US 2022/0088005 A1 · BROMODOMAIN INHIBITORS FOR ANDROGEN RECEPTOR-DRIVEN CANCERS

Abstract

Methods for treating certain androgen receptor-positive forms of cancer using inhibitors of the CREB binding protein bromodomain are disclosed. In some methods, the AR-positive forms of cancer may be breast cancer, including triple negative forms, hormone receptor positive forms, and HER2-positive forms. In other methods, the AR-positive forms of cancer may be prostate cancer, including metastatic castration resistant prostate cancer. In some embodiments, methods of treating prostate cancer comprise the step of administering to a patient in need thereof the compound (1R,3R)-3-[(7S)-2-[(R)-(5-fluoro-2-methoxyphenyl)(hydroxy)methyl]-6-(methoxycarbonyl)-7-methyl-3H,6H,7H,8H,9H-imidazo[4,5-f]quinolin-3-yl]cyclohexane-1-carboxylic acid, or a pharmaceutically acceptable salt thereof.

Claims23

Dependent claims

A method of treating breast cancer in a patient comprising administering to the patient in need thereof a therapeutically effective amount of a pharmaceutical composition comprising a compound of formula (I):

or a pharmaceutically acceptable salt thereof, wherein:
R1 is H or —OH;
each R2 is independently selected from C1-C6 alkyl, halogen, —CN, and —OR3, wherein the alkyl is optionally substituted with one or more halogen;
each R3 is independently C1-C6 alkyl, wherein the alkyl is optionally substituted with one or more halogen;
and
n is 0, 1, 2, or 3.

3 more elements

Dependencies are inferred from the claim text.

Bromodomain inhibitors for androgen receptor-driven cancers

Life of this patent

Bromodomain inhibitors for androgen receptor-driven cancers

Life of this patent

Abstract

Claims23