`
`
`
`
`UNITED STATES PATENT AND TRADEMARK OFFICE
`_____________________________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`_____________________________
`
`
`NOVARTIS PHARMACEUTICALS CORPORATION,
`Petitioner
`
`v.
`
`
`PLEXXIKON INC.,
`Patent Owner
`
`_____________________________
`
`Case No.: PGR2018-00069
`_____________________________
`
`PETITION FOR POST-GRANT REVIEW OF
`U.S. PATENT NO. 9,844,539
`
`
`
`
`Mail Stop PATENT BOARD
`Patent Trial and Appeal Board
`United States Patent and Trademark Office
`P.O. Box 1450
`Alexandria, Virginia 22313–1450
`Submitted Electronically via the Patent Review Processing System
`
`
`

`

`Petition for Post-Grant Review of U.S. Patent No. 9,844,539
`
`
`TABLE OF CONTENTS
`
`I. 
`
`INTRODUCTION ........................................................................................... 1 
`
`II.  MANDATORY DISCLOSURES UNDER 37 C.F.R. § 42.8 ......................... 5 
`
`A. 
`
`B. 
`
`C. 
`
`D. 
`
`Real Parties-in-Interest .......................................................................... 5 
`
`Related Matters ...................................................................................... 5 
`
`Lead and Back-Up Counsel ................................................................... 6 
`
`Service Information ............................................................................... 6 
`
`III. 
`
`PAYMENT OF FEES UNDER 37 C.F.R. § 42.15(A) ................................... 6 
`
`IV.  REQUIREMENTS FOR PETITION UNDER 37 C.F.R. § 42.204 ................ 6 
`
`A.  Grounds for Standing (37 C.F.R. § 42.204(a)) ..................................... 6 
`
`B. 
`
`C. 
`
`D. 
`
`Identification of Challenge and Relief Requested ................................ 7 
`
`Claim Construction (37 C.F.R. § 42.204(b)(3)) .................................... 8 
`
`Level Of Skill In The Art ...................................................................... 8 
`
`V. 
`
`THE ʼ539 PATENT ......................................................................................... 8 
`
`A. 
`
`B. 
`
`The Challenged Claims ......................................................................... 8 
`
`The ʼ539 Patent Family ....................................................................... 11 
`
`VI. 
`
`IT IS MORE LIKELY THAN NOT THAT PETITIONER WILL PREVAIL
` ....................................................................................................................... 12 
`
`A. 
`
`PGR-Eligibility Of The ʼ539 Patent .................................................... 12 
`
`1. 
`
`2. 
`
`3. 
`
`The Standard For Claiming Benefit To An Earlier-
`Filed Application....................................................................... 14 
`
`The Standard For Written Description, 35 U.S.C.
`§ 112(a) ..................................................................................... 14 
`
`P2 Fails To Provide Written Description Support
`For The Challenged Claims ...................................................... 18 
`
`
`
`
`i
`
`

`

`4. 
`
`Petition for Post-Grant Review of U.S. Patent No. 9,844,539
`
`
`The Challenged Claims Are Not Entitled To
`Benefit Under 35 U.S.C. § 120 Because They Fail
`To Meet The Enablement Requirement Under 35
`U.S.C. § 112 .............................................................................. 46 
`
`B. 
`
`Ground 1: Because The Challenged Claims Are Not
`Entitled To Benefit Of P2 Or Any Earlier Application,
`They Are Anticipated By The ʼ185 Patent Under 35
`U.S.C. § 102(a) (AIA) ......................................................................... 67 
`
`1. 
`
`2. 
`
`The Standard For Anticipation Under 35 U.S.C.
`§ 102(a) (AIA) .......................................................................... 67 
`
`The Challenged Claims Are Anticipated By The
`ʼ185 Patent ................................................................................ 68 
`
`C. 
`
`Ground 2: All Of The Challenged Claims Are Invalid
`Under 35 U.S.C. § 112(a) (AIA) For Failure To Meet
`The Written Description Requirement ................................................ 70 
`
`D.  Ground 3: All Of The Challenged Claims Are Invalid
`Under 35 U.S.C. § 112(a) (AIA) For Failure To Meet
`The Enablement Requirement ............................................................. 71 
`
`VII.  CONCLUSION ............................................................................................. 71 
`
`
`
`
`
`
`
`
`
`
`ii
`
`

`

`Petition for Post-Grant Review of U.S. Patent No. 9,844,539
`
`
`
`
`TABLE OF AUTHORITIES
`
` Page(s)
`
`Cases
`AbbVie Deutschland GmbH & Co., KG v. Janssen Biotech, Inc.,
`759 F.3d 1285 (Fed. Cir. 2014) .......................................................................... 17
`
`Ariad Pharm., Inc. v. Eli Lilly and Co.,
`598 F.3d 1336 (Fed. Cir. 2010) (en banc) .................................................... 14, 17
`
`Brenner v. Manson,
`383 U.S. 519 ................................................................................................. 48, 66
`
`Carnegie Mellon Univ. v. Hoffman-La Roche Inc.,
`541 F.3d 1115 (Fed. Cir. 2008) .......................................................................... 18
`
`Fujikawa v. Wattanasin,
`93 F.3d 1559 (Fed. Cir. 1996) ...................................................................... 16, 17
`
`Genentech Inc. v. Novo Nordisk A/S,
`108 F.3d 1361 (Fed. Cir. 1997) .......................................................................... 47
`
`Hollmer v. Harari,
`681 F.3d 1351 (Fed. Cir. 2012) .......................................................................... 14
`
`In re Fouche,
`439 F.2d 1237 (C.C.P.A. 1971) .......................................................................... 49
`
`In re Gosteli,
`872 F.2d 1008 (Fed. Cir. 1989) .................................................................... 18, 69
`
`In re NTP, Inc.,
`654 F.3d 1268 (Fed. Cir. 2011) .......................................................................... 14
`
`In re Ruschig,
`379 F.2d 990 (C.C.P.A. 1967) ................................................................ 15, 16, 18
`
`In re Schreiber,
`128 F.3d 1473 (Fed. Cir. 1997) .......................................................................... 67
`
`
`
`
`iii
`
`

`

`Petition for Post-Grant Review of U.S. Patent No. 9,844,539
`
`
`In re Wands,
`858 F.2d 731 (Fed. Cir. 1988) ............................................................................ 48
`
`Inguran, LLC v. Premium Genetics (UK) Ltd.,
`PGR 2015-00017 (PTAB Dec. 22, 2015) ..................................................... 13, 14
`
`Novozymes A/S v. DuPont Nutrition Biosciences APS,
`723 F.3d 1336 (Fed. Cir. 2013) .................................................................... 17, 40
`
`Paice LLC v. Ford Motor Co.,
`881 F.3d 894 (Fed. Cir. Feb. 1, 2018) ................................................................ 14
`
`Peters v. Active Mfg. Co.,
`129 U.S. 530 (1889) ............................................................................................ 70
`
`Plexxikon Inc. v. Novartis Pharmaceuticals Corporation,
`Civil Action No. 4:17-cv-04405 HSG (EDL) (N.D. Cal.) ............................. 5, 70
`
`Purdue Pharma L.P. v. Faulding Inc.,
`230 F.3d 1320 (Fed. Cir. 2000) .................................................................... 15, 18
`
`Rasmusson v. SmithKline Beecham Corp.,
`413 F.3d 1318 (Fed. Cir. 2005) .................................................................... 48, 62
`
`Upsher-Smith Labs v. Pamlab, L.L.C.,
`412 F.3d 1319 (Fed. Cir. 2005) .......................................................................... 70
`
`Statutes
`
`35 U.S.C. § 100(i) ................................................................................................ 1, 13
`
`35 U.S.C. § 102(a) ...........................................................................1, 3, 7, 12, 13, 67
`
`35 U.S.C. § 112 .............................................................................................. 1, 14, 47
`
`35 U.S.C. § 120 .................................................................................................... 1, 14
`
`Other Authorities
`
`MPEP 2164.05(a) ..................................................................................................... 52
`
`
`
`
`
`
`
`
`iv
`
`

`

`Petition for Post-Grant Review of U.S. Patent No. 9,844,539
`
`
`EXHIBITS CITED IN THIS PETITION
`
`Exhibit
`No.
`
`1001
`
`Special
`Designation
`(if
`applicable)
`ʼ539 patent Wu et al., U.S. Patent No. 9,844,539 B2, “Compounds
`and Methods for Kinase Modulation, and Indications
`Therefor” (Dec. 19, 2017).
`
`Description
`
`1002
`
`Baran Dec.
`
`Declaration of Phil S. Baran, Ph.D.
`
`P2
`
`U.S. Application No. 12/669,450
`(PCT/US2008/070124)
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`P3 Prosecution History, October 4, 2013 Office Action
`
`P3 Prosecution History, June 5, 2014 Notice of
`Abandonment
`
`P4 Prosecution History, April 3, 2015 Office Action
`
`P4 Prosecution History, August 3, 2015 Amendment
`and Reply
`
`P4 Prosecution History, September 3, 2015 Office
`Action
`
`P4 Prosecution History, Examiner’s Summary of
`January 15, 2016 Interview
`
`P4 Prosecution History, Statement of Substance of
`Interview
`
`P4 Prosecution History, April 18, 2016 Notice of
`Abandonment
`
`P5 Prosecution History, February 19, 2016 Preliminary
`Amendment
`
`P5 Prosecution History, April 18, 2016 Office Action
`
`v
`
`1004
`
`1005
`
`1006
`
`1007
`
`1008
`
`1009
`
`1010
`
`1011
`
`1012
`
`1013
`
`1014
`
`
`
`
`

`

`
`
`
`
`Martin
`
`Düfert
`
`Kinzel
`
`Jedinák
`
`Tyrrell
`
`Hämmerle
`
`Cox
`
`Petition for Post-Grant Review of U.S. Patent No. 9,844,539
`
`
`P5 Prosecution History, July 20, 2016 Amendment and
`Response
`
`P5 Prosecution History, September 2, 2016 Notice of
`Allowance
`
`Martin et al., “Palladium-Catalyzed Suzuki-Miyaura
`Cross-Coupling Reactions Employing Dialkylbiaryl
`Phosphine Ligands,” 41 (11) ACCOUNTS OF CHEMICAL
`RESEARCH 1461-1473 (Nov. 2008)
`
`Düfert et al., “Suzuki-Miyaura Cross-Coupling of
`Unprotected, Nitrogen-Rich Heterocycles: Substrate
`Scope and Mechanistic Investigation,” 135 J. AM.
`CHEM. SOC. 12877-12885 (Aug. 2013)
`
`Kinzel et al., “A New Palladium Precatalyst Allows for
`the Fast Suzuki-Miyaura Coupling Reactions of
`Unstable Polyfluorophenyl and 2-Heteroaryl Boronic
`Acids” 132(40) J. AM. CHEM. SOC. 14073-75 (Oct.
`2010)
`
`Jedinák et al., “The Suzuki−Miyaura Cross-Coupling
`Reaction of Halogenated Aminopyrazoles: Method
`Development, Scope, and Mechanism of
`Dehalogenation Side Reaction,” 82 J. ORG. CHEM. 157-
`169 (Dec. 2016)
`Elizabeth Tyrrell and Phillip Brookes, “The Synthesis
`and Applications of Heterocyclic Boronic Acids,”
`2003(4) Synthesis 469-483
`
`Hämmerle et al., “A guideline for the arylation of
`positions 4 and 5 of thiazole via Pd-catalyzed cross-
`coupling reactions,” 66 TETRAHEDRON 8051-8059
`(Aug. 2010).
`
`Paul A. Cox et al., “Protodeboronation of
`heteroaromatic, vinyl and cyclopropyl boronic acids:
`pH-rate profiles, auto-catalysis and dispropotionation,”
`138(29) J. Am. Chem. Soc. 9145-57, 9152 (2016)
`
`vi
`
`1015
`
`1016
`
`1017
`
`1018
`
`1019
`
`1020
`
`1021
`
`1022
`
`1023
`
`
`
`
`

`

`Petition for Post-Grant Review of U.S. Patent No. 9,844,539
`
`
`Suzuki Nobel
`Lecture
`
`Akira Suzuki, “Cross-Coupling Reactions Of
`Organoboranes: An Easy Way to Construct C–C Bonds
`(Nobel Lecture),” 50 ANGEW. CHE. INT. ED. 6723-6737
`(2011)
`
`Li and
`Gribble
`
`ʼ185 patent
`
`P6
`
`
`
`Li and Gribble (Eds.), Palladium in Heterocyclic
`Chemistry: A Guide for the Synthetic Chemist (2d ed.
`2006)
`
`Tara R. Rheault, U.S. Patent No. 7,994,185, “Benzene
`Sulfonamide Thiazole and Oxazole Compounds,” (Aug.
`9, 2011)
`
`U.S. Patent Application No. 15/260,042 (filed Sept. 8,
`2016)
`
`P6 Prosecution History November 21, 2016 Preliminary
`Amendment
`
`1024
`
`1025
`
`1026
`
`1027
`
`1028
`
`
`
`
`vii
`
`

`

`Petition for Post-Grant Review of U.S. Patent No. 9,844,539
`
`
`Pursuant to 35 U.S.C. §§ 321-328 and 37 C.F.R. Part 42, Petitioner
`
`respectfully requests that the Board institute a post-grant review of claims 1, 2, 4-9,
`
`11, 12, and 14-19 (the “Challenged Claims”) of U.S. Patent No. 9,844,539 (“the
`
`ʼ539 patent”) (Ex. 1001) and determine that each of the Challenged Claims should
`
`be cancelled as unpatentable.
`
`I.
`
`INTRODUCTION
`
`The ʼ539 patent, entitled “Compounds and Methods for Kinase Modulation,
`
`and Indications Therefor,” issued on December 19, 2017. The patent is assigned to
`
`Plexxikon Inc. (“Plexxikon”). The ʼ539 patent claims priority to U.S. Application
`
`No. 12/669,450 (PCT/US2008/070124) (“P2”), filed on July 16, 2008, through a
`
`series of four continuation applications and claims earliest priority to provisional
`
`application No. 60/959,907 (“P1”), filed July 17, 2007.
`
`The ʼ539 patent is eligible for PGR because it contains at least one claim –
`
`including each of the Challenged Claims – whose effective date is after the March
`
`16, 2013 effective date of the Leahy-Smith America Invents Act (AIA). This
`
`results from the fact that the Challenged Claims are not entitled to the benefit of
`
`the July 16, 2008 filing date of P2 or the earlier provisional application because P2
`
`does not satisfy the written description and enablement requirements of 35 U.S.C.
`
`§ 112 (pre-AIA) as required for benefit under 35 U.S.C. § 120. AIA § 6(f)(2)(A);
`
`AIA § (3)(n)(1); 35 U.S.C. § 100(i). Ex. 1002, Declaration of Phil S. Baran, Ph.D.
`
`
`
`1
`
`

`

`Petition for Post-Grant Review of U.S. Patent No. 9,844,539
`
`
`(“Baran Dec.”) ¶ 8. Specifically, P2 discloses enormous genera of chemical
`
`compounds which cover an effectively incalculable number of compounds, but
`
`provides no “blaze marks” to direct a person of ordinary skill to the subgenera of
`
`the Challenged Claims. Moreover, while the subgenera of the Challenged Claims
`
`cover trillions of compounds, there are only three examples in P2 that fall within
`
`the scope of the claims, and none where L1 is a bond, which constitute
`
`approximately half of the compounds covered by Challenged Claims 1, 2, 4-9 and
`
`all of the compounds covered by Challenged Claims 11, 12, 14-19. P2 thus fails to
`
`meet the written description requirement of § 112. P2 also fails to meet the
`
`enablement requirement of § 112 because it does not enable a person of ordinary
`
`skill to make the full scope of claimed compounds wherein L1 is a bond, nor does it
`
`meet the how-to-use/utility prong of the enablement requirement because it does
`
`not disclose any data showing that claimed compounds wherein L1 is a bond
`
`achieve the desired results of the invention, viz. activity on protein kinases.
`
`Because the Challenged Claims are not entitled to claim the benefit of P2 or
`
`the earlier provisional application, the earliest possible priority date is April 19,
`
`2013, the filing date of the next continuation application, U.S. Application No.
`
`13/866,353 (“P3”). 1 Because the earliest possible priority date of April 19, 2013 is
`
`1 In fact, none of the applications in the chain of continuations leading to the ʼ539
`
`patent satisfies the § 112 requirements, but for purposes of the instant Petition it is
`
`
`
`2
`
`

`

`Petition for Post-Grant Review of U.S. Patent No. 9,844,539
`
`
`after the March 16, 2013 effective date of the AIA, the claims of the ʼ539 patent
`
`are subject to the first-inventor-to-file provisions of the AIA and are thus PGR-
`
`eligible. AIA § 3(n)(1).
`
`Moreover, because the earliest possible effective date of the Challenged
`
`Claims is April 19, 2013, the Challenged Claims are anticipated under AIA 35
`
`U.S.C. § 102(a)(1) by U.S. Patent 7,994,185 (“the ʼ185 patent”), which issued on
`
`August 9, 2011. The ʼ185 patent discloses and claims specific compounds falling
`
`within the scope of each of the Challenged Claims, including dabrafenib, the active
`
`ingredient of a commercial pharmaceutical product sold by Petitioner under the
`
`trade name Tafinlar®.2 Plexxikon has accused dabrafenib of infringing the
`
`Challenged Claims in pending district court litigation in the Northern District of
`
`California. As set out in Ground 1 below, each of the Challenged Claims should
`
`be cancelled as anticipated by the ʼ185 patent.
`
`The Examiner made a comparable rejection during prosecution of U.S.
`
`Application No. 13/866,353 (“P3”), one of the earlier applications in the chain of
`
`only necessary to show that the Challenged Claims are not entitled to the benefit of
`
`P2 or the earlier provisional application to establish that the’539 patent is PGR-
`
`eligible.
`
`2 Tafinlar® was originally developed and sold by GlaxoSmithKline (“GSK”).
`
`Petitioner purchased all rights to make, use and sell Tafinlar® from GSK in 2015.
`
`
`
`3
`
`

`

`Petition for Post-Grant Review of U.S. Patent No. 9,844,539
`
`
`continuations in the ʼ539 patent family. P3 was filed on April 19, 2013, and
`
`sought to claim priority to its parent application, P2. The Examiner determined
`
`that the claims of P3 were not entitled to the priority date of the parent application,
`
`on grounds that the parent application “fails to provide adequate support [i.e.,
`
`written description] or enablement” in the manner provided by 35 U.S.C. § 112.
`
`Ex. 1005 at 3. Because P3 was only entitled to its actual filing date of April 19,
`
`2013, the Examiner found the claims invalid based (inter alia) on the prior art ʼ185
`
`patent. Id. at 11-13. Rather than address the rejection, Plexxikon abandoned the
`
`P3 application. Inexplicably, the Examiner did not apply this same analysis to the
`
`ʼ539 patent. The Examiner’s failure to apply this analysis and to find the claims of
`
`the ʼ539 patent to be unpatentable was a mistake that should be corrected by the
`
`Board.
`
`For the same reasons that the ʼ539 patent is not entitled to the benefit of P2
`
`or any earlier applications, the Challenged Claims are invalid for failure to meet
`
`the written description and enablement requirements of AIA 35 U.S.C. § 112(a).
`
`The specification of the ʼ539 patent is the same as the specification of P2 and is
`
`deficient for the same reasons. There were no changes in the state of the art
`
`between the filing date of P2 and the filing date of the Challenged Claims that have
`
`a material effect on the written description or enablement analyses. Accordingly,
`
`Ground 2 of this Petition is that the Challenged Claims are invalid for failure to
`
`
`
`4
`
`

`

`Petition for Post-Grant Review of U.S. Patent No. 9,844,539
`
`
`meet the written description requirement of AIA 35 U.S.C. § 112(a), while
`
`Ground 3 is that the Challenged Claims are invalid for failure to meet the
`
`enablement requirement of AIA 35 U.S.C. § 112(a).
`
`As shown below, there is a very strong likelihood (and certainly it is more
`
`likely than not) that Petitioner will prevail in establishing that all of the Challenged
`
`Claims of the ’539 patent should be canceled. Petitioner thus asks the Board to
`
`grant post-grant review and determine that the Challenged Claims of the ’539
`
`patent are, in fact, unpatentable.
`
`II.
`
`A.
`
` MANDATORY DISCLOSURES UNDER 37 C.F.R. § 42.8
` Real Parties-in-Interest
`Novartis Pharmaceuticals Corporation (“NPC”) is the real party-in-interest.
`
`B.
`
` Related Matters
`The ʼ539 patent is asserted in the Second Amended Complaint for Patent
`
`Infringement filed on December 20, 2017 in Plexxikon Inc. v. Novartis
`
`Pharmaceuticals Corporation, Civil Action No. 4:17-cv-04405-HSG (EDL), filed
`
`August 3, 2017, in the United States District Court for the Northern District of
`
`California.
`
`A petition for Inter Partes Review of U.S. Patent No. 9,469,640 (the ʼ640
`
`patent) is filed concurrently herewith. The ʼ640 patent is also asserted in the
`
`above-referenced lawsuit in the Northern District of California. The claims of the
`
`ʼ640 patent are similar to the claims of the ʼ539 patent.
`
`
`
`5
`
`

`

`Petition for Post-Grant Review of U.S. Patent No. 9,844,539
`
`
`Additionally, U.S. Application No. 15/656,990 (filed July 21, 2017) is
`
`currently pending before the Office and claims priority to the application that
`
`issued as the ʼ539 patent.
`
`C.
`
` Lead and Back-Up Counsel
`
`Lead Counsel
`
`Back-Up Counsel
`
`Robert H. Underwood (Reg. # 45170)
`MCDERMOTT WILL & EMERY LLP
`28 State Street
`Boston, MA 02109
`Telephone: (617) 535-4093
`Fax: (617) 535-3800
`Email: runderwood@mwe.com
`
`Thomas P. Steindler (Pro Hac
`Pending)
`MCDERMOTT WILL & EMERY LLP
`500 N. Capitol Street, NW
`Washington, DC 20002
`Telephone: (202) 756-8000
`Fax: (202) 756-8087
`E-mail: tsteindler@mwe.com
`
`D.
`
`Service Information
`
`
`Documents may be delivered by hand to the addresses of lead and back-up
`
`counsel, listed above. Petitioner consents to electronic service by e-mail at the
`
`above-listed e-mail addresses of Lead and Back-Up Counsel.
`
`III. PAYMENT OF FEES UNDER 37 C.F.R. § 42.15(A)
`Petitioner authorizes the Office to charge the filing fee specified by 37
`
`C.F.R. § 42.15(b), and any other necessary fee, to Deposit Account No. 50-0417.
`
`IV. REQUIREMENTS FOR PETITION UNDER 37 C.F.R. § 42.204
` Grounds for Standing (37 C.F.R. § 42.204(a))
`A.
`Petitioner certifies that it has standing to request, and is not barred from
`
`requesting, post-grant review of the ʼ539 patent pursuant to 35 U.S.C. § 321.
`
`
`
`6
`
`

`

`Petition for Post-Grant Review of U.S. Patent No. 9,844,539
`
`
`Neither Petitioner nor any privy of Petitioner has filed any civil action challenging
`
`the validity of any claim of the ʼ539 patent or previously requested post-grant
`
`review of the ʼ539 patent.
`
`As discussed below, the Challenged Claims have an effective filing date that
`
`is after March 16, 2013, and are therefore eligible for PGR. See AIA
`
`§§ 6(f)(2)(A); 3(n)(1).
`
`In addition, Petitioner also certifies that it files this Petition less than nine
`
`months after the date of the grant of the ʼ539 patent, December 19, 2017.
`
`B.
`
`
`
`Identification of Challenge and Relief Requested
`
`Petitioner requests that the Board review and cancel claims 1, 2, 4-9, 11, 12,
`
`and 14-19 of the ʼ539 patent based on the grounds set forth under 35 U.S.C. §§
`
`101, 102, 103 and 112. This petition presents evidence of unpatentability and
`
`establishes that it is more likely than not that the Petitioner will prevail in
`
`establishing that all of the Challenged Claims are unpatentable. The charts below
`
`summarize how the claims may be grouped for the instant challenge, and the
`
`grounds for unpatentability as to each claim. Where more than one ground exists
`
`for a claim, the ground(s) relying on additional references should be treated as
`
`alternative(s).
`
`Ground No.
`1
`
`35 USC
`§ 102(a)(1)
`
`
`
`Claims
`1, 2, 4-9,
`11, 12,
`14-19
`
`7
`
`Description
`Anticipated by the ʼ185 patent
`
`

`

`Petition for Post-Grant Review of U.S. Patent No. 9,844,539
`
`
`§ 112(a)
`
`§ 112(a)
`
`2
`
`3
`
`C.
`
`Lack of written description
`
`Lack of enablement
`
`1, 2, 4-9,
`11, 12,
`14-19
`1, 2, 4-9,
`11, 12,
`14-19
` Claim Construction (37 C.F.R. § 42.204(b)(3))
`Petitioner believes each of the claim terms should be given their plain and
`
`ordinary meaning and does not propose any specific constructions for any of the
`
`claim terms.
`
`D.
`
` Level Of Skill In The Art
`A person of ordinary skill in the art would have a Ph.D. or equivalent degree
`
`in organic or medicinal chemistry, and 2-3 years of post-graduate experience
`
`working in medicinal chemistry, synthetic organic chemistry, and/or kinase
`
`chemistry, including in the development of potential drug candidates. A person of
`
`ordinary skill in the art would also include a person who has a Bachelor’s or
`
`Master’s degree in organic chemistry or medicinal chemistry if such a person had
`
`more years of experience in medicinal chemistry and/or the development of
`
`potential drug candidates. Baran Dec. ¶ 24.
`
`V. THE ʼ539 PATENT
` The Challenged Claims
`A.
`The ʼ539 patent has a total of 30 claims. Petitioner challenges claims 1, 2,
`
`4-9, 11, 12, and 14-19. Claims 1, 2, 4-8, 11, 12, and 14-18 are compound claims
`
`
`
`8
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`

`

`Petition for Post-Grant Review of U.S. Patent No. 9,844,539
`
`
`(“Compound Claims”). Claims 9 and 19 are composition claims (“Composition
`
`Claims”). Each of the Challenged Claims is reproduced below:
`
`1.
`
`A compound of formula (Ia):
`
` (Ia)
`
`or a pharmaceutically acceptable salt thereof,
`wherein:
`
`L1 is a bond or —N(H)C(O)—;
`each R1 is optionally substituted lower alkyl or optionally
`
`substituted heteroaryl;
`R2 is hydrogen or halogen;
`
`R4 is hydrogen;
`
`R3 is optionally substituted lower alkyl or optionally
`
`substituted aryl;
`
`m is 0, 1, 2, or 3; and
`
`Ar is a monocyclic heteroaryl containing 5 to 6 atoms
`wherein at least one atom is nitrogen.
`The compound of claim 1, wherein R2 is hydrogen.
`2.
`The compound of claim 1, wherein R3 is optionally
`4.
`substituted phenyl.
`The compound of claim 1, wherein R3 is phenyl
`5.
`substituted with one or more substituents selected from the
`group consisting of fluoro, lower alkyl, fluoro substituted lower
`
`
`
`9
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`

`

`Petition for Post-Grant Review of U.S. Patent No. 9,844,539
`
`
`alkyl, lower alkoxy, fluoro substituted lower alkoxy, lower
`alkylthio, and fluoro substituted lower alkylthio.
`The compound of claim 1, wherein R3 is phenyl
`6.
`substituted with one or more fluoro.
`The compound of claim 1, wherein one of the R1
`7.
`substituents is optionally substituted lower alkyl containing 1-4
`carbon atoms.
`The compound of claim 1, wherein one of the R1
`8.
`substituents is optionally substituted heteroaryl.
`9.
`A pharmaceutical composition comprising a compound
`of claim 1 and a pharmaceutically acceptable carrier or
`excipient.
`11. A compound of formula (Ia):
`
` (Ia)
`
`or a pharmaceutically acceptable salt thereof,
`wherein:
`
`L1 is a bond;
`each R1 is optionally substituted lower alkyl or optionally
`
`substituted heteroaryl;
`R2 is hydrogen or halogen;
`
`R4 is hydrogen;
`
`R3 is optionally substituted lower alkyl or optionally
`
`substituted aryl;
`
`
`
`10
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`

`

`Petition for Post-Grant Review of U.S. Patent No. 9,844,539
`
`
`m is 0, 1, 2, 3, 4, or 5; and
`
`Ar is a monocyclic heteroaryl containing 5 to 6 atoms
`
`wherein at least one atom is nitrogen.
`12. The compound of claim 11, wherein R2 is hydrogen.
`14. The compound of claim 11, wherein R3 is optionally
`substituted phenyl.
`15. The compound of claim 11, wherein R3 is phenyl
`substituted with one or more substituents selected from the
`group consisting of fluoro, lower alkyl, fluoro substituted lower
`alkyl, lower alkoxy, fluoro substituted lower alkoxy, lower
`alkylthio, and fluoro substituted lower alkylthio.
`16. The compound of claim 11, wherein R3 is phenyl
`substituted with one or more fluoro.
`17. The compound of claim 11, wherein one of the R1
`substituents is optionally substituted lower alkyl containing 1-4
`carbon atoms.
`18. The compound of claim 11, wherein one of the R1
`substituents is optionally substituted heteroaryl.
`19. A pharmaceutical composition comprising a compound
`of claim 11 and a pharmaceutically acceptable carrier or
`excipient.
`The ʼ539 Patent Family
`
`B.
`
`
`The series of patent applications that led to the ʼ539 patent is depicted
`
`below. The relevant applications have been identified using the designations P1
`
`through P6.
`
`
`
`11
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`

`Petition for Post-Grant Review of U.S. Patent No. 9,844,539
`
`
`
`
`
`
`VI.
`
`IT IS MORE LIKELY THAN NOT THAT PETITIONER WILL
`PREVAIL
`
`Post-grant review is limited to patents described in section 3(n)(1) of the
`
`PGR-Eligibility Of The ʼ539 Patent
`
`A.
`
`AIA. Thus, only patents with an effective filing date after March 16, 2013 are
`
`eligible for post-grant review. AIA §§ 6(f)(2)(A); 3(n)(1). Here, because the ʼ539
`
`patent contains at least one claim (including each of the Challenged Claims) that is
`
`not entitled to the benefit of the July 16, 2008 filing date of P2, the earliest possible
`
`
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`12
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`Petition for Post-Grant Review of U.S. Patent No. 9,844,539
`
`
`priority date is April 19, 2013, the filing date of the next continuation application,
`
`P3.3 Because the earliest possible priority date of April 19, 2013 is after the
`
`March 16, 2013 effective date of the AIA, the claims of the ʼ539 patent are subject
`
`to the first-inventor-to-file provisions of the AIA and are thus PGR-eligible. AIA
`
`§ 3(n)(1); 35 U.S.C. § 100(i); Inguran, LLC v. Premium Genetics (UK) Ltd., PGR
`
`2015-00017 (PTAB Dec. 22, 2015) (Paper No. 8 at 9-11) (a patent granted from a
`
`transitional application (i.e. a patent application filed on or after March 16, 2013
`
`claiming the benefit of an earlier filing date prior to March 16, 2013) is available
`
`for post-grant review “if the patent contains, or the corresponding application
`
`contained at any time, 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”).
`
`
`3 As noted above (supra, n. 1), neither P3 nor any of the other applications in the
`
`chain of continuations leading to the ʼ539 patent satisfies the § 112 requirements,
`
`but for purposes of the instant Petition it is only necessary to show that the
`
`Challenged Claims are not entitled to the benefit of P2 or the earlier provisional
`
`application to establish that the’539 patent is PGR-eligible.
`
`
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`13
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`

`

`Petition for Post-Grant Review of U.S. Patent No. 9,844,539
`
`
`1.
`
`The Standard For Claiming Benefit To An Earlier-Filed
`Application
`
`In order to claim the benefit of an earlier-filed priority application under 35
`
`U.S.C. § 120, the earlier-filed application must meet the written description and
`
`enablement requirements of 35 U.S.C. § 112(a) (AIA).4 35 U.S.C. § 120; Inguran,
`
`LLC, supra (Paper No. 8 at 9-10); Paice LLC v. Ford Motor Co., 881 F.3d 894,
`
`906 (Fed. Cir. Feb. 1, 2018); In re NTP, Inc., 654 F.3d 1268, 1277 (Fed. Cir.
`
`2011). Moreover, “if any application in the priority chain fails to make the
`
`requisite disclosure of subject matter, the later filed application is not entitled to
`
`the benefit of the filing date of applications preceding the break in the priority
`
`chain.” Hollmer v. Harari, 681 F.3d 1351, 1355 (Fed. Cir. 2012).
`
`The Standard For Written Description, 35 U.S.C. § 112(a)
`
`2.
`35 U.S.C. § 112(a) provides that “[t]he specification shall contain a written
`
`description of the invention.” “[T]he description must clearly allow persons of
`
`ordinary skill in the art to recognize that the inventor invented what is claimed. In
`
`other words, the test for sufficiency is whether the disclosure of the application
`
`relied upon reasonably conveys to those skilled in the art that the inventor had
`
`possession of the claimed subject matter as of the filing date.” Ariad Pharm., Inc.
`
`
`4 Section 4(c) of the AIA redesignated 35 U.S.C. § 112 ¶ 1 as 35 U.S.C. § 112(a).
`
`125 Stat. at 296.
`
`
`
`14
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`

`Petition for Post-Grant Review of U.S. Patent No. 9,844,539
`
`
`v. Eli Lilly and Co., 598 F.3d 1336, 1351 (Fed. Cir. 2010) (en banc) (citations and
`
`quotations omitted).
`
`Where a claim recites a specific combination of variables, the specification
`
`must direct the person of ordinary skill to that specific combination; a general
`
`disclosure that encompasses the specific combination is not sufficient to satisfy the
`
`written description requirement. As the Court explained in In re Ruschig, 379 F.2d
`
`990, 995-96 (C.C.P.A. 1967):
`
`It is an old custom in the woods to mark trails by making blaze marks
`on the trees. It is no help in finding a trail or in finding one’s way
`through the woods where the trails have disappeared — or have not
`yet been made, which is more like the case here — to be confronted
`simply by a large number of unmarked trees. Appellants are pointing
`to trees. We are looking for blaze marks which single out particular
`trees.
`
`Where the claimed invention is not “specifically named or mentioned in any
`
`manner [in the application as filed], one is left to selection from the myriads of
`
`possibilities encompassed by the broad disclosure, with no guide indicating or
`
`directing that this particular selection should be made rather than any of the many
`
`others which could also be made.” Id. at 995; see also Purdue Pharma L.P. v.
`
`Faulding Inc., 230 F.3d 1320, 1326-27 (Fed. Cir. 2000) (“[O]ne cannot disclose a
`
`forest in the original application, and then later pick a tree out of the forest and say
`
`‘here is my invention’. In order to satisfy the written description requir