UNITED STATES PATENT AND TRADEMARK OFFICE
`_________________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`_________________
`
`ARGENTUM PHARMACEUTICALS LLC
`Petitioner,
`
`v.
`
`KAKEN PHARMACEUTICAL CO., LTD. and VALEANT
`PHARMACEUTICALS INTERNATIONAL, INC.
`Patent Owner
`_________________
`
`U.S. Patent No. 7,214,506
`Issue Date: May 8, 2007
`Title: Method for Treating Onychomycosis
`_________________
`
`Inter Partes Review No. 2017-01429
`
`
`
`Petition For Inter Partes Review Under
`35 U.S.C. §§ 311-319 and 37 C.F.R. § 42.100 et seq.
`
`
`
`

`

`Patent No. 7,214,506
`Petition For Inter Partes Review
`
`
`
`
`TABLE OF CONTENTS
`EXHIBIT LIST ......................................................................................................... ix 
`I. 
`INTRODUCTION ........................................................................................... 1 
`II.  MANDATORY NOTICES (37 C.F.R. § 42.8(a)(1)) ...................................... 1 
`A. 
`Real Party-In-Interest Under 37 C.F.R. § 42.8(b)(1) .............................. 1 
`B. 
`Related Matters Under 37 C.F.R. § 42.8(b)(2) ........................................ 1 
`C. 
`Lead And Back-Up Counsel Under 37 C.F.R. § 42.8(b)(3) .................... 2 
`D. 
`Service Information Under 37 C.F.R. § 42.8(b)(4) ................................. 2 
`E. 
`Service on Patent Owner Under 37 C.F.R. § 42.105(a) and 42.106(a) .... 2 
`III.  GROUNDS FOR STANDING (37 C.F.R. §§ 42.101 and 42.104) .................. 3 
`IV.  PAYMENT OF FEES (37 C.F.R. § 42.103) .................................................... 3 
`V.  A STATEMENT OF THE PRECISE RELIEF REQUESTED (§
`42.22(a)(1)) ...................................................................................................... 3 
`IDENTIFICATION OF CHALLENGES (§ 42.104(b)) ................................. 3 
`VI. 
`VII.  SUMMARY OF THE ’506 PATENT ............................................................. 5 
`A.  Overview ............................................................................................... 5 
`B. 
`The ’506 Patent...................................................................................... 6 
`C. 
`Prosecution History ............................................................................. 10 
`D. 
`Challenged Claims of the ’506 Patent ................................................. 14 
`VIII.  EFFECTIVE FILING DATE OF THE CHALLENGED CLAIMS ............. 16 
`A. 
`The JP Priority Document Does Not Support Treating a Subject
`Having Onychomycosis ...................................................................... 18 
`The JP Priority Document Does Not Disclose “topically
`
`B. 
`
`
`
`ii
`
`

`

`Patent No. 7,214,506
`Petition For Inter Partes Review
`
`
`
`
`administering to a nail of said subject having onychomycosis a
`therapeutically effective amount of an antifungal compound
`represented by the [chemical formula].” ............................................. 19 
`The First Disclosure of the Claimed Elements was July 11, 2000 ...... 21 
`C. 
`IX.  APPLICABLE LAW AND LEVEL OF SKILL IN THE ART .................... 21 
`X. 
`CLAIM-BY-CLAIM EXPLANATION OF GROUNDS FOR
`UNPATENTABILITY .................................................................................. 23 
`A.  Ground 1: Claims 1 and 2 of the ’506 Patent Are Obvious Over
`Japanese Pat. App. Pub. No. 10- 226639 in View of Ogura. .............. 23 
`i.  JP ’639 teaches “a method for treating a subject having
`onychomycosis wherein the method comprises topically
`administering to a nail of said subject having onychomycosis a
`therapeutically effective amount of an antifungal compound” ........... 24 
`ii.  Ogura Discloses the Antifungal Activities of Azolylamine
`Compounds Including KP-103, i.e. a Compound Falling Within the
`Scope of the Claims ............................................................................. 26 
`iii.  It Would Have Been Obvious to One of Ordinary Skill in the
`Art to Combine JP ’639 and Ogura. .................................................... 27 
`Ground 2: Claims 1 and 2 of the ’506 Patent Are Obvious Over
`U.S. Pat. No. 5,391,367 in View of Ogura .......................................... 32 
`i.  The ’367 Patent Teaches “a method for treating a subject
`having onychomycosis wherein the method comprises topically
`administering to a nail of said subject having onychomycosis a
`therapeutically effective amount of an antifungal compound” ........... 33 
`ii.  Ogura Discloses the Antifungal Activities of Azolylamine
`Compounds Including KP-103. ........................................................... 34 
`iii.  It Would Have Been Obvious to One of Ordinary Skill in the
`Art to Combine the Teachings of the ’367 Patent and Ogura. ............ 34 
`Ground 3: Claims 1 and 2 of the ’506 Patent Are Obvious Over
`
`B. 
`
`C. 
`
`
`
`iii
`
`

`

`Patent No. 7,214,506
`Petition For Inter Partes Review
`
`
`
`
`Hay in View of Ogura ......................................................................... 37 
`i.  Hay teaches “a method for treating a subject having
`onychomycosis wherein the method comprises topically
`administering to a nail of said subject having onychomycosis a
`therapeutically effective amount of an antifungal compound” ........... 38 
`ii.  Ogura Discloses the Antifungal Activities of Azolylamine
`Compounds Including KP-103. ........................................................... 39 
`iii.  It Would Have Been Obvious to One of Ordinary Skill in the
`Art to Combine Hay and Ogura. ......................................................... 39 
`D.  Ground 4: Claims 1 and 2 of the ’506 Patent Are Obvious Over JP
`’639 in View of the Kaken Abstracts .................................................. 42 
`i.  JP ’639 Teaches “a method for treating a subject having
`onychomycosis wherein the method comprises topically
`administering to a nail of said subject having onychomycosis a
`therapeutically effective amount of an antifungal compound” ........... 43 
`ii.  The Kaken Abstracts Disclose the Antifungal Activities of KP-
`103. ...................................................................................................... 44 
`iii.  It Would Have Been Obvious to One of Ordinary Skill in the
`Art to Combine the Teachings of JP ’639 and the Kaken Abstracts. . 45 
`Ground 5: Claims 1 and 2 of the ’506 Patent Are Obvious Over the
`’367 Patent in View of the Kaken Abstracts. ...................................... 49 
`i.  The ’367 Patent Teaches “a method for treating a subject
`having onychomycosis wherein the method comprises topically
`administering to a nail of said subject having onychomycosis a
`therapeutically effective amount of an antifungal compound” ........... 49 
`ii.  The Kaken Abstracts Disclose the Antifungal Activities of KP-
`103. ...................................................................................................... 50 
`iii.  It Would Have Been Obvious to One of Ordinary Skill in the
`Art to Combine the Teachings of the ’367 Patent and the Kaken
`Abstracts. ............................................................................................. 50 
`
`E. 
`
`
`
`iv
`
`

`

`Patent No. 7,214,506
`Petition For Inter Partes Review
`
`
`
`F. 
`
`Ground 6: Claims 1 and 2 of the ’506 Patent Are Obvious over
`Hay in View of the Kaken Abstracts. .................................................. 53 
`i.  Hay Teaches “a method for treating a subject having
`onychomycosis wherein the method comprises topically
`administering to a nail of said subject having onychomycosis a
`therapeutically effective amount of an antifungal compound” ........... 53 
`ii.  The Kaken Abstracts Disclose the Antifungal Activities of KP-
`103. ...................................................................................................... 54 
`iii.  It Would Have Been Obvious to One of Ordinary Skill in the
`Art to Combine the Teachings of Hay and the Kaken Abstracts. ....... 54 
`XI.  ANY EVIDENCE PATENTEE AND LICENSEE MAY OFFER
`RELATING TO SECONDARY CONSIDERATIONS WILL NOT BE
`ADEQUATE TO OVERCOME THE OBVIOUSNESS OF THE
`CLAIMS ........................................................................................................ 57 
`A. 
`The Alleged Unexpected Results of the Invention are Insufficient
`to Overcome the Strong Case of Obviousness Presented Herein ....... 59 
`i.  The Alleged Unexpected Results Presented During Prosecution
`were Known Beneficial Results. ......................................................... 59 
`ii.  The Data Presented in the ’506 Specification is Flawed and
`Does Not Provide Evidence of an Unexpected Effect. ....................... 62 
`iii.  The ’506 Patent Specification Demonstrates that the Claimed
`Compounds do not Eradicate the Infection as Claimed by
`Patentees. ............................................................................................. 63 
`Any Alleged Commercial Success of Valeant’s Jublia® Product is
`Insufficient to Overcome the Strong Case of Obviousness
`Presented Herein .................................................................................. 64 
`XII.  CONCLUSION .............................................................................................. 65 
`CERTIFICATION OF WORD COUNT ................................................................. 66 
`CERTIFICATE OF SERVICE ................................................................................ 67
`
`B. 
`
`
`
`v
`
`

`

`Patent No. 7,214,506
`Petition For Inter Partes Review
`
`
`
`
`TABLE OF AUTHORITIES
`
` Page(s)
`
`Cases
`Allergan, Inc. v. Apotex Inc.,
`754 F.3d 952 (Fed. Cir. 2014), cert. denied, 135 S. Ct. 956 (2015) ................... 58
`Cohesive Techs., Inc. v. Waters Corp.,
`543 F.3d 1351 (Fed. Cir. 2008) .......................................................................... 14
`Cubist Pharms., Inc. v. Hospira, Inc.,
`75 F. Supp. 3d 641, 667 (D. Del. 2014), aff'd, 805 F.3d 1112 (Fed.
`Cir. 2015), cert. denied, 136 S. Ct. 2393 (2016) ................................................ 57
`Graham v. John Deere Co. of Kansas City,
`383 U.S. 1 (1966) ................................................................................................ 22
`Honeywell Int’l, Inc. v. United States,
`609 F.3d 1292 (Fed. Cir. 2010) .......................................................................... 21
`Hyatt v. Dudas,
`492 F.3d 1365 (Fed. Cir. 2007) .......................................................................... 16
`In re Chu,
`66 F.3d 292 (Fed. Cir. 1995) .............................................................................. 16
`In re Gershon,
`372 F.2d 535 (C.C.P.A. 1967) ............................................................................ 62
`In re Kao,
`639 F.3d 1057 (Fed. Cir. 2011) .................................................................... 57, 64
`In re NTP, Inc.,
`654 F.3d 1268 (Fed. Cir. 2011) .......................................................................... 16
`In re Skoll,
`523 F.2d 1392 (C.C.P.A. 1975) .......................................................................... 62
`
`
`
`vi
`
`

`

`Patent No. 7,214,506
`Petition For Inter Partes Review
`
`
`King Pharms., Inc. v. Eon Labs, Inc.,
`616 F.3d 1267 (Fed. Cir. 2010) .......................................................................... 64
`Lockwood v. Am. Airlines, Inc.,
`107 F.3d 1565 (Fed. Cir. 1997) .......................................................................... 17
`Media Techs. Licensing, LLC v. Upper Deck Co.,
`596 F.3d 1334 (Fed. Cir. 2010) .......................................................................... 64
`Pfizer, Inc. v. Apotex, Inc.,
`480 F.3d 1348 (Fed. Cir. 2007) .......................................................................... 58
`Ruiz v. A.B. Chance Co.,
`234 F.3d 654 (Fed. Cir. 2000) ............................................................................ 27
`Vas–Cath Inc. v. Mahurkar,
`935 F.2d 1555 (Fed. Cir. 1991) .......................................................................... 16
`Western Union Co. v. MoneyGram Payment Sys.,
`626 F.3d 1361 (Fed. Cir. 2010) .......................................................................... 58
`Statutes
`35 U.S.C. § 102(a) ................................................................................................... 24
`35 U.S.C. § 102(b) ............................................................................................passim
`35 U.S.C. § 103(a) ............................................................................................passim
`35 U.S.C. § 112 .................................................................................................. 16, 17
`35 U.S.C. § 312(a)(3) ................................................................................................. 4
`Regulations
`37 C.F.R. § 42.8(a)(1)) ............................................................................................... 1
`37 C.F.R. § 42.8(b)(1) ................................................................................................ 1
`37 C.F.R. § 42.8(b)(2) ................................................................................................ 1
`37 C.F.R. § 42.8(b)(3) ................................................................................................ 2
`vii
`
`
`
`

`

`Patent No. 7,214,506
`Petition For Inter Partes Review
`
`
`37 C.F.R. § 42.8(b)(4) ................................................................................................ 2
`37 C.F.R. § 42.10(b) .................................................................................................. 2
`37 C.F.R. § 42.101 ..................................................................................................... 3
`37 C.F.R. § 42.103 ..................................................................................................... 3
`37 C.F.R. § 42.104 ..................................................................................................... 3
`37 C.F.R. § 42.105(a) ................................................................................................. 2
`37 C.F.R. § 42.106(a) ................................................................................................. 2
`
`
`
`
`
`
`
`viii
`
`

