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`Case 1:18-cv-00202-IMK Document 1-1 Filed 10/30/18 Page 1 of 240 PageID #: 16
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`EXHIBIT A
`EXHIBIT A
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`Case 1:18-cv-00202-IMK Document 1-1 Filed 10/30/18 Page 2 of 240 PageID #: 17
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`11111111111111111111111111101111M1j111111101111111111
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`(10) Patent No.: (cid:9)
`(45) Date of Patent: (cid:9)
`
`US 9,549,938 B2
`*Jan. 24, 2017
`
`(12) United States Patent (cid:9)
`Baker et al. (cid:9)
`
`(54)
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`(71)
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`(72)
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`BORON-CONTAINING SMALL MOLECULES
`
`Applicant: Anacor Pharmaceuticals, Inc., Palo
`Alto, CA (US)
`
`Inventors: Stephen J. Baker, Collegeville, PA
`(US); Tsutomu Akama, Sunnyvale, CA
`(US); Vincent S. Hernandez,
`Watsonville, CA (US); Karin M. Hold,
`Belmont, CA (US); Kirk Maples. San
`Jose, CA (US): Jacob J. Plattner,
`Berkeley, CA (US); Virginia Sanders,
`San Francisco, CA (US); Yong-Kang
`Zhang, San Jose, CA (US); Gregory T.
`Fieldson, Morgantown, WV (US);
`James J. Leyden, Malvern, CA (US)
`
`(73)
`
`Assignee: (cid:9) Anacor Pharmaceuticals, Inc., Palo
`Alto, CA (US)
`
`CO7F 5/04 (cid:9)
`CO7H 19/06 (cid:9)
`CO7H 19/16 (cid:9)
`CO7H 21/00 (cid:9)
`CO7H 23/00 (cid:9)
`A6IK 31/70 (cid:9)
`A61K 31/7076 (cid:9)
`A6IK 9/00 (cid:9)
`A6IK 47/10 (cid:9)
`A6IK 9/08 (cid:9)
`U.S. Cl.
`CPC (cid:9)
`
`(52)
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`(2006.01)
`(2006.01)
`(2006.01)
`(2006.01)
`(2006.01)
`(2006.01)
`(2006.01)
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`(2006.01)
`(2006.01)
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` A6IK 31/69 (2013.01); A61K 9/0012
`(2013.01); A61K 9/08 (2013.01); A6IK 31/70
`(2013.01); A61K 31/7076 (2013.01); A6IK
`47/10 (2013.01); CO7F 5/025 (2013.01); CO7F
`5/04 (2013.01); CO7H 19/06 (2013.01); C0711
`19/16 (2013.01); CO7H 21/00 (2013.01);
`CO7H 23/00 (2013.01)
`Field of Classification Search
` 514/64
`USPC (cid:9)
`See application file for complete search history.
`
`( )
`
`Notice: (cid:9)
`
`Subject to any disclaimer, the term of this
`patent is extended or adjusted under 35
`U.S.C. 154(b) by 0 days.
`
`(58)
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`This patent is subject to a terminal dis-
`claimer.
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`(56)
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`References Cited
`
`
`
`
`
`Appl. No.: 15/068,352
`
`Filed: (cid:9)
`
`Mar. 11, 2016
`
`(60)
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`(65)
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`Prior Publication Data
`Jun. 30, 2016
`US 2016/0184334 Al (cid:9)
`Related U.S. Application Data
`Continuation of application No. 15/046,322, filed on
`Feb. 17, 2016, which is a continuation of application
`No. 14/537,771, filed on Nov. 10, 2014, which is a
`continuation of application No. 14/201,459, filed on
`Mar. 7, 2014, now Pat. No. 9,353,133, which is a
`continuation of application No. 13/356,488, filed on
`Jan. 23, 2012, now Pat. No. 8,722,917, which is a
`continuation of application No. 12/629,753, filed on
`Dec. 2, 2009, now Pat. No. 8,115,026, which is a
`division of application No. 11/505,591, filed on Aug.
`16, 2006, now Pat. No. 7,767,657, which is a
`continuation-in-part of application No. 11/357,687,
`filed on Feb. 16, 2006, now Pat. No. 7,582,621,
`application No. 15/068,352, filed on Mar. 11, 2016,
`which is a continuation-in-part of application No.
`13/874,329, filed on Apr. 30, 2013, now Pat. No.
`8,889,656, which is a continuation of application No.
`13/224,252, filed on Sep. 1, 2011, now Pat. No.
`8,440,642, which is a continuation of application No.
`12/507,010, filed on Jul. 21, 2009, now Pat. No.
`8,039,451, which is a continuation of application No.
`11/357,687.
`(60) Provisional application No. 60/654,060, filed on Feb.
`16, 2005, provisional application No. 60/755,227,
`(Continued)
`
`(51) Int. Cl.
`A6IK 31/69
`CO7F 5/02
`
`(2006.01)
`(2006.01)
`
`U.S. PATENT DOCUMENTS
`
`2,260,336 A
`2,741,548 A
`2.831,866 A
`
`10/1941 Prescott et al.
`4/1956 Darling et al.
`4/1958 Freeman et al.
`(Continued)
`
`FOREIGN PATENT DOCUMENTS
`
`EP
`EP
`
`1/2000
`0969531 (cid:9)
`8/2000
`0765331 81 (cid:9)
`(Continued)
`
`OTHER PUBLICATIONS
`
`U.S. Appl. No. 13/673,860, filed Nov. 9, 2012, Anacor Phamiaceu-
`ticals, Inc.
`
`(Continued)
`
`Primary Examiner— Rei-Tsang Shiao
`(74) Attorney, Agent, or Firm — Morgan, Lewis &
`Bockius LLP
`
`(57) (cid:9)
`
`ABSTRACT
`
`This invention relates to compounds useful for treating
`fungal infections, more specifically topical treatment of
`onychomycosis and/or cutaneous fungal infections. This
`invention is directed to compounds that are active against
`fungi and have properties that allow the compound, when
`placed in contact with a patient, to reach the particular part
`of the skin, nail, hair, claw or hoof infected by the fungus.
`In particular the present compounds have physiochemical
`properties that facilitate penetration of the nail plate.
`
`6 Claims, 63 Drawing Sheets
`
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`

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`Case 1:18-cv-00202-IMK Document 1-1 Filed 10/30/18 Page 3 of 240 PageID #: 18
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`US 9,549,938 B2
`Page 2
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`Related U.S. Application Data (cid:9)
`
`filed on Dec. 30, 2005, provisional application No. (cid:9)
`60/746,361, filed on May 3, 2006. (cid:9)
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