IP Library › Granted Patent US 8,450,374
Granted Patent B2
US 8,450,374 · App. 12/826,242 · Granted May 28, 2013

Pan-antagonists for the androgen receptor and androgen receptor mutants associated with anti-androgen withdrawal

Inventors: John Tze-tzun Koh (West Grove, PA); Paula Lynn McGinley (Langhorne, PA); Hongmu Pan (Newark, DE); Robert Sikes (Newark, DE)
Assignee: University of Delaware
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Quick Facts
Patent No.
US 8,450,374
App. No.
12/826,242
Granted
May 28, 2013
Kind
B2
Abstract

Disclosed herein are novel antagonists of the androgen receptor and androgen receptor mutations associated with clinical failure of currently prescribed anti-androgens and use of said antagonists in the treatment of conditions associated with inappropriate activation of the androgen receptor.

Claims (6)

1. A compound of the formula:

wherein R 1 is phenyl phenoxy, benzoyl, phenylthio or benzyl, said R 1 being substituted with alkyl, branched alkyl, alkoxy, branched alkoxy, aryl, aryloxy, alkylamido, alkylcarbamoyl, or acyl; said provided that, when R 1 is substituted with alkyl or branched alkyl, the alkyl or branched alkyl is further substituted with amino, alkylamino, dialkylamino, arylamino, acyl, ester, carboxyl, hydroxyl, alkoxy, sulfonyl or cyano; further provided that, when R 1 is substituted with alkoxy, branched alkoxy, aryl, aryloxy, alkylamido, alkylcarbamoyl, or acyl, the alkoxy, branched alkoxy, aryl, aryloxy, alkylamido, alkylcarbamoyl, or acyl is further optionally substituted with alkyl, amino, alkylamino, dialkylamino, arylamino, acyl, ester, carboxyl, hydroxyl, alkoxy, sulfonyl or cyano.

2. The compound of claim 1 , wherein said compound is selected from the group consisting of:

wherein R 2 is alkyl, alkoxy, aryl, branched alkyl, branched alkyloxy, alkylamino, dialkylamino, aryloxy, arylamino, acyl, alkylamido, or alkylcarbamoyl, provided that, when R 2 is alkyl or branched alkyl, the alkyl or branched alkyl is substituted with amino, alkylamino, dialkylamino, carboxyl, ester, hydroxy, alkoxy, sulfonyl or cyano; further provided that, when R 2 is alkoxy, aryl, branched alkyloxy, alkylamino, dialkylamino, aryloxy, arylamino, acyl, alkylamido, or alkylcarbamoyl is optionally substituted with alkyl, amino, alkylamino, dialkylamino, carboxyl, ester, hydroxy, alkoxy, sulfonyl or cyano.

3. The compound of claim 2 , selected from the group consisting of:

4. A pharmaceutical composition comprising a compound of claim 1 .

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 17, 2010
From: KOH, JOHN TZE-TZUAN; SIKES, ROBERT; PAN, HONGMU; MCGINLEY, PAULA LYNN
To: UNIVERSITY OF DELAWARE
Reel/Frame 025005/0081 →
Continuity (2)
Provisional Application 61221318 · Jun 29, 2009
Related Publication 20100331418A1 · Dec 30, 2010