UNITED STATES PATENT AND TRADEMARK OFFICE
`_______________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`_______________
`
`ACRUX DDS PTY LTD. & ACRUX LIMITED
`Petitioners
`
`v.
`
`KAKEN PHARMACEUTICAL CO., LTD. and
`VALEANT PHARMACEUTICALS INTERNATIONAL, INC.
`Patent Owner and Licensee
`_______________
`
`Patent No. 7,214,506
`Issue Date: May 8, 2007
`Title: Method for Treating Onychomycosis
`_______________
`
`
`
`PETITION
`to Institute an Inter Partes Review of
`U.S. Patent No. 7,214,506
`Under
`35 U.S.C. §§ 311-319 and
`37 C.F.R. § 42.100 et seq.
`
`
`
`Mail Stop PATENT BOARD
`Patent Trial and Appeal Board
`United States Patent and Trademark Office
`PO Box 1450
`Alexandria, Virginia 22313–1450
`Submitted Electronically via the Patent Review Processing System
`
` 
`
` 
`
`

`
`TABLE OF CONTENTS
`
`TABLE OF AUTHORITIES ................................................................................... vi 
`
`EXHIBIT LIST ........................................................................................................ ix 
`
`I. 
`
`A STATEMENT OF THE PRECISE RELIEF REQUESTED
`(§ 42.22(a)(1)) .................................................................................................. 1 
`
`II. 
`
`GROUNDS FOR STANDING (§ 42.104(a)) ................................................. 1 
`
`III.  MANDATORY NOTICES ............................................................................. 2 
`
`IV.  PAYMENT OF FEES (37 C.F.R. § 42.103) ................................................... 3 
`
`V. 
`
`IDENTIFICATION OF CHALLENGES (§ 42.104(b)) ................................. 3 
`
`VI.  SUMMARY OF THE ’506 PATENT ............................................................. 5 
`
`A.  Overview ............................................................................................... 5 
`
`B. 
`
`C. 
`
`D. 
`
`The ’506 Patent ..................................................................................... 5 
`
`Prosecution History ............................................................................... 9 
`
`Challenged Claims of the ’506 Patent ................................................. 13 
`
`VII.  EFFECTIVE FILING DATE OF THE CHALLENGED CLAIMS ............. 14 
`
`A. 
`
`B. 
`
`The JP Priority Document Does Not Support Treating a Subject
`Having Onychomycosis ...................................................................... 16 
`
`The JP Priority Document Does Not Disclose “topically
`administering to a nail of said subject having onychomycosis a
`therapeutically effective amount of an antifungal compound
`represented by the [chemical formula].” ............................................. 18 
`
`C. 
`
`The First Disclosure of the Claimed Elements was July 11, 2000 ..... 19 
`
`VIII.  APPLICABLE LAW AND LEVEL OF SKILL IN THE ART .................... 20 
`
`IX.  CLAIM-BY-CLAIM EXPLANATION OF GROUNDS FOR
`UNPATENTABILITY .................................................................................. 21 
`
` 
`
` 
`
`

`
`Acrux’s Petition for IPR of U.S. Patent No. 7,214,506
`
`A.  Ground 1: The Methods of Claims 1 and 2 of the ’506 Patent
`Would Have Been Obvious Over Japanese Pat. App. Pub. No. 10-
`226639 in View of Ogura. ................................................................... 21 
`
`i. 
`
`ii. 
`
`iii. 
`
`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” ............................................................... 22 
`
`Ogura Discloses the Antifungal Activities of Azolylamine
`Compounds Including KP-103, i.e. a Compound Falling
`Within the Scope of the Claims ................................................ 24 
`
`It Would Have Been Obvious to One of Ordinary Skill in
`the Art to Combine JP ’639 and Ogura to Arrive at the
`Method Recited in Claims 1 and 2. ........................................... 25 
`
`B. 
`
`Ground 2: The Methods of Claims 1 and 2 of the ’506 Patent
`Would Have Been Obvious Over U.S. Pat. No. 5,391,367 in View
`of Ogura ............................................................................................... 30 
`
`i. 
`
`ii. 
`
`iii. 
`
`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” ............................................................... 30 
`
`Ogura Discloses the Antifungal Activities of Azolylamine
`Compounds Including KP-103, i.e. a Compound Falling
`Within the Scope of the Claims ................................................ 31 
`
`It Would Have Been Obvious to One of Ordinary Skill in
`the Art to Combine the Teachings of the ’367 Patent and
`Ogura to Arrive at the Methods Recited in Claims 1 and 2. .... 32 
`
`C. 
`
`Ground 3: The Methods of Claims 1 and 2 of the ’506 Patent
`Would Have Been Obvious Over Hay in View of Ogura ................... 35 
`
`i. 
`
`Hay Teaches “a method for treating a subject having
`onychomycosis wherein the method comprises topically
`administering to a nail of said subject having
`
` 
`
`ii
`
`

