UNITED STATES PATENT AND TRADEMARK OFFICE
`____________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`____________
`
`DR. REDDY’S LABORATORIES, INC.
`Petitioner
`
`v.
`
`POZEN INC.
`Patent Owner
`
`U.S. Patent No. 8,557,285
`Issue Date: October 15, 2013
`
`Title: PHARMACEUTICAL COMPOSITIONS FOR
`THE COORDINATED DELIVERY OF NSAIDS
`
`
`
`Inter Partes Review No. Unassigned
`
`PETITION FOR INTER PARTES REVIEW
`OF U.S. PATENT NO. 8,557,285 AND
`MANDATORY NOTICES UNDER 37 C.F.R. § 42.8
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`Lupin Exh. 1027
`
`

`
`
`
`TABLE OF CONTENTS
`
`Page
`
`TABLE OF AUTHORITIES ................................................................................... iii
`TABLE OF ABBREVIATIONS ............................................................................... v
`EXHIBIT LIST ....................................................................................................... vii
`I.
`INTRODUCTION ........................................................................................... 1
`II. MANDATORY NOTICES UNDER 37 C.F.R. § 42.8 ................................... 1
`A.
`Real Party-In-Interest - 37 C.F.R. § 42.8(b)(1) ..................................... 1
`B.
`Related Matters - 37 C.F.R. § 42.8(b)(2) .............................................. 1
`C.
`Lead and Back-Up Counsel Under 37 C.F.R. § 42.8(b)(3) .................. 2
`D.
`Service Information Under 37 C.F.R. § 42.8(b)(4) ............................... 2
`III. GROUNDS FOR STANDING – 37 C.F.R. § 42.104(A) ............................... 3
`IV. OVERVIEW OF CHALLENGE - 37 C.F.R. § 42.104(B) ............................. 4
`V.
`STATEMENT OF THE PRECISE RELIEF REQUESTED AND
`THE REASONS THEREFOR – 37 C.F.R. § 42.22(a) ................................. 12
`A.
`Background of the ‘285 Patent ............................................................ 12
`1.
`The ‘285 Patent Family and Predecessor Applications ............ 12
`2.
`The ‘285 Patent Specification ................................................... 13
`3.
`The Prosecution History Of The ‘285 Patent ........................... 17
`4.
`The Litigation ............................................................................ 20
`5.
`Horizon’s Citizen Petition and FDA Response ........................ 21
`THE LEVEL OF ORDINARY SKILL IN THE ART ........................ 24
`CLAIM CONSTRUCTION ................................................................ 24
`1.
`“Comprising …Naproxen Surrounded by a Coating” .............. 26
`2.
`“Inhibit” .................................................................................... 28
`
`B.
`C.
`
`i
`
`

`
`
`
`D.
`
`“at least a portion of said esomeprazole” .................................. 30
`3.
`The ‘285 Patent Claims are Invalid ..................................................... 31
`1.
`Ground 1: The Effective Filing Date is No Earlier
`than May 16, 2005 and the Plachetka Publication
`Anticipates Claims 1 – 4 and Renders them Obvious .............. 31
`a.
`The Disclosure in the Pre-2003 Applications ................. 31
`b.
`No Disclosure in the Pre-2003 Applications
`Supports the ‘285 Patent Claims .................................... 35
`The ‘285 Patent Claims 1 – 4 May Not Claim
`Priority to the Pre-2003 Applications and the
`Plachetka Publication is Invalidating Prior Art .............. 40
`Ground 2: Even if Entitled to a June 1, 2001 Priority
`Date, Claims 1 – 4 of the ‘285 Patent are Obvious
`Over Depui, Daneshmend, Lundberg and Clissold .................. 43
`a.
`The Primary References ................................................. 43
`i. WO 97125064 (“Depui”) ..................................... 43
`ii. WO 00/78293 (“Lundberg”) ................................ 44
`iii. WO 00/26185 (“Phillips”) .................................... 45
`iv. Clissold ................................................................. 46
`b. With Both Motivation and a Reasonable
`Expection of Success, the Presence of Only
`Two Options – Coated or Uncoated – Made
`Uncoated Esomeprazole Obvious to Try ........................ 47
`The Prior Art Did not “Teach Away” from
`Esomeprazole Formulations Without an Enteric
`Coating ............................................................................ 49
`Secondary Considerations fail to Overcome the
`Evidence Of Obviousness ......................................................... 54
`IV. CONCLUSION .............................................................................................. 56
`
`
`
`c.
`
`2.
`
`c.
`
`3.
`
`
`
`ii
`
`

`
`
`
`TABLE OF AUTHORITIES
`
`Page
`
`
`
`Cases
`Ariad Pharms., Inc. v. Eli Lilly & Co., 598 F.3d. 1336 (Fed. Cir. 2010) (en
`banc) ..................................................................................................................... 33
`In re Cuozzo Speed Techs., LLC, 2015 U.S. App. LEXIS 1699 (Fed. Cir.
`Feb. 4, 2015) ......................................................................................................... 24
`KSR Int’l Co. v. Teleflex Inc., 550 U.S. 398 (2007) ................................................ 52
`Leapfrog Enters. Inc. v. Fisher-Price Inc., 485 F.3d 1157 (Fed. Cir. 2007) ........... 55
`Macuato USA v. BOS GMBH & KG, IPR2012-00010 Paper 18, Jan. 24,
`2012 ........................................................................................................................ 3
`Richardson-Vicks Inc. v. Upjohn Co., 122 F.3d 1476 (Fed. Cir. 1997) .................. 55
`
`
`Rules, Regulations and Statutes
`35 U.S.C. § 102(b) ............................................................................................... 6, 40
`35 U.S.C. § 314(a) ..................................................................................................... 1
`35 U.S.C. § 315(b) ..................................................................................................... 3
`37 C.F.R. § 42.100(b) .............................................................................................. 24
`37 C.F.R. § 42.104(a) ................................................................................................. 3
`37 C.F.R. § 42.104(b) ................................................................................................ 4
`37 C.F.R. § 42.22(a) ................................................................................................. 12
`37 C.F.R. § 42.8 ......................................................................................................... 1
`37 C.F.R. § 42.8(b)(1) ................................................................................................ 1
`37 C.F.R. § 42.8(b)(2) ................................................................................................ 1
`37 C.F.R. § 42.8(b)(3) ................................................................................................ 2
`37 C.F.R. § 42.8(b)(4) ................................................................................................ 2
`
`
`
`iii
`
`

`
`
`
`D.N.J. L. Pat. R. 4.1 – 4.6 ........................................................................................ 24
`Fed. R. Civ. P. 41(a)(1)(A)(i) .................................................................................... 3
`
`Other Authorities
`Morrison & Boyd, Organic Chemistry, (Prentice-Hall, Inc., Englewood
`Cliffs, New Jersey, 3d ed. 1992) .......................................................................... 30
`Pilbrant and Cederberg, “Development of an Oral Formulation of
`Omeprazole,” Scand. J. Gastroenterol., 20(Suppl. 108):113-120 (1985) ..... 47, 51
`Sachs et al., “Review Article: The Control of Gastric Acid and
`Helicobacter Pylori Eradication,” Aliment Pharmacol. Ther., 14:1383-
`1401 (2000) ........................................................................................................... 50
`The Oxford Encyclopedic English Dictionary (Oxford Univ, Press, N.Y.,
`1991) ..................................................................................................................... 30
`The Random House Dictionary of the English Language, p. 732 (Random
`House, Inc., N.Y. 1966) ........................................................................................ 30
`Warren and Marshall, “Unidentified Curved Bacilli on Gastric Epithelium
`in Active Chronic Gastritis,” Lancet, I:1273-1275 (1983) ................................... 50
`
`
`
`iv
`
`
`
`
`
`

`
`TABLE OF ABBREVIATIONS
`
`
`
`
`
`
`
`
`Abbreviation
`‘216 Application
`‘285 patent
`‘588 Application
`‘855 application
`‘907 patent
`ANDA
`Clissold
`
`Explanation
`U.S. Application No. 10/158,216
`U.S. Patent No. 8,557,285 B2
`U.S. Provisional Application No. 60/294,588
`U.S. Application No. 13/215,855
`U.S. Patent No. 6,926,907 B2
`Abbreviated New Drug Application
`Omeprazole- A Preliminary Review of its
`Pharmacodynamic and Pharmacokinetic Properties, and
`Therapeutic Potential in Peptic Ulcer Disease and
`Zollinger-Ellison Syndrome, Drugs 32: 15-47 (1986), by
`Stephen P. Clissold and Deborah M. Campoli-Richards
`WO 97/25064
`Refers to the indicated example
`Refers to the indicated exhibit
`Food and Drug Administration
`Horizon Pharma, Inc., current licensee of the ‘285 patent
`and distributor of its commercial embodiment Vimovo®
`Howden et al., “Effects of Single and Repeated Doses of
`Omeprazole in Gastric Acid and Pepsin Secretion in Man,”
`Gut, 25, 707-710 (1984) (“Howden”)
`Information Disclosure Statement
`WO 00/78293
`Non-steroidal anti-inflammatory
`Dr. Reddy’s Laboratories, Inc.
`WO 00/26185
`Pilbrant and Cederberg, “Development of an Oral
`Formulation of Omeprazole,” Scand. J. Gastroenterol.,
`20(Suppl. 108):113-120 (1985) (“Pilbrant”) 
`Plachetka publication US2003/0069255
`Pozen
`Owner of the ‘285 patent, Pozen, Inc.
`PPI
`Proton Pump Inhibitor
`pre-2003 applications The ‘588 and ‘216 Applications
`Prichard et al., “Omeprazole: A Study of Its Inhibition of
`Prichard
`Gastric pH and Oral Pharmacokinetics After Morning or
`Evening Dosage,” Gastroenterol., 88:64-69 (1985)
`
`Depui
`Ex.___
`Exh. ___
`FDA
`Horizon
`
`Howden
`
`IDS
`Lundberg
`NSAID
`Petitioner
`Phillips
`Pilbrant
`
`
`
`v
`
`

`
`(“Prichard”)
`Horizon Pharma. and Pozen Inc. v. Dr. Reddy’s
`Laboratories, Inc. & Dr. Reddy’s Laboratories, Ltd.
`District of New Jersey, Civil Action No. 3-11-cv-02317
`(consolidated for discovery purposes with 3-13-cv-00091,
`3-11-cv-04275, 13-cv-04022 and 13-cv-03038)
`Tolman et al., “The Effects of Oral Doses of Lansoprazole
`and Omeprazole on Gastric pH,” J. Clin. Gastroenterol,
`24(2):65-70 (1997) (“Tolman”)
`All emphasis in quoted text has been added unless noted
`
`
`
`
`
`the Litigation
`
`Tolman
`
`Emphasis
`
`
`
`
`
`vi
`
`

`
`
`
`
`
`
`
`Exhibit No.
`1001
`1002
`1003
`1004
`1005
`
`1006
`
`1007
`
`1008
`
`1009
`
`1010
`1011
`1012
`1013
`1014
`1015
`1016
`1017
`1018
`1019
`1020
`
`1021
`
`EXHIBIT LIST
`
`
`Description
`United States Patent No. 8,557,285 B2
`United States Patent No. 8,852,636 B2
`United States Patent No. 8,858,996 B2
`United States Patent No. 6,926,907 B2
`Second Amended Complaint, Horizon Pharma. and Pozen
`Inc. v. Dr. Reddy’s Laboratories, Inc. & Dr. Reddy’s
`Laboratories, Ltd. District of New Jersey, Civil Action Nos.
`3-11-cv-02317, Docket Entry No. 226, February 25, 2014
`First Amended Complaint, Horizon Pharma. and Pozen Inc.
`v. Dr. Reddy’s Laboratories, Inc. & Dr. Reddy’s
`Laboratories, Ltd. District of New Jersey, Civil Action Nos.
`3-13-cv-00091, Docket Entry No. 62, February 25, 2014
`Print of ECF Docket of AstraZeneca AB, et. al. and Pozen
`Inc. v. Dr. Reddy’s Laboratories, Inc. & Dr. Reddy’s
`Laboratories, Ltd. District of New Jersey, Civil Action Nos.
`3-13-cv-06157
`Email correspondence between Alan H. Pollack and Ravin
`Patel, dated October 30 – 31, 2014
`Notice Of Voluntary Dismissal, AstraZeneca AB, et. al. and
`Pozen Inc. v. Dr. Reddy’s Laboratories, Inc. & Dr. Reddy’s
`Laboratories, Ltd. District of New Jersey, Civil Action No.
`3:13-cv-06157
`Pozen’s Responses to DRL’s Invalidity Contentions
`US Provisional Patent Application No. 60/294,588
`US Application No. 10/158,216
`US Application No. 11/129,320
`US Application No. 12/553,804
`US Application No. 13/215,855
`US Application No. 14/045,156
`US Application No. 14/244,471
`Letter of Pozen’s counsel dated 5/2/14
`Claim Construction Opinion of Judge Pisano dated 5/1/13
`Prosecution History of ‘855 Application (issued as ‘285
`patent)
`US 2003/0069255 A1, Published April 10, 2003
`vii
`
`

`
`
`
`
`
`Exhibit No.
`1022
`
`1023
`
`1024
`1025
`1026
`
`1027
`
`1028
`
`1029
`
`1030
`1031
`1032
`1033
`1034
`1035
`
`1036
`
`1037
`
`1038
`1039
`1040
`1041
`
`1042
`
`1043
`
`Description
`Prosecution History of ‘156 Application (issued as ‘636
`patent)
`Prosecution History of ‘471 Application (issued as ‘996
`patent)
`Horizon’s Citizen Petition, dated February 4, 2014
`FDA Response to Horizon’s Citizen Petition
`Morrison & Boyd, Organic Chemistry, (Prentice-Hall, Inc.,
`Englewood Cliffs, New Jersey, 3d ed. 1992), p. 49
`The Random House Dictionary of the English Language, p.
`732 (Random House, Inc., N.Y. 1966)
`The Oxford Encyclopedic English Dictionary (Oxford Univ,
`Press, N.Y., 1991). p. 730
`Clissold et al., “Omeprazole: A Preliminary Review of Its
`Pharmacodynamic and Pharmacokinetic Properties, and
`Therapeutic Potential in Peptic Ulcer Disease and Zollinger-
`Ellison Syndrome,” Drugs, 32, 15-47 (1986)
`WO 97/25064 published July 17, 1997 (“Depui”)
`WO 00/78293 published December 28, 2000 (“Lundberg”)
`WO 00/26185 published May 11, 2000 (“Phillips”)
`Nexium® Package Insert, February 2001
`Vimovo® Package Insert
`The Random House College Dictionary, p. 1035 (Random
`House, Inc., N.Y. 1988)
`Declaration of Arthur H. Kibbe, Ph.D. in Support of Inter
`Partes Review
`United States Patent No. 5,601,843 issued February 11,
`1997 (“’843 patent”)
`www.merriam-webster.com/dictionary/inhibit
`Zegerid® Package Insert
`Curriculum Vitae of Arthur Kibbe
`Provisional Application No. 60/294,588 (“’588
`provisional”)
`Brown and Yeomans, “Prevention of Gastrointestinal
`Adverse Effects of Nonsteroidal Anti-Inflammatory Drugs,”
`Drug Safety, Dec. 21 (6):503-512 (1999) (“Brown”)
`Bjorkman, “Nonsteroidal Anti-Inflammatory Drug-Induced
`Gastrointestinal Injury,” Am. J. Med, 101(Suppl. 1A) 25S-
`32S (1996) (“Bjorkman”)
`viii
`
`

`
`
`
`
`
`Exhibit No.
`1044
`
`1045
`
`1046
`
`1047
`
`1048
`
`1049
`1050
`1051
`
`1052
`
`1053
`
`1054
`
`1055
`
`1056
`
`Description
`Wallace, “How do NSAIDs cause ulcer disease?” Bailliere’s
`Clinical Gastroenterology,14(1):147-159 (2000)
`(“Wallace”)
`Scarpignato et al., “Prevention and Treatment of Non-
`Steroidal Anti-Inflammatory Drug-Induced Gastro-
`Duodenal Damage: Rational for the Use of Antisecretory
`Compounds,” Ital. J. Gastroenterol. Hepatol., 31 (Suppl.
`I):S63-72 (1999), PZ00096216-PZ00096225
`(“Scarpignato”)
`Daneshmend et al., “Abolition by Omeprazole of Aspirin
`Induced Gastric Mucosal Injury in Man,” Gut, v. 31, 514-
`517 (1990) (“Daneshmend”)
`Sachs et al., “Review Article: The Control of Gastric Acid
`and Helicobacter Pylori Eradication,” Aliment Pharmacol.
`Ther., 14:1383-1401 (2000), AZV00293734-AZV00293752
`(“Sachs”)
`Warren and Marshall, “Unidentified Curved Bacilli on
`Gastric Epithelium in Active Chronic Gastritis,” Lancet,
`I:1273-1275 (1983) (“Warren”)
`Prilosec® PDR 2000
`Nexium® Package Insert, February 2001
`U.S. Patent No. 5,877,192 issued March 2, 1999 (“’192
`patent”)
`U.S. Patent No. 5,714,504 issued February 3, 1998 (“’504
`patent”)
`Chandramouli et al., “Prevention and Management of
`NSAID-Induced Gastropathy,” Journal of Pharmaceutical
`Care in Pain and Symptom Control, v. 8(4) 27-40 (2000)
`(“Chandramouli”)
`U.S. Patent No. 6,319,519 issued November 20, 2001 (“’519
`patent”)
`Howden et al., “Effects of Single and Repeated Doses of
`Omeprazole in Gastric Acid and Pepsin Secretion in Man,”
`Gut, 25, 707-710 (1984) (“Howden”)
`Prichard et al., “Omeprazole: A Study of Its Inhibition of
`Gastric pH and Oral Pharmacokinetics After Morning or
`Evening Dosage,” Gastroenterol., 88:64-69 (1985)
`(“Prichard”)
`
`ix
`
`

`
`Exhibit No.
`1057
`
`1058
`
`1059
`
`1060
`
`1061
`1062
`
`1063
`1064
`
`1065
`
`1066
`
`Description
`Tolman et al., “The Effects of Oral Doses of Lansoprazole
`and Omeprazole on Gastric pH,” J. Clin. Gastroenterol,
`24(2):65-70 (1997) (“Tolman”)
`Ramage et al., Br. J. Clin. Pharmac. (1985), 19, 9-12
`(“Ramage”)
`Akdamar et al., Am. J. of Gastroenterology, 1982, v. 77, No.
`12, 902-904 (“Akdamar”)
`Wilson et al., “Effects of Misoprostol on Gastric Acid and
`Mucus Secretion in Man,” Dig. Dis. Sci., 31(Suppl. 2):126S-
`129S (1986) (“Wilson”)
`Remington’s Pharmaceutical Sciences, 17th ed., (1985).
`Kibbe A.H., Ed., “Handbook of Pharmaceutical Excipients,”
`3rd Ed., 2000.
`Naprocyn Physicians’ Desk Reference (2000), p. 2631-32
`Pilbrant and Cederberg, “Development of an Oral
`Formulation of Omeprazole,” Scand. J. Gastroenterol.,
`20(Suppl. 108):113-120 (1985) (“Pilbrant”)
`Miner et al., “Clinical Trial: Evaluation of Gastric Acid
`Suppression with Three Doses of Immediate-Release
`Esomeprazole in the Fixed-Dose Combination of PN 400
`(Naproxen/Esomeprazole Magnesium) Compared with
`Naproxen 500 mg and Enteric-Coated Esomeprazole 20 mg:
`A Randomized, Open-Label, Phase I Study in Healthy
`Volunteers,” Alim. Pharmacol. Ther., 32:414-424 (2010)
`(“Miner”)
`Non-confidential excerpts from the deposition transcript of
`Jeff Sherman MD, Horizon Pharma’s 30(b)(6) witness
`
`x
`
`
`
`
`
`
`
`

`
`
`
`I.
`
`INTRODUCTION
`
`Dr. Reddy’s Laboratories, Inc. (“Petitioner”) requests inter partes review of
`
`claims 1 – 4 of U.S. Patent No. 8,557,285 (“the ‘285 patent”) (Exh. 1001), owned
`
`by Pozen, Inc. (“Pozen”). A petition for inter partes review must demonstrate “a
`
`reasonable likelihood that the petitioner would prevail with respect to at least one
`
`of the claims challenged in the petition.” 35 U.S.C. § 314(a).
`
`Claims 1 - 4 of the ‘285 patent are invalid on two grounds: (1) the claims of
`
`the ‘285 patent are not supported by the two earliest claimed priority applications,
`
`and claims 1 - 4 are anticipated and obvious over the publication of the earliest
`
`non-provisional application in the priority chain; (2) even if Pozen could establish
`
`priority to its earliest priority applications, claims 1 - 4 remain obvious over the
`
`prior art.
`
`II. MANDATORY NOTICES UNDER 37 C.F.R. § 42.8
`
`
`A. Real Party-In-Interest - 37 C.F.R. § 42.8(b)(1)
`
`The Real-Parties-In-Interest are Petitioner Dr. Reddy’s Laboratories, Inc.,
`
`and its parent company, Dr. Reddy’s Laboratories, Ltd., an Indian company.
`
`B. Related Matters - 37 C.F.R. § 42.8(b)(2)
`
`Petitioner identifies the following related judicial matters:
`
`
`
`1
`
`

`
`
`
`1. Horizon Pharma, Inc. and Pozen Inc. v. Dr. Reddy’s
`Laboratories, Inc. & Dr. Reddy’s Laboratories, Ltd., 3:11-cv-
`02317-MLC-DEA (D.N.J.);
`2. Horizon Pharma, Inc. and Pozen Inc. v. Dr. Reddy’s
`Laboratories, Inc. & Dr. Reddy’s Laboratories, Ltd., 3:13-cv-
`00091-MLC-DEA (D.N.J.);
`3. Horizon Pharma Inc., and Pozen Inc. v. Lupin Ltd. & Lupin
`Pharmaceuticals, Inc. 3:11-cv-04275-MLC-DEA (D.N.J);
`4. Horizon Pharma
`Inc., and Pozen
`Inc.
`v. Mylan
`Pharmaceuticals, Inc.,3:13-cv-04022 (D.N.J.);
`5. Horizon Pharma Inc., AstraZeneca AB, AstraZeneca LP and
`Pozen Inc. v. Actavis Labs., FL, et. al. 3:13-cv-03038-MLC-
`DEA (D.N.J.) (collectively, “the Litigation”).
`
`Because the New Jersey District Court reassigned these matters from Judge Joel A.
`
`Pisano to Judge Mary L. Cooper on February 9, 2015, earlier references to these
`
`matters may include a suffix “JAP-DEA.”
`
`C. Lead and Back-Up Counsel Under 37 C.F.R. § 42.8(b)(3)
`
`Petitioner appoints Alan H. Pollack (Reg. No. 39,802) of Budd Larner, P.C.
`
`as lead counsel, and Louis H. Weinstein (Reg. No. 45,205) of Budd Larner, P.C. as
`
`back-up counsel.
`
`D.
`
`Service Information Under 37 C.F.R. § 42.8(b)(4)
`
`Service of any documents to lead and back-up counsel can be made via hand
`
`delivery to Budd Larner, P.C., 150 JFK Parkway, Short Hills, N.J. 07078.
`
`
`
`2
`
`

`
`
`
`Petitioner consents
`
`to service by email at apollack@buddlarner.com and
`
`lweinstein@buddlarner.com.
`
`III. GROUNDS FOR STANDING – 37 C.F.R. § 42.104(a)
`
`Petitioner certifies that the ‘285 patent is available for inter partes review,
`
`and that Petitioner is not barred or estopped from requesting an inter partes review
`
`on the grounds identified in the petition. Petitioner filed this petition less than one
`
`year after the February 25, 2014 service of Amended Complaints in the Litigation
`
`(Exhs. 1005, 1006). The petition is thus timely under 35 U.S.C. § 315(b).
`
`Pozen filed a complaint that asserted infringement of the ‘285 patent against
`
`Petitioner on October 23, 2013, but that complaint was never served. The
`
`electronic docket of that case shows neither the filing of any waiver of service nor
`
`any evidence of personal service on Petitioner. See Exh. 1007. While Pozen and
`
`Petitioner discussed the possibility of a waiver of service, see Exh. 1008, Petitioner
`
`never executed any waiver of service. Even if it had, because Pozen voluntarily
`
`dismissed this complaint pursuant to Fed. R. Civ. P. 41(a)(1)(A)(i), (see Exh.
`
`1009), such service would be discounted for the purpose of assessing the timeliness
`
`of this petition. See Macuato USA v. BOS GMBH & KG, IPR2012-00010 Paper 18,
`
`Jan. 24, 2012, pp. 15 – 16 (“The Federal Circuit has consistently interpreted the
`
`effect of such dismissals as leaving the parties as though the action had never been
`
`
`
`3
`
`

`
`
`
`brought….Accordingly, the dismissal of the earlier action against Macauto Taiwan
`
`nullifies the effect of the alleged service of the complaint on Petitioner.”).
`
`IV. OVERVIEW OF CHALLENGE - 37 C.F.R. § 42.104(b)
`
`Petitioner requests that claims 1 – 4 of the ‘285 patent be held unpatentable
`
`based on the following grounds:
`
`Ground 1. Claims 1 - 4 are anticipated or rendered obvious by
`
`US2003/0069255 (Exh. 1021, “the Plachetka Publication”) The Plachetka
`
`Publication published on April 10, 2003, more than two years before the filing of
`
`any application to which the ‘285 patent may claim priority. The effective filing
`
`date of the ‘285 patent claims is no earlier than May 16, 2005 because applications
`
`filed before this date cannot support the ‘285 patent claims. Five of its features are
`
`absent from those applications. The Plachetka Publication (Exh. 1021) anticipates
`
`the ‘285 patent claims, and renders them obvious.
`
`The ’285 patent claims pharmaceutical formulations that combine the two
`
`active ingredients naproxen and esomeprazole ostensibly in a way that lowers the
`
`risk of stomach injury for people taking naproxen repeatedly. Naproxen is a non-
`
`steroidal anti-inflammatory (“NSAID”), which is a class of pain relievers that also
`
`includes aspirin and ibuprofen. Although NSAIDs relieve pain, their repeated use
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`can injure the stomach. Naproxen is the active ingredient in the pain relief
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`medication Aleve.™ Esomeprazole is an acid inhibitor from a class of drugs
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`
`
`4
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`

`
`
`
`known as proton pump inhibitors (“PPIs”). Esomeprazole is the active ingredient
`
`in the anti-ulcer medication Nexium.™
`
`The ‘285 patent admits that NSAID/PPI combinations are not new, and that
`
`others had already combined them to lessen the risk of stomach injury. The
`
`specification, however, contends that coordinating the release of naproxen and
`
`esomeprazole so that all of the esomeprazole is released before any of the naproxen
`
`is released distinguishes the invention from prior art and provides a therapeutic
`
`benefit. Exh. 1001, 2:30 – 31. In order to release naproxen and esomeprazole in
`
`this coordinated manner, naproxen may be in a core coated to prevent its release
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`until reaching a desired pH, and uncoated esomeprazole may be in an outer layer
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`designed to release first. See e.g., ‘285 patent Fig. 2 (Exh. 1001, sheet 1).
`
`The ‘285 patent issued on October 15, 2013 from App. No. 13/215,855
`
`(Exh. 1015, “the ‘216 Application”), a fourth-generation descendent application of
`
`Prov. App. 60/294,588 (Exh. 1011, “the ‘588 Application”), filed June 1, 2001.
`
`The ‘285 patent claims priority to the ‘588 Application and App. No. 10/158,216
`
`(Exh. 1012, “the ‘216 Application”), filed May 31, 2002 (collectively, “the pre-
`
`2003 applications”). Despite the claim of priority, the ‘285 patent claims are not
`
`supported by the pre-2003 applications because the claims are broader than the
`
`disclosure in the pre-2003 applications in five ways, as explained in detail
`
`below. The ‘216 Application published as the Plachetka Publication (Exh. 1021)
`
`
`
`5
`
`

`
`
`
`on April 10, 2003, more than one year prior to the next application in the chain,
`
`App. No. 11/129,320 (Exh. 1013), filed May 16, 2005. Therefore, the Plachetka
`
`Publication
`
`is prior art
`
`to
`
`the ‘285 patent claims under 35 U.S.C. §
`
`102(b). Although the Plachetka Publication does not support claims 1 - 4 of the
`
`‘285 patent, it anticipates those claims and renders them obvious. The following
`
`figure shows the application chain and the priority break.
`
`
`
`6
`
`

`
`The Application Chain that Preceded US Patent No. 8,557,285
`
`US Prov. App.
`
`60/294,588
`
`June 1,2001
`
`May 31, 2002
`
`"Plachetka
`
`' bIj1:aj:i..
`U
`on
`
`'5.
`
`“pre-2003
`
`applications"
`
`‘The ‘.216 Application ._
`.
`Does Not Sunpc_>r&he
`
`‘Z85 Patent claims
`
`
`
`
`
`App. No.
`
`10/158,216
`
`US2003/
`
`_
`fil"i3"I’i1-
`'
`
`0069255 Publishes
`.. .
`F\l'\l'lFI
`AD“ -----'lU. ZUU5
`
`
`Mmthan
`One Year
`
`Plachetka
`
`Publication
`
`the ’285 Claims
`
`and/or Renders
`
`Them Obvious
`
`
`
`Appl. No.
`
`11/129,320
`
`May '16, 2005
`
`Appl. No.
`
`12/553,804
`
`September 3, 2009
`
`*‘‘*PP'- N0
`
`13/215555
`
`ALlgLlSt 23,
`
`7
`
`

`
`
`
`Under the broadest reasonable construction standard, the ‘285 patent claims
`are broad enough to encompass formulations with any or all of the following
`features:
`• releases most of its naproxen immediately at any pH;
`• releases all of its naproxen slowly at any pH;
`• delays release of most of its esomeprazole until reaching a particular pH;
`• does not have “coordinated release;” or
`• may be administered orally or in any other manner.
`
`The break in the priority arises because neither of the two pre-2003 applications
`
`has written description to support a naproxen/esomeprazole formulation with any
`
`of these features.
`
`Indeed, these features are contrary to much of what the pre-2003
`
`applications
`
`do
`
`disclose.
`
`The
`
`pre-2003
`
`applications
`
`disclose
`
`naproxen/esomeprazole formulations that:
`
`• release no naproxen immediately, and delays naproxen release until
`reaching a pH of 3.5 or 4;
`• prevents the release all of their naproxen until reaching a pH of 3.5 or 4 (as
`opposed to merely slowing it down, i.e., “inhibiting” it);
`• releases all their esomeprazole immediately regardless of pH;
`• have “coordinated release;” and
`• are orally administered.
`
`All claims of the ‘285 patent require, inter alia, a “unit dosage” (i.e., a “single
`
`entity for drug administration,” Exh. 1001, 4:42), with “naproxen surrounded by a
`
`
`
`8
`
`

`
`
`
`coating that inhibits its release from said unit dosage form unless said dosage form
`
`is in a medium with a pH of 3.5 or higher.” The broadest reasonable construction
`
`of the ‘285 patent claims, and the one proffered by Pozen in the Litigation, permits
`
`most of the naproxen to be released immediately regardless of pH and to be outside
`
`of this inhibition coating.
`
`Moreover, the ‘285 patent claims all recite a coating that “inhibits” naproxen
`
`release until reaching a pH of 3.5, rather than “preventing” it. The meaning of
`
`“inhibit” is broader than “prevent.” Because “inhibit” means either to slow down
`
`or to stop, the ‘285 patent claims read on a naproxen release coating that merely
`
`decreases the rate of naproxen release, instead of preventing release, until the
`
`composition “is in a medium of pH of 3.5 or higher.”
`
`The disclosure of the pre-2003 applications only describes immediate
`
`release esomeprazole and other acid inhibitors from the unit dosage and no portion
`
`subject to a delayed release by being coated with an enteric coating. The ‘285
`
`patent claims are broader because they require only “a portion” of the
`
`esomeprazole to be outside of an enteric coating and to be immediate released.
`
`Finally, contrary to the disclosure in the pre-2003 applications, none of the
`
`claims of the ‘285 patent recite “coordinated delivery” or “coordinated release” as
`
`an element. Similarly, none recite an “oral administration” element.
`
`
`
`9
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`

