Paper No. ___
`Filed: December 14, 2016
`
`UNITED STATES PATENT AND TRADEMARK OFFICE
`____________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`____________
`
`GRÜNENTHAL GMBH,
`
`Petitioner
`
`v.
`
`ANTECIP BIOVENTURES II LLC,
`
`Patent Owner.
`____________
`
`U.S. Patent No. 9,283,239
`____________
`
`PETITION FOR POST GRANT REVIEW
`
`

`

`TABLE OF CONTENTS
`
`I.
`
`INTRODUCTION ...........................................................................................1
`
`II. MANDATORY NOTICES UNDER 37 C.F.R. § 42.8...................................3
`
`A.
`
`B.
`
`C.
`
`D.
`
`Real Party-in-Interest (§ 42.8(b)(1)) .....................................................3
`
`Related Matters (§ 42.8(b)(2)) ..............................................................3
`
`Lead and Backup Counsel (§ 42.8(b)(3))..............................................3
`
`Service Information (§ 42.8(b)(4))........................................................4
`
`PAYMENT OF FEES .....................................................................................4
`
`TIME FOR FILING PETITION......................................................................4
`
`GROUNDS FOR STANDING........................................................................4
`
`IDENTIFICATION OF CHALLENGED CLAIMS AND
`RELIEF SOUGHT...........................................................................................5
`
`III.
`
`IV.
`
`V.
`
`VI.
`
`VII. THE ’239 PATENT PROSECUTION HISTORY..........................................5
`
`VIII. CLAIM CONSTRUCTION ............................................................................8
`
`IX.
`
`X.
`
`PERSON OF ORDINARY SKILL IN THE ART ..........................................9
`
`THE ’239 PATENT IS ELIGIBLE FOR PGR................................................9
`
`A.
`
`The Pre-AIA Applications Fail to Describe or Enable the
`Dosing Regimens Limitation of Claim 1. ...........................................11
`
`1.
`
`2.
`
`The Pre-AIA Applications Fail to Provide Proper
`Written Description of the Dosing Regimens
`Limitation..................................................................................12
`
`The Pre-AIA Applications Fail to Properly Enable
`the Dosing Regimens Limitation. .............................................15
`
`B.
`
`The Pre-AIA Applications Fail to Describe or Enable the
`Duration of Pain Limitation of Claim 2. .............................................18
`i
`
`

`

`C.
`
`The Pre-AIA Applications Fail to Describe or Enable the
`Percentage of Zoledronic Acid Present in Dosage Form
`Limitation of Claim 17........................................................................19
`
`XI. HOW THE CHALLENGED CLAIMS ARE
`UNPATENTABLE........................................................................................19
`
`A.
`
`Ground 1: Lack of Written Description for Claims 1-17
`Under 35 U.S.C. § 112 ........................................................................19
`
`1.
`
`2.
`
`Claims 1-17: “about 80 to about 500 mg
`zoledronic acid within a period of six months”........................19
`
`Claim 17: “a dosage form containing at least 10%
`zoledronic acid” ........................................................................25
`
`B.
`
`Ground 2: Lack of Enablement of Claims 1-17 Under
`35 U.S.C. § 112 ...................................................................................26
`
`1.
`
`2.
`
`Claim 1-17: “A method of treating complex
`regional pain syndrome” “to a human being in
`need thereof”.............................................................................26
`
`Claim 2: “wherein the human being experiences
`pain relief that lasts for a duration of at least 48
`hours”........................................................................................28
`
`C.
`
`Ground 3: Claims 1, 2, 4, and 9-17 Are Anticipated by
`or Obvious over Fox............................................................................30
`
`1.
`
`Claim 1......................................................................................32
`
`a.
`
`“A method of treating complex regional pain
`syndrome”.......................................................................32
`
`i.
`
`ii.
`
`CRPS Is Characterized by Pain,
`Allodynia, and Hyperalgesia................................32
`
`CRPS Has Inflammatory and
`Neuropathic Pain Components.............................33
`
`iii.
`
`Claim Construction ..............................................35
`
`ii
`
`

