Small-molecule inhibitors of the androgen receptor

US8119660B2 · kind B2 · utility

Assignee

• The Regents of the University of California · US

Inventors

• Marc Diamond · Chesterfield, US
• Jeremy Jones · Pasadena, US
• Adam Renslo · Oakland, US

Key dates

• Filing date: Mar 4, 2010
• Grant date: Feb 21, 2012
• Expiry date: Mar 4, 2030

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P35/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention provides a method of inhibiting an androgen receptor by administering a compound of Formula I:or a compound of Formula II:wherein R1, R2, R3 and R8 are each independently hydrogen or C1-6 alkyl. R4 is absent or is hydrogen, C1-6 alkyl or C1-6 alkyl-OH. R5 is hydrogen, C1-6 alkyl or —NR6R7. R6 and R7 are each independently hydrogen or C1-6 alkyl, or are combined with the nitrogen to which they are attached to form a heterocycloalkyl having from 5 to 7 ring members. L is a linker of C1-6 alkylene, C2-6 alkenylene, C2-6 alkynylene or C3-6 cycloalkylene. The compounds of Formula I include the salts, hydrates and prodrugs thereof. Each R9 is H, C1-6 alkyl, —OH or —O—C1-6 alkyl. The compounds of Formulas I and II include the salts, hydrates and prodrugs thereof. By administering the compound of Formula I or II, the method inhibits the androgen receptor.