(12) Unlted States Patent
`(10) Patent N0.:
`US 8,183,274 B2
`
`Sawyers et a1.
`(45) Date of Patent:
`May 22, 2012
`
`USOO8183274B2
`
`(54) TREATMENT OF HYPERPROLIFERATIVE
`4
`v
`v
`DISORDERS \‘NITH DIARYLHYDANTOIN
`COMPOUNDS
`
`(75)
`
`Inventors: Charles L. Sawyers, New York, NY
`.
`-
`.
`.
`y
`,
`(CUASL
`gng’leSAlngelfb’.
`(U )s W 19
`-
`lens mg 13“
`(CN); Samedy 011k, Costa Mesa, CA
`(US); Chris Tran, New York, NY (US);
`-
`JOh“ wongV‘Pat’ Nanuet’ NY (Us)
`_
`_
`.
`(73) Ass1gnee: The Regents of the Unlvers1ty of
`California, Oakland, CA (US)
`
`:1:
`
`.
`-
`) Not1ce.
`
`(
`
`-
`-
`-
`-
`Subject. to any d1scla1mer, the term ofth1s
`patent 1s extended or adjusted under 35
`U.S.C. 154(b) by 0 days.
`
`(21) App] NO. 12/708 523
`’
`"
`’
`.
`a” Ffid
`
`R91&2m°
`
`(65)
`
`Prior Publication Data
`
`118 2010/0172975281
`
`Jul.8.2010
`
`Related US. Application Data
`
`(62) Division of application No. 11/433,829, filed on May
`15, 2006, now Pat. No. 7,709,517.
`
`(60)
`
`Provisional application No. 60/680,835, filed on May
`13, 2005, provisional application No. 60/750,351,
`filed on Dec. 15, 2005, provisional application No.
`60/756,552,
`filed on Jan.
`6, 2006, provisional
`application No. 60/786,837, filed on Mar. 29, 2006.
`
`Int. Cl.
`
`(51)
`
`(52)
`(58)
`
`(56)
`
`(2006.01)
`A61K 31/4166
`(2006.01)
`A61K 31/4184
`(2006.01)
`C07D 233/86
`
`514/391; 548/3211; 548/3014
`US. Cl.
`.......... ..
`Field of Classification Search ...................... .. None
`See application file for complete search history.
`
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`(Continued)
`
`Primary Examiner 7 Yong Chu
`Assistant Examiner 7 Michael Barker
`
`(74) Attorney, Agent, or Firm 7 Venable LLP; Michael A.
`Gollin; Lars H. Genieser
`
`ABSTRACT
`(57)
`The present invention relates to diarylhydantoin compounds,
`including diarylthiohydantoins, and methods for synthesiz-
`ing them and using them in the treatment of hormone refrac-
`tory prostate cancer.
`
`40 Claims, 29 Drawing Sheets
`
`MYLAN PHARMS. INC. EXHIBIT 1131 PAGE 1
`
`

`

`US 8,183,274 B2
`
`Page 2
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