`

`iv.
`
`Fox Describes a Method for Treating
`CRPS ....................................................................36
`
`“comprising orally administering” .................................40
`
`“zoledronic acid” ............................................................40
`
`“to a human being in need thereof”................................41
`
`wherein the human being receives about 80
`mg to about 500 mg of zoledronic acid
`within a period of six months .........................................42
`
`b.
`
`c.
`
`d.
`
`e.
`
`2.
`
`3.
`
`4.
`
`5.
`
`6.
`
`7.
`
`Claim 2......................................................................................45
`
`Claims 4, 9, 10, 12-14...............................................................46
`
`Claims 11 and 15.......................................................................48
`
`Claim 16....................................................................................49
`
`Claim 17....................................................................................49
`
`Alternatively, Claims 1, 2, 4, and 9-17 Are
`Obvious Over Fox.....................................................................50
`
`D.
`
`Ground 4: Claims 1-17 Are Obvious over Fox in view of
`Manicourt, de Castro, and Zaspel........................................................51
`
`1.
`
`2.
`
`3.
`
`4.
`
`Claim 1......................................................................................51
`
`Claims 3 and 5-8 .......................................................................60
`
`Claims 9-16...............................................................................61
`
`Claim 17....................................................................................62
`
`E.
`
`F.
`
`Ground 5: Claims 1-17 Are Obvious over Fox in view of
`Manicourt, de Castro, and Zaspel, in further view of
`McHugh...............................................................................................62
`
`No Secondary Considerations of Nonobviousness support
`patentability.........................................................................................64
`
`iii
`
`

`

`XII. GROUNDS ARE NOT REDUNDANT........................................................65
`
`XIII. CONCLUSION..............................................................................................65
`
`iv
`
`

`

`TABLE OF AUTHORITIES
`
`Cases
`AK Steel Corp. v. Sollac,
`344 F.3d 1234 (Fed. Cir. 2003) .....................................................................10
`
`Ariad Pharms., Inc. v. Eli Lilly & Co.,
`598 F.3d, 1336 (Fed. Cir. 2010) ................................................................9, 13
`
`Catalina Mktg. Intl. v. Coolsavings.com, Inc.,
`289 F.3d 801 (Fed. Cir. 2002) .......................................................................35
`
`ClearValue, Inc. v. Pearl River Polymers, Inc.,
`668 F.3d 1340 (Fed. Cir. 2012) .....................................................................43
`
`Genentech, Inc. v. Novo Nordisk, A/S,
`108 F.3d 1361 (Fed. Cir. 1997) .....................................................................10
`
`In re Petering,
`301 F.2d 676 (CCPA 1962))................................................................... 47, 50
`
`In re Wands,
`858 F.2d (Fed. Cir. 1988) ....................................................................... 10, 26
`
`In re Wertheim,
`541 F.2d 257 (C.C.P.A. 1976).......................................................................25
`
`In re Wright,
`999 F.2d 1557 (Fed. Cir. 1993) .............................................................. 27, 29
`
`Ineos USA LLC v. Berry Plastics Corp.,
`783 F.3d 865 (Fed. Cir. 2015) ................................................................ 43, 48
`
`Jansen v. Rexall Sundown, Inc.,
`342 F.3d 1329 (Fed. Cir. 2003) .....................................................................36
`
`Martin v. Mayer, 823 F.2d 500 (Fed. Cir. 1987).....................................................22
`
`Nat’l Recovery Techs., Inc. v. Magnetic Separation Sys., Inc.,
`166 F.3d 1190 (Fed. Cir. 1999) .....................................................................10
`v
`
`

`

`Purdue Pharma L.P. v. Faulding Inc.,
`230 F.3d 1320 (Fed. Cir. 2000) .............................................................. 14, 22
`
`Titanium Metals Corp. v. Banner,
`778 F.2d 775 (Fed. Cir. 1985) ................................................................ 47, 50
`
`Vas-Cath, Inc. v. Mahurkar,
`935 F.2d 1555 (Fed. Cir. 1991) .....................................................................20
`
`Verdegaal Bros. v. Union Oil Co. of California,
`814 F.2d 628 (Fed. Cir. 1987) .......................................................................31
`
`Statutes
`
`35 U.S.C. § 102..........................................................................................................5
`
`35 U.S.C. § 102(a) .....................................................................................................5
`
`35 U.S.C. § 103......................................................................................................5, 7
`
`35 U.S.C. § 112............................................................................................... 5, 9, 10
`
`35 U.S.C. § 321(c) .....................................................................................................4
`
`35 C.F.R. § 42.100(b) ................................................................................................8
`
`35 C.F.R. § 42.202 .....................................................................................................4
`
`35 C.F.R. § 42.204 .....................................................................................................4
`
`37 C.F.R. § 42.15(a)...................................................................................................4
`
`37 C.F.R. § 42.203(a).................................................................................................4
`
`37 C.F.R. § 42.8 .........................................................................................................3
`
`37 C.F.R. § 42.8(b)(1)................................................................................................3
`
`37 C.F.R. § 42.8(b)(2)................................................................................................3
`
`37 C.F.R. § 42.8(b)(3)................................................................................................3
`
`37 C.F.R. § 42.8(b)(4)................................................................................................4
`
`vi
`
`

