`
`
`UNITED STATES PATENT AND TRADEMARK OFFICE
`
`
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`
`
`
`
`
`
`
`ARGENTUM PHARMACEUTICALS LLC,
`Petitioner
`
`v.
`
`COSMO TECHNOLOGIES LIMITED,
`Patent Owner.
`
`U.S. Patent No. 9,320,716 to Villa et al.
`Issue Date: April 26, 2016
`Title: Controlled Release and Taste Masking Oral Pharmaceutical Compositions
`
`
`
`
`Inter Partes Review No.: IPR2018-00080
`
`
`
`
`
`Petition for Inter Partes Review of U.S. Patent No. 9,320,716 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
`
`

`

`
`
`I. 
`
`II. 
`
`III. 
`
`Petition for Inter Partes Review
`of U.S. Patent No. 9,320,716
`
`CONTENTS
`
`INTRODUCTION ........................................................................................... 1 
`
`OVERVIEW .................................................................................................... 1 
`
`STANDING (37 C.F.R. § 42.104(a); PROCEDURAL
`STATEMENTS) .............................................................................................. 1 
`
`IV.  MANDATORY NOTICES (37 C.F.R. § 42.8(a)(1)) ...................................... 2 
`
`A. 
`
`B. 
`
`Each Real Party-In-Interest (37 C.F.R. § 42.8(b)(1)) ........................... 2 
`
`Notice of Related Matters (37 C.F.R. § 42.8(b)(2)) .............................. 2 
`
`1. 
`
`2. 
`
`Judicial Matters ........................................................................... 2 
`
`Administrative Matters ............................................................... 2 
`
`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)): ................... 3 
`
`V. 
`
`STATEMENT OF THE PRECISE RELIEF REQUESTED AND THE
`REASONS THEREFORE (37 C.F.R. § 42.22(a)) .......................................... 3 
`
`VI.  THE ’716 PATENT ......................................................................................... 4 
`
`A. 
`
`Claim Construction ............................................................................... 5 
`
`VII.  A PERSON OF ORDINARY SKILL IN THE ART ...................................... 6 
`
`VIII.  IDENTIFICATION OF CHALLENGE (37 C.F.R. § 42.104(b)) ................... 7 
`
`IX. 
`
`INVALIDITY ANALYSIS ............................................................................. 9 
`
`A.  Ground 1: U.S. Patent No. 5,681,584 Anticipates Claims 1-29 ........... 9 
`
`1. 
`
`2. 
`
`3. 
`
`Disclosure of the ’584 Patent .................................................... 10 
`
`Analysis of Independent Claims 1, 12 and 22 .......................... 10 
`
`Analysis of Dependent Claims.................................................. 19 
`
`B. 
`
`Ground 2: Claims 1-29 are Rendered Obvious by U.S. Patent
`No. 5,681,584 ...................................................................................... 23 
`
`i
`
`

`

`1. 
`
`2. 
`
`The Level of Ordinary Skill in the Pertinent Art and the
`Scope and Content of the Prior Art ........................................... 24 
`
`Differences Between the Claims and the Prior Art .................. 25 
`
`C. 
`
`Ground 3: U.S. Patent No. 5,811,388 Anticipates Claims 1-7, 9,
`11-17, 19 and 21-29 ............................................................................ 39 
`
`1. 
`
`2. 
`
`3. 
`
`Disclosure of the ’388 Patent .................................................... 39 
`
`Analysis of Independent Claims 1, 12 and 22 .......................... 40 
`
`Analysis of Dependent Claims 2-7, 9, 11, 13-17, 19, 21,
`and 23-29 ................................................................................... 50 
`
`D.  Ground 4: U.S. Patent No. 5,811,388 Renders Obvious Claims
`1- 29 ..................................................................................................... 53 
`
`1. 
`
`2. 
`
`Differences Between the Claims and the Prior Art .................. 53 
`
`Reasonable Expectation of Success .......................................... 62 
`
`E. 
`
`Ground 5: U.S. Patent No. 5,811,388 in View of U.S. Patent
`No. 5,681,584 Renders Obvious Claims 8, 10, 18, and 20 ................. 63 
`
`1. 
`
`Differences Between the Claims and the Prior Art .................. 63 
`
`F. 
`
`Objective Indicia of Non-Obviousness ............................................... 65 
`
`1. 
`
`2. 
`
`3. 
`
`4. 
`
`No Long-Felt Unmet Need ....................................................... 66 
`
`No Failure of Others ................................................................. 67 
`
`No Unexpected Results Over the Closest Prior Art .................. 67 
`
`No Commercial Success ........................................................... 68 
`
`X. 
`
`CONCLUSION .............................................................................................. 68 
`
`
`
`ii
`
`
`