`

`Patent No. 7,214,506
`Petition For Inter Partes Review
`
`
`
`
`EXHIBIT LIST
`
`EXHIBIT
`
`DESCRIPTION
`
`1001
`
`1002
`
`1003
`
`1004
`
`1005
`
`1006
`
`1007
`
`1008
`
`1009
`
`1010
`
`1011
`
`1012
`
`U.S. Pat. No. 7,214,506 to Tatsumi et al. (“’506 Patent”)
`
`Certified English Translation of Japanese Pat. App. No. 11/214369
`and Japanese Pat. App. No. 11/214369 (“JP priority document”)
`
`Press Release: “Valeant Pharmaceuticals Announces FDA Approval
`of Jublia® for the Treatment of Onychomycosis” (dated June 9,
`2014), at http://ir.valeant.com/news-releases/2014/09-06-2014, last
`accessed on July 29, 2016.
`
`Orange Book Excerpt for Valeant’s Jublia® Product, “Approved
`Drug Products with Therapeutic Equivalence Evaluations,” at
`http://www.accessdata.fda.gov/scripts/cder/ob/patent_info.cfm?Prod
`uct_No=001&Appl_No+203567&Appl_type=N, (last accessed on
`October 26, 2016).
`
`Declaration of Kenneth Walters
`
`Prosecution History of U.S. Pat. No. 7,214,506 (June 14, 2006)
`
`U.S. Pat. No. 5,620,994 to Naito et al.
`
`U.S. Pat. No. 5,716,969 to Naito et al.
`
`Comparison between the Priority Document (see Ex. 1002) and U.S.
`Pat. App. No. 10/685,266 (“’266 application”)
`
`Publication of PCT/JP00/04617 (filed July 11, 2000).
`
`Certified English Translation of Japanese Pat. App. Pub. No. 10-
`226639 and Japanese Pat. App. Pub. No. 10-226639 (“JP ’639”)
`
`“Synthesis and Antifungal Activities of (2R,3R)-2-Aryl-1-azolyl-3-
`(substituted amino)-2-butanol Derivatives as Topical Antifungal
`Agents.” Ogura, H. et al., Chem. Pharm. Bull, 47(10) 1417-1425
`(1999) (“Ogura”)
`
`
`
`ix
`
`

`

`Patent No. 7,214,506
`Petition For Inter Partes Review
`
`
`
`1013
`
`1014
`
`1015
`
`1016
`
`1017
`
`1018
`
`1019
`
`1020
`
`1021
`
`U.S. Pat. No. 5,391,367 to DeVincentis (“’367 patent”)
`
`“Tioconazole nail solution—an open study of its efficacy in
`onychomycosis.” Hay, R.J., et al., Clinical and Experimental
`Dermatology, 10:111-115 (1985) (“Hay” or “Hay 1985”)
`
`Abstracts F78, F79 and F80 from Abstracts of the Interscience
`Conference on Antimicrobial Agents and Chemotherapy (ICAAC),
`36th ICAAC, held on September 15-18, 1996 (1996) (“Kaken
`Abstracts”)
`
`“Bioavailability, skin- and nail penetration of topically applied
`antimycotics.” Stuttgen, G. and Bauer, E., Mycoses, 25(2): 74-80
`(1992) (“Stuttgen and Bauer”)
`
`“Ciclopirox nail lacquer 8%: in vivo penetration into and through
`nails and in vitro effect on pig skin.” Ceschin-Roques C.G., et al.,
`Skin Pharmacol, 4: 89-94 (1991) (“Ceschin-Roques”)
`
`“Absorption of amorolfine through human nail.” Franz, T.J.,
`Dermatol, 184(Suppl 1): 18-20 (1992) (“Franz”)
`
`“Nail penetration of the antifungal oxiconazole after repeated topical
`application in healthy volunteers, and the effect of acetylcysteine.”
`van Hoogdalem, E.J. et al., Eur J Pharm Sci 5: 119-127 (1997)
`(“van Hoogdalem”)
`
`“The effect of keratolytic agents on the permeability of three
`imidazole antimycotic drugs through the human nail.” Quintanar-
`Guerrero, D. et al., Drug Dev Ind Pharm, 24: 685-690 (1998)
`(“Quintanar-Guerrero”)
`
`“In vitro permeability of the human nail and of a keratin membrane
`from bovine hooves: Influence of the partition coefficient
`octanol/water and the water solubility of drugs on their permeability
`and maximum flux.” Mertin, D. and Lippold, B.C., Journal of
`Pharmacy and Pharmacology, 49(1): 30-34 (1997) (“Merton and
`Lippold I”)
`
`
`
`x
`
`

`

`Patent No. 7,214,506
`Petition For Inter Partes Review
`
`
`“In vitro permeability of the human nail and of a keratin membrane
`from bovine hooves: Penetration of chloramphenicol from lipophilic
`vehicles and a nail lacquer.” Mertin, D. and Lippold, B.C., Journal
`of Pharmacy and Pharmacology, 49(3): 241-245 (1997) (“Mertin
`and Lippold II”)
`
`“In vitro permeability of the human nail and of a keratin membrane
`from bovine hooves: Prediction of the penetration rate of
`antimycotics through the nail plate and their efficacy.” Mertin, D.
`and Lippold, B.C., Journal of Pharmacy and Pharmacology, 49(9):
`866-872 (1997) (“Mertin and Lippold III”)
`
`“Enhancing effect of N-acetyl-L-cysteine or 2-mercaptoethanol on
`the in vitro permeation of 5-fluorouracil or tolnaftate through the
`human nail plate.” Kobayashi Y. et al., Chem Pharm Bull 46: 1797-
`1802 (1998) (“Kobayashi”)
`
`“Pharma Giant Valeant Enters the Super Bowl Fray With a Toe
`Fungus Ad.” Heine, C. AdWeek. (Jan. 27, 2015)
`
`“Management of Onychomycoses.” Niewerth, M. and Korting, H.C.,
`Drugs 58(2):283-296 (1999) (“Niewerth and Korting”)
`
`“Diffusion of water through dead plantar, palmar and torsal human
`skin and through toe nails.” Burch, G.E. and Winsor, T., Arch Derm
`Syphilol 53: 39-41 (1946) (“Burch and Winsor”)
`
`“A comparative study of the physicochemical properties of human
`keratinized tissues.” Baden H.P., et al., Biochim Biophys Acta
`322:269–278 (1973) (“Baden”)
`
`“The azole antifungal drugs.,” Hay, R.J., Journal of Antimicrobial
`Chemotherapy 20: 1-5 (1987) (“Hay 1987”)
`
`“Amorolfine nail lacquer: a novel formulation.” Marty, J.L., Journal
`of the European Academy of Dermatology and Venereology 4
`(Supp. 1)(1995) S17-S21 (1995) (“Marty”)
`
`
`1022
`
`1023
`
`1024
`
`1025
`
`1026
`
`1027
`
`1028
`
`1029
`
`1030
`
`
`
`xi
`
`

`

`Patent No. 7,214,506
`Petition For Inter Partes Review
`
`
`“Epidemiology and ecology of onychomycosis.” Summerbell, R.C.,
`Dermatology, 194 (Supp. 1): 32-36 (1997) (“Summerbell”)
`
`“Ecology and epidemiology of dermatophyte infections.” Aly, R., J.
`Am. Acad. Dermatol., 31:S21–S25 (1994) (“Aly”)
`
`“Onychomycosis: therapeutic update.” Scher, R.K., Journal of the
`American Academy of Dermatology, 40 (Suppl):S21–6 (1999)
`(“Scher”)
`
`“New therapies for onychomycosis.” Odom, R. B., Journal of the
`American Academy of Dermatology, 35:3(2): S26-S30 (1996)
`(“Odom”)
`
`“Miconazole alcoholic solution in the treatment of mycotic nail
`infections.” Vanderdonckt, J., et al., Mykosen, 19(7):251-256 (1975)
`(“Vanderdonckt”)
`
`“Comparison of Two Topical Preparations for the Treatment of
`Onychomycosis: Melaleuca alternifolia (Tea Tree) Oil and
`Clotrimazole.” Buck, D.S. et al., The Journal of Family Practice,
`38(6): 601-605 (1994) (“Buck”)
`
`“Amorolfine- A Review of its Pharmacological Properties and
`Therapeutic Potential in the Treatment of Onychomycosis and Other
`Superficial Fungal Infections.” Haria, M. and Bryson, H.M., Drugs,
`49(1): 103-120 (1995) (“Haria”)
`
`“Measurement of water vapor loss through human nail in vivo.”
`Spruit, D., J Invest Dermatol, 56(5): 359-361 (1971) (“Spruit”)
`
`“Physicochemical characterization of the human nail: I. Pressure
`sealed apparatus for measuring nail plate permeabilities.” Walters,
`K.A., Flynn, G.L. and Marvel, J.R., J Invest Dermatol, 76: 76-79
`(1981) (“Walters 1981”)
`
`
`1031
`
`1032
`
`1033
`
`1034
`
`1035
`
`1036
`
`1037
`
`1038
`
`1039
`
`
`
`xii
`
`

