IN THE UNITED STATES PATENT AND TRADEMARK OFFICE
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`
`INNOPHARMA LICENSING, INC., INNOPHARMA LICENSING LLC,
`INNOPHARMA INC., INNOPHARMA LLC,
`MYLAN PHARMACEUTICALS INC., and MYLAN INC.,
`Petitioner
`
`v .
`
`SENJU PHARMACEUTICAL CO., LTD., BAUSCH & LOMB, INC., and
`BAUSCH & LOMB PHARMA HOLDINGS CORP.,
`Patent Owner.
`
`U.S. Patent No. 8,871,813 to Sawa et al.
`Issue Date: October 28, 2014
`Title: Aqueous Liquid Preparation Containing
`2-Amino-3-(4-
`bromobenzoyl) Phenylacetic Acid
`
`Inter Partes Review No.: IPR2016-00090
`
`Petition for Inter Partes Review of U.S. Patent No. 8,871,813 Under
`35 U.S.C. §§ 311-319 and 37 C.F.R. §§ 42.1-.80, 42.100-.123
`
`Mail Stop “PATENT BOARD”
`Patent Trial and Appeal Board
`U.S. Patent and Trademark Office
`P.O. Box 1450
`Alexandria, VA 22313-1450
`
`

`
`TABLE OF CONTENTS
`
`I.
`II.
`III.
`
`Page
`INTRODUCTION ...........................................................................................1
`OVERVIEW....................................................................................................1
`STANDING (37 C.F.R. § 42.104(a); PROCEDURAL
`STATEMENTS)..............................................................................................2
`IV. MANDATORY NOTICES (37 C.F.R. § 42.8(a)(1))......................................2
`A.
`Each Real Party-In-Interest (37 C.F.R. § 42.8(b)(1)) ...........................2
`B.
`Notice of Related Matters (37 C.F.R. § 42.8(b)(2))..............................3
`1.
`Judicial Matters...........................................................................3
`2.
`Administrative Matters ...............................................................3
`Designation of Lead and Back-Up Counsel and Service (37
`C.F.R. §§ 42.8(b)(3), 42.8(b)(4), 42.10(a), and 42.10(b)):...................5
`STATEMENT OF THE PRECISE RELIEF REQUESTED AND THE
`REASONS THEREFORE (37 C.F.R. § 42.22(a))..........................................6
`THE ’813 PATENT.........................................................................................6
`A.
`Claim Construction................................................................................7
`VII. PERSON OF SKILL IN THE ART (“POSA”) & STATE OF THE
`ART .................................................................................................................7
`VIII. IDENTIFICATION OF CHALLENGE (37 C.F.R. § 42.104(b)).................10
`A.
`The Scope and Content of the Prior Art..............................................11
`1.
`Aqueous Ophthalmic Preparation of Bromfenac......................11
`2.
`Tyloxapol and Related Surfactants in NSAID Aqueous
`Ophthalmic Preparations.......................................................11
`
`V.
`
`VI.
`
`C.
`
`i
`
`

`
`B.
`
`C.
`
`3.
`
`(ii)
`
`Ground 1: Claims 1-27 Are Unpatentable Under 35 U.S.C.
`§ 103(a) over Ogawa in light of Sallmann..........................................12
`1.
`Ogawa (EX1004) and Sallmann (EX1009) ..............................13
`2.
`Independent Claims 1, 7, and 13...............................................15
`a.
`Claim 1............................................................................15
`(i)
`It would have been obvious to substitute
`tyloxapol from Sallmann’s Example 2 for
`polysorbate 80 in Ogawa’s Example 6.................19
`Sallmann teaches that the amount of
`tyloxapol is sufficient to stabilize the
`bromfenac, or in the alternative it would
`have been obvious to do so according to the
`teachings of Sallmann and Ogawa.....................23
`Claim 7............................................................................26
`b.
`Claim 13..........................................................................27
`c.
`Dependent Claims.....................................................................27
`a.
`Claims 2, 8, and 14—Sodium Sulfite.............................28
`b.
`Claims 3 and 15—Sodium Salt of Bromfenac ...............29
`c.
`Claims 4, 6, 10, 12, 16, 18, 21, 23, —Bromfenac
`Sodium and Tyloxapol Concentrations and
`Additional Additives....................................................29
`(i)
`Bromfenac Sodium Concentration.......................29
`(ii)
`Tyloxapol Concentration......................................31
`(iii) Additional Additives ............................................33
`Claims 5, 11, 17, and 22—pH Ranges ...........................35
`d.
`Claims 9, 19, and 20—Storage Stability ........................36
`e.
`Claims 24-26—No Preservative.....................................38
`f.
`Claim 27—Additional Additives....................................39
`g.