`

`P.T.A.B.
`Inguran, LLC v. Premium Genetics (UK) Ltd.,
`Case PGR2015-00017, Paper 8 (P.T.A.B. Dec. 22, 2015)..............................9
`
`vii
`
`

`

`Exh. No.
`1001
`1002
`1003
`1004
`1005
`
`1006
`
`1007
`
`1008
`
`1009
`1010
`1011
`1012
`1013
`1014
`1015
`1016
`1017
`1018
`1019
`
`EXHIBIT LIST
`
`Description
`Declaration of Dr. Stephen Bruehl, Ph.D.
`Curriculum vitae of Dr. Stephen Bruehl, Ph.D.
`U.S. Patent No. 9,283,239 (“the ’239 patent”)
`U.S. Patent Pub. No. 2004/0063670 (“the Fox application”)
`D.H. Manicourt, et al., “Role of Alendronate Therapy for
`Posttraumatic Complex Regional Pain Syndrome Type I of the Lower
`Extremity,” 50(11) Arthritis & Rheumatism 3690 (Nov. 2004)
`(“Manicourt”)
`A.P.C. de Castro, et al., “Zoledronic acid to treat complex regional
`pain syndrome type I in adult: case report,” 12(1) Rev. Dor. Sao
`Paulo 71 (Mar. 2011) (“de Castro”)
`J. Zaspel, et al., “Treatment of early stage CRPS I – cortisone
`(methylprednisolone) versus bisphosphonate (zoledronic acid),”
`German Congress for Orthopedics and Trauma Surgery. 71st Annual
`Meeting of the German Society of Trauma Surgery, 93rd Meeting of
`the German Society of Orthopedics and Orthopedic Surgery, 48th
`Meeting of the Professional Association of Specialists in Orthopedics.
`Berlin, October 24-27, 2007. Düsseldorf: German Medical Science
`GMS Publishing House; 2007. DocP23-1583 (October 9, 2007)
`(“Zaspel”)
`Catherine McHugh, Thomas Leonard, et al., “MER-101 tablets: A
`pilot bioavailability study of a novel oral formulation of zoledronic
`acid,” Molecular Cancer Therapeutics, Volume 6, Issue 11
`Supplement pp. B194 (November 2007) (“McHugh”)
`U.S. App. No. 14/635,857 (“the ’857 Application”) File History
`U.S. Provisional App. No. 61/646,538 (“the ’538 provisional”)
`U.S. Provisional App. No. 61/647,478 (“the ’478 provisional”)
`U.S. Provisional App. No. 61/654,292 (“the ’292 provisional”)
`U.S. Provisional App. No. 61/654,383 (“the ’383 provisional”)
`U.S. Provisional App. No. 61/655,541 (“the ’541 provisional”)
`U.S. Provisional App. No. 61/655,527 (“the ’527 provisional”)
`U.S. Provisional App. No. 61/762,225 (“the ’225 provisional”)
`U.S. Provisional App. No. 61/764,563 (“the ’563 provisional”)
`U.S. Provisional App. No. 61/767,647 (“the ’647 provisional”)
`U.S. Provisional App. No. 61/767,676 (“the ’676 provisional”)
`viii
`
`