`

`Patent No. 7,214,506
`Petition For Inter Partes Review
`
`
`
`1040
`
`“Physicochemical characterization of the human nail: Permeation
`pattern for water and the homologous alcohols and differences with
`respect to the stratum corneum.” Walters, K.A., Flynn, G.L. and
`Marvel, J.R., J Pharm Pharmacol 35: 28-33 (1983) (“Walters
`1983”)
`
`“Penetration of the human nail plate: the effects of vehicle pH on the
`permeation of miconazole.” Walters, K.A., Flynn, G.L. and Marvel,
`J.R., J Pharm Pharmacol, 37: 498-499 (1985) (“Walters 1985 I”)
`
`“Physicochemical characterization of the human nail: solvent effects
`on the permeation of homologous alcohols.” Walters, K.A., Flynn,
`G.L. and Marvel, J.R., J Pharm Pharmacol, 37: 771-775 (1985)
`(“Walters 1985 II”)
`
`Jublia® (efinaconazole) topical solution, 10% [package insert].
`Valeant Pharmaceuticals North America LLC; 5/2016.
`
`Declaration of Jeff Karr (“Karr Declaration”)
`
`Excerpt from the Acrux DDS Pty Ltd. Corporate Website, page
`entitled “About Acrux,” at http://www.acrux.com.au/about/, last
`accessed on October 27, 2016.
`
`Excerpt from the Acrux DDS Pty Ltd. Corporate Website, page
`entitled “Product Pipeline,” at http://www.acrux.com.au/what-we-
`do/research-development/product-pipeline/, last accessed on
`October 27, 2016.
`
`Declaration of Maurizio Del Poeta
`
`“Onychomycosis: Pathogenesis, Diagnosis, and Management,” by
`Elewski, B., Clinical Microbiology Reviews, 11:415-429 (1998)
`(“Elewski”)
`
`xiii
`
`1041
`
`1042
`
`1043
`
`1044
`
`1045
`
`1046
`
`1047
`
`1048
`
`
`
`
`
`

`

`Patent No. 7,214,506
`Petition For Inter Partes Review
`
`I.
`
`
`INTRODUCTION
`Argentum Pharmaceuticals LLC (“Petitioner”) requests that the Board
`
`institute inter partes review of and cancel claims 1-2 of U.S. Patent No. 7,214,506
`
`(“the ’506 patent”) (Ex. 1001), which is assigned to Kaken Pharmaceutical Co.,
`
`Ltd. (“Kaken”). Inter partes review of claims 1-2 of the ’506 patent was instituted
`
`in IPR2017-00190 on May 1, 2017, based on a petition filed by Acrux DDS Pty
`
`Ltd. and Acrux Limited (“Acrux IPR”). Petitioner hereby files its own Petition on
`
`the same grounds as those instituted in the Acrux IPR and concurrently seeks to
`
`join the instituted Acrux IPR proceeding (IPR2017-00190). A motion for joinder
`
`with IPR2017-00190 is being filed concurrently with this Petition.
`
`II. MANDATORY NOTICES (37 C.F.R. § 42.8(a)(1))
`A. Real Party-In-Interest Under 37 C.F.R. § 42.8(b)(1)
`The real parties-in-interest for this Petition are: Argentum Pharmaceuticals
`
`LLC; Intelligent Pharma Research LLC; APS GP LLC; and APS GP Investors
`
`LLC.
`
`B. Related Matters Under 37 C.F.R. § 42.8(b)(2)
`IPR2017-00190 (filed Nov. 2, 2016; instituted May 1, 2017) is the inter
`
`partes review to which this Petition seeks joinder.
`
`U.S. Patent Application No. 15/405,171 is currently pending in the Office as
`
`a reissue application of the ’506 patent, which Patent Owner filed on Jan. 12, 2017.
`
`
`
`1
`
`

`

`Patent No. 7,214,506
`Petition For Inter Partes Review
`
`
`
`C.
`
`Lead And Back-Up Counsel Under 37 C.F.R. § 42.8(b)(3)
`Lead Counsel
`Teresa Stanek Rea, Reg. No. 30,427
`Crowell & Moring LLP
`Intellectual Property Group
`1001 Pennsylvania Ave, NW
`Washington, DC 20004-2595
`(202) 624-2620
`TRea@Crowell.com
`Back-Up Counsel
`Shannon M. Lentz
`Reg. No. 65,382
`Crowell & Moring LLP
`Intellectual Property Group
`1001 Pennsylvania Ave, NW
`Washington, DC 20004-2595
`(202) 624-2897
`SLentz@Crowell.com
`
`Tyler C. Liu
`Reg. No. 72,126
`Argentum Pharmaceuticals, LLC
`(202) 749-8605
`TLiu@agpharm.com
`
`A Power of Attorney pursuant to 37 C.F.R. § 42.10(b) is filed herewith.
`
`D.
`Service Information Under 37 C.F.R. § 42.8(b)(4)
`Please direct all correspondence regarding this Petition to lead counsel at the
`
`above address. Petitioner consents to service by email at: TRea@Crowell.com and
`
`SLentz@Crowell.com and TLiu@agpharm.com.
`
`E.
`Service on Patent Owner Under 37 C.F.R. § 42.105(a) and 42.106(a)
`This petition is being served via FedEx® on counsel of record according to
`
`the USPTO PAIR database: Denis Polyn, Bausch & Lomb Incorporated, 1400
`
`North Goodman Street, Rochester, NY 14609.
`
`
`
`2
`
`

`

`Patent No. 7,214,506
`Petition For Inter Partes Review
`
`
`III. GROUNDS FOR STANDING (37 C.F.R. §§ 42.101 and 42.104)
`Petitioner hereby certifies that the patent for which review is sought is
`
`available for inter partes review, and that the Petitioner is not barred or estopped
`
`from requesting an inter partes review challenging the patent claims on the
`
`Grounds identified in the petition.
`
`IV. PAYMENT OF FEES (37 C.F.R. § 42.103)
`The Office is authorized to charge the required fee, and any fee deficiencies
`
`and credit overpayments to Deposit Acct. No. 05-1323, Customer ID No. 23911.
`
`V. A STATEMENT OF THE PRECISE RELIEF REQUESTED (§
`42.22(a)(1))
`Petitioner respectfully requests that the Board institute inter partes review
`
`(“IPR”) and cancel claims 1 and 2 of the ’506 patent (Ex. 1001) in light of the
`
`grounds presented herein.
`
`VI.
`
`IDENTIFICATION OF CHALLENGES (§ 42.104(b))
`Petitioner requests cancellation of claims 1 and 2 of the ’506 patent as
`
`unpatentable under 35 U.S.C. § 103(a)(Pre-AIA). The grounds of invalidity of
`
`claims 1 and 2 are summarized below:1
`
`
`1 The grounds listed herein are consistent with those presented in the Acrux IPR
`
`and on which the Board instituted IPR of the challenged claims. IPR2017-00190,
`
`Institution Decision, Paper 12 at page 25.
`
`
`
`3
`
`

`

`Patent No. 7,214,506
`Petition For Inter Partes Review
`
`
`
`Ground
`No.
`
`Claim
`Nos.
`
`1, 2
`
`Proposed Statutory Rejections for the Claims of the
`’506 patent
`Obvious under 35 U.S.C. § 103(a) over Japanese Pat. App.
`Pub. No. 10-226639 (“JP ’639”) (Ex. 1011) in view of
`Ogura (Ex. 1012).
`
`1, 2
`
`Obvious under 35 U.S.C. § 103(a) over U.S. Pat. No.
`5,391,367 (“the ’367 patent”) (Ex. 1013) in view of Ogura
`(Ex. 1012).
`1, 2 Obvious under 35 U.S.C. § 103(a) over Hay (Ex. 1014) in
`view of Ogura (Ex. 1012).
`1, 2 Obvious under 35 U.S.C. § 103(a) over JP ’639 (Ex. 1011)
`in view of the Kaken Abstracts (Ex. 1015).
`1, 2 Obvious under 35 U.S.C. § 103(a) over the ’367 patent (Ex.
`1013) in view of the Kaken Abstracts (Ex. 1015).
`1, 2 Obvious under 35 U.S.C. § 103(a) over Hay (Ex. 1014) in
`view of the Kaken Abstracts (Ex. 1015).
`
`1
`
`2
`
`3
`
`4
`
`5
`
`6
`
`Pursuant to 35 U.S.C. § 312(a)(3), a copy of every patent and printed
`
`publication on which Petitioner relies is submitted herewith as an Exhibit.
`
`In support of these grounds for unpatentability, Petitioner submits the expert
`
`declaration of Dr. Kenneth A. Walters (Ex.1005 (“Walters Declaration”), as well
`
`as the declaration of Dr. Maurizio Del Poeta, Ph.D., (Ex. 1047 (“Del Poeta
`
`Declaration”)) to discuss the relevant field and art in general, and the factual and
`
`opinion bases underlying Petitioner’s Grounds 1-6.2
`
`
`2 Petitioner is willing to work with Acrux and rely solely on Dr. Walters’
`
`
`
`4
`
`

`

`Patent No. 7,214,506
`Petition For Inter Partes Review
`
`
`VII. SUMMARY OF THE ’506 PATENT
`A. Overview
`The ’506 Patent was filed as U.S. Patent Application No. 10/685,266 (“’266
`
`application”) on October 14, 2003. The ’506 patent is a divisional of now-
`
`abandoned U.S. Patent Application No. 10/031,929 (“’929 application”). The ’929
`
`application was a national-stage entry of PCT/JP00/04617, filed on July 11, 2000.
`
`The ’506 patent and the ’929 application claim priority to Japanese Patent
`
`Application No. 11/214369 (“JP priority document”; Ex. 1002), filed on July 28,
`
`1999. The inventors named on the face of the ’506 patent are Yoshiyuki Tatsumi,
`
`Mamoru Yokoo, Kosho Nakamura, and Tadashi Arika. The ’506 patent is
`
`assigned on its face to Kaken and, based on publicly available information, is
`
`believed to be licensed to Valeant Pharmaceuticals International, Inc., and its
`
`subsidiary, Valeant Pharmaceuticals North America LLC, is the New Drug
`
`Application (“NDA”) holder (collectively, “Valeant”). (See Ex. 1003).
`
`
`declaration and testimony and will withdraw the expert declaration of Dr. Del
`
`Poeta upon agreement of Acrux to jointly rely on Dr. Walters. However, in the
`
`event that an agreement is not reached, Petitioner is prepared to rely on the
`
`declaration and testimony of Dr. Del Poeta. This position is more explicitly
`
`explained in the concurrently filed Motion for Joinder.
`
`
`
`5
`
`

`

`Patent No. 7,214,506
`Petition For Inter Partes Review
`
`
`
`The ‘506 patent is listed in the FDA’s “Approved Drug Products with
`
`Therapeutic Equivalence Evaluations” (“Orange Book”) as covering Valeant’s
`
`Jublia® product. (See Ex. 1004).
`
`B.
`The ’506 Patent
`The ’506 patent (Ex. 1001) is entitled “Method for Treating
`
`Onychomycosis.” Onychomycosis, also referred to as tinea unguium, is one type
`
`of superficial mycosis affecting humans and animals. (Id., 9:32-25.)3 See also Ex.
`
`1005, ¶41; Ex. 1047, ¶41. Onychomycosis is a disease of the nail and is
`
`characterized by symptoms such as opacity, tylosis (thickening), and destruction
`
`and deformation of the nail plate. (Ex. 1001, 2:21-25.) Tinea unguium can form in
`
`the nail and is a type of dermatophytosis. (Id.) In humans, onychomycosis is
`
`caused mainly by the microorganism species Trichophyton rubrum and
`
`Trichophyton mentagrophytes. (Id., 9:36-37.) See also Ex. 1005, ¶41; Ex. 1047,
`
`¶41. Onychomycosis can also be caused by C. albicans, a nondermatophyte. (Ex.
`
`1047, ¶41.) Thus, a desirable antifungal drug for the treatment of onychomycosis
`
`is one that is effective against both dermatophytes and nondermatophytes. Id.
`
`The ’506 patent defines the term “nail” as including “nail plate, nail bed, nail
`
`
`3 Citations to patents herein will be presented as “x:y,” where x represents the
`
`column number and y represents the line number.
`
`
`
`6
`
`

`

`Patent No. 7,214,506
`Petition For Inter Partes Review
`
`
`matrix, further side nail wall, posterial nail wall, eponychium and hyponychium
`
`which make up a tissue around thereof.” (Ex. 1001, 4:65-67; Ex. 1005, ¶49; Ex.
`
`1047, ¶49.) It was known at the time of the filing of the ’506 patent that the most
`
`common form of onychomycosis “begin[s] at the hyponychium.” (Ex. 1047, ¶103;
`
`Ex. 1048, 417.)
`
`The ’506 patent explains that oral treatments for tinea unguium existed at the
`
`time of the invention but that “there are many cases where the patient stops taking
`
`the drug or that takes the drug irregularly, since they have to take the drug for a
`
`long period . . . in order to completely cure tinea unguium. It is thought that this is
`
`a main cause of difficulty of curing tinea unguium completely.” (Id., 2:27-32.)
`
`Accordingly, the ’506 patent explains that a topical preparation is more desirable
`
`because it would improve patient compliance and have less systemic side effects
`
`than the oral preparation. (Id., 2:36-39.) See also Ex. 1005, ¶43; Ex. 1047, ¶43.
`
` The ’506 patent notes that “the simple application on [the] nail plate” of an
`
`existing antifungal agent for topical use did not display an antifungal effect in the
`
`nail because these agents “could not sufficiently permeate the thick keratin” in the
`
`nail plate. (Ex. 1001, 2:40-45.) Accordingly, it was an object of the ’506 patent to
`
`provide a therapeutic topical agent, which exhibits an effect on tinea unguium and
`
`has “good per