`
`Acrux’s Petition for IPR of U.S. Patent No. 7,214,506
`
`onychomycosis a therapeutically effective amount of an
`antifungal compound” ............................................................... 35 
`
`Ogura Discloses the Antifungal Activities of Azolylamine
`Compounds Including KP-103, i.e. a Compound Falling
`Within the Scope of the Claims ................................................ 36 
`
`It Would Have Been Obvious to One of Ordinary Skill in
`the Art to Combine Hay and Ogura to Arrive at the
`Methods Recited in Claims 1 and 2. ......................................... 36 
`
`ii. 
`
`iii. 
`
`D.  Ground 4: The Methods of Claims 1 and 2 of the ’506 Patent
`Would Have Been Obvious Over JP ’639 in View of the Kaken
`Abstracts .............................................................................................. 40 
`
`i. 
`
`ii. 
`
`iii. 
`
`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” ............................................................... 41 
`
`The Kaken Abstracts Disclose the Antifungal Activities of
`KP-103, i.e. a Compound Falling Within the Scope of the
`Claims ....................................................................................... 41 
`
`It Would Have Been Obvious to One of Ordinary Skill in
`the Art to Combine the Teachings of JP ’639 and the Kaken
`Abstracts to Arrive at the Method Recited in Claims 1 and
`2. ................................................................................................ 43 
`
`E. 
`
`Ground 5: The Methods of Claims 1 and 2 of the ’506 Patent
`Would Have Been Obvious Over the ’367 Patent in View of the
`Kaken Abstracts. ................................................................................. 47 
`
`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” ............................................................... 47 
`
` 
`
`iii
`
`

`
`Acrux’s Petition for IPR of U.S. Patent No. 7,214,506
`
`ii. 
`
`iii. 
`
`The Kaken Abstracts Disclose the Antifungal Activities of
`KP-103, i.e. a Compound Falling Within the Scope of the
`Claims ....................................................................................... 47 
`
`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 to Arrive at the Methods Recited in Claims
`1 and 2. ...................................................................................... 48 
`
`F. 
`
`Ground 6: The Methods of Claims 1 and 2 of the ’506 Patent
`Would Have Been Obvious over Hay in View of the Kaken
`Abstracts. ............................................................................................. 51 
`
`i. 
`
`ii. 
`
`iii. 
`
`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” ............................................................... 51 
`
`The Kaken Abstracts Disclose the Antifungal Activities of
`KP-103, i.e. a Compound Falling Within the Scope of the
`Claims ....................................................................................... 51 
`
`It Would Have Been Obvious to One of Ordinary Skill in
`the Art to Combine the Teachings of Hay and the Kaken
`Abstracts to Arrive at the Methods Recited in Claims 1 and
`2. ................................................................................................ 52 
`
`X.  GIVEN THE OVERWHELMINGLY STRONG OBVIOUSNESS
`CASE, ANY EVIDENCE PATENTEE AND LICENSEE MAY
`OFFER RELATING TO SECONDARY CONSIDERATIONS IS NOT
`ADEQUATE TO OVERCOME THE FINDING THAT THE
`ASSERTED CLAIMS OF THE ‘506 PATENT WOULD HAVE
`BEEN OBVIOUS AS A MATTER OF LAW .............................................. 55 
`
`A. 
`
`The Alleged Unexpected Results of the Invention are Insufficient
`to Overcome the Strong Case of Obviousness Presented Herein ....... 57 
`
`i. 
`
`The Alleged Unexpected Results Argued by Patentee
`During Prosecution were Actually Known Beneficial
`Results of the Use of KP-103 in the Treatment of
`Onychomycosis. ........................................................................ 57 
`iv
`
` 
`
`

`
`Acrux’s Petition for IPR of U.S. Patent No. 7,214,506
`
`ii. 
`
`iii. 
`
`The Data Presented in the ’506 Specification is Flawed and
`Does Not Provide Evidence of an Unexpected Effect
`Because There is No Evidence that the Tested Drugs are
`Equipotent. ................................................................................ 60 
`
`The ’506 Patent Specification Demonstrates that the
`Claimed Compounds do not Eradicate the Infection as
`Claimed by Patentees. ............................................................... 61 
`
`B. 
`
`Any Alleged Commercial Success of Valeant’s Jublia® Product is
`Insufficient to Overcome the Strong Case of Obviousness
`Presented Herein .................................................................................. 62 
`
`XI.  CONCLUSION .............................................................................................. 63 
`
`
`
`v
`
`   
`
` 
`
`

`
`Acrux’s Petition for IPR of U.S. Patent No. 7,214,506
`
`TABLE OF AUTHORITIES
`
`Cases 
`Allergan, Inc. v. Apotex Inc.,
`754 F.3d 952 (Fed. Cir. 2014) .............................................................................. 56
`
`Cohesive Techs., Inc. v. Waters Corp.,
`543 F.3d 1351 (Fed. Cir. 2008) ............................................................................ 13
`
`Cubist Pharms., Inc. v. Hospira, Inc.,
`75 F. Supp. 3d 641 (D. Del. 2014), aff'd,
`805 F.3d 1112 (Fed. Cir. 2015), cert. denied,
`136 S. Ct. 2393 (2016) .......................................................................................... 55
`
`Graham v. John Deere Co. of Kansas City,
`383 U.S. 1 (1966) .................................................................................................. 20
`
`Honeywell Int’l, Inc. v. United States,
`609 F. 3d 1292 (Fed. Cir. 2010) ........................................................................... 20
`
`Hyatt v. Dudas,
`492 F.3d 1365 (Fed. Cir. 2007) ............................................................................ 15
`
`In re Chu,
`66 F.3d 292 (Fed. Cir. 1995) ................................................................................ 15
`
`In re Gershon,
`372 F.2d 535 (C.C.P.A. 1967) .............................................................................. 60
`
`In re Kao,
`639 F.3d 1057 (Fed. Cir. 2011) ..................................................................... 55, 62
`
`In re NTP, Inc.,
`654 F.3d 1268 (Fed. Cir. 2011) ............................................................................ 15
`
`In re Skoll,
`523 F.2d 1392 (C.C.P.A. 1975) ............................................................................ 60
`
`King Pharms., Inc. v. Eon Labs, Inc.,
`616 F.3d 1267 (Fed. Cir. 2010) ............................................................................ 62
`
` 
`
`vi
`
`

`
`Acrux’s Petition for IPR of U.S. Patent No. 7,214,506
`
`Lockwood v. Am. Airlines, Inc.,
`107 F.3d 1565 (Fed. Cir. 1997) ............................................................................ 15
`
`Media Techs. Licensing, LLC v. Upper Deck Co.,
`596 F.3d 1334 (Fed. Cir. 2010) ............................................................................ 62
`
`Pfizer, Inc. v. Apotex, Inc.,
` 480 F.3d 1348 (Fed. Cir. 2007) .................................................................... 55, 56
`
`Ruiz v. A.B. Chance Co.,
`234 F. 3d 654 (Fed. Cir. 2000) ............................................................................. 25
`
`Vas–Cath Inc. v. Mahurkar,
`935 F.2d 1555 (Fed. Cir. 1991) ............................................................................ 15
`
`Western Union Co. v. MoneyGram Payment Sys.,
`626 F.3d 1361 (Fed. Cir. 2010) ............................................................................ 55
`
`Statutes 
`
`35 U.S.C. § 102(a) ................................................................................................... 22
`
`35 U.S.C. § 102(b) ........................................................................................... passim
`
`35 U.S.C. § 103(a) ........................................................................................... passim
`
`35 U.S.C. § 112 ................................................................................................. 15, 16
`
`35 U.S.C. § 312(a)(1) ................................................................................................. 3
`
`35 U.S.C. § 312(a)(3) ................................................................................................. 4
`
`Regulations 
`
`37 C.F.R. § 42.10(b) .................................................................................................. 3
`
`37 C.F.R. § 42.100 ..................................................................................................... 1
`
`37 C.F.R. § 42.101 ..................................................................................................... 1
`
`37 C.F.R. § 42.101(a) ................................................................................................. 1
`
`37 C.F.R. § 42.101(b) ................................................................................................ 1
`
`37 C.F.R. § 42.101(c) ................................................................................................. 1
`vii
`
` 
`
`

`
`Acrux’s Petition for IPR of U.S. Patent No. 7,214,506
`
`37 C.F.R. § 42.103 ..................................................................................................... 3
`
`37 C.F.R. § 42.104(a) ................................................................................................. 1
`
`37 C.F.R. § 42.104(b) ................................................................................................ 3
`
`37 C.F.R. § 42.8(b)(1) ................................................................................................ 2
`
`37 C.F.R. § 42.8(b)(2) ................................................................................................ 2
`
`37 C.F.R. § 42.8(b)(3) ................................................................................................ 2
`
`37 C.F.R. § 42.8(b)(4) ................................................................................................ 3
`
`
`
`viii
`
`
`
` 
`
`

`
`Acrux’s Petition for IPR of U.S. Patent No. 7,214,506
`
`EXHIBIT LIST
`
`DESCRIPTION
`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 ad Topical Antifungal
`Agents.” Ogura, H. et al., Chem. Pharm. Bull, 47(10) 1417-1425
`(1999) (“Ogura”)
`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”)
`
`EXHIBIT
`1001
`1002
`
`1003
`
`1004
`
`1005
`1006
`1007
`1008
`1009
`
`1010
`1011
`
`1012
`
`1013
`1014
`
`1015
`
`1016
`
` 
`
`ix
`
`

`
`EXHIBIT
`1017
`
`1018
`
`1019
`
`1020
`
`1021
`
`1022
`
`1023
`
`1024
`
`1025
`
`1026
`
`Acrux’s Petition for IPR of U.S. Patent No. 7,214,506
`
`DESCRIPTION
`“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”)
`“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”)
`
` 
`
`x
`
`

`
`EXHIBIT
`1027
`
`1028
`
`1029
`
`1030
`
`1031
`
`1032
`
`1033
`
`1034
`
`1035
`
`1036
`
`1037
`
`1038
`
`1039
`
`Acrux’s Petition for IPR of U.S. Patent No. 7,214,506
`
`DESCRIPTION
`“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”)
`“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”)
`
` 
`
`xi
`
`

`
`EXHIBIT
`1040
`
`1041
`
`1042
`
`1043
`
`1044
`1045
`
`1046
`
`Acrux’s Petition for IPR of U.S. Patent No. 7,214,506
`
`DESCRIPTION
`“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: 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.
`
`xii
`
`
`
` 
`
`

`
`Acrux’s Petition for IPR of U.S. Patent No. 7,214,506
`
`I.
`
`A STATEMENT OF THE PRECISE RELIEF REQUESTED
`(§ 42.22(a)(1))
`
`Petitioners, Acrux DDS Pty Ltd. and Acrux Limited, (“Acrux” or
`
`“Petitioners”), respectfully request that the United States Patent and Trademark
`
`Office (“USPTO”) institute inter partes review (“IPR”) under 35 U.S.C. §§ 311–
`
`319 and 37 C.F.R. §§ 42.100 et seq., and cancel claims 1 and 2 of U.S. Patent No.
`
`7,214,506 (“the ’506 patent”) (Ex. 1001), assigned to Kaken Pharmaceutical Co.,
`
`Ltd. (“Kaken”), as invalid under 35 U.S.C. § 103(a)(pre-AIA) in light of the
`
`grounds presented herein.
`
`II. GROUNDS FOR STANDING (§ 42.104(a))
`Petitioners hereby certify that the ’506 patent for which review is sought is
`
`available for IPR. Specifically: (1) neither Petitioner is an owner of the ’506 patent,
`
`see § 42.101; (2) before the date on which this Petition for review was filed, the
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`Petitioners, who are the only real parties-in-interest, have not filed a civil action
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`challenging the validity of a claim of the ’506 patent, see § 42.101(a); (3)
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`Petitioners requesting this proceeding have not filed this Petition more than one
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`year after the date on which at least one of the Petitioners, Petitioners’ real party-
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`in-interest, or a privy of Petitioners was served with a complaint alleging
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`infringement of the ’506 patent, see § 42.101(b); and (4) neither of the Petitioners,
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`who are the only real parties-in-interest, nor a privy of Petitioners is estopped from
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`challenging the claims on the grounds identified in this petition, see § 42.101(c).
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` 
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`1
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`