`

`1020
`1021
`
`1022
`1023
`1024
`1025
`1026
`1027
`1028
`1029
`1030
`1031
`
`1032
`
`1033
`1034
`1035
`1036
`
`1037
`
`1038
`
`1039
`
`1040
`1041
`
`1042
`
`U.S. Provisional App. No. 61/803,721 (“the ’721 provisional”)
`U.S. App. No. 13/894,274 (abandoned after Final Rejection in favor
`of Continuing App. No. 15/014,994) (“the ’274 application”) File
`History, Pages 1-300
`U.S. App. No. 13/894,274 File History, Pages 301-600
`U.S. App. No. 13/894,274 File History, Pages 601-800
`U.S. App. No. 13/894,274 File History, Pages 801-1000
`U.S. App. No. 13/894,274 File History, Pages 1001-1300
`U.S. App. No. 13/894,274 File History, Pages 1301-1600
`U.S. App. No. 13/894,274 File History, Pages 1601-1900
`U.S. App. No. 13/894,274 File History, Pages 1901-2200
`U.S. App. No. 13/894,274 File History, Pages 2201-2450
`U.S. App. No. 13/894,274 File History, Pages 2451-2724
`U.S. App. No. 14/063,979, issued as Pat. No. 8,802,658
`(Continuation-in-Part) (“the ’979 application”)
`U.S. App. No. 14/279,232, issued as Pat. No. 9,149,487
`(Continuation) (“the ’232 application”)
`U.S. Patent No. 9,216,168
`U.S. Patent No. 9,408,862
`U.S. Patent No. 7,704,977
`G.D. Schott, “Bisphosphonates for pain relief in reflex sympathetic
`dystrophy?” 350 The Lancet: Commentary (October 18, 1997).
`(“Schott”)
`S. Adami, et al., “Bisphosphonate therapy of reflex sympathetic
`dystrophy syndrome,” 56(201-204) Annals of the Rheumatic Diseases
`(1997). (“Adami”)
`J.F. Maillefert, et al.,“Treatment of refractory
`reflex sympathetic dystrophy with pamidronate,” 54(687) Ann.
`Rheum. Dis.(1995). (“Maillefert”)
`K. Siminoski, et al.,“Intravenous pamidronate
`for treatment of reflex sympathetic dystrophy during breast feeding,”
`15(10) Journal of Bone and Mineral Research (2000). (“Siminoski”)
`[Reserved]
`B. Cortet, et al., “Treatment of severe, recalcitrant reflex sympathetic
`dystrophy: assessment of efficacy and safety of the second generation
`bisphosphonate pamidronate,” 16(1) Clinical rheumatology (1997).
`(“Cortet”)
`J.N. Robinson, et al., “Efficacy of pamidronate in
`
`ix
`
`

`

`1043
`
`1044
`
`1045
`
`1046
`
`1047
`
`1048
`
`1049
`
`1050
`
`complex regional pain syndrome type I,” 5(3) Pain Medicine (2004).
`(“Robinson”)
`Kubalek, et al., “Treatment of reflex sympathetic dystrophy with
`pamidronate: 29 cases,” 40 Rheumatology 1394-1397 (2001).
`(“Kubalek”)
`H. Merskey and N. Bogduk, Classification of Chronic Pain:
`Descriptions of Chronic Pain Syndromes and Definitions of Pain
`Terms, 2nd ed. IASP Press (1994). (“Merskey and Bogduk”)
`S. Bruehl, “An Update on the Pathophysiology of Complex Regional
`Pain Syndrome,” 113 Anesthesiology 713-725 (2010).
`S. Bruehl, et al., “External validation of IASP diagnostic criteria for
`Complex Regional Pain Syndrome and proposed research diagnostic
`criteria 81 Pain 147-154 (1999).
`R.N. Harden, et al., “Validation of proposed diagnostic criteria (the
`‘‘Budapest Criteria”) for Complex Regional Pain Syndrome,” 150
`Pain 268-274 (2010).
`G.J. Bennett and Y.K. Xie, “A peripheral mononeuropathy in rat that
`produces disorders of pain sensation like those seen in man,” 33 Pain
`87-107 (1988).
`M. Daeman, et al., “Neurogenic Inflammation and Reflex
`Sympathetic Dystrophy,” 64(4) Acta Orthopaedica Belgica (1998).
`Z. Seltzer, R. Dubner, and Y. Shir, “A novel behavioral model of
`neuropathic pain disorders produced in rats by partial sciatic nerve
`injury,” 43 Pain 205-218 (1990).
`
`x
`
`

`

`I.
`
`INTRODUCTION
`
`Complex regional pain syndrome (“CRPS”) is a condition characterized by
`
`severe, continuing pain, usually following an injury or other triggering event,
`
`where the pain is disproportionate in intensity or duration to the pain that would
`
`normally be expected from the triggering event. Exh. 1001, ¶ 39-40. U.S. Patent
`
`No. 9,283,239 (Exh. 1003) claims methods of treating CRPS by orally
`
`administering about 80 mg to about 500 mg zoledronic acid to a human being
`
`within a period of six months. Exh. 1003, claims 1-17. However, those claimed
`
`inventions were not novel because methods for treating CRPS by oral
`
`administration of zoledronic acid were already well-known in the prior art at the
`
`time of the alleged invention of the ’239 patent.
`
`The earliest possible filing date for any claim of the ’239 patent is May 14,
`
`2012.1 But much earlier than May 2012, since at least the 1990s, bisphosphonates,
`
`including zoledronic acid, had been in widespread commercial use as treatments
`
`for osteoporosis and other diseases involving problems with bone resorption. Exh.
`
`1001, ¶ 54-55. CRPS had been known to involve enhanced bone resorption, and
`
`1 As discussed in Section X and subsections A and B of Section XI below, none of
`
`the claims of the ’239 patent is entitled to this filing date. Regardless, the cited
`
`prior art pre-dates even this May 2012 filing date.
`
`

`

`therefore various researchers had investigated the use of bisphosphonates for
`
`treatment of CRPS. By 2012, a large and growing body of literature and clinical
`
`studies demonstrated that bisphosphonates, including zoledronic acid, were
`
`effective in treating CRPS. Exh. 1001, ¶ 153.
`
`Indeed, during the prosecution of the application underlying the ’239 patent,
`
`the Examiner maintained that the use of zoledronic acid to treat CRPS was taught
`
`by the prior art, and only allowed the ’239 patent claims on the basis that it would
`
`not have been obvious to use an amount of zoledronic acid from about 80 to about
`
`500 mg over a period of 6 months. See Exh. 1009, at 00426. Yet at least eight
`
`years before the Patent Owner applied for the ’239 patent, U.S. Patent Application
`
`Publication No. 2004/0063670 (Exh. 1004) disclosed the use of orally
`
`administered zoledronic acid, including about 80 mg to about 500 mg over six
`
`months, to treat the exact type of pain that constitutes CRPS: inflammatory and
`
`neuropathic pain, allodynia, and hyperalgesia. Exh. 1004, ¶¶ 75-77; Exh. 1001, ¶¶
`
`120-126.
`
`As shown in this Petition, and supported by the expert declaration of Dr.
`
`Stephen Bruehl (Exh. 1001), all of the claims of the ’239 Patent are anticipated by
`
`Fox or, at a minimum, are obvious over Fox in combination with other prior art
`
`showing the efficacy of zoledronic acid in treating CRPS. The claims are also
`
`invalid for insufficient written description and lack of enablement. Accordingly,
`
`2
`
`

`

`Petitioner Grünenthal GmbH (“Petitioner”) requests post-grant review (“PGR”) of
`
`claims 1-17 of the ’239 patent.
`
`II. MANDATORY NOTICES UNDER 37 C.F.R. § 42.8
`
`A.
`
`Real Party-in-Interest (§ 42.8(b)(1))
`
`The real parties-in-interest are Petitioner Grünenthal GmbH and Thar
`
`Pharmaceuticals Inc. Petitioner Grünenthal GmbH owns 100% of Thar
`
`Pharmaceuticals Inc.
`
`B.
`
`Related Matters (§ 42.8(b)(2))
`
`As of the filing date of this Petition and to Petitioner’s best knowledge, the
`
`’239 Patent is not involved in any judicial or administrative matters that would
`
`affect, or be affected by, a decision in this proceeding.
`
`C.
`
`Lead and Backup Counsel (§ 42.8(b)(3))
`
`Lead Counsel
`Bruce C. Haas
`Registration No. 32,734
`FITZPATRICK, CELLA, HARPER &
`SCINTO
`1290 Avenue of the Americas
`New York, NY 10104
`Tel: 212-218-2290
`Fax: 212-218-2200
`bhaas@fchs.com
`
`Back-up Counsel
`Justin J. Oliver
`Registration No. 44,986
`FITZPATRICK, CELLA, HARPER &
`SCINTO
`975 F Street, NW
`Washington, D.C. 20004
`Tel: 202-530-1010
`Fax: 202-530-1055
`joliver@fchs.com
`
`3
`
`

`

`D.
`
`Service Information (§ 42.8(b)(4))
`
`Please direct all correspondence to lead and back-up counsel at the above
`
`addresses. Petitioner consents to electronic service to GrunenthalPGR@fchs.com
`
`and at the e-mail addresses above.
`
`III. PAYMENT OF FEES
`
`Pursuant to 37 C.F.R. §§ 42.203(a) and 42.15(a), the required fees are
`
`submitted herewith. If additional fees are due during this proceeding, the Office is
`
`authorized to charge Deposit Account No. 50-3939.
`
`IV. TIME FOR FILING PETITION
`
`The ’239 patent issued on March 15, 2016 and the instant Petition was
`
`timely filed on or before the date that is nine months after the date of the grant of
`
`the patent. 35 U.S.C. § 321(c); 37 C.F.R. § 42.202.
`
`V.
`
`GROUNDS FOR STANDING
`
`Pursuant to 37 C.F.R. § 42.204(a), Petitioner certifies that the ’239 patent is
`
`available for PGR, and that Petitioner is not barred or estopped from requesting
`
`PGR of the ’239 patent challenging the patent claims on the grounds identified in
`
`this Petition.
`
`The ’239 patent is available for PGR pursuant to the America Invents Act
`
`(“AIA”), Pub. L. No. 112-29, § 3(n)(1), 125 Stat. 284, 293 (2011), because, as
`
`4
`
`

`

`explained below in Sections X and XI, at least one claim has an effective filing
`
`date on or after March 16, 2013.
`
`VI.
`
`IDENTIFICATION OF CHALLENGED CLAIMS AND RELIEF
`SOUGHT
`
`Petitioner respectfully requests post grant review of claims 1-17 of the ’239
`
`patent and cancellation of claims 1-17 as unpatentable under 35 U.S.C. §§ 102,
`
`103, and/or 112. It is more likely than not that claims 1-17 are unpatentable in
`
`view of the following prior art references and unpatentability grounds:
`
`Ground Claims
`1
`1-17
`
`2
`
`3
`
`4
`
`5
`
`Statutory Basis
`35 U.S.C. §112
`(written
`description)
`35 U.S.C. §112
`(enablement)
`35 U.S.C. §
`102(a) or 35
`U.S.C. § 103
`35 U.S.C. § 103
`
`1-17
`
`1, 2, 4, 9-17
`
`1-17
`
`1-17
`
`35 U.S.C. § 103
`
`Prior Art References
`
`Fox (Exh. 1004)
`
`Fox (Exh. 1004)
`Manicourt (Exh. 1005)
`De Castro (Exh. 1006)
`Zaspel (Exh. 1007)
`Fox (Exh. 1004)
`Manicourt (Exh. 1005)
`De Castro (Exh. 1006)
`Zaspel (Exh. 1007)
`McHugh (Exh. 1008)
`
`VII. THE ’239 PATENT PROSECUTION HISTORY
`
`The ’239 patent, entitled “Compositions for Oral Administration of
`
`Zoledronic Acid or Related Compounds for Treating Complex Regional Pain
`5
`
`

`

`Syndrome,” issued on March 15, 2016 from U.S. Application No. 14/635,857 (“the
`
`’857 application”) (Exh. 1009) filed on March 2, 2015. The ’857 application
`
`claims priority to a chain of three U.S. non-provisional patent applications and 11
`
`provisional applications, identified in the following table (the “Related
`
`Applications”):
`
`Patent Application/Patent No.
`Provisional App. No. 61/646,538
`Provisional App. No. 61/647,478
`Provisional App. No. 61/654,292
`Provisional App. No. 61/654,383
`Provisional App. No. 61/655,541
`Provisional App. No. 61/655,527
`Provisional App. No. 61/762,225
`Provisional App. No. 61/764,563
`Provisional App. No. 61/767,647
`Provisional App. No. 61/767,676
`Provisional App. No. 61/803,721
`App. No. 13/894,274 (abandoned after Final
`Rejection in favor of Continuing App. No.
`15/014,994)
`App. No. 14/063,979, issued as Pat. No.
`8,802,658 (Continuation-in-Part)
`App. No. 14/279,232, issued as Pat. No.
`9,149,487 (Continuation)
`
`Filing Date
`May 14, 2012
`May 15, 2012
`June 1, 2012
`June 1, 2012
`June 5, 2012
`June 5, 2012
`Feb. 7, 2013
`Feb. 14, 2013
`Feb. 21, 2013
`Feb. 21, 2013
`Mar. 20, 2013
`
`Exhibit
`1010
`1011
`1012
`1013
`1014
`1015
`1016
`1017
`1018
`1019
`1020
`
`May 14, 2013
`
`1021
`
`Oct. 25, 2013
`
`May 15, 2014
`
`1022
`
`1023
`
`The only independent claim of the ’857 application as originally filed did
`
`not include a dosing regimen limitation. Exh. 1009, at 00066. Certain claims as
`
`originally filed did include limitations related to dosing regimens. Id. at 00066-67,
`
`claims 3, 4, 6, 11-13, 15-18. During prosecution, Patent Owner submitted twelve
`
`6
`
`

