Benzo [c] isoxazoloazepine bromodomain inhibitors and uses thereof
AssigneeConstellation Pharmaceuticals, Inc.
InventorsBrian K. Albrecht, Michael Charles Hewitt, Victor S. Gehling, Rishi G. Vaswani
Life of this patent
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Abstract
The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
Claims24
A compound of Formula (I):
- or a pharmaceutically acceptable salt thereof, wherein:
- R1 is hydrogen or (C1-C6)alkyl;
- R2 is optionally substituted 5-6 membered heteroaryl;
- phenyl ring A is optionally substituted;
- and
- R4 is selