`G.  Ground 4A: Claims 1-9 Are Obvious Over Cortes and Kohn 1991 .............. 62 
`1.  Cortes and Kohn 1991 are prior art ............................................................. 62 
`2.  POSA had a reason to select the methyl compound of Cortes or Kohn 1991
`as a lead compound ............................................................................................ 62 
`3.  POSA had a Reason to modify the Methyl Substituent to a Methoxymethyl
`
`63 
`H.  Ground 4B: Claims 10-13 Are Obvious Over Cortes, Kohn 1991, And ’729
`Patent ..................................................................................................................... 65 
`VIII.THERE ARE NO SECONDARY CONSIDERATIONS OF
`NONOBVIOUSNESS ............................................................................................. 66 
`IX. THE CLAIMS ARE NOT ENTITLED TO THE PROVISIONAL FILING
`DATE ....................................................................................................................... 68 
`
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`2
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`X. THE BOARD SHOULD NOT DECLINE TO INSTITUTE BASED ON ITS
`
`X.  THE BOARD SHOULD NOT DECLINE TO INSTITUTE BASED ON ITS
`DISCRETIONARY AUTHORITY UNDER 35 U.S.C. § 325(d) .......................... 70 
`DISCRETIONARY AUTHORITY UNDER 35 U.S.C. § 325(d) ........................ ..7O
`XI. CLAIMS CHART FOR DEPENDENT CLAIMS 2 AND 9-13 ....................... 71 
`XII.PAYMENT OF FEES ....................................................................................... 71 
`
`
`
`XI. CLAIMS CHART FOR DEPENDENT CLAIMS 2 AND 9-13 ..................... ..71
`
`XII.PAYI\/[ENT OF FEES ..................................................................................... ..71
`
`
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`3
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`
`EXHIBIT LIST
`Exhibit Name
`Ex. #
`1001 U.S. Patent No. RE38,551 (“the ’551 patent”)
`1002 Declaration of Dr. Binghe Wang
`1003 Declaration of Dr. Clayton Heathcock from IPR2014-01126
`1004 Joint Statement of Uncontested Facts
`1005 U.S. Patent No. 5,773,475 (“the ’475 Patent”)
`1006 Excerpt from U.S. Patent Application No. 08/818,688
`1007 District Court Claim Construction Opinion
`1008 Philippe LeGall, 2-Substituted-2-acetamido-N-benzylacetamides.
`Synthesis, Spectroscopic and Anticonvulsant Properties (Dec. 1987)
`(“LeGall”)
`1009 U.S. Patent No. 5,378,729 (“the ’729 Patent”)
`1010 Choi et al., Trimethylsilyl Halides: Effective Reagents for the Synthesis of
`β-Halo Amino Acid Derivatives, Tet. Lett., Vol. 36(39), pg. 7011 (1995)
`(“Choi 1995”)
`1011 Purdie et al., The Alkylation of Sugars, J.A.C.S.Vol. 83, pg. 1021 (1903)
`(“Purdie”)
`1012 Kohn et al., Preparation and Anticonvulsant Activity of a Series of
`Functionalized α-Heteroatom-Substituted Amino Acids, J. Med. Chem.
`Vol. 34, pg. 2444 (1991) (“Kohn 1991”)
`1013 Silverman, R. B., The Organic Chemistry of Drug Design and Drug
`Action, Academic Press (1992) (“Silverman”)
`1014 Development of New Stereoisomeric Drugs, U.S. F.D.A., May 1, 1992
`1015 Cortes et al., Effect of Structural Modification of the Hydantoin Ring on
`Anticonvulsant Activity, J. Med. Chem., Vol. 28, pg. 601 (1985)
`(“Cortes 1985”)
`1016 LeGall et al., Synthesis of Functionalized Non-Natural Amino Acid
`Derivatives via Amidoalkylation Transformations, Int. J. Peptide
`Protein Res. Vol. 32, pg. 279 (1988) (“LeGall 1988”)
`
`4
`
`

`

`
`
`1017 Kohn et al., Synthesis and Anticonvulsant Activities of α-Heterocyclic α-
`Acetamido-N-benzylacetamide Derivatives, J. Med. Chem. Vol. 36, pg.
`3350 (1993)
`1018 Kohn et al., Preparation and Anticonvulsant Activity of a Series of
`Functionalized α-Aromatic and α-Heteroaromatic Amino Acids, J. Med.
`Chem. Vol. 33, pg. 919 (1990)
`1019 U.S. Patent No. 5,654,301 (“the ’301 Patent”)
`1020 Patent Term Extension Request in U.S. Patent No. 5,654,301
`1021 FDA Guideline for Industry, November 1994
`1022 Schmidt, R., Dose-Finding Studies in Clinical Drug Development, Eur. J.
`Clin. Pharmacol, Vol. 34, pg. 15 (1988)
`1023 Isbell, H. S., The Optical Rotation of the Various Asymmetric Carbon
`Atoms in the Hexose and Pentose Sugars, B. S. Jour. Research, Vol. 5, pg.
`1041 (1929)
`1024 Wilson and Gisvold’s Textbook of Organic Medicinal Chemistry,
`Physicochemical Properties in Relation to Biologic Action, (Delgado J.
`N. & Remers W. A., eds. 1991) (Wilson)
`1025 Thornber, C. W., Isosterism and Molecular Modification in Drug Design,
`Chem. Soc. Rev., Vol. 8(4) (1979)
`1026 Reissue Declaration in Reissue of U.S. Patent No. 5,773,475
`1027 Subpoena directed to The University of Houston
`1028 Texas Public Information Act Requests and Responses
`1029 Zhou et al., Decisions under Uncertainty: the Fuzzy Compromise
`Decision Support Problem, Eng. Opt. Vol. 20, pg. 21 (1992)
`1030 Mistree et al., A Decsion-Based Perspective for the Design of Methods
`for Systems Design, (1989)
`1031 Mistree et al., A Decision-based Approach to Concurrent Design,
`Concurrent Engineering: Contemporary Issues and Modern Design
`Tools, (Parsaei, H. R. & Sullivan W. G. Eds. 1993)
`1032 Ingram W. T., Concerning Periodic Points in Mappings of Continua, J.
`Am. Math. Soc., Vol. 104(2) (1988)
`1033 Mattson, Current Challenges in the Treatment of Epilepsy, Neurology,
`Vol. 44(suppl. 5), pg. 84 (1994)
`
`

`

`
`
`
`
`
`
`
`1034 Löscher et al., New Avenues for Anti-Epileptic Drug Discovery and
`Development, Nature Reviews: Drug Discovery, Vol. 12, pg. 12 (2013)
`
`1035 Cohen authorized amendment in U.S. Patent Application No. 08/818,688
`
`
`
`
`
`6
`
`

`

`
`
`
`Petitioner Breckenridge Pharmaceutical, Inc. (“Petitioner” or
`
`“Breckenridge”) requests that the Board institute inter partes review (“IPR”) of
`
`claims (1-13) of U.S. Patent No. RE 38,551 to Kohn (“the ’551 patent”) (Ex.
`
`1001), and that these claims be canceled as unpatentable over the prior art. Inter
`
`partes review of claims 1-13 of the ’551 patent, was instituted in IPR2016-00204
`
`on May 23, 2016, based on a petition filed by Argentum Pharmaceuticals LLC
`
`(“Argentum”). For the sake of completeness and efficiency, the present Petition is
`
`substantially identical to the petition in IPR2016-00204. Petitioner is requesting
`
`however, that the Board institute only on the Grounds instituted in IPR2016-00204,
`
`i.e., Grounds 3A and 3B as to claims 1-13. A Motion for Joinder with IPR2016-
`
`00204 is filed concurrently with this Petition.
`
`
`
`
`
`I. MANDATORY NOTICES UNDER 37 C.F.R. § 42.8
`
`A. Real Parties-In-Interest under 37 C.F.R. § 42.8(b)(1)
`
`Pursuant to 37 C.F.R. § 42.8(b)(1), Petitioner certifies that Breckenridge,
`
`Pensa Pharma S.A., and Corporacion Quimico Farmaceutica Esteve, S.A., MSN
`
`Laboratories Pvt. Ltd., MSN Pharmachem Pvt. Ltd., and Vennoot Pharmaceuticals,
`
`LLC are the real parties-in-interest.
`
`
`
`B. Related Matters under 37 C.F.R. § 42.8(b)(2)
`
`
`
`Pursuant to 37 C.F.R. § 42.8(b)(2), Petitioner is aware of the following
`
`matters: Argentum Pharmaceuticals LLC v. Research Corporation Technologies,
`
`
`
`7
`
`

`

`
`
`Inc., IPR2016-00204; Mylan Pharmaceuticals Inc. v. Research Corporation
`
`Technologies, Inc., IPR2016-01101; Actavis, Inc. et al. v. Research Corporation
`
`Technologies, Inc., IPR2014-01126; Ex Parte Reexamination Control No.
`
`90/013,709; and the proceedings listed in the table below.
`
`Case Caption
`UCB, Inc. et al. v. Teva Pharmaceuticals USA Inc.
`et al., 1:13-cv-01148-LPS (D. Del.)
`UCB, Inc. et al. v. Accord Healthcare Inc. et al.,
`1:13-cv-01206-LPS (D. Del.)
`UCB, Inc. et al. v. Alembic Pharmaceuticals Ltd.,
`1:13-cv-01207-LPS (D. Del.)
`UCB, Inc. et al. v. Amneal Pharmaceuticals, LLC
`et al., 1:13-cv-01208-LPS (D. Del.)
`UCB, Inc. et al. v. Apotex Corp. et al., 1:13-cv-
`01209-LPS (D. Del.)
`UCB, Inc. et al. v. Aurobindo Pharma Ltd. et al.,
`1:13-cv-01210-LPS (D. Del.)
`UCB, Inc. et al. v. Breckenridge Pharmaceutical
`Inc. et al., 1:13-cv-01211-LPS (D. Del.)
`UCB, Inc. et al. v. Glenmark Generics Inc. USA et
`al., 1:13-cv-01212-LPS (D. Del.)
`UCB, Inc. et al. v. Hetero USA Inc. et al., 1:13-cv-
`01213-LPS (D. Del.)
`UCB, Inc. et al. v. Mylan Pharmaceuticals Inc. et
`al., 1:13-cv-01214-LPS (D. Del.)
`UCB, Inc. et al. v. Ranbaxy Laboratories Ltd. et
`al., 1:13-cv-01215-LPS (D. Del.)
`UCB, Inc. et al. v. Sandoz Inc., 1:13-cv-01216-
`LPS (D. Del.)
`UCB, Inc. et al. v ScieGen Pharmaceuticals Inc. et
`al., 1:13-cv-01217-LPS (D. Del.)
`UCB, Inc. et al. v Sun Pharma Global FZE et al.,
`1:13-cv-01218-LPS (D. Del.)
`UCB, Inc. et al. v. Watson Laboratories Inc. -
`Florida et al., 1:13-cv-01219-LPS (D. Del.)
`
`Disposition
`
`closed
`
`pending
`
`pending, consolidated with
`1:13-cv-01206-LPS (D. Del.)
`pending, consolidated with
`1:13-cv-01206-LPS (D. Del.)
`pending, consolidated with
`1:13-cv-01206-LPS (D. Del.)
`pending, consolidated with
`1:13-cv-01206-LPS (D. Del.)
`pending, consolidated with
`1:13-cv-01206-LPS (D. Del.)
`closed
`
`closed
`
`pending, consolidated with
`1:13-cv-01206-LPS (D. Del.)
`closed
`
`closed
`
`closed
`
`pending, consolidated with
`1:13-cv-01206-LPS (D. Del.)
`pending, consolidated with
`1:13-cv-01206-LPS (D. Del.)
`
`
`
`8
`
`

`

`
`
`UCB, Inc. et al. v. Zydus Pharmaceuticals (USA)
`Inc. et al., 1:13-cv-01220-LPS (D. Del.)
`UCB, Inc. et al. v. Apotex Corp. et al., 1:14-cv-
`00834-LPS (D. Del.)
`UCB, Inc. et al. v. Sun Pharma Global FZE et al.,
`1:13-cv-05514 (N.D. Ill.)
`UCB, Inc. et al., v. Zydus Pharmaceuticals (USA),
`Inc. et al., 3:13-cv-04021 (D.N.J.)
`UCB, Inc. et al. v. Aurobindo Pharma Ltd. et al.,
`1:16-cv-00451-UNA (D. Del.)
`UCB, Inc. et al. v. Hetero USA Inc. et al., 1:16-cv-
`00452-UNA (D. Del.)
`
`
`pending, consolidated with
`1:13-cv-01206-LPS (D. Del.)
`pending, consolidated with
`1:13-cv-01206-LPS (D. Del.)
`closed
`
`closed
`
`pending
`
`pending
`
`In IPR2014-01126, Patent Owner avoided trial against the ’551 patent by
`
`challenging the prior art status of LeGall.1 Prelim. Resp. 27-30. In UCB, Inc. et.
`
`al. v. Accord Healthcare, Inc. et. al., C.A. No. 1:13-cv-1206-LPS (D. Del.), Patent
`
`Owner admitted that LeGall “constitutes a ‘printed publication’ within the meaning
`
`of 35 U.S.C. § 102(b).” Ex. 1004 at ¶ 87.
`
`
`
`
`
`
`
`1 Breckenridge recognizes the Board’s decision to institute Grounds 3A and 3B in
`
`IPR2016-00204 does not rely on LeGall. Discussions of LeGall are included
`
`herein to provide consistency with Argentum’s petition in IPR2016-00204 and also
`
`a subsequent petition filed by Mylan Pharmaceuticals Inc. in IPR2016-01101,
`
`which is substantially identical to Argentum’s petition.
`
`
`
`9
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`

`
`
`
`
`
`C.
`
`Lead and Backup Counsel under 37 C.F.R. § 42.8(b)(3)
`
`Backup Counsel:
`Daniel R. Evans, Esq.
`Registration No. 55,868
`MERCHANT & GOULD P.C.
`191 Peachtree Street, NE
`Suite 3800
`Atlanta, GA 30303
`Main Telephone: (404) 954-5100
`Main Facsimile: (404) 954-5099
`devans@merchantgould.com
`
`
`
`Lead Counsel:
`Matthew L. Fedowitz, Esq.
`Registration No. 61,386
`MERCHANT & GOULD P.C.
`1900 Duke Street
`Suite 600
`Alexandria, VA 22314
`Main Telephone: (703) 684-2500
`Main Facsimile: (703) 684-2501
`mfedowitz@merchantgould.com
`
`
` Power of Attorney is being filed concurrently herewith in accordance with
`
` A
`
`37 C.F.R. § 42.10(b).
`
`
`
`D.
`
`Service Information under 37 C.F.R. § 42.8(b)(4)
`
`Papers concerning this matter should be served by EXPRESS MAIL,
`
`hand-delivery, or electronic mail at the following address:
`
`
`
`
`
`Mailing Address: Matthew L. Fedowitz, Esq.
`Merchant & Gould P.C.
`1900 Duke Street, Suite 600
`Alexandria, VA 22314
`Electronic Mail: mfedowitz@merchantgould.com
`Main Telephone: 703-684-2500
`Main Facsimile: 703-684-2501
`
`
`
`
`
`
`
`
`10
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`

`

`
`
`
`
`
`
`
`
`II. REQUIREMENTS FOR IPR UNDER 37 C.F.R. § 42.104
`
`A. Grounds For Standing Under 37 C.F.R. § 42.104(a)
`
`Pursuant to 37 C.F.R. § 42.104(a), Petitioner hereby certifies that the ’551
`
`patent is available for inter partes review, and that the Petitioner is not barred or
`
`estopped from requesting inter partes review of the challenged claims of the ’551
`
`patent on the grounds identified in this Petition. Neither Petitioner nor any privy of
`
`Petitioner has received a final written decision under 35 U.S.C. § 318(a) with
`
`respect to any claim of the ’551 patent on any ground that was raised or could have
`
`been raised by Petitioner or its privies in any inter partes review, post grant
`
`review, or covered business method patent review.
`
`Identification of Challenge and Precise Relief Requested,
`B.
`37 C.F.R. § 42.104(b)
`
` Petitioner requests cancellation of claims 1-13 of the ’551 patent on
`
`
`
`Grounds 3A and 3B, but has listed the grounds of unpatentability found in the
`
`Petition for IPR2016-00204 to provide full disclosure of the record:
`
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`
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`11
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`

`
`
`
`Ground
`
`Claims
`
`1A
`1B
`
`2A
`2B
`
`3A
`3B
`
`4A
`4B
`
`
`1, 3-8
`2, 9-13
`1-9
`10-13
`1-9
`10-13
`1-9
`10-13
`
`Reference(s)
`
`Choi and Kohn 1991
`Choi, Kohn 1991, and ’729 patent
`
`Basis
`§ 102(b) LeGall
`LeGall and ’729 patent
`§ 103
`§ 103
`§ 103
`§ 103
`§ 103
`§ 103
`§ 103
`
`Kohn 1991 and Silverman
`Kohn 1991, Silverman, and ’729 patent
`
`Cortes and Kohn 1991
`Cortes, Kohn 1991, and ’729 patent
`
`Grounds 1-4 are substantially identical to the grounds presented in the
`
`petition in IPR2016-00204, including Grounds 3A and 3B that were instituted by
`
`the Board, challenging the same claims over the same prior art and using the same
`
`arguments and expert testimony. Each of Grounds 1-4 identifies a different prior
`
`art compound that independently would have served as a “starting reference point
`
`or points,” from which a person of ordinary skill in the art (“POSA”) would have
`
`easily arrived at lacosamide—the compound claimed in the ’551 patent. See Eisai
`
`Co. Ltd. v. Dr. Reddy’s Labs. Ltd., 533 F.3d 1353, 1359 (Fed. Cir. 2008); Altana
`
`Pharma AG v. Teva Pharms. USA, Inc., 566 F.3d 999, 1008-1009 (Fed. Cir. 2009)
`
`(affirming the selection of up to “18 exemplary compounds” as lead compounds
`
`and rejecting the notion that chemical obviousness requires “only a single lead
`
`compound”).
`
`
`
`12
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`

`
`
`
`This case presents a unique set of facts that establish the uncommon instance
`
`in which a patent claim to a compound is anticipated and/or rendered obvious.
`
`Here, the compound lacosamide was first disclosed in the thesis of the graduate
`
`student of the ’551 patent’s named inventor approximately eight years before the
`
`relevant patent application was filed. Even putting aside that novelty destroying
`
`reference, at least three other specific combinations of prior art would have
`
`directed a person of ordinary skill in the art directly to lacosamide and its use. This
`
`is not a case of selecting a single favorable lead compound so that one preordains
`
`the obviousness analysis. Rather, this petition presents four separate examples of
`
`applying clear teachings in the prior art (as summarized in the figure below) to
`
`establish that the claims to lacosamide are unpatentable.
`
`Moreover, the prior art contained repeated statements directing one to use
`
`the R-isomer. The various references stressed that the R-isomer was the
`
`biologically active isomer. Finally, the therapeutic composition and method claims
`
`in the ’551 patent add no specific limitations other than standard, generic
`
`limitations, such as a “pharmaceutical carrier” and “administering to said animal.”
`
`With the prior art data confirming the anticonvulsant activity of the compounds,
`
`those generic limitations cannot render the claimed subject matter patentable.
`
`
`
`13
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`

`

`
`
`
`
`Petitioner supports its challenges with a Declaration of Dr. Binghe Wang
`
`
`
`(“Wang Decl.”) (Ex. 1002) prepared for IPR2016-002042, as well as a Declaration
`
`
`2 The Wang Decl. is an exact copy of Dr. Wang’s declaration from IPR2106-
`
`00204, which was relied upon by the Board in that proceeding. Dr. Wang’s
`
`IPR2016-00204 Declaration is cited in this Petition to avoid unnecessary cost and
`
`to advance efficiency in this instance. As mentioned above, this Petition is
`
`presented along with a motion to join IPR2016-00204, and by using the same
`
`
`
`14
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`

`

`
`
`of Dr. Clayton H. Heathcock (“Heathcock Decl.”) (Ex. 1003) from IPR2014-
`
`01126.
`
`
`
`III. SUMMARY OF THE ’551 PATENT
`
`The ’551 patent lists Harold Kohn as its sole inventor and Research
`
`Corporation Technologies, Inc. as the assignee. The ’551 patent is a reissue of U.S.
`
`Patent No. 5,773,475 (“the ’475 patent”) (Ex. 1005), which issued from U.S.
`
`Patent Application No. 08/818,688 (“the ’688 application”) filed on March 17,
`
`1997, and which claims priority to U.S. Provisional Application No. 60/013,522
`
`filed on March 15, 1996 (the earliest possible effective date). As explained in Part
`
`IX, infra, the ’551 patent is not entitled to the earlier 1996 priority date.
`
`Claim 1 is the sole independent claim in the ’551 patent. Claim 1 reads:
`
`1. A compound in the R configuration having the
`
`formula:
`
`wherein
`
`
`
`
`Declaration, Petitioner has eliminated the need for analysis of another declaration
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`or the addition of a new expert.
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`15
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`Ar is phenyl which is unsubstituted or substituted with at
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`least one halo group;
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`Q is lower alkoxy, and
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`Q1 is methyl.
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`Claims 2-9 are compound claims depending directly or indirectly from claim 1.
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`Claim 8 is lacosamide, specified by its chemical name: “The compound according
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`to claim 1 which is (R)-N-Benzyl 2-Acetamido-3-methoxypropionamide.” The
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`structure of lacosamide is shown below (wherein Ar is benzyl, Q is methoxy, and
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`Q1 is methyl):
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`Claim 10 recites “[a] therapeutic composition comprising an anticonvulsant
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`effective amount of a compound according to any one of claims 1-9 and a
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`pharmaceutical carrier therefor.”
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`Claims 11-13 are method claims. Claim 11 reads:
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`11. A method of treating central nervous system disorders in an
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`animal comprising administering to said animal in need thereof an
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`anticonvulsant effective amount of a compound according to any one
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`of claims 1-9.
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`16
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`Claim 12 depends from claim 11 and specifies that the “the animal is a
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`mammal.” Claim 13 depends from claim 12 and specifies that “the mammal is a
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`human.”
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`IV. PREVIOUS PETITIONS
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`As mentioned above, in IPR2016-00204, filed by Argentum Pharmaceuticals
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`LLC, an unrelated party, the Board instituted review of claims 1-9 (Ground 3A),
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`based on Kohn 1991 and Silverman, and of claims 10-13 (Ground 3B), based on
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`Kohn 1991, Silverman, and the ’729 patent. On May 25, 2016, Mylan
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`Pharmaceuticals Inc. filed a petition which is substantially identical to the petition
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`in IPR2016-00204 along with a Motion for Joinder requesting joinder as to
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`Grounds 3A-3B only. See IPR2016-01101, Paper Nos. 2 and 3.
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`The Board previously declined to institute a review in IPR2014-01126.
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`There, Patent Owner argued that LeGall was not shown to be prior art, and the
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`Board agreed. (Prelim. Resp. 27-30.) The Board also found that the petition failed
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`to establish a reasonable likelihood on three asserted grounds of unpatentability: (1)
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`anticipation by the ’301 patent, (2) anticipation by LeGall, and (3) obviousness over
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`LeGall and the ’729 patent. See IPR2014-01126, Paper 22 (“Dec.”). For the first
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`ground (anticipation by the ’301 patent), the petitioners alleged that claims 39-44 of
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`the ’301 patent, together with preferences recited in the ’301 patent, anticipate
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`lacosamide. The Board disagreed, finding no anticipation based on the preferred
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`17
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`genus of compounds. Dec. 6-9. For the second ground (anticipation by LeGall), the
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`Board found that LeGall was not shown to be a “printed publication” under §
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`102(b). Id. at 12-13. Finally, the third ground was denied for the same reason as the
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`second. Id. at 14.
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`Breckenridge was one of many petitioners in IPR2014-01126. The
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`petitioners in IPR2014-01126 were Actavis, Inc., Actavis Laboratories FL, Inc.,
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`Actavis Pharma, Inc., Amneal Pharmaceuticals of New York, LLC, Aurobindo
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`Pharma Ltd., Aurobindo Pharma USA, Inc., Breckenridge, Vennoot
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`Pharmaceuticals, LLC, Sandoz Inc., Sun Pharma Global FZE, and Sun
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`Pharmaceuticals Industries, Ltd. Breckenridge notes Grounds 3A and 3B for which
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`it requests joinder in its accompanying Motion for Joinder are different from the
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`three asserted grounds of unpatentability in IPR2014-01126, which the Board
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`denied. Breckenridge also notes that in IPR2016-00204, the Board found that the
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`asserted grounds in IPR2014-001126 were different than the asserted grounds in
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`IPR2016-00204. Paper 19, p. 9, footnote 7 in IPR2016-00204.
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`V. CLAIM CONSTRUCTION UNDER 37 C.F.R. § 42.104(b)(3)
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`
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`A.
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`“Therapeutic Composition” in Claim 10
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`In UCB, Inc. et al. v. Accord Healthcare Inc. et al., 1:13-cv-01206-LPS (D.
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`Del.), the court construed one term in the ’551 patent: “therapeutic
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`composition,” which appears only in the preamble of claim 10. To the extent Patent
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`18
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`
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`Owner attempts to rely on the district court’s construction, that construction was
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`unnecessary and, in any event, is not the broadest reasonable interpretation
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`(“BRI”).
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`First, claim 10 is a product claim that recites two limitations: an
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`“anticonvulsant effective amount” of the compound, and a “pharmaceutical
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`carrier.”3 The body of the claim sets forth all limitations of the claimed invention.
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`The preamble, “a therapeutic composition,” does not “give life, meaning, and
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`vitality” to the claim, but merely describes an intended purpose, and is therefore
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`non-limiting. See Rowe v. Dror, 112 F.3d 473, 478 (Fed. Cir. 1997) (“[W]here a
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`patentee defines a structurally complete invention in the claim body and uses the
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`preamble only to state a purpose or intended use for the invention, the preamble is
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`not a claim limitation.”).
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`Second, the term “therapeutic composition” does not specify any additional
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`physical structure or physical components other than the two recited in the body of
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`the claim. The ’551 patent does not provide a definition of the term “therapeutic
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`composition”, nor does the patent use that term in any special manner, other than
`
`introducing the claimed compound in a pharmaceutical carrier. By definition, a
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`3 Claim 10 reads in full: “A therapeutic composition comprising [1] an
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`anticonvulsant effective amount of a compound according to any one of claims 1-9
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`and [2] a pharmaceutical carrier therefor.”
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`19
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`compound within the genus, together with a pharmaceutical carrier, is a therapeutic
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`composition within the meaning of claim 10.
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`Third, the BRI of “therapeutic composition” is not confined to the additional
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`limitations imposed by the district court. Specifically, applying Phillips, the district
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`court construed the term to mean “[a] composition suitable for use as a treatment
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`regimen over an extended period of time (chronic administration).” Ex. 1007 at 5.
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`The BRI cannot be limited to only a composition that is administered “over an
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`extended period of time” and for “chronic administration.” Nothing in the claim
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`limits the composition to “chronic administration.” See Ex. 1001 cols. 9-10
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`(reciting a litany of acceptable dosage forms and excipients).
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`Additionally, the claims do not numerically limit the term “anticonvulsant
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`effective amount.” Applying the BRI, this term should be construed to mean any
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`amount that could provide an anticonvulsant effective amount of the compound
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`when administered. The specification again does not define a specific range, but
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`does provide various ranges as guidance. For instance, the ’551 patent states that
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`“[a] unit dosage form can, for example, contain the principal active compound in
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`amounts ranging from about 5 to about 1000 mg.” Ex. 1001 at 10:52-57. The ’551
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`patent also states that the compositions can contain “from about 1 to about 750
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`mg/ml of carrier,” id. at 10:59, or “preferred . . . between about 5 and 100 mg of
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`active compound,” id. at 9:23-26, or “at least 1% of active compound,” id. at 9:17-
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`
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`20
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`18. At a minimum, a composition containing about 5 to about 1000 mg of the
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`claimed compound, and a pharmaceutical carrier, is a “therapeutic composition”
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`within the meaning of claim 10.
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`
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`B.
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`“A Compound in the R Configuration” in Claim 1
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`Petitioner does not believe that the phrase “a compound in the R
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`configuration” in claim 1 needs to be construed. Patent Owner, however, put that
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`phrase into issue in IPR2014-01126. Patent Owner’s preliminary response did not
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`propose a construction of the term but instead quibbled that the petitioners’
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`construction “improperly fails to treat the R stereoisomer, the S stereoisomer and
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`the racemic mixture as the different compounds that they are.” Prelim. Resp. at 13.
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`Here, the BRI of “a compound in the R configuration” covers R-isomer
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`compounds, whether the R-isomer is substantially pure or mixed with the S-
`
`isomer, such as a racemic mixture or isomerically enriched mixture. But the claim
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`does not cover pure S-isomer, which would have no R-isomer. The declaration of
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`Prof. Wang explains why a POSA would have this understanding. Ex. 1002,
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`Section IA, ¶¶ 9-13.
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`Claim 2 confirms this construction, which further limits claim 1 to
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`“substantially enantiopure.” Applying claim differentiation, claim 2 further
`
`restricts the amount of S-isomer that is included in the scope of the claim,
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`specifying that the compound be “substantially enantiopure.” The ’551 patent
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`
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`21
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`explains that “substantially enantiomerically pure” can include at most about10%
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`(w/w) of the S-isomer. Ex. 1001 at 5:11-19.
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`Claim 9 also confirms the above construction, which specifies the
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`“compound according to claim 8”—i.e., (R)-N-benzyl-2-acetamido-3-
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`methoxypropionamide—“contains at least 90% (w/w) R stereoisomer.” Because
`
`claim 9 depends from claim 1, and because claim 9 includes compositions having
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`up to 10% (w/w) of the S-isomer, so must claim 1. Moreover, claim 1 does not limit
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`the amount of R- or S-isomer present in the composition—only that it cannot be
`
`solely S. Nor does the specification provide any lower numerical limit for claim 1,
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`other that it cannot be solely S. To the extent Patent Owner argues that claim 1
`
`requires any level of enantiomeric purity beyond the presence of a single R-isomer
`
`molecule, then claims 2 and 9 are nonsensical and the Board should hold all claims
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`indefinite under 35 U.S.C. § 112, second paragraph. See BlackBerry Corp. v.
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`MobileMedia Ideas LLC, IPR2013-00036 (Paper 65) (terminating IPR after finding
`
`claims indefinite).
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`VI. LEVEL OF SKILL AND KNOWLEDGE IN THE ART
`
`
`As of March 15, 1996 (the earliest possible effective date), a hypothetical
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`POSA would “be aware of all the pertinent prior art” at the time of the alleged
`
`invention. Custom Accessories, Inc. v. Jeffrey-Allan Indus.