Paper No. ______
`
`Filed on behalf of Sawai
`By: Kenneth J. Burchfiel
`
`Travis B. Ribar
`
`Chidambaram S. Iyer
`
`Sughrue Mion, PLLC
`
`2100 Pennsylvania Ave., NW
`
`Washington, DC 20037
`
`Telephone: 202-293-7060
`
`Facsimile: 202-293-7860
`
`email:
`kburchfiel@sughrue.com
`
`
`
`tribar@sughrue.com
`
`
`
`ciyer@sughrue.com
`
`
`IN THE UNITED STATES PATENT AND TRADEMARK OFFICE
`__________________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`__________________
`
` SAWAI USA, INC., AND SAWAI PHARMACEUTICAL CO., LTD.
`Petitioners
`
`v.
`
`NISSAN CHEMICAL INDUSTRIES LTD.
`Patent Owner
`__________________
`
`Case No. IPR2015-01647
`Patent No. 5,856,336
`__________________
`
`
`PETITION FOR INTER PARTES REVIEW
`OF U.S. PATENT NO. 5,856,336
`
`
`
`
`

`

`TABLE OF CONTENTS
`
`Page
`
`TABLE OF AUTHORITIES ...................................................................................... IV
`
`EXHIBITS CITED ...................................................................................................... VI
`
`I.
`
`II.
`
`INTRODUCTION .............................................................................................. 1
`
`COMPLIANCE WITH REQUIREMENTS FOR AN INTER
`PARTES REVIEW PETITION .......................................................................... 5
`
`A. Grounds for Standing ............................................................................ 5
`
`B.
`
`Payment of Fee for Inter Partes Review ............................................... 5
`
`C. Mandatory Notices (37 C.F.R. §42.8(b)) .............................................. 5
`
`1.
`
`2.
`
`3.
`
`4.
`
`5.
`
`Each Real Party-in-Interest (37 C.F.R. §42.8(b)(1)) .................. 5
`
`Related Matters (37 C.F.R. §42.8(b)(2)) .................................... 5
`
`Lead and Backup Counsel (37 C.F.R. §42.8(b)(3)) .................... 6
`
`Service Information (37 C.F.R. §42.8(b)(4)) .............................. 7
`
`Power of Attorney (37 C.F.R. §42.10(b)) ................................... 7
`
`D.
`
`Statement of precise relief requested .................................................... 7
`
`E.
`
`F.
`
`Identification of Prior Art and Challenged Claims ............................... 7
`
`Supporting Evidence Relied Upon ........................................................ 7
`
`III. THE ʼ336 PATENT ............................................................................................ 8
`
`A.
`
`Field of the ʼ336 Patent ......................................................................... 8
`
`B.
`
`C.
`
`Claims 1 and 2 of the ʼ336 Patent ......................................................... 9
`
`The Broadest Reasonable Construction of Claim Terms ...................... 9
`
`IV. THE EFFECTIVE FILING DATE OF CLAIMS 1 AND 2 OF
`THE ʼ336 PATENT IS, AT THE EARLIEST, AUGUST 3, 1988 ................ 10
`
`
`
`
`
`i
`
`

`

`A.
`
`B.
`
`C.
`
`D.
`
`Single species claims require full written description
`support in order to be entitled to benefit of priority ............................ 11
`
`The failure of JP ʼ224 and JP ʼ585 to name a calcium salt
`is fatal to any benefit claim ................................................................. 12
`
`JP ʼ224 does not provide written description support for a
`½ calcium salt ...................................................................................... 13
`
`JP ʼ585 does not contain written description support for a
`½ calcium salt ...................................................................................... 14
`
`V. MEVALONOLACTONES IN THE TREATMENT OF
`HYPERCHOLERSTEROLEMIA ................................................................... 15
`
`VI. GROUND 1: CLAIMS 1 AND 2 OF THE ʼ336 PATENT ARE
`OBVIOUS OVER PICARD IN VIEW OF KESSELER ................................ 25
`
`A.
`
`Picard discloses derivatives of compactin useful in
`inhibiting HMG-CoA reductase .......................................................... 25
`
`1.
`
`2.
`
`3.
`
`A POSA would have selected Picard’s Example 3
`compound as a lead compound ................................................. 26
`
`Patent Owner admitted that the ½ calcium salt of
`Picard’s Example 3 compound is prior art................................ 29
`
`A POSA would have found it obvious to change
`the R2 isopropyl group to a cyclopropyl group ......................... 29
`
`B.
`
`Kessler provides data showing the superior activity of
`analogous cyclopropyl-substituted compounds .................................. 31
`
`1.
`
`A POSA would have found it obvious to substitute
`a ½ calcium salt for the sodium salt .......................................... 36
`
`2.
`
`The methods of claim 2 would have been obvious ................... 38
`
`C.
`
`D.
`
`Patent Owner cannot rely on ex parte Declaration
`evidence submitted during prosecution ............................................... 39
`
`The results shown in the Declarations were not
`unexpected ........................................................................................... 39
`
`
`
`
`
`ii
`
`