`

`
`TABLE OF AUTHORITIES
`
` Page(s)
`
`Cases
`
`In re Aller,
`220 F.2d 454 (C.C.P.A. 1955) ............................................................................ 34
`
`Amneal Pharms. LLC v. Hospira, Inc.,
`IPR2016- 01577, Paper 11 (Decision to Institute) (P.T.A.B. Feb. 9
`2017) ................................................................................................................... 67
`
`Amneal Pharms. LLC v. Purdue Pharma L.P.,
`IPR2016-01412, Paper 9 (P.T.A.B. Feb. 14, 2017) ........................................ 9, 66
`
`Amneal Pharms. LLC v. Purdue Pharma L.P.,
`IPR2016-01413, Paper 9 (P.T.A.B. Jan. 18, 2017) ........................................ 9, 39
`
`Amneal Pharms., LLC v. Supernus Pharms., Inc.,
`IPR2013-00368, Paper 8 (P.T.A.B. Dec. 17, 2013) ........................................... 66
`
`In Re Baxter Travenol Labs.,
`952 F.2d 388 (Fed. Cir. 1991) ...................................................................... 29, 55
`
`Biomarin Pharmaceutical Inc. v. Genzyme Therapeutic Products Ltd.
`Partnership,
`IPR2013-00534, Paper 81 (P.T.A.B. Feb. 23, 2015) .............................. 34, 35, 36
`
`Boston Sci. Scimed, Inc. v. Cordis Corp.,
`554 F.3d 982 (Fed. Cir. 2009) ............................................................................ 23
`
`Bristol-Myers Squibb Co. v. Ben Venue Labs.,
`246 F.3d 1368 (Fed. Cir. 2001) .......................................................................... 65
`
`Chi Mei Innolux Corp. v. Semiconductor Energy Lab. Co., Ltd.,
`IPR2013-00028, Paper 14 (P.T.A.B. Mar. 21, 2014) ........................................... 8
`
`Coalition For Affordable Drugs II, LLC v. Cosmo Technologies, Ltd.,
`IPR2015-00988, Paper 8 (P.T.A.B. Oct. 7, 2015) .............................................. 26
`
`iii
`
`
`

`

`Cuozzo Speed Techs., LLC v. Lee,
`136 S. Ct. 2131 (2016) .......................................................................................... 6
`
`In re De Blauwe,
`736 F.2d 699 (Fed. Cir. 1984) ............................................................................ 67
`
`In re Depomed,
`Case No. 2016-1378, Slip Op. at 6-7 (Fed. Cir. Feb. 21, 2017) ................... 38, 63
`
`In re Fout,
`675 F.2d 297 (C.C.P.A. 1982) ............................................................................ 60
`
`Friskit, Inc. v. Real Networks, Inc.,
`306 F. App’x 610 (Fed. Cir. 2009) ..................................................................... 66
`
`In re Fulton,
`391 F.3d 1195 (Fed. Cir. 2004) .................................................................... 37, 62
`
`Graham v. John Deere Co. of Kansas City,
`383 U.S. 1 (1966) .................................................................................... 23, 24, 25
`
`Iron Grip Barbell Co. v. USA Sports, Inc.,
`392 F.3d 1317 (Fed. Cir. 2004) .................................................................... 66, 67
`
`Kennametal Inc. v. Ingersoll Cutting Tool Co.,
`780 F.3d 1376 (Fed. Cir. 2015) ...................................................................... 9, 18
`
`Koios Pharm LLC v. Medac Gesellschaft Fur Klinische
`Spezialpraparate,
`IPR2016-01370, Paper 13 (P.T.A.B. Feb. 8, 2017) ................................ 37, 61, 66
`
`KSR Int’l Co. v. Teleflex Inc.,
`550 U.S. 398 (2007) ............................................................................................ 36
`
`Lupin Ltd. et al. v. Senju Pharmaceutical Co., Ltd.,
`IPR2015-01099, Paper 69 (P.T.A.B. Sep. 12, 2016) .................................... 59, 65
`
`In re Mayne,
`104 F.3d 1339 (Fed. Cir. 1997) .................................................................... 59, 65
`
`In re Merchant,
`575 F.2d 865 (C.C.P.A. 1978) ............................................................................ 67
`
`iv
`
`
`

`

`In re Mouttet,
`686 F.3d 1322 (Fed. Cir. 2012) .................................................................... 37, 62
`
`Newell Cos., Inc. v. Kenney Mfg. Co.,
`864 F.2d 757 (Fed. Cir. 1988) ............................................................................ 65
`
`Ormco Corp. v. Align Tech., Inc.,
`463 F.3d 1299 (Fed. Cir. 2006) .......................................................................... 67
`
`Par Pharm. Inc. v. Novartis AG,
`IPR2016-01479, Paper 8 (Institution Decision) (P.T.A.B. Feb. 15,
`2017) ................................................................................................................... 38
`
`In re Paulson,
`30 F.3d 1475 (Fed. Cir. 1994) .............................................................................. 9
`
`In re Peterson,
`315 F.3d 1325 (Fed. Cir. 2003) .......................................................................... 67
`
`Pfizer, Inc. v. Apotex, Inc.,
`480 F.3d 1348 (Fed. Cir. 2008) .......................................................................... 65
`
`Purdue Pharma L.P. v. Epic Pharma, LLC,
`811 F.3d 1345 (Fed. Cir. 2016) .................................................................... 18, 49
`
`Santarus, Inc. v. Par Pharm., Inc.,
`694 F.3d 1344 (Fed. Cir. 2012) .................................................................... 29, 55
`
`Sharp Corp. v. Surpass Tech Innovation LLC,
`IPR2015-00021, Paper 10 (P.T.A.B. Mar. 18, 2015) ........................................... 8
`
`In re Siebentritt,
`372 F.2d 566 (C.C.P.A. 1967) ............................................................................ 60
`
`In re Spada,
`911 F.2d 705 (Fed. Cir. 1990) ................................................................ 17, 49, 60
`
`In re Translogic Tech., Inc.,
`504 F.3d 1249 (Fed. Cir. 2007) ............................................................................ 6
`
`Vandenberg v. Dairy Equip. Co.,
`740 F.2d 1560 (Fed. Cir. 1984) .......................................................................... 68
`
`v
`
`
`

`

`Wm. Wrigley Jr. Co. v. Cadbury Adams USA LLC,
`683 F.3d 1356 (Fed. Cir. 2012) .................................................................... 18, 49
`
`Statutes
`
`35 U.S.C. § 102 ...................................................................................................... 8, 9
`
`35 U.S.C. § 102(b) ..................................................................................... 7, 9, 25, 39
`
`35 U.S.C. § 103 .......................................................................................................... 8
`
`35 U.S.C. § 119 .......................................................................................................... 6
`
`35 U.S.C. § 119(a) ..................................................................................................... 7
`
`35 U.S.C. § 120 .......................................................................................................... 6
`
`35 U.S.C. § 325(d) ............................................................................................... 9, 39
`
`Other Authorities
`
`37 C.F.R. § 42.6(d) .................................................................................................... 7
`
`37 C.F.R. § 42.8(a)(1) ................................................................................................ 2
`
`37 C.F.R. § 42.8(b)(1) ................................................................................................ 2
`
`37 C.F.R. § 42.8(b)(2) ................................................................................................ 2
`
`37 C.F.R. §§ 42.8(b)(3) .............................................................................................. 3
`
`37 C.F.R. § 42.8(b)(4) ................................................................................................ 3
`
`37 C.F.R. § 42.10(a) ................................................................................................... 3
`
`37 C.F.R. § 42.10(b) .............................................................................................. 1, 3
`
`37 C.F.R. §42.15(a) .................................................................................................... 1
`
`37 C.F.R. § 42.22(a) ................................................................................................... 3
`
`37 C.F.R. § 42.63(e) ................................................................................................... 1
`
`37 C.F.R. § 42.100(b) ................................................................................................ 6
`
`vi
`
`
`

`

`37 C.F.R. § 42.104(a) ................................................................................................. 1
`37 C.F.R. § 42.104(a) ................................................................................................. 1
`
`37 C.F.R. § 42.104(b) ................................................................................................ 7
`37 CPR. § 42.104(b) ................................................................................................ 7
`
`37 C.F.R. § 42.106(a) ................................................................................................. 1
`37 CPR. § 42.106(a) ................................................................................................. 1
`
`M.P.E.P. § 2133 ......................................................................................................... 7
`M.P.E.P. § 2133 ......................................................................................................... 7
`
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`Vii
`
`vii
`
`
`

`

`
`
`TABLE OF EXHIBITS
`
`Petitioner
`Exhibit #
`1001
`
`Description
`U.S. Patent No. 9,320,716 to Villa et al., “Controlled Release and
`Taste Masking Oral Pharmaceutical Compositions”
`U.S. Patent No. 8,784,888 to Villa et al., “Controlled Release and
`Taste Masking Oral Pharmaceutical Composition”
`Reserved
`Reserved
`Reserved
`Declaration of Hartmut Derendorf, Ph.D.
`Curricula Vitae of Hartmut Derendorf, Ph.D.
`U.S. Patent No. 5,681,584 to Savastano et al., “Controlled Release
`Drug Delivery Device”
`U.S. Patent No. 5,811,388 to Friend et al., “Delivery of Drugs to the
`Lower GI Tract”
`U.S. Patent No. 6,239,120 to Hallgren et al., “Method and Means for
`Treating Glomerulonephritis”
`U.S. Patent Appl. Pub. No. 2006/0134208 to Villa et al., “Controlled
`Release and Taste Masking Oral Pharmaceutical Composition”
`1012 Markman Opinion and Order in Cosmo Technologies Limited v.
`Alvogen Pine Brook, LLC., C.A. No. 15-193-LPS, ECF Nos. 167,
`168 (D. Del. Sept. 7, 2016).
`Amendment and Response to Advisory Action filed on February 21,
`2014 in U.S. Patent Appl. No. 13/617,138
`Substitute Specification (Clean Copy) filed on April 29, 2013 in U.S.
`Patent Appl. No. 13/617,138
`Amendment After Final filed on April 29, 2013 in U.S. Patent Appl.
`No. 13/617,138
`Amendment and Response to Office Action filed on July 1, 2013 in
`U.S. Patent Appl. No. 13/617,138
`U.S. Patent No. 6,607,751 to Odidi et al., “Controlled Release
`Delivery Device for Pharmaceutical Agents Incorporating Microbial
`Polysaccharide Gum”
`is as Effective as Oral
`Campieri et al., Oral Budesonide
`Prednisolone in Active Crohn’s Disease, Gut, 41:209-214 (1997)
`Reserved
`
`1002
`
`1003
`1004
`1005
`1006
`1007
`1008
`
`1009
`
`1010
`
`1011
`
`1013
`
`1014
`
`1015
`
`1016
`
`1017
`
`1018
`
`1019
`
`viii
`
`
`

`

`1020
`1021
`1022
`
`1023
`
`1024
`
`1025
`1026
`
`1027
`1028
`1029
`1030
`
`1031
`1032
`1033
`
`1034
`
`1035
`
`1036
`
`1037
`
`1038
`
`1039
`
`Reserved
`Reserved
`PCT International Publication No. WO 96/36318, “Three-Phase
`Pharmaceutical Form With Constant and Controlled Release of
`Amorphous Active Ingredient for Single Daily Application”
`U.S. Patent No. 5,342,625 to Hauer et al., “Pharmaceutical
`Compositions Comprising Cyclosporins”
`PCT International Publication No. WO 99/39700, “Pharmaceutical
`compositions in form of nanoparticles comprising lipidic substances
`and amphiphilic substances and related preparation process”
`FDA Inactive Ingredient Guide 1996/1997
`Handbook of Pharmaceutical Excipients (Wade and Weller, eds., 2d
`ed. 1994)
`Reserved
`Remington: The Science and Practice of Pharmacy, Vol. 1 (1995)
`Reserved
`Hawley’s Condensed Chemical Dictionary (John Wiley & Sons,
`Inc., 13th ed. 1997)
`Reserved
`Entocort® EC Highlights of Prescribing Information
`Svensson et al., Hydration of an Amphiphilic Excipient, Gelucire
`44/14, 2004, <hal-00015990>
`U.S. Patent No. 6,395,300 to Straub et al., “Porous Drug Matrices
`and Methods of Manufacture Thereof”
`Flanders et al., The Control of Drug Release From Conventional
`Melt Granulation Matrices, Drug Development & Industrial
`Pharmacy, 13(6):1001-1022 (1987)
`Gandhi et al., Extrusion and Spheronization in the Development of
`Oral Controlled-Release Dosage Forms, Pharmaceutical Sci. &
`Tech. Today 2(4):160 (1999)
`US Patent No. 4,880,830
`Formulation”
`Daly et al., The Effect of Anionic Surfactants on the Release of
`Chlorpheniramine from a Polymer Matrix Tablet, Int’l J. of
`Pharmaceutics, 18:201-05 (1984)
`S.S. Davis, The Design and Evaluation of Controlled Release
`Dosage Forms for Oral Delivery, S.T.P. Pharma 3(5):412-417
`(1987)
`
`to Alan Rhodes, “Slow Release
`
`ix
`
`
`

`

`1040
`
`1041
`
`1042
`1043
`
`1044
`
`1045
`
`1047
`
`1048
`
`1049
`1050
`
`1051
`
`1052
`
`U.S. Patent No. 5,849,327 to Berliner et al., “Delivery of Drugs to
`the Lower Gastrointestinal Tract”
`U.S. Patent No. 5,643,602 to , “Oral Composition for the Treatment
`of Inflammatory Bowel Disease”
`U.S. Provisional Application No. 60/080,274 filed on April 1, 1998
`Gliko-Kabir et al., Low Swelling, Crosslinked Guar and Its Potential
`Use as a Colon-Specific Drug Carrier, Pharm. Research 15(7):1019-
`1025 (1998)
`See A Blume, B Arnold, HU Weltzien, Effects of a synthetic
`lysolecithin analog on
`the phase
`transition of mixtures of
`phosphatidylethanolamine and phosphatidylcholine, FEBS Letters
`(1976)
`Qiu et al., Design of sustained-release matrix systems for a highly
`water-soluble compound, ABT-089, Int’l J. of Pharmaceutics 157:43-
`52 (1997)
`1046 M. Efentakis et al., The Influence of Surfactants on Drug Release
`from a Hydrophobic Matrix, Int’l J. Pharm. 70:153-58 (1991)
`Uceris® website, https://www.uceris.com/tablet/ (accessed on March
`5, 2017)
`Santarus’ CEO Discusses FDA Approval Of UCERIS (Budesonide)
`For The Induction Of Remission In Patients With Active, Mild To
`Moderate Ulcerative Colitis (Transcript) (Jan. 15, 2013)
`Uceris® Instant Savings Program
`Transcript of the Second Quarter 2014 Earnings Conference Call of
`Salix Pharmaceuticals, Ltd.
`L.W. Doner, Determining Sugar Composition of Food Gum
`Polysaccharides by HPTLC, Chromatographia 2001, 53, May (No.
`9/10)
`Amendment filed on January 15, 2013 in U.S. Patent Appl. No.
`13/617,138
`Specification of U.S. Patent Application No. 10/009,532
`Specification of 12/210,969 application
`Specification of 13/249,839 application
`Specification of 13/462,409 application
`Final Office Action of March 6, 2013 in U.S. Patent Appl. No.
`13/617,138
`Applicant-Initiated Interview Summary of April 23, 2013 in U.S.
`Patent Appl. No. 13/617,138
`
`1053
`1054
`1055
`1056
`1057
`
`1058
`
`x
`
`
`

`

`1059
`
`1060
`1061
`
`1062
`
`Original Specification as filed on September 14, 2012 in U.S. Patent
`Appl. No. 13/617,138
`Orange Book Listing of Uceris® (accessed on March 8, 2017)
`Hawley’s Condensed Chemical Dictionary (John Wiley & Sons,
`Inc., 13th ed. 1997)
`N. Robinson, Surface Interaction of Lecithin and Lysolecithin, J. of
`Pharmacy and Pharmacology, 12(1) 609-616 (1960)
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`xi
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`
`