`
`
`
`Because all claims of the ‘285 patent exceed the scope of the disclosure in
`
`the pre-2003 applications (and do so in five ways), they cannot look to the pre-
`
`2003 applications for priority, and are invalidated by the Plachetka Publication.
`
`Ground 2. Claims 1 – 4 are obvious over Depui, Lundberg, Phillips and/or
`
`Clissold (Exhs. 1030, 1031, 1032, 1029). These references are properly combined
`
`because the sole purpose of esomeprazole in the ‘285 patent claims is to raise pH.
`
`One of ordinary skill knew that esomeprazole would raise pH even if half were
`
`destroyed by stomach acid, and also knew that repeated administration of the
`
`claimed formulation would cause less and less of esomeprazole to be destroyed.
`
`Thus, even if the Plachetka Publication were unavailable as prior art, other
`
`prior art renders the ‘285 patent claims invalid. Indeed, the specification of the
`
`‘285 patent acknowledges that “others have disclosed strategies for combining the
`
`two active agents for therapeutic purposes” but asserts that such prior art
`
`combinations did “not provide for coordinated drug release or for reducing
`
`intragastric acid levels to a non-toxic level prior to the release of NSAID….” Exh.
`
`1001, 2:26-37. According to the ‘285 patent, “coordinated drug release” of the
`
`naproxen and esomeprazole in the unit dosage distinguishes the invention from the
`
`prior art. Id.
`
`
`
`10
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`

`
`
`
`Another element in all claims of the ‘285 patent is: “esomeprazole, wherein
`
`at least a portion of said esomeprazole is not surrounded by an enteric coating”1 is
`
`obvious. Indeed, this feature is not described by the ‘285 patent as distinguishing
`
`the invention from prior art. In the prosecution of the ‘285 patent, Pozen relied on
`
`this element to discount PPI prior art that lacked an enteric coating and argued that
`
`this art was not properly combined because it also included buffering materials like
`
`sodium bicarbonate. But none one of the ‘285 patent claims exclude buffers, and
`
`two of the eight composition Examples include generous amounts of sodium
`
`bicarbonate (between 80 – 90 % by weight). See Exh. 1001, 17:49 – 20:36, Ex. 7-
`
`8. In addition, esomeprazole in the invention serves only to raise pH (as opposed to
`
`treating various stomach injuries as it does in the prior art), and one of ordinary
`
`skill knew that uncoated esomprazole in a combination product would raise pH
`
`enough to protect the stomach from naproxen.
`
`
`1 The term “enteric coating” appears in both the ‘907 and ‘285 patent claims. In
`the Litigation, Judge Pisano construed this term in the ‘907 patent to mean “a
`delayed release coating”, and recognized that it is “commonly and perhaps
`frequently pH-dependent.” Exh. 1019, p. 12. Petitioner accepts this definition here.
`See also Exh. 1036, Kibbe Decl. ¶ 68.
`
`
`
`11
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`

`
`
`
`V.
`
`STATEMENT OF THE PRECISE RELIEF REQUESTED AND THE
`REASONS THEREFOR – 37 C.F.R. § 42.22(a)
`
`A. Background of the ‘285 Patent
`
`1.
`
`The ‘285 Patent Family and Predecessor Applications
`
`As shown in the figure on page 7, and reflected on the face of the ‘285
`
`patent, Exh. 1001, the ‘285 patent issued from a series of five applications. All are
`
`entitled “Pharmaceutical Compositions for the Coordinated Delivery of NSAIDs,”
`
`and speak to compositions combining an acid inhibitor and an NSAID and related
`
`methods. All name John R. Plachetka as their sole inventor. The ‘285 patent family
`
`also includes other applications filed after the five applications that lead to the ‘285
`
`patent. See Exh. 1002, 1003, 1022 and 1023.
`
`NSAIDs relieve pain, but their continual use poses a risk of stomach
`
`problems, such as ulcers. See Exh. 1036, Declaration of Arthur H. Kibbe (“Kibbe
`
`Decl.”) ¶ 39. The combination of an acid inhibitor with an NSAID lessens that risk
`
`by raising the pH of the stomach. All of this was known before June 1, 2001, the
`
`earliest claimed priority date of the ‘285 patent. Id. ¶¶ 40 – 41.
`
`The specifications highlight naproxen as a preferred NSAID. They also
`
`highlight esomeprazole, which is the S-enantiomer of omeprazole, as a preferred
`
`acid inhibitor among the class of “PPI” a