`

`E.
`
`The results shown in the Declarations do not compare the
`claimed compound with the closest compounds of the
`prior art ................................................................................................ 40
`
`VII. PATENT OWNER DISCLAIMED THE COMPOUND OF
`CLAIMS 1 AND 2 OF THE ‘336 PATENT ................................................... 41
`
`A.
`
`Introduction ......................................................................................... 41
`
`B.
`
`C.
`
`D.
`
`E.
`
`F.
`
`G.
`
`H.
`
`Disclaimer of a claim .......................................................................... 48
`
`Patent Owner disclaimed the compound of claim 1 of the
`ʼ336 Patent during prosecution of its grandparent
`application ........................................................................................... 49
`
`The subject matter that Patent Owner lost in the
`interferences ........................................................................................ 53
`
`Canceled claim 10 was merely an obvious analog of the
`claims that Patent Owner lost in the interferences .............................. 55
`
`Claim 1 of the ‘336 Patent is obvious over the claims
`Patent Owner lost in the interferences ................................................ 57
`
`Claim 1 of the ‘336 Patent should “suffer the same
`consequences that would have befallen” if it were
`included in the interferences ............................................................... 58
`
`Evidence submitted during prosecution of the ʼ336 Patent
`does not compare the compound of formula A of claims
`1 and 2 of the ʼ336 Patent with the compounds lost in the
`interferences ........................................................................................ 58
`
`VIII. PATENT OWNER’S BURDEN IN THE PROPOSED IPR .......................... 60
`
`IX. CONCLUSION ................................................................................................. 60
`
`
`
`
`
`
`
`iii
`
`

`

`TABLE OF AUTHORITIES
`
`CASES
`
`Ariad Pharm., Inc. v. Eli Lilly & Co., 598 F.3d 1336, 1352 (Fed. Cir.
`2010) (en banc) .............................................................................................. 11, 12
`
`Daiichi Sankyo Co., Ltd. v. Matrix Labs., Ltd., 619 F.3d 1346, 1354
`(Fed. Cir. 2010) ............................................................................................. 21, 22
`
`Fujikawa v. Wattanasin, 93 F.3d 1559 (Fed. Cir. 1996) .............................. 2, 42, 53
`
`In re Deckler, 977 F.2d 1449, 1452 (Fed. Cir. 1992) ....................................... 46, 58
`
`In re Fout, 675 F.2d 297 ..........................................................................................37
`
`In re Nomiya, 509 F.2d 566, 570-71 (CCPA 1975) .................................................37
`
`In re Ogiue, 517 F.2d 1382, 1390 (CCPA 1975) .............................................. 48, 52
`
`In re Ruschig, 379 F.2d 990, 995 (CCPA 1967) .............................................. 11, 12
`
`Lockwood v. Am. Airlines, 107 F.3d 1565, 1571–72 (Fed. Cir. 1997) ....................11
`
`Motionpoint Corp., Petitioner, CBM2014-00066, 2014 WL
`3704044, at *14 (July 23, 2014) ...........................................................................12
`
`Novozymes A/S v. DuPont Nutrition Biosciences APS, 723 F.3d
`1336, 1350 (Fed. Cir. 2013) .......................................................................... 11, 12
`
`Otsuka Pharm. Co., Ltd. v. Sandoz, Inc., 678 F.3d 1280, 1295 (Fed.
`Cir. 2012) ....................................................................................................... 21, 23
`
`Takeda Chem. Indus. v. Alphapharm Pty., Ltd., 492 F.3d 1350, 1356
`(Fed. Cir. 2007) ....................................................................................................22
`
`STATUTES
`
`35 U.S.C. § 102(a) ...................................................................................................25
`
`35 U.S.C. § 102(e) ...................................................................................................25
`
`35 U.S.C. § 103 .......................................................................................................... 1
`
`35 U.S.C. § 103(a) .................................................................................................7, 8
`
`
`
`
`
`iv
`
`