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`Acrux’s Petition for IPR of U.S. Patent No. 7,214,506
`
`Acrux DDS Pty Ltd. (“Acrux DDS”), a subsidiary of Acrux Limited, is a
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`pharmaceutical company dedicated to developing and commercializing specialty
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`and generic topical pharmaceuticals. See Ex. 1045. Acrux DDS has successfully
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`developed and commercialized a number of pharmaceutical products and is
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`currently developing an antifungal
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`formulation
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`for
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`the
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`treatment of
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`onychomycosis, which is in the same technical field as the alleged inventions
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`claimed in the ’506 patent. See Ex. 1046.
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`III. MANDATORY NOTICES
`Pursuant to 37 C.F.R. § 42.8(b)(1), Petitioners are the only real parties-in-
`
`interest for this Petition.
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`Pursuant to 37 C.F.R. § 42.8(b)(2), there are no other judicial or
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`administrative matters that would likely affect, or be affected by, a decision in this
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`proceeding.
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`Pursuant to 37 C.F.R. § 42.8(b)(3), Petitioners provide the following
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`designation of counsel:
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`Lead Counsel:
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`
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`E. Anthony Figg (Reg. No. 27,195)
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`Back-up Counsel:
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`Aydin H. Harston (Reg. No. 65,249)
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`Electronic Service:
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`efigg@rothwellfigg.com; aharston@rothwellfigg.com;
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`litigationparalegals@rothwellfigg.com
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` 
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`2
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`