`Ground 2: Claims 1-27 Are Unpatentable Under 35 U.S.C.
`§ 103(a) over Ogawa in light of Sallmann and Fu..............................40
`1.
`Overview of Fu (EX1011) ........................................................40
`2.
`Independent Claims 1, 7, and 13...............................................43
`3.
`Dependent Claims.....................................................................44
`
`ii
`
`

`
`D.
`
`Claims 4, 6, 10, 12, 16, 18, and 21—Tyloxapol
`Concentration..................................................................45
`Ground 3: Claims 1-27 Are Unpatentable Under 35 U.S.C.
`§ 103(a) over Ogawa in light of Sallmann and Yasueda ....................47
`1.
`Overview of Yasueda (EX1012)...............................................47
`2.
`Independent Claims 1, 7, and 13...............................................50
`3.
`Dependent Claims.....................................................................52
`a.
`Claims 4, 6, 10, 12, 16, 18, and 21—Tyloxapol
`Concentration..................................................................53
`Objective Indicia of Nonobviousness .................................................54
`1.
`No Unexpected Results Over the Closest Prior Art..................55
`a.
`Tyloxapol’s Stabilizing Effects ......................................56
`b.
`Scope of Stabilizing Effects ...........................................57
`Other Objective Indicia.............................................................57
`2.
`IX. CONCLUSION..............................................................................................60
`
`E.
`
`a.
`
`iii
`
`

`
`TABLE OF AUTHORITIES
`
`Page(s)
`
`Federal Cases
`Amneal Pharms., LLC v. Supernus Pharms., Inc.
`IPR2013-00368...................................................................................................55
`Chapman v. Casner
`315 Fed. App’x 294 (Fed. Cir. 2009) ...........................................................30, 36
`Ecolab, Inc. v. FMC Corp.
`569 F.3d 1335 (Fed. Cir. 2009) ..........................................................................18
`Friskit, Inc. v. Real Networks, Inc.
`306 F. App’x 610 (Fed. Cir. 2009) .....................................................................58
`Galderma Labs., L.P., v. Tolmar, Inc.
`737 F.3d 731 (Fed. Cir. 2013) ......................................................................30, 32
`In re Aller
`220 F.2d 454, 458 (C.C.P.A. 1955)..............................................................25, 32
`In re Baxter Travenol Labs.
`952 F.2d 388 (Fed. Cir. 1991) ......................................................................25, 38
`
`In re De Blauwe
`736 F.2d 699 (Fed. Cir. 1984) ............................................................................55
`In re Malagari
`499 F.2d 1297 (C.C.P.A. 1974)..........................................................................36
`In re Merchant
`575 F.2d 865 (C.C.P.A. 1978)............................................................................55
`
`In re Johnston
`435 F.3d 1381 (Fed. Cir. 2006) ..........................................................................39
`In re Peterson
`315 F.3d, 1325, 1329-30 (Fed. Cir. 2003) .................................24, 25, 32, 36. 57
`In re Woodruff
`919 F.2d 1575 (Fed. Cir. 1990) ....................................................................24, 36
`
`iii
`
`

`
`InnoPharma Licensing Inc., et al. v. Senju Pharm. Co., Ltd.
`IPR2015-00902............................................................................................passim
`Iron Grip Barbell Co., Inc., v. USA Sports, Inc.
`392 F.3d 1317 (Fed. Cir. 2004) ..........................................................................30
`
`KSR International Co. v. Teleflex Inc.
`550 U.S. 398 (2007)..................................................................................2, 23, 33
`Lupin Ltd.. v. Senju Pharm. Co., Ltd., IPR2015-01097....................................passim
`Lupin Ltd.. v. Senju Pharm. Co., Ltd., IPR2015-01105....................................passim
`Metrics, Inc. v. Senju Pharm. Co., Ltd., IPR2014-01043.................................passim
`Newell Cos., Inc. v. Kenney Mfg. Co.
`864 F.2d 757 (Fed. Cir. 1988) ............................................................................55
`Ormco Corp. v. Align Tech., Inc.
`463 F.3d 1299 (Fed. Cir. 2006) ..........................................................................58
`Purdue Pharma Prods. L.P. v. Par Pharm., Inc.
`377 Fed App’x 978 (Fed. Cir. 2010) ..................................................................59
`Sakraida v. AG Pro, Inc.
`425 U.S. 273 (1976)...........................................................................................23
`
`Santarus v. Par Pharm
`694 F.3d 1344 (Fed. Cir. 2012) ....................................................................25, 38
`Sinclair & Carroll Co., v. Interchemical Corp.
`325 U.S. 327 (1945)............................................................................................21
`Stratoflex, Inc. v. Aeroquip Corp.