`

`Information Disclosure Statements identifying over 320 references for
`
`consideration.
`
`On July 28, 2015, the Examiner issued a non-final rejection of all claims of
`
`the ’857 application under 35 U.S.C. § 103 over several prior art references
`
`including “Zoledronic acid to treat complex regional pain syndrome type I in adult.
`
`Case report” (“De Castro”). Exh. 1009, at 00276-81. The Examiner found “[i]t
`
`would have been obvious to one of ordinary skill in the art at the time of the instant
`
`invention to treat CRPS in a human by orally administering zoledronic acid.” Id.
`
`at 00279. With respect to the dependent claims that included limitations related to
`
`dosing regimens, the Examiner found “[o]ne of ordinary skill in the art would have
`
`been motivated to administer the zoledronic acid in [the claimed amounts and at
`
`the claimed frequencies] because the prior art shows that CRPS can be successfully
`
`treated via the administration of bisphosphonates in a variety of schedules and
`
`amounts” and “it is not inventive to discover the optimum or workable ranges by
`
`routine experimentation.” Id. at 00280. All claims were also provisionally
`
`rejected on the ground of nonstatutory double patenting as being unpatentable over
`
`claims of several copending applications. Id. at 00282-89.
`
`In an attempt to overcome the Examiner’s rejections, Patent Owner amended
`
`the claims to for the first time include the following dosing regimen limitation:
`
`“wherein the human being receives about 80 to about 600 mg of zoledronic acid
`
`7
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`

`

`within a period of two months” (Exh. 1009, at 00363) and filed a terminal
`
`disclaimer. Id. at 00403. Ultimately, however, in order to overcome the prior art
`
`the Examiner required the claims to be amended to recite: “wherein the human
`
`being receives about 80 to about 500 mg of zoledronic acid within a period of six
`
`months.” Id. at 00426. The examiner reasoned that given the low oral
`
`bioavailability of bisphosphonates, “[o]ne of skill in the art would not have found
`
`it obvious to administer an oral dose that was significantly less than the estimated
`
`dose, and still effectively control CRPS for a full six months.” Id. at 00427.
`
`VIII. CLAIM CONSTRUCTION
`
`The following claim terms of the ’239 patent require construction and should
`
`be given the proposed constructions set forth below. The reasons why the Board
`
`should adopt these proposed claim constructions are given in detail below in
`
`Petitioner’s arguments. Unless a specific construction is proposed below, the
`
`terms in the ’239 patent claims should be given their broadest reasonable
`
`interpretation in light of the specification. 37 C.F.R. § 42.100(b).
`
`Claim Term
`“A method of treating
`complex regional pain
`syndrome”
`
`“to a human being in need
`thereof”
`“experiences pain relief
`
`Claim(s) Proposed Construction
`1
`A limiting preamble requiring that the
`claimed method be performed “for the
`purpose of diagnosing, curing, mitigating,
`or preventing pain in a patient having
`CRPS.” See Exh. 1003, col. 3, ll. 28-32.
`“to a human being with CRPS in need of
`treatment of pain”
`Non-limiting statement of an intended
`
`1
`
`2
`
`8
`
`

`

`that lasts for a duration of
`at least 48 hours”
`
`result of the claimed method
`
`IX. PERSON OF ORDINARY SKILL IN THE ART
`
`The ’239 patent is directed to the use of claims methods of treating CRPs by
`
`administering zoledronic acid. For this patent, a POSA would have an M.D. or a
`
`Ph.D. in a pain medicine relevant discipline, such as clinical health psychology or
`
`neuroscience, and 3 to 5 years of experience in the treatment or study of chronic
`
`pain management. Exh. 1001, ¶¶ 36-37.
`
`X.
`
`THE ’239 PATENT IS ELIGIBLE FOR PGR
`
`A patent that issues from an application filed after March 16, 2013, that
`
`claims priority to an application filed before March 16, 2013, is available for PGR
`
`“if the patent contains . . . at least one claim that was not disclosed in compliance
`
`with the written description and enablement requirements of § 112(a) in the earlier
`
`application for which the benefit of an earlier filing date prior to March 16, 2013
`
`was sought.” Inguran, LLC v. Premium Genetics (UK) Ltd., Case PGR2015-
`
`00017, Paper 8 at 11 (P.T.A.B. Dec. 22, 2015).
`
`To meet the written description requirement of 35 U.S.C. § 112, the earlier
`
`application(s) must “reasonably convey[ ] to those skilled in the art that the
`
`inventor had possession of the claimed subject matter as of the filing date. Ariad
`
`Pharms., Inc. v. Eli Lilly & Co., 598 F.3d, 1336, 1351 (Fed. Cir. 2010). In essence,
`
`the specification must describe an invention in a manner “understandable to [a]
`9
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`