`

`
`
`I.
`
`Petition for Inter Partes Review
`of U.S. Patent No. 9,320,716
`
`INTRODUCTION
`Argentum Pharmaceuticals LLC (“Petitioner”) petitions for Inter Partes
`
`Review (“IPR”), and seeks cancellation of Claims 1-29 (“challenged claims”) of
`
`U.S. Patent No. 9,320,716 (“the ’716 patent”) (EX1001), which is assigned to
`
`Cosmo Technologies Limited (“Patent Owner”).
`
`II. OVERVIEW
`The ’716 patent generally claims a composition of a well-known drug—
`
`budesonide—for the treatment of inflammatory bowel disease, a disease that
`
`budesonide was known to treat. The other claim limitations provide only common
`
`classes of excipients used in formulations containing budesonide. Nothing new is
`
`claimed.
`
`III. STANDING (37 C.F.R. § 42.104(a); PROCEDURAL STATEMENTS)
`Petitioner certifies that: (1) the ’716 patent is available for IPR; and (2)
`
`Petitioner is not barred or estopped from requesting IPR of any claim of the ’716
`
`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). Authorization to charge the prescribed fees
`
`to Deposit Account No. 19-0741 is being provided concurrently through the
`
`Financial Manager function of the PTAB E2E filing system. In the event of any
`
`fee deficiency or omission, the Office is hereby authorized to charge fees under 37
`
`C.F.R. §42.15(a) and any other required fees to Deposit Account No. 19-0741.
`
`1
`
`

`

`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))
`Argentum Pharmaceuticals LLC; Intelligent Pharma Research LLC; APS
`
`GP LLC; and APS GP Investors LLC.
`
`B. Notice of Related Matters (37 C.F.R. § 42.8(b)(2))
`1.
`Judicial Matters
`The ’716 patent is currently the subject of the following litigations: Cosmo
`
`Technologies Limited et al. v. Mylan Pharmaceuticals Inc., 16-cv-00152 (D. Del.);
`
`Cosmo Technologies Ltd. et al. v. Lupin Ltd. et al., 15-cv-00669 (D. Del.); Cosmo
`
`Technologies Limited et al. v. Alvogen Pine Brook, Inc., 15-cv-00193 (D. Del.);
`
`Cosmo Technologies Ltd. et al. v. Actavis Laboratories FL, Inc., 15-cv-00164 (D.
`
`Del.); Cosmo Technologies Limited et al. v. Par Pharmaceutical, Inc., 15-cv-
`
`00116 (D. Del.).
`
`Administrative Matters
`
`2.
`At least the following related ’716 patent family members exist: U.S. Patent
`
`No. 7,410,651 (“the ’651 patent”); U.S. Patent No. 8,784,888 (“the ’888 patent”);
`
`U.S. Patent No. RE 43,799 (“the ’799 patent”) formally U.S. Patent No. 8,029,823
`
`(“the ’823 patent”); U.S. Patent No. 8,293,273 (“the ’273 patent”); U.S. Patent No.
`
`7,431,943 (“the ’943 patent”); U.S. Patent No. 9,532,954 (“the ’954 patent”); U.S.
`
`Patent No. 7,410,652 (“the ’652 patent”); U.S. App. No. 14/514,967; and U.S.
`
`App. No. 15/369,296.
`
`2
`
`

`

`In IPR2017-01035, the Board has already instituted trial for all claims of the
`
`’716 patent on each of the grounds raised herein. An inter partes review of the
`
`’888 patent (IPR2017-01034) was terminated prior to institution.
`
`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
`Michael Houston
`Reg. No. 58,486
`FOLEY & LARDNER LLP
`321 North Clark Street, Suite 2800
`Chicago, Illinois 60654
`312-832-4500
`mhouston@foley.com
`
`Back-Up Counsel
`Joseph P. Meara
`Reg. No. 44,932
`James McParland, Ph.D.
`Reg. 69,440
`FOLEY & LARDNER LLP
`150 East Gilman St.
`Madison, WI 53703-1482
`608-258-4303
`jmeara@foley.com
`
`
`Tyler C. Liu
`Reg. No. 72,126
`Argentum Pharmaceuticals LLC
`202-749-8605
`TLiu@agpharm.com
`
`
`
`V.
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`Petitioner consents to email service at the above addresses.
`
`STATEMENT OF THE PRECISE RELIEF REQUESTED AND THE
`REASONS THEREFORE (37 C.F.R. § 42.22(a))
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`Petitioner requests IPR and cancellation of Claims 1-29 of the ’716 patent.
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`Petitioner’s full statement of the reasons for the relief requested is set forth in
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`detail below.
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`3
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`

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`VI. THE ’716 PATENT
`The ’716 patent has three independent claims (Claims 1, 12 and 22). Claim 1
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`recites a controlled release oral pharmaceutical composition comprising: (i)
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`budesonide in an amount effective to treat intestinal inflammatory disease; (ii) a
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`macroscopically homogenous structure comprising: (a) at least one lipophilic
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`compound and (b) at least one hydrophilic compound, wherein the macroscopically
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`homogenous structure controls the release of the budesonide; and (iii) a gastro-
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`resistant coating on the macroscopically homogenous structure that prevents
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`release of budesonide in the stomach, wherein the macroscopically homogenous
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`structure is a tablet. EX1001, 10:12–26; EX1006, ¶39. Claims 12 and 22 are
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`similar to Claim 1 except that Claim 12 requires “at least one amphiphilic
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`compound” rather than the “at least one lipophilic compound” of Claim 1, whereas
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`Claim 21 requires “at least one amphiphilic compound” and “at least one lipophilic
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`compound.” EX1001, 11:4- 15; 12:9-25; EX1006, ¶39.
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`Generally, the claims are directed to compositions with compounds having a
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`recited property (e.g., “lipophilic compounds,” “hydrophilic compounds” or
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`“amphiphilic compounds”) rather than specific compounds. Id. at ¶41. The claims
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`may alternatively recite a class of compounds (e.g., “methacrylic acid polymers,”
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`“cellulose derivatives,” “hydroxyalkyl cellulose” or Markush groups of
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`compounds). Id. Only in some instances do the claims recite a specific compound
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`4
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`(e.g., dependent Claim 10 reciting stearic acid) but even then, the specific
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`compound is coupled with any “hydrophilic compound” or anything that may
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`function as a “gastro-resistant coating.” Id. Petitioner offers these observations to
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`show the broad scope of the claims.
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`A. Claim Construction
`The District of Delaware provided the following constructions with respect
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`to the ’716 patent and other related patents:
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`
`
`Term
`“matrix”
`“macroscopically
`homogeneous
`composition” or
`“macroscopically
`homogeneous
`structure”
`“outer hydrophilic
`matrix”
`
`“lipophilic matrix”
`
`Construction
`A homogeneous structure in all its volume
`A composition of uniform structure throughout, as
`observed by the naked eye
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`A matrix with an affinity for water within which other
`matrices are incorporated
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`A matrix having an affinity for lipids and a poor affinity
`towards aqueous fluids
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`“amphiphilic matrix” A matrix containing amphiphilic substances, and as a
`result having both an affinity for lipids and an affinity for
`water
`The temperature at which solid and liquid phases of a
`compound are at equilibrium
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`“melting point”
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`EX1012 (Order), 2. Petitioner notes that some of the claims of the ’716 patent may
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`not recite these same terms. Nevertheless, the Markman Opinion provides meaning
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`5
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`to terms such as “hydrophilic,” “lipophilic,” and “amphiphilic”—terms which
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`appear in the claims of the ’716 patent, and which Petitioner asserts are consistent
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`with their broadest reasonable interpretation (“BRI”). 37 C.F.R. § 42.100(b);
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`EX1006, ¶¶45-46. To the extent the same terms are contained in the ’716 patent
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`(e.g., “macroscopically homogeneous structure”), Petitioner asserts that, at the very
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`least, the BRI should encompass the district court’s constructions. 37 C.F.R. §
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`42.100(b); EX1006, ¶46.
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`All remaining claim terms should be given their BRI, i.e., their ordinary and
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`customary meaning as would have been understood by a POSA at the time, in the
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`context of the entire patent disclosure. Id.; Cuozzo Speed Techs., LLC v. Lee, 136
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`S. Ct. 2131, 2144-46 (2016); In re Translogic Tech., Inc., 504 F.3d 1249, 1257
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`(Fed. Cir. 2007).
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`VII. A PERSON OF ORDINARY SKILL IN THE ART
`The ’716 patent claims priority under 35 U.S.C. § 119 to two Italian patent
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`applications, MI2000A000422 and MI99A001317, filed March 3, 2000 and June
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`14, 1999, respectively. The ’716 patent claims priority under 35 U.S.C. § 120 to
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`U.S. Application No. 10/009,532 filed as International Application No.
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`PCT/EP00/05356 on June 9, 2000. The relevant potential priority date of the ’716
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`6
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`patent is June 9, 2000.1 Even under the June 14, 1999 date, the claims of the ’716
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`patent are invalid based on the cited prior art. EX1006, ¶48.
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`As of June 9, 2000, a POSA in the relevant field would have had education
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`or experience in the field of drug delivery systems, including controlled release
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`compositions. Id. at ¶34. The education and experience levels may vary between
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`POSAs, with some having a bachelor’s degree in the chemical or pharmaceutical
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`arts (e.g., pharmacy or pharmaceutics) plus five years of relevant work experience,
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`and others holding more advanced degrees—e.g., Ph.D. or Pharm.D.—while
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`having fewer years of experience. Id. at ¶35.
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`VIII. IDENTIFICATION OF CHALLENGE (37 C.F.R. § 42.104(b))
`Petitioner respectfully requests IPR of Claims 1-29 of the ’716 patent on
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`each specific ground of unpatentability outlined below. Per 37 C.F.R. § 42.6(d),
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`copies of the references are filed herewith. In support of the proposed grounds, this
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`Petition includes the declaration of Dr. Hartmut Derendorf (EX1006), explaining
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`what the art would have conveyed to a POSA as of the priority date of the ’716
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`patent.
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`
`
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`1 See M.P.E.P. § 2133 (“The 1-year time bar is measured from the U.S. filing date.
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`. . . A rejection under pre-AIA 35 U.S.C. § 102(b) cannot be overcome by . . .
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`foreign priority dates . . . .”); see also 35 U.S.C. § 119(a).
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`7
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`mmChallen ; ed
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`3
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`’388 patent
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`1-7, 9, 11-17, 19,
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`35 U.S.C.§102
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`35 U.S.C.§103
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`8, 10, 18 and 20
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`’388 patent
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`35 use § 103
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`’388 .atent and ’584 .atent
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`35 U.S.C. § 103
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`Prior art references in addition to the primary references listed above provide
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`further background in the art, motivation to combine the teachings of these
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`references, and/or support for why a POSA would have had a reasonable
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`expectation of success to arrive at the purported invention recited in the challenged
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`claims.
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`Moreover, the fact that a reference was disclosed to the Examiner is not a
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`bar to institution of an IPR. For example, the Board instituted IPR in Sharp Corp.
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`v. Surpass Tech Innovation LLC, IPR2015-00021, Paper 10 (P.T.A.B. Mar. 18,
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`2015) even though the petitioner relied on previously considered references,
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`because the petitioner presented different arguments that “shed[] a different light
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`on the [repeated] reference.” Id. at 14; Chi Mei Innolux Corp. v. Semiconductor
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`Energy Lab. Co., Ltd, IPR2013-00028, Paper 14 at 10 (P.T.A.B. Mar. 21, 2014)
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`(instituting IPR where the petitioner submitted an expert declaration even though
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`the same arguments and prior art were allegedly considered).
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`