`

`35 U.S.C. § 112 ........................................................................................................11
`35 U.S.C. § 112 ...................................................................................................... ..11
`
`
`
`RULES
`RULES
`
`MPEP § 2308.03 ......................................................................................................59
`MPEP § 2308.03 .................................................................................................... ..59
`
`Rule 637(c)(4)(ii) .....................................................................................................53
`Rule 637(c)(4)(ii) ................................................................................................... ..53
`
`
`
`REGULATIONS
`REGULATIONS
`
`37 C.F.R. § 42.100(b) ................................................................................................ 9
`37 C.F.R. § 42.100(b) .............................................................................................. ..9
`
`37 C.F.R. § 42.104(a) ................................................................................................. 5
`37 C.F.R. § 42.104(a) ............................................................................................... ..5
`
`37 C.F.R. § 42.104(b) ................................................................................................ 7
`37 C.F.R. § 42.104(b) .............................................................................................. ..7
`
`37 C.F.R. § 42.104(b)(3) ............................................................................................ 9
`37 C.F.R. § 42.104(b)(3) .......................................................................................... ..9
`
`37 C.F.R. § 42.104(b)(4) ............................................................................................ 7
`37 C.F.R. § 42.104(b)(4) .......................................................................................... ..7
`
`37 C.F.R. § 42.104(b)(5) ............................................................................................ 7
`37 C.F.R. § 42.104(b)(5) .......................................................................................... ..7
`
`37 C.F.R. § 42.22(a)(1) .............................................................................................. 7
`37 C.F.R. § 42.22(a)(1) ............................................................................................ ..7
`
`37 C.F.R. § 42.22(a)(2) .............................................................................................. 7
`37 C.F.R. § 42.22(a)(2) ............................................................................................ ..7
`
`37 C.F.R. §42.8(b)(1) ................................................................................................. 5
`37 C.F.R. §42.8(b)(1) ............................................................................................... ..5
`
`37 C.F.R. §42.8(b)(2) ................................................................................................. 5
`37 C.F.R. §42.8(b)(2) ............................................................................................... ..5
`
`37 C.F.R. §42.8(b)(3) ................................................................................................. 6
`37 C.F.R. §42.8(b)(3) ............................................................................................... ..6
`
`42 C.F.R. § 42.65(b) ................................................................................................39
`42 C.F.R. § 42.65(b) .............................................................................................. ..39
`
`
`
`
` v
`
`

`

`EXHIBITS CITED
`
`Ex. 1001 U.S. Patent No. 5,856,336 to Fujikawa et al. (“the ʼ336 Patent”)
`
`Ex. 1002 U.S. Patent Application Ser. No. 07/233,752
`
`Ex. 1003 U.S. Patent Application Ser. No. 07/631,092
`
`Ex. 1004 U.S. Patent Application Ser. No. 07/233,752
`
`Ex. 1005
`
`File history of Interference 102, 648
`
`Ex. 1006
`
`File history of Interference 102,975
`
`Ex. 1007
`
`Executed service of summons on Sawai USA, Inc. in Kowa Company,
`Ltd., et al. v. Sawai USA, Inc., et al., USDC SDNY, Civil Action No.
`14-cv-5575
`
`Ex. 1008
`
`Executed service of summons on Sawai Pharmaceuticals Co., Ltd. in
`Kowa Company, Ltd., et al. v. Sawai USA, Inc., et al., USDC SDNY,
`Civil Action No. 14-cv-5575
`
`Ex. 1009 U.S. Patent No. 4,761,419 (“Picard”)
`
`Ex. 1010 U.S. Patent No. 4,925,852 (“Kesseler”)
`
`Ex. 1011 U.S. Patent No. 4,375,475 (“Willard”)
`
`Ex. 1012 Declaration of Dr. Milton Brown
`
`Ex. 1013 Certified English translation of JP 63-193606 (as submitted in U.S.
`Application Serial No. 07/233,752) (“JP ’606)
`
`Ex. 1014 Certified English translation of JP 63-15585 (as submitted in U.S.
`Application Serial No. 07/233,752) (“JP ʼ585)
`
`Ex. 1015 Certified English translation of JP 62-207224 (as submitted in U.S.
`Application Serial No. 07/233,752)(“JP ’224”)
`
`Ex. 1016
`
`Illingworth, R., An Overview of Lipid-Lowering Drugs, Drugs, Vol.
`36, Supp. 3, 63-71 (1988)(“Illingworth 1988”)
`
`
`
` vi
`
`