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`skilled artisan and show that the inventor actually invented the invention claimed.”
`
`Id. To meet the enablement requirement of 35 U.S.C. § 112, the earlier
`
`application(s) must teach those skilled in the art how to make and use the full
`
`scope of the claimed invention without “undue experimentation.” Genentech, Inc.
`
`v. Novo Nordisk, A/S, 108 F.3d 1361, 1365 (Fed. Cir. 1997) (citing Wands, 858
`
`F.2d at 736-37). “When a range is claimed, there must be reasonable enablement
`
`of the scope of the range.” AK Steel Corp. v. Sollac, 344 F.3d 1234, 1244 (Fed.
`
`Cir. 2003). A specification that “provides a starting point from which one of skill
`
`in the art can perform further research in order to practice the claimed invention”
`
`does not fulfill the enablement requirement. Nat’l Recovery Techs., Inc. v.
`
`Magnetic Separation Sys., Inc., 166 F.3d 1190, 1198 (Fed. Cir. 1999).
`
`Here, ten of the provisional applications underlying the ’239 patent were
`
`filed before March 16, 2013. But the claims of the ’239 patent are not described or
`
`enabled by any of the pre-AIA applications, see Section X below, or even by the
`
`’239 patent specification itself, as discussed in Section XI.B below. The pre-AIA
`
`applications do not describe or enable the full scope of the dosing regimen
`
`limitation recited in claim 1 and incorporated into all of the dependent claims. Exh.
`
`1003, claims 2-17. Furthermore, the pre-AIA applications do not even mention, let
`
`alone enable or describe, the limitation related to the duration of pain relief recited
`
`10
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`

`

`in claim 2, or the amount of zoledronic acid in a dosage form recited in claim 17.
`
`Therefore, the ’239 patent is available for PGR.
`
`A.
`
`The Pre-AIA Applications Fail to Describe or Enable the Dosing
`Regimens Limitation of Claim 1.
`
`Claim 1 of the ’239 patent recites a range of dosing regimens “wherein the
`
`human being receives about 80 to about 500 mg of zoledronic acid within a period
`
`of six months.” However, none of the pre-AIA applications provide information
`
`sufficient to describe or enable the entire range of dosing regimens found in claim
`
`1. Regarding Patent Owner’s failure to satisfy the written description requirement,
`
`as discussed below, the first eight pre-AIA applications fail to provide sufficient
`
`information from which a POSA would have understood that the claimed invention
`
`included a dosing regimen comprised of an amount within any particular dosing
`
`period.
`
`While, the ninth and tenth pre-AIA applications do include dosing regimens
`
`comprised of an amount within a particular period, as also discussed below, they
`
`fail to properly describe the dosing regimen limitation because they fail to direct a
`
`POSA to the particular range claimed. Regarding Patent Owner’s failure to satisfy
`
`the enablement requirement, as discussed below, the first six and the eighth pre-
`
`AIA applications fail to provide information from which a POSA might determine
`
`how long to administer zoledronic acid in order to effectively treat CRPS. As also
`
`11
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`

`

`discussed below, the seventh, ninth and tenth provisional applications
`
`indiscriminately provide possible dosing regimens that fall within and outside the
`
`claimed range of dosing regimens and thus fail to enable a POSA to practice the
`
`full range of dosing regimens.
`
`1.
`
`The Pre-AIA Applications Fail to Provide Proper Written
`Description of the Dosing Regimens Limitation.
`
`There is nothing in the pre-AIA applications from which a POSA would
`
`have concluded that a dosing regimen comprised of a particular amount of
`
`zoledronic acid and a corresponding dosing period is an aspect of the alleged
`
`invention. In fact, the first time the claimed dosing regimen limitation appeared
`
`was via an Examiner’s Amendment made on February 2, 2016 during the
`
`prosecution of the ’857 application (issued as the ’239 patent) in order to overcome
`
`the Examiner’s rejections based on the prior art. Exh. 1009, at 00425-26.
`
`Information re