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`IX.
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`INVALIDITY ANALYSIS
`A. Ground 1: U.S. Patent No. 5,681,584 Anticipates Claims 1-29
`Anticipation under 35 U.S.C. § 102 requires that each and every element of
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`the claimed invention be disclosed expressly or inherently in a single prior art
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`reference. In re Paulson, 30 F.3d 1475, 1478-79 (Fed. Cir. 1994). “[A] reference
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`can anticipate a claim even if it ‘[d]oes not expressly spell out’ all the limitations
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`arranged or combined as in the claim.” Kennametal Inc. v. Ingersoll Cutting Tool
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`Co., 780 F.3d 1376, 1381 (Fed. Cir. 2015).
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`U.S. Patent No. 5,681,584 (“the ’584 patent”) (EX1008) anticipates Claims
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`1- 29 of the ’716 patent. The ’584 patent, entitled “Controlled Release Drug
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`Delivery Device,” issued on October 28, 1997. Accordingly, the ’584 patent is prior
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`art under 35 U.S.C. § 102(b). Although the ’584 patent was disclosed to the PTO
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`(with 112 other references) during prosecution of the application that led to the
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`’716 patent, it was not addressed during its prosecution. While the ’584 patent was
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`cited by the Examiner during prosecution of a (prior) related family member (i.e.,
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`the ’888 patent), this does not bar institution of this IPR under 35 U.S.C. § 325(d).
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`Amneal Pharms. LLC v. Purdue Pharma L.P., IPR2016-01412, Paper 9 at 19
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`(P.T.A.B. Feb. 14, 2017); Amneal Pharms. LLC v. Purdue Pharma L.P., IPR2016-
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`01413, Paper 9 at 23 (P.T.A.B. Jan. 18, 2017).
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`9
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`Disclosure of the ’584 Patent
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`1.
`The ’584 patent discloses coated time-controlled tablets that release an
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`active agent intermittently or at a pre-selected region of the gastro-intestinal tract.
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`EX1008