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`Acrux’s Petition for IPR of U.S. Patent No. 7,214,506
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`Post and Delivery:
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`ROTHWELL, FIGG, ERNST & MANBECK, P.C., 607
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`14th Street, N.W., Suite 800, Washington, DC 20005
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`Telephone:
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`Facsimile:
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`202-783-6040
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`202-783-6031
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`Pursuant to 37 C.F.R. § 42.8(b)(4), papers concerning this matter should be
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`served on both E. Anthony Figg and Aydin H. Harston as identified above, and as
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`appropriate to the foregoing mailing/email addresses.
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`A power of attorney is filed herewith according to 37 C.F.R. § 42.10(b).
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`IV. PAYMENT OF FEES (37 C.F.R. § 42.103)
`Pursuant to 35 U.S.C. § 312(a)(1) and 37 C.F.R. § 42.103, the required IPR
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`request and post-institution fees are authorized for payment from Deposit Account
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`No. 02-2135. If additional fees are due or if an overpayment has been made, the
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`Commissioner is authorized to deduct or credit the correct amount to Deposit
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`Account No. 02-2135.
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`V.
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`IDENTIFICATION OF CHALLENGES (§ 42.104(b))
`Petitioners request inter partes review and cancellation of claims 1 and 2 of
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`the ’506 Patent as unpatentable under 35 U.S.C. § 103(a)(Pre-AIA). The grounds
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`of invalidity of claims 1 and 2 are summarized below:
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`3
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`Acrux’s Petition for IPR of U.S. Patent No. 7,214,506
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`Ground
`No.
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`1
`
`Claim
`Nos.
`1, 2
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`Proposed Statutory Rejections for the Claims of the
`’506 patent
`Obvious under 35 U.S.C. § 103(a) over Japanese Pat. App.
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`Pub. No. 10-226639 (“JP ’639”) (Ex. 1011) in view of
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`Ogura (Ex. 1012).
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`1, 2
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`Obvious under 35 U.S.C. § 103(a) over U.S. Pat. No.
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`5,391,367 (“the ’367 patent”) (Ex. 1013) in view of Ogura
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`(Ex. 1012).
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`1, 2
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`Obvious under 35 U.S.C. § 103(a) over Hay (Ex. 1014) in
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`view of Ogura (Ex. 1012).
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`1, 2
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`Obvious under 35 U.S.C. § 103(a) over JP ’639 (Ex. 1011)
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`in view of the Kaken Abstracts (Ex. 1015).
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`1, 2
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`Obvious under 35 U.S.C. § 103(a) over the ’367 patent (Ex.
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`1013) in view of the Kaken Abstracts (Ex. 1015).
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`1, 2
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`Obvious under 35 U.S.C. § 103(a) over Hay (Ex. 1014) in
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`view of the Kaken Abstracts (Ex. 1015).
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`2
`
`3
`
`4
`
`5
`
`6
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`Pursuant to 35 U.S.C. § 312(a)(3), a copy of every patent and printed
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`publication on which Petitioners rely is submitted herewith as an Exhibit.
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` 
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`4
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`Acrux’s Petition for IPR of U.S. Patent No. 7,214,506
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`VI. SUMMARY OF THE ’506 PATENT
`A. Overview
`The ’506 Patent was filed as U.S. Patent Application No. 10/685,266 (“’266
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`application”) on October 14, 2003. The ’506 patent is a divisional of now-
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`abandoned U.S. Patent Application No. 10/031,929 (“’929 application”). The ’929
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`application was a national-stage entry of PCT/JP00/04617, filed on July 11, 2000.
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`The ’506 patent and the ’929 application claim priority to Japanese Patent
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`Application No. 11/214369 (“JP priority document”; Ex. 1002), filed on July 28,
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`1999. The inventors named on the face of the ’506 patent are Yoshiyuki Tatsumi,
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`Mamoru Yokoo, Kosho Nakamura, and Tadashi Arika. The ’506 patent is
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`assigned on its face to Kaken and, based on publicly available information, is
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`believed to be licensed to Valeant Pharmaceuticals International, Inc., and its
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`subsidiary, Valeant Pharmaceuticals North America LLC, is the New Drug
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`Application (“NDA”) holder (collectively, “Valeant”). (See Ex. 1003).
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`The ‘506 patent is listed in the FDA’s “Approved Drug Products with
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`Therapeutic Equivalence Evaluations” (“Orange Book”) as covering Valeant’s
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`Jublia® product. (See Ex. 1004).
`
`B.
`The
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`The ’506 Patent
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`’506 patent
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`(Ex. 1001)
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`is entitled “Method
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`for Treating
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`Onychomycosis.” Onychomycosis, also referred to as tinea unguium, is one type
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`5
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`Acrux’s Petition for IPR of U.S. Patent No. 7,214,506
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`of superficial mycosis affecting humans and animals. (Id. at 9:32-25.)1 See also
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`Ex. 1005, at ¶41. Onychomycosis is a disease of the nail and is characterized by
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`symptoms such as opacity, tylosis (thickening), and destruction and deformation of
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`the nail plate. (Ex. 1001 at 2:21-25.) Tinea unguium can form in the nail and is a
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`type of dermatophytosis. (Id.) In humans, onychomycosis is caused mainly by the
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`microorganism species Trichophyton rubrum and Trichophyton mentagrophytes.
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`(Id. at 9:36-37.) See also Ex. 1005, at ¶41.
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`The ’506 patent defines the term “nail” as including “nail plate, nail bed, nail
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`matrix, further side nail wall, posterial nail wall, eponychium and hyponychium
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`which make up a tissue around thereof.” (Ex. 1001 at 4:65-67; Ex. 1005, at ¶42.)
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`The ’506 patent explains that oral treatments for tinea unguium existed at the
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`time of the invention but that “there are many cases where the patient stops taking
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`the drug or that takes the drug irregularly, since they have to take the drug for a
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`long period . . . in order to completely cure tinea unguium. It is thought that this is
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`a main cause of difficulty of curing tinea unguium completely.” (Id. at 2:27-32.)
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`Accordingly, the ’506 patent explains that a topical preparation is more desirable
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`because it would improve patient compliance and have less systemic side effects
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`than the oral preparation. (Id. at 2:36-39.) See also Ex. 1005, at ¶43.
`                                                            
`1 Citations to patents herein will be presented as “x:y,” where x represents the
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`column number and y represents the line number.
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` 
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`6
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`Acrux’s Petition for IPR of U.S. Patent No. 7,214,506
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`The ’506 patent notes that “simple application on nail plate” of an existing
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`antifungal agent for topical use did not display an antifungal effect in the nail
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`because these agents “could not sufficiently permeate the thick keratin” in the nail
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`plate. (Ex. 1001, at 2:40-45.) Accordingly, it was an object of the ’506 patent to
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`provide a therapeutic topical agent, which exhibits an effect on tinea unguium and
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`has “good permeability, good retention capacity and conservation of high activity
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`in nail