`

`Ex. 1017
`
`Illingworth, R., Lipid-Lowering Drugs, An Overview of Indications
`and Optimum Therapeutic Use, Drugs, Vol. 33, 259-279
`(1987)(“Illingworth 1987”)
`
`Ex. 1018
`
`Endo, A., Compactin (ML-236B) and Related Compounds as
`Potential Cholesterol-Lowering Agents that Inhibit HMG-CoA
`Reductase, Journal of Medicinal Chemistry, Vol. 28, No. 4 (April,
`1985)(“End 1985”)
`
`Ex. 1019 Nakamura, C., et al., Mode of Interaction of ß-Hydroxy-ß-
`methylglyutaryl Coenzyme A Reductase with Strong Binding
`Inhibitors: Compactin and Related Compounds, Biochemistry, Vol.
`24, 1364-1376 (1985) (“Nakamura”)
`
`Ex. 1020 Alberts, A., et al., Mevinolin: A highly potent competitive inhibitor of
`hydroxymethylglutaryl-coenzyme A reductase and a cholesterol-
`lowering agent, Proc. Natl. Acad. Sci. USA, Vol. 77, No. 7, 3957-
`3961 (July 1980) (“Alberts 1980”)
`
`Ex. 1021
`
`Endo, A., et al., Competitive Inhibition of 3-Hydroxy-3-
`Methylglutaryl Coenzyme A Reductase by ML-236A and ML-236B
`Fungal Metabolites, Having Hypocholesterolemic Activity, FEBS
`Letters, Vol. 72, No. 2, 323-326 (Dec. 1976) (“Endo 1976”)
`
`Ex. 1022 Brown, M., et al., Induction of 3-Hydroxy-3-methylglutaryl
`Coenzyme A Reductase Activity in Human Fibroblasts Incubates with
`Compactin “(ML-236B), a Competitive Inhibitor of the Reductase,
`Journal of Biological Chemistry, Vol. 253, No. 4, 1121-1128 (Feb.
`25, 1978)(“Brown 1978”)
`
`Ex. 1023
`
`Stokker, G., et al., 3-Hydroxy-3-methylglutaryl-coenzyme A
`Reductase Inhibitors. 1. Structural Modifications of 5-Substituted 3,5-
`Dihydroxypentanoic Acids and Their Lactone Derivatives, Journal of
`Medicinal Chemistry, Vol. 28, 347-358 (1985) (“Stokker”)
`
`Ex. 1024 Brown, A., et al., Crystal and Molecular Structure of Compactin, a
`New Antifungal Metabolite from Penicillium brevicompactum,
`Journal of Chemical Society, Perkins I, 1165-1170 (1976) (“Brown
`1976”)
`
`Ex. 1025 U.S. Patent No. 4,925,825 (Tachi)
`
`
`
` vii
`
`

`

`Ex. 1026 U.S. Patent No. 4,450,171 (Hoffman)
`EX.
`1026
`U.S. Patent No. 4,450,171 (Hoffman)
`
`Ex. 1027 U.S. Patent No. 4,686,237 (Anderson)
`EX.
`1027
`U.S. Patent No. 4,686,237 (Anderson)
`
`Ex. 1028 U.S. Patent No. 4,448,784 (Glamkowski)
`EX.
`1028
`U.S. Patent No. 4,448,784 (Glamkowski)
`
`Ex. 1029 U.S. Patent No. 4,613,610 (Wareing)
`EX.
`1029
`U.S. Patent No. 4,613,610 (Wareing)
`
`Ex. 1030 U.S. Patent No. 4,735,958 (Roth)
`EX.
`1030
`U.S. Patent No. 4,735,958 (Roth)
`
`Ex. 1031 U.S. Patent No. 4,681,893 (Roth)
`EX.
`1031
`U.S. Patent No. 4,681,893 (Roth)
`
`Ex. 1032 U.S. Patent No. 4,647,576 (Hoefle)
`EX.
`1032
`U.S. Patent No. 4,647,576 (Hoefle)
`
`Ex. 1033
`EX.
`1033
`
`EP-A-0221025 (Wareing)
`EP—A—0221025 (Wareing)
`
`
`
`
`
`
`
` viii
`Viii
`
`

`

`
`
`I.
`
`
`
`INTRODUCTION
`
`U.S. Patent No. 5,856,336 (“the ʼ336 Patent”) claims the following
`
`compound (“claimed compound”), and a method of using the compound to treat
`
`disorders including hyperplipidemia (Ex. 1001, at 32:20-40):
`
`
`
`The claimed compound is limited to a single salt form, which is the “½”
`
`calcium salt in which the divalent calcium ion is bonded to two of the active
`
`moieties shown in the formula. Claim 1 of the ‘336 patent, and method-of-use
`
`claim 2 which depends from it, are invalid as obvious under 35 U.S.C. § 103
`
`because the compound and its use are nothing more than obvious variants of prior
`
`art compounds, directed to precisely the same use, disclosed in two references,
`
`Picard (Ex. 1009) and Kesseler (Ex. 1010). The specific prior art compounds
`
`disclosed in these references differ in minor respects from the claimed compound,
`
`which is attained by a single change in structure from either prior art reference. In
`
`Picard, which identifies an isopropyl substituent as having superior activity, the
`
`isopropyl substituent is changed to cyclopropyl, which is a structural isomer that is
`
`specifically named by Picard as a preferred lower alkyl group. Ex. 1009, at 4:25-
`
`
`
`1
`
`

`

`
`
`30. In Kesseler, which directly compares the superior activity of a cyclopropyl
`
`compound to its isopropyl analog, the fused-ring quinoline structure of the claimed
`
`compound is opened, to the corresponding 6-membered nitrogen containing ring
`
`and phenyl ring present in quinoline. Ex. 1010. Each of the references, alone and
`
`in combination, discloses superior activity of specific compounds that have propyl
`
`group substituents, and Kesseler points specifically to the superior activity of
`
`cyclopropyl versus isopropyl groups. Both references disclose lead compounds that
`
`are reasoned choices for further development, based on specific activity data.
`
`A unique circumstance in the present case is that the grandparent application
`
`of the ʼ336 patent was involved in two interferences, one of which involved the
`
`same Picard patent at issue here (Ex. 1009). Interf. Nos. 102,648 and 102,975, Ex.
`
`1005 and 1006, respectively. Patent Owner (Fujikawa) lost both interferences,
`
`because a third party (Wattanasin) was found to be the first inventor, and all of
`
`Fujikawa's claims were canceled. This decision was affirmed by the Federal
`
`Circuit. Fujikawa v. Wattanasin, 93 F.3d 1559 (Fed. Cir. 1996).
`
`Patent Owner's arguments and admissions concerning Picard in the
`
`interferences are highly relevant to the present IPR. Patent Owner requested the
`
`interference with Picard, by asserting that Fujikawa’s claims defined the same
`
`patentable invention as Picard. Ex. 1005, pp. 130-32. With respect to its own
`
`claims reciting both isopropyl- and cyclopropyl-substituted analogs, Patent Owner
`
`
`
`2
`
`

`

`
`
`urged that there was “clear overlap” between Picard’s claims and all of Patent
`
`Owner’s claims, and unequivocally stated:
`
`Moreover, there is absolutely no evidence of record that the
`
`varying species embraced by both claims are patentably distinct from
`
`the unsubstituted [Picard] compound discussed above. (Id. at 132).
`
`After being informed that an interference would be declared in the near
`
`future in accordance with this request (id. at 419), Patent Owner canceled the claim
`
`corresponding to ʼ336 patent claim 1 (Claim 10), to keep it out of the interference.
`
`Id. at 422. Although Patent Owner stated that this compound exhibits “unobvious
`
`and distinguishing properties” with respect to the other claims proposed for the
`
`interference, it submitted no evidence and provided no hint as to what these
`
`“distinguishing properties” might be. Id. at 423 By canceling Claim 10 to avoid
`
`the interference, Patent Owner disclaimed the subject matter that would become
`
`claim 1 of the ‘336 Patent. See the discussion in the Petition below.
`
`Picard voluntarily dropped out of the interference, leaving Patent Owner and
`
`Wattanasin as parties. Ex. 1005, p. 27. Patent Owner then sought to reintroduce
`
`Claim 10 into the interference, but only as a separate count, which required a
`
`showing that Wattansin provided written description for the claimed cyclopropyl
`
`substituent. Id. at 35. Patent Owner repeatedly argued that the disclosure of an
`
`isopropyl compound disclosed by Wattanasin would directly lead a person skilled
`
`
`
`3
`
`

`

`
`
`in the art to select cyclopropyl as a substituent, and thus attain the subject matter
`
`that is now claimed in the ’336 Patent:
`
`[T]he Wattanasin application repeatedly exemplifies isopropyl.
`
`Indeed, isopropyl is mentioned by name as an alternate substituent at
`
`the 2-position. Having been taught that isopropyl is an acceptable
`
`substituent and within the scope of Wattanasin's invention, those of
`
`skill in the art would readily arrive at the selection of cyclopropyl,
`
`out of the disclosure of cycloalkyl of 3-7 carbon atoms, as the next
`
`logical, and analogous compound, isomerically related to
`
`exemplified species.… It is well established that isomeric species
`
`are expected to behave in similar fashion, in the absence of evidence
`
`to the contrary. (Id. at 226).
`
`These statements are unquestionably correct, as shown below. Patent Owner
`
`cannot now reverse course, and is bound by its admissions concerning the
`
`substitution of cyclopropyl for isopropyl isomers, as the next logical step for
`
`modification of an isopropyl compound. It is precisely the same next logical step
`
`for modification of Picard’s Example 3 isopropyl compound, to attain the
`
`cyclopropyl compound that is claimed in the ʼ336 Patent.
`
`
`
`4
`
`

`

`
`
`II. COMPLIANCE WITH REQUIREMENTS FOR AN INTER PARTES REVIEW
`PETITION
`A. Grounds for Standing
`
`Pursuant to 37 C.F.R. § 42.104(a), Petitioner certifies that the ʼ336 Patent is
`
`available for inter partes review and that Petitioner is not barred or estopped from
`
`requesting an inter partes review challenging the ʼ336 Patent claims on the
`
`grounds identified herein. Petitioners certify that this Petition is served within one
`
`year of the date the Petitioner was served with a complaint alleging infringement.
`
`Ex.1007, Ex. 1008 (showing service on July 31, 2014).
`
`B.
`
`Payment of Fee for Inter Partes Review
`
`The Director is authorized to charge the fees specified by 37 C.F.R. §
`
`42.15(a) to Deposit Account No. 194880.
`
`C. Mandatory Notices (37 C.F.R. §42.8(b))
`
`1.
`
`Each Real Party-in-Interest (37 C.F.R. §42.8(b)(1))
`
`
`
`The real parties-in-interest for this petition are Sawai USA, Inc., and Sawai
`
`Pharmaceutical Co., Ltd. Petitioner also notes that Sawai USA, Inc. has minority
`
`shareholders, Stason Pharmaceuticals, Inc. and Chia Scheng Investment Co., Ltd.
`
`Neither Stason Pharmaceuticals, Inc. nor Chia Scheng Investment Co., Ltd. are real
`
`parties-in-interest.
`
`2.
`
`Related Matters (37 C.F.R. §42.8(b)(2))
`
`Petitioners Sawai USA, Inc. and Sawai Pharmaceuticals Co., Ltd. are
`
`
`
`5
`
`

`

`
`
`defendants in the following litigation involving the ʼ336 Patent: Kowa Company,
`
`Ltd. et al v. Sawai USA, Inc. et al., 1:14-cv-05575 (S.D.N.Y. 2014). The ʼ336
`
`Patent is also involved in litigation in the following actions: Kowa Company, Ltd.
`
`et al. v. Mylan, Inc. et al., 1:14-cv-02647 (S.D.N.Y. 2014); Kowa Company, Ltd. et
`
`al. v. Zydus Pharmaceuticals (USA) Inc. et al., 1:14-cv-02760 (S.D.N.Y. 2014);
`
`Kowa Company, Ltd. et al v. Orient Pharma Co., Ltd., 1:14-cv-02759 (S.D.N.Y.
`
`2014); Kowa Company, Ltd. et al v. Amneal Pharmaceuticals, LLC, 1:14- cv-
`
`02758 (S.D.N.Y. 2014); and Kowa Company, Ltd. et al. v. Aurobindo Pharma
`
`Limited et al., 1:14-cv-02497 (S.D.N.Y. 2014).
`
`A Petition for inter partes review, IPR2015-01069, was filed April 18, 2015
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`by Mylan Pharmaceuticals Inc. and Mylan Inc. Patent Owner filed a preliminary
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`response on July 28, 2015.
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`In addition, Petitioner is filing concurrently another Petition for IPR of the
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`‘336 Patent based on a different ground of obviousness. See IPR 2015-01648.
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`3.
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`Lead and Backup Counsel (37 C.F.R. §42.8(b)(3))
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`Lead counsel is Kenneth J. Burchfiel (Reg. No. 31,333;
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`kburchfiel@sughrue.com). Backup counsel are Travis B. Ribar (Reg. No. 61,446;
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`tribar@sughrue.com); Chidambaram S. Iyer (Reg. No. 43,355;
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`ciyer@sughrue.com); Michael R. Dzwonczyk (Reg. No. 36,787;
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`mdzwonczyk@sughrue.com); and Azy S. Kokabi (Reg. No. 58,902;
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`akokabi@sughrue.com).
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`The mailing address for each is:
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`Sughrue Mion, PLLC
`2100 Pennsylvania Ave., NW
`Washington, DC 20037
`Phone: 202-293-7060
`Fax: 202-293-7860
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`Service Information (37 C.F.R. §42.8(b)(4))
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`4.
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`Petitioners consent to electronic service by e-mail at the e-mail addresses of
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`lead and back-up counsel provided above.
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`5.
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`Power of Attorney (37 C.F.R. §42.10(b))
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`A power of attorney from Sawai USA, Inc. and Sawai Pharmaceutical Co.,
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`Ltd. accompanies this Petition.
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`D.
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`Statement of precise relief requested
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`Pursuant to 37 C.F.R. § 42.22(a)(1), 37 C.F.R. § 42.22(a)(1), and 37 C.F.R.
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`§ 42.104(b), claims 1 and 2 of the ʼ336 Patent are unpatentable under 35 U.S.C. §
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`103 for the following reasons, and the cancellation of these claims is requested.
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`E.
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`Identification of Prior Art and Challenged Claims
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`Ground 1: Claims 1 and 2 are unpatentable under 35 U.S.C. §103(a) as
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`being obvious over Picard (Ex. 1009) in view of Kesseler (Ex. 1010).
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`F.
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`Supporting Evidence Relied Upon
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`Pursuant to 37 C.F.R. § 42.22(a)(2), 37 C.F.R. § 42.104(b)(4) and 37 C.F.R.
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`§ 42.104(b)(5), a full statement of the reasons why each of claims 1 and 2 of the
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`ʼ336 Patent should be held unpatentable under 35 U.S.C. § 103(a) is provided in
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`this Petition, with reference to supporting evidence including the exhibits identified
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`above. Petitioner relies on the expert Declaration of Dr. Milton Brown. (Ex. 1012)
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`Dr. Brown is the Director of the Drug Discovery Program (DDP) at the
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`Georgetown University Medical Center (GUMC, or University), which manages
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`and supports the University drug discovery and development efforts. He has more
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`than 18 years of experience in drug discovery (Ex. 1012, ¶¶ 1-12.) Dr. Brown’s
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`curriculum vitae is attached to his declaration.
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`III. THE ʼ336 PATENT
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`The ʼ336 Patent issued on January 5, 1999, from Application Ser. No.
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`07/883,398, filed May 15, 1992 (Ex. 1002); which was a divisional of Ser. No.
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`07/631,092, filed December 19, 1990 (Ex. 1003); which was a continuation of Ser.
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`No. 07/233,752, filed August 19, 1988 (Ex. 1004).
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`A.
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`Field of the ʼ336 Patent
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`The ʼ336 Patent ʼ336 is directed to mevalonolactones having a quinoline
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`ring structures as well as their pharmaceutical uses as anti-hyperlipidemic,
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`hypolipoproteinemic and anti-atherosclerotic agents. Ex. 1001, at 1:5-10 (i.e.,
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`column 1, lines 5-10; hereinafter, the notation X:Y denotes column:line).
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`B. Claims 1 and 2 of the ʼ336 Patent
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`Claims 1 and 2 of the ʼ336 Patent are:
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`1. A compound of the formula,
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`
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`Z= —CH(OH)—CH2—CH(OH)—CH2—COO.½Ca.
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`2. A method for reducing hyperlipidemia, hyperlipoproteinemia or