`713 F.2d 1530 (Fed. Cir. 1983) ....................................................................58, 59
`Sundance, Inc. v. DeMonte Fabricating Ltd.
`550 F.3d 1356 (Fed Cir. 2008) ...........................................................................13
`Tandon Corp. v. United States Int’l Trade Comm’n
`831 F.2d 1017 (Fed. Cir. 1987) ..........................................................................19
`Titanium Metals Corp. of Amer. v. Banner
`778 F.2d 775, 227 USPQ 773 (Fed. Cir. 1985)............................................32, 45
`
`iv
`
`

`
`Tokai Corp. v. Eason Enters., Inc.
`632 F.3d 1358 (Fed. Cir. 2011) ..........................................................................59
`Wm. Wrigley Jr. Co. v. Cadbury Adams USA LLC
`683 F.3d 1356 (Fed Cir. 2012).....................................................................22, 52
`Statutes
`35 U.S.C. § 103(a) .......................................................................................12, 40, 47
`37 C.F.R. § 42(a)(1)...................................................................................................2
`37 C.F.R. § 42.6(d) ..................................................................................................10
`37 C.F.R. § 42.8(b)(1)................................................................................................2
`37 C.F.R. § 42.8(b)(2)................................................................................................3
`37 C.F.R. § 42.8(b)(3)................................................................................................5
`37 C.F.R. § 42.10(b) ..................................................................................................2
`37 C.F.R. § 42.22(a)...................................................................................................6
`37 C.F.R. § 42.63(e)...................................................................................................2
`37 C.F.R. § 42.100(b) ................................................................................................7
`37 C.F.R. § 42.104(a).................................................................................................2
`37 C.F.R. § 42.104(b) ..............................................................................................10
`37 C.F.R. § 42.106(a).................................................................................................2
`
`v
`
`

`
`InnoPharma
`Exhibit #
`1001
`
`1002
`
`1003
`1004
`
`1005
`
`1006
`
`1007
`
`1008
`
`1009
`
`1010
`
`1011
`
`1012
`
`1013
`
`Petitioner’s Exhibit List
`
`Description
`
`Sawa et al., U.S. Patent No. 8,871,813, “Aqueous Liquid Preparation
`Containing 2-Amino-3-(4-Bromobenzoyl) Phenylacetic Acid”
`Certified English translation of: Hara, Yoshiyuki , “Bromfenac
`sodium hydrate,” Clinics & Drug Therapy 19:1014-1015 (2002)
`
`Declaration of Paul A. Laskar, Ph.D.
`Ogawa et al., U.S. Patent No. 4,910,225, “Locally Administrable
`Therapeutic Composition for Inflammatory Disease”
`Desai et al., U.S. Patent No. 5,603,929, “Preserved Ophthalmic
`Drug Compositions Containing Polymeric Quaternary Ammonium
`Compounds”
`Desai, et al., U.S. Patent No. 5,558,876, “Topical Ophthalmic
`Acidic Drug Formulations”
`Certified English translation of “Bromfenac sodium hydrate” in the
`Japanese Pharmacopoeia 2001 Edition: 27-29, Yakuji Nippo
`Limited (2001)
`FDA approved “BROMDAYTM (bromfenac ophthalmic solution,
`.09%) Product Label,” U.S. Approval: March 24, 2005, ISTA
`Pharmaceuticals, Inc.
`Sallmann et al., U.S. Patent No. 6,107,343, “Ophthalmic And Aural
`Compositions Containing Diclofenac Potassium”
`Guttman et al., “Solubilization of Anti-inflammatory steroids by
`Aqueous Solutions of Triton-WR-1339,” Journal of Pharmaceutical
`Sciences 50: 305-307 (1961)
`Fu et al., Australian Patent No. AU-B-22042/88, “Preservative
`System For Ophthalmic Formulations”
`Yasueda et al., U.S. Patent No. 6,274,609, “Aqueous Liquid
`Pharmaceutical Composition Containing as Main Component
`Benzopyran Derivative”
`U.S. Patent Application No. 13/687,242, Office Action of August 1,
`2013
`
`vi
`
`

`
`InnoPharma
`Exhibit #
`1014
`
`1015
`
`1016
`
`1017
`
`1018
`
`1019
`
`1020
`
`1021
`
`1022
`
`1023
`
`1024
`
`1025
`
`Description
`
`U.S. Patent Application No. 10/525,006, Applicant Remarks in
`support of amendment March 26, 2008
`U.S. Patent Application No. 10/525,006, Applicant Remarks in
`support of amendment, September 6, 2011
`The Pharmacopeia of the United States of America, Thirty-Eighth
`Revision and the National Formulary, Thirty-Third Edition
`Kapin, et. al., International Patent No. WO 2002/13804, “Method
`for Treating Angiogenesis-Related Disorders Using Benzoyl
`Phenylacetic Acid”
`Flach, Allan., “Topical Nonsteroidal Antiinflammatory Drugs for
`Ophthalmic Uses,” Ophthalmic NSAIDs: 77-83 (1996)
`Schott, H., “Comparing the Surface Chemical Properties and the
`Effect of Salts on the Cloud Point of a Conventional Nonionic
`Surfactant, Octoxynol 9 (Triton X-100), and of Its Oligomer,
`Tyloxapol (Triton WR-1339),” Journal of Colloid and Interface
`Science 205: 496-502 (1998)
`Regev, O., et al., “Aggregation Behavior of Tyloxapol, a Nonionic
`Surfactant Oligomer, in Aqueous Solution,” Journal of Colloid and
`Interface Science 210: 8-17 (1999)
`Aviv, H., International Patent No. WO 94/05298, “Submicron
`Emulsions as Ocular Drug Delivery Vehicles”
`Bergamini et al., U.S. Patent No. 5,597,560, “Diclofenac And
`Tobramycin Formulations For Ophthalmic And Otis Topical Use”
`U.S. Patent Application No. 13/687,242, Applicant Remarks in
`support of amendment, November 28, 2012
`Excerpt of Plaintiffs’ Opening Markman Brief filed in Senju Pharm.