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`atherosclerosis, which comprises administering an effective amount of the
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`compound of formula A as defined in claim 1.
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`Ex. 1001, at 32:20-40; Ex. 1012, ¶ 13.
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`C. The Broadest Reasonable Construction of Claim Terms
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`Pursuant to 37 C.F.R. § 42.104(b)(3) and 37 C.F.R. § 42.100(b), Petitioner
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`states that the broadest reasonable interpretation of claim 1 includes all isomeric
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`forms of the compound: “these compounds may have at least one or two
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`asymmetric carbon atoms and may have at least two to four optical isomers. The
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`compounds of the formula I include all of these optical isomers and all of the
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`mixtures thereof.” See Ex. 1001, at 2:66-3:2. A person of ordinary skill in the art
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`(POSA) would have understood that the compound of Claim 1 of the ʼ336 Patent
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`includes four optical isomers and mixtures thereof. Ex. 1012 at ¶ 14.
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`For purposes of this Petition, a POSA would have held an advanced degree,
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`such as an M.S. or a doctorate in one of the fields of medicinal or synthetic
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`chemistry, pharmacology, with 3 to 5 years of experience working in the field of
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`drug discovery who was familiar with mevalonolactones, including natural, semi-
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`synthetic and fully synthetic derivatives of compactin and mevinoline and related
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`compounds, and their pharmaceutical uses as anti-hyperlipidemic,
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`hypolipoproteinemic and anti-atherosclerotic agents. Ex. 1012 at ¶ 15.
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`IV. THE EFFECTIVE FILING DATE OF CLAIMS 1 AND 2 OF THE ʼ336 PATENT IS, AT
`THE EARLIEST, AUGUST 3, 1988
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`The ʼ336 Patent claims benefit of Japanese Patent Applications JP 63-
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`193606 (filed August 3, 1988), JP 63-15585 (filed January 26, 1988), and JP 62-
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`207224 (filed August 20, 1987) (references to the Japanese applications herein are
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`to the certified translations submitted by Patent Owner during prosecution of the
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`‘752 grandparent application). Ex. 1015 (JP ʼ224), Ex. 1014 (JP ʼ585), and Ex.
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`1013 (JP ʼ606). However, neither JP ʼ585 nor JP ʼ224 provides written description
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`for a ½ calcium salt, as specifically required by claims 1 and 2 of the ʼ336 Patent.
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`The earliest effective filing date for the ʼ336 Patent is no earlier than the filing date
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`of JP ‘606. Petitioner submits that these translations constitute admissions by
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`Patent Owner regarding the disclosure of the Japanese priority documents.
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`A.
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`Single species claims require full written description support in
`order to be entitled to benefit of priority
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`“[A] description that merely renders the invention obvious does not satisfy
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`the [written description] requirement” of 35 U.S.C. § 112. Ariad Pharm., Inc. v.
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`Eli Lilly & Co., 598 F.3d 1336, 1352 (Fed. Cir. 2010) (en banc) (quoting
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`Lockwood v. Am. Airlines, 107 F.3d 1565, 1571–72 (Fed. Cir. 1997)). This is
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`emphasized in those cases where an applicant has described a broad genus in its
`
`specification, yet has claimed only a single compound. In those cases, “[t]he
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`question [of written description support is]…whether the [] application ‘discloses
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`the [variants], specifically, as something appellants actually invented,’” not
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`whether it would have been obvious to have arrived at the single compound given
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`the disclosure of the broader genus. Novozymes A/S v. DuPont Nutrition
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`Biosciences APS, 723 F.3d 1336, 1350 (Fed. Cir. 2013), quoting In re Ruschig, 379
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`F.2d 990, 995 (CCPA 1967).
`
`Merely disclosing a broad genus does not provide written description
`
`support for an individually claimed species. Ruschig, 379 F.2d at 994 (“Surely,
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`given time, a chemist could name (especially with the aid of a computer) all of the
`
`half million compounds within the scope of the broadest claim, which claim is
`
`supported by the broad disclosure. This does not constitute support for each
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`compound individually when separately claimed.”), cited by the PTAB with
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`approval in Motionpoint Corp., Petitioner, CBM2014-00066, 2014 WL 3704044,
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`at *14 (July 23, 2014).
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`“[T]he written description requirement prohibits a patentee from ‘leaving it
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`to the ... industry to complete an unfinished invention.’” Novozymes, 723 F.3d at
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`1350, citing Ariad, 598 F.3d at 1353. A patentee cannot merely disclose a broad
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`chemical genus and then successfully claim individual compounds within that
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`genus without a disclosure sufficient to show that they possessed the individual
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`compounds. See, e.g., Novozymes, 723 F.3