`Co., Ltd. et al. v. InnoPharma Licensing, Inc. et al., C.A. No. 1:15-
`cv-03240-JBA-KMW (D.N.J.) D.I. 16 (Aug. 10, 2015).
`U.S. Patent Application No. 13/687,242, Applicant Remarks in
`support of amendment, October 22, 2013
`
`vii
`
`

`
`InnoPharma
`Exhibit #
`1026
`
`1027
`
`1028
`
`1029
`
`1030
`
`1031
`
`1032
`
`1033
`
`1034
`
`Description
`
`"monohydrate," Webster’s New World Dictionary of the
`American Language: 920, New World Dictionaries / Simon and
`Schuster (1980).
`"Voltaren," Orange Book: Approved Drug Products with
`Therapeutic Equivalence Evaluations, Appl. No. N020037, U.S.
`FDA, accessed at
`http://www.accessdata.fda.gov/scripts/cder/ob/docs/obdetail.cfm?
`A ppl_No=020037&TABLE1=OB_Rx
`Yanni et al., U.S. Patent No. 5,475,034, "Topically
`Administrable Compositions Containing 3-Benzoylphenylacetic
`Acid Derivatives for Treatment of Ophthalmic Inflammatory
`Disorders".
`"ISTA Pharmaceuticals Submits New Drug Application for
`XibromTM QD (once-daily), News Release, ISTA
`Pharmaceuticals (December 20, 2007)
`Prince, S., et al., "Analysis of benzalkonium chloride and its
`homologs: HPLC versus HPCE," Journal of Pharmaceutical
`and Biomedical Analysis 19: 877-882, Elsevier Science B.V.,
`Netherlands (1999)
`"Acular®" and "AzoptTM," Physician’s Desk Reference 54:
`486- 487, 491-492 (2000).
`Doughty, M., "Medicines Update for optical practitioners- Part
`11," Optician 5853 (223), (2002).
`Reddy, Indra K., Ocular Therapeutics and Drug Delivery: A
`Multi-Disciplinary Approach: 42-43, 390 (1996).
`Fan, T., "Determination of Benzalkonium Chloride in
`Ophthalmic Solutions Containing Tyloxapol by Solid-Phase
`Extraction and Reversed-Phase High-Performance Liquid
`Chromatography," Journal of Pharmaceutical Sciences 82 (11):
`1172-1174, American Pharmaceutical Association, United
`States (1993).
`
`viii
`
`

`
`InnoPharma
`Exhibit #
`1035
`
`1036
`
`1037
`
`1038
`
`1039
`
`1040
`1041
`
`1042
`
`1043
`
`1044
`
`1045
`
`1046
`
`Description
`
`Wong, Michelle, International Patent No. WO 94/15597,
`"Ophthalmic Compositions Comprising
`Benzyllauryldimethylammonium Chloride" (filed January 11,
`1993; issued July 21, 1994).
`Guy et al., U.S. Patent No. 5,540,930, "Suspension of
`Loteprednol Etabonate for Ear, Eye, or Nose Treatment" (filed
`October 25, 1993; issued July 30, 1996).
`FDA approved "ALREXTM (loteprednol etabonate ophthalmic
`suspension) 0.2% Product Label," U.S. Approval: 1998, Bausch
`& Lomb Pharmaceuticals.
`etabonate
`FDA approved
`"LOTEMAXTM (loteprednol
`ophthalmic suspension) 0.5% Product Label," U.S. Approval:
`1998, Bausch & Lomb Pharmaceuticals.
`"TOBRADEX®" Physician’s Desk Reference 54: 490 (2000).
`
`"Alomide® 0.1%" Physician’s Desk Reference 50: 469 (1996).
`Johnson, R., et al., U.S. Patent No. 2,880,130, "Anti-
`Inflammatory Steroid Solutions".
`Johnson, R., et al., U.S. Patent No. 2,880,138, "Anti-
`Inflammatory Steroid Solutions".
`Kawabata, et al., Canadian Patent No. CA 2 383 971 A1,
`“Prophylactic and Therapeutic Medicaments for Ophthalmic
`Uses”.
`Patani, G., et al., "Bioisoterism: A Rational Approach in
`Drug Design," Chem. Rev. 96: 3147-3176 (1996).
`FDA approved "XIBROMTM (bromfenac ophthalmic
`solution, .09%) Product Label," ISTA Pharmaceuticals, Inc.
`Senju Pharmaceutical Co., Ltd. Press Releases, "The approval of
`BRONUCK® (bromfenac sodium hydrate ophthalmic solution)
`as an import drug in China," http://www.senju.co.jp/, accessed at
`http://www.senju.co.jp/english/news/__icsFiles/afieldfile/2009/11
`/1 8/2009111814br.pdf, published November 17, 2009, 1 page.
`
`ix
`
`

`
`InnoPharma
`Exhibit #
`1047
`
`1048
`
`1049
`
`1050
`
`1051
`1052
`
`1053
`
`Description
`
`FDA approved "PROLENSATM (bromfenac ophthalmic
`solution, 0.07%) Product Label," U.S. Approval: April 5, 2013,
`Bausch & Lomb Incorporated
`
`"Borax (Sodium tetraborate)," Biochemicals and Reagents:
`175, Sigma-Aldrich (2000-2001).
`Ali, et al., U.S. Patent No. 6,071,904, "Process for
`Manufacturing Ophthalmic Suspensions".
`Story, M., et al., European Patent No. 0274870, "Micelles
`containing a non-steroidal antiinflammatory compound"
`(filed December 12, 1987; issued July 7, 1988)
`
`“DuractTM,” Physician’s Desk Reference 52:3035-3037 (1998).
`Curriculum Vitae of Paul A. Laskar, Ph.D.
`U.S. Patent Application No. 10/525,006, Applicant Remarks in
`support of amendment Oct. 25, 2010
`
`x
`
`

`
`I.
`
`INTRODUCTION
`InnoPharma Licensing, Inc., InnoPharma Licensing LLC, InnoPharma Inc.,
`
`InnoPharma LLC, Mylan Pharmaceuticals Inc., and Mylan Inc. (collectively,
`
`“Petitioner”) petition for Inter Partes Review, seeking cancellation of claims 1-27
`
`(“challenged claims”) of U.S. Patent No. 8,871,813 (“the ’813 patent”) (EX1001),
`
`owned by Senju Pharmaceutical Co., Ltd. (“Patent Owner”).
`
`II. OVERVIEW
`The Board has already issued its Decision Instituting Inter Partes Review
`
`(“Decision”) on all challenged claims of
`
`the ’813 patent based on the
`
`Ogawa/Sallmann prior art. Lupin Ltd. v. Senju Pharm. Co., Ltd., IPR2015-01105
`
`[Paper No. 9, p. 15]. In its Decision, the Board found that Petitioner Lupin Ltd. and
`
`Lupin Pharmaceuticals Inc. (collectively “Lupin”) had demonstrated a reasonable
`
`likelihood that claims 1-27 of the ’ 813 patent are obvious. Id. The Board instituted
`
`IPR of the challenged claims on the ground that claims 1-27 are reasonably likely to
`
`be obvious over Ogawa and Sallmann. Id. at pg. 16. Petitioner hereby files its own
`
`petition that raises obviousness in view of Ogawa and Sallmann and concurrently
`
`seeks to join the instituted IPR proceedings.
`
`The challenged claims of the ’813 patent are primarily directed to an aqueous
`
`formulation of bromfenac (a non-steroidal anti-inflammatory drug (“NSAID”)) with
`
`tyloxapol (a non-ionic surfactant) with the inclusion of other components such as
`
`1
`
`

`
`Petition for Inter Partes Review
`of U.S. Patent No. 8,871,813
`
`boric acid, sodium tetraborate, and water. At the relevant time, tyloxapol was a
`
`known non-ionic surfactant in aqueous formulations of NSAIDs while bromfenac
`
`was a known NSAID previously formulated with another non-ionic surfactant,
`
`polysorbate 80. Thus, the purported inventors of the aqueous preparations of the
`
`challenged claims did nothing more than switch polysorbate 80 for tyloxapol (both
`
`well-known non-ionic surfactants). Swapping known alternatives from the prior
`
`art, according to their known functions to achieve predictable results, is not
`
`innovation. KSR International Co. v. Teleflex Inc., 550 U.S. 398, 416 (2007).
`
`III.
`
`STANDING (37 C.F.R. § 42.104(a); PROCEDURAL STATEMENTS)
`Petitioner certifies that (1) the ’813 patent is available for IPR; and (2)
`
`Petitioner is not barred or estopped from requesting IPR of any claim of the ’813
`
`patent on the grounds identified herein. This Petition is filed in accordance with 37
`
`C.F.R. § 42.106(a). Filed herewith are a Power of Attorney and an Exhibit List
`
`pursuant to § 42.10(b) and § 42.63(e). The required fee is paid through online credit
`
`card, and the Office is authorized to charge any fee deficiencies and credit
`
`overpayments to Deposit Acct. No. 160605 (Customer ID No. 00826).
`
`IV. MANDATORY NOTICES (37 C.F.R. § 42.8(a)(1))
`A.
`Each Real Party-In-Interest (37 C.F.R. § 42.8(b)(1))
`
`2
`
`

`
`Petition for Inter Partes Review
`of U.S. Patent No. 8,871,813
`
`The real parties in interest for this petition are InnoPharma Licensing Inc.,
`
`InnoPharma Licensing LLC,
`
`InnoPharma Inc.,
`
`InnoPharma LLC, Mylan
`
`Pharmaceuticals Inc., and Mylan Inc.
`
`B.
`
`Notice of Related Matters (37 C.F.R. § 42.8(b)(2))
`1.
`Judicial Matters
`The ’813 patent is currently the subject of the following litigations: Senju
`
`Pharm. Co., Ltd. et al. v. InnoPharma Licensing, Inc. et al., C.A. 1:15-cv-03240
`
`(D.N.J.); Senju Pharm. Co., Ltd., et al. v. Lupin, Ltd. et al., C.A. No. 1:15-cv-00335
`
`(D.N.J.); Senju Pharm. Co., Ltd., et al. v. Apotex, Inc., et al., C.A. No. 1:15-cv-00336
`
`(D.N.J.); Senju Pharm. Co., Ltd., et al v. InnoPharma Licensing, Inc. et al., C.A. No.
`
`1:14-cv-06893 (D.N.J.); Senju Pharm. Co., Ltd., et al v. Paddock Labs., LLC et al.,
`
`C.A. No. 1:15-cv-00087-SLR (D. Del.); Senju Pharma. Co., Ltd., et al v. Paddock
`
`Labs., LLC et al., C.A. No. 1:15-cv-00337 (D.N.J.); Senju Pharm. Co., Ltd., et al v.
`
`Metrics, Inc., C.A. No. 1:14-cv-03962 (D.N.J.); and Senju Pharm. Co., Ltd., et al v.
`
`Watson Labs., Inc., C.A. No. 1:15-cv-05591 (D.N.J.).
`
`Administrative Matters
`2.
`U.S. Patent No. 8,871,813 (“the ’813 patent”) is the subject of a petition for
`
`inter partes
`
`reviews
`
`(IPR2015-01105)
`
`filed by Lupin Ltd.
`
`and Lupin
`
`Pharmaceuticals (collectively “Lupin”) on April 23, 2015, which was instituted on
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`October 27, 2015 as to claims 1-27. Petitioner seeks joinder with that IPR, for the
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`Petition for Inter Partes Review
`of U.S. Patent No. 8,871,813
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`reasons expressed in the concurrently filed Motion for Joinder under 35 U.S.C. §
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`315(c), 37 C.F.R. §§ 42.22 and 42.122(b).
`
`Petitioner is also aware of at least the following related family members:
`
`application No. 14/483,903 (“the ’903 application”), now U.S. Patent No. 8,927,606
`
`(“the ’606 patent”), which is a division of application No. 14/261,720 (“the ’720
`
`application”), now the ’813 patent, which is a division of application No. 14/165,976
`
`(“the ’976 application”), now U.S. Patent No. 8,754,131 (“the ’131 patent”), which
`
`is a division of application No. 13/687,242 application (“the ’242 application”), now
`
`U.S. Patent No. 8,669,290 (“the ’290 patent”), which is a division of application No.
`
`13/353,653 (“the ’653 application”), now U.S. Pat. No. 8,497,304 (“the ’304
`
`patent”), which is a division of application No. 10/525,006 (“the ’006 application”),
`
`now U.S. Patent No. 8,129,431 (“the ’431 patent”), which was the U.S. National
`
`Stage of PCT Application No. PCT/JP2004/000350 (“the ’350 application”), which
`
`claimed priority to Japanese Application No. 2003-12427. Related family member
`
`applications U.S. Application Serial Nos. 14/269,692 and 14/502,014 are currently
`
`pending before the Patent Office.
`
`U.S. Patent No. 8,669,290 (“the ’290 patent”) is the subject of the following
`
`inter partes reviews: IPR2014-01043 filed by Metrics Inc., which was settled on
`
`July 8, 2015; IPR2015-00902 filed by Petitioner on March 19, 2015, which was
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`Petition for Inter Partes Review
`of U.S. Patent No. 8,871,813
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`instituted on August 7, 2015 as to claims 1-30; IPR2015-01099 filed by Lupin on
`
`April 23, 2015, which was instituted on October 27, 2015 as to claims 1-30.
`
`U.S. Patent No. 8,129,431 (“the ’431 patent”) is the subject of the following
`
`inter partes reviews: IPR2014-01041 filed by Metrics Inc., which was settled on
`
`July 8, 2015; IPR2015-00903 filed by Petitioner on March 19, 2015, which was
`
`instituted on August 7, 2015 as to claims 1-22; IPR2015-01871 filed by Lupin on
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`September 4, 2014.
`
`U.S. Patent No. 8,754,131 (“the ’131 patent”) is the subject of a petition for
`
`inter partes reviews (IPR2015-01097) filed by Lupin on April 23, 2015, which was
`
`instituted on October 27, 2015 as to claims 1-30.
`
`U.S. Patent No. 8,927,606 (“the ’606 patent”) is the subject of a petition for
`
`inter partes reviews (IPR2015-01100) filed by Lupin on April 23, 2015, which was
`
`instituted on October 27, 2015 as to claims 1-30.
`
`Petitioners have filed concurrently with this Petition, Petitions for inter partes
`
`review of the following U.S. Patents related to the ’813 patent: U.S. Patent Nos.
`
`8,754,131 and 8,927,606.
`
`C.
`
`Designation of Lead and Back-Up Counsel and Service (37 C.F.R.
`§§ 42.8(b)(3), 42.8(b)(4), 42.10(a), and 42.10(b)):
`Lead Counsel:
`Jitendra Malik, Ph.D.
`(Registration No. 55,823;
`
`jitty.malik@alston.com). Backup Counsel: Hidetada James Abe (Registration No.
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`Petition for Inter Partes Review
`of U.S. Patent No. 8,871,813
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`61,182;
`
`james.abe@alston.com); Lance Soderstrom (Registration No. 65,405;
`
`lance.soderstrom@alston.com). Please direct all correspondence to lead counsel at:
`
`4721 Emperor Boulevard, Suite 400, Durham, North Carolina 27730. Petitioner
`
`consents to email service. Telephone: (919) 862-2200. Facsimile: (919) 862-2260.
`
`V.
`
`STATEMENT OF THE PRECISE RELIEF REQUESTED AND THE
`REASONS THEREFORE (37 C.F.R. § 42.22(a))
`
`Petitioners request IPR and cancellation of claims 1-27. Petitioners’ full
`
`statement of the reasons for the relief requested is set forth in detail below.
`
`VI. THE ’813 PATENT
`The challenged claims of the ’813 patent are directed to a stable aqueous
`
`liquid preparation. The ’813 patent has three independent claims (claims 1, 7, and
`
`13). Independent claim 1 is directed to a stable aqueous liquid preparation consisting
`
`essentially of: (a) about 0.05 w/v % to about 0.2 w/v % of 2-amino-3-(4-
`
`bromobenzoyl)phenylacetic acid or a pharmacologically acceptable salt thereof or a
`
`hydrate thereof; (b) tyloxapol in an amount sufficient to stabilize component (a); (c)
`
`boric acid; (d) sodium tetraborate; and (e) water; ; and wherein said stable liquid
`
`preparation is formulated for ophthalmic administration.
`
`(EX1001, 11:30-42).1
`
`1 Citations are as follows: X:YY-ZZ (col:lines; patent); X:Y:Z (page:col:para;
`
`journal article); X:Y (page:para; journal article).
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`Petition for Inter Partes Review
`of U.S. Patent No. 8,871,813
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`Independent claim 7 is similar to claim 1, but the principal difference is that it recites
`
`a stability: “wherein the stable aqueous liquid preparation is characterized in that
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`greater than about 90% of the original amount of the first component remains in the
`
`preparation after storage at about 60°C. for 4 weeks.”
`
`(EX1001, 12:9-12).
`
`Independent claim 13 is similar to claim 1, but is different in that it affirmatively
`
`excludes mannitol. (EX1001, 12:50-51).
`
`Claim Construction
`A.
`Petitioner believes that no terms or phrases require specific construction for
`
`the purpose of this IPR.
`
`Indeed, the Board recently determined that “express
`
`construction of any claim term is not necessary” for the purposes of rendering a
`
`decision to institute review of the ’813 patent. Lupin Ltd., v. Senju Pharm. Co., Ltd.,
`
`IPR2015-01105 [Paper No. 9, pg. 7]. Therefore, in accordance with 37 C.F.R. §
`
`42.100(b),
`
`the challenged claims must be given their broadest
`
`reasonable
`
`interpretation in light of the specification of the ’813 patent.
`
`VII. PERSON OF SKILL IN THE ART (“POSA”) & STATE OF THE ART
`
`A POSA would have had education and/or experience in the field of
`
`ophthalmic formulations and drug delivery, and knowledge of the scientific
`
`literature concerning the same, specifically pharmaceutical
`
`formulations for
`
`ophthalmic
`
`administration,
`
`including
`
`those
`
`comprising
`
`anti-inflammatory
`
`compounds (such as NSAIDs) as of 2003. The education and experience levels may
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`Petition for Inter Partes Review
`of U.S. Patent No. 8,871,813
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`vary between persons of ordinary skill, with some persons holding a basic
`
`Bachelor’s degree, but with 5-10 years of relevant work experience, or others
`
`holding more advanced degrees—e.g., Pharm.D., Ph.D., or M.D.—but having fewer
`
`years of experience. A POSA may work as part of a multi-disciplinary team and
`
`draw upon not only his or her own skills, but also take advantage of certain
`
`specialized skills of others in the team, to solve a given problem. (EX1003, ¶ 20).
`
`As of January 21, 2003, the state of the art pertinent to the ’813 patent was
`
`such that aqueous liquid preparations containing NSAIDs (including bromfenac) and
`
`tyloxapol were disclosed, and well known. For example, Desai disclosed a
`
`formulation that included bromfenac and tyloxapol, and benzalkonium chloride
`
`(“BAC”), in addition to other ingredients.
`
`(EX1005, Abstract; 2:18-23, 3:30-45,
`
`6:13-16, 6:25-28; EX1017, 4:1-23, 6:8-9, 8:13-22, Formulation 3; EX1003, ¶¶ 31,
`
`39).
`
`It was also known that NSAID compounds were suitable and desirable for
`
`ophthalmic administration (EX1018, 1:1; EX1003, ¶¶ 25-26), and that the NSAID
`
`bromfenac was specifically described in ophthalmic formulations in the prior art.
`
`(EX1002, 2:1:2; EX1003, ¶¶ 29-31, 76). Likewise, ethoxylated octylphenol
`
`surfactants, including tyloxapol, have been used to stabilize NSAIDs in ophthalmic
`
`preparations for at least a half-century and were described in combination with the
`
`NSAIDs diclofenac and ketorolac (together with BAC) more than a year before the
`
`effective filing date. (EX1010, 3:1; EX1003, ¶¶ 32-37). BAC was widely used—
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`Petition for Inter Partes Review
`of U.S. Patent No. 8,871,813
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`indeed one of the most widely used—preservative excipients in ophthalmic
`
`formulations. (EX1030, 2:1:1; EX1003, ¶ 32-33).
`
`It was also well-known that NSAIDs bearing acidic groups such as a carboxyl
`
`group (like bromfenac, diclofenac, ketorolac, and others) could be incompatible with
`
`quaternary ammonium compounds such as BAC in ophthalmic formulations,
`
`because they could form a complex with the quaternary ammonium compounds.
`
`(EX1006, 1:10-24; EX1005, 1:27-34; EX1022, 2:18-24; EX1035, 4:1-5; EX1003,
`
`¶ 33).
`
`Indeed, bromfenac and diclofenac are considered acidic NSAID drugs.
`
`(EX1053, 1; EX1003, ¶ 41, n. 10). Moreover, the prior art taught that these
`
`complexes could result
`
`in precipitate formation, adversely affecting the
`
`preservative activity of BAC and reducing the activity of the acidic NSAID.
`
`(EX1035, 4:11-17; EX1011, 5:1-7; EX1003, ¶ 33). Indeed, even the patentee has
`
`admitted as much. (EX1001, 1:57-62; EX1003, ¶ 41, n. 10).2
`
`2 As the patentee explained “[b]enzalkonium chloride is a widely used preservative
`
`in ophthalmic solutions. However, benzalkonium chloride and other quaternary
`
`ammonium compounds are generally considered to be incompatible with ophthalmic
`
`compositions of drugs with acidic groups, such as nonsteroidal anti-inflammatory
`
`drugs. These preservatives lose their ability to function as they form complexes with
`
`the charged drug compounds.” (EX1001, 1:57-62).
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`Petition for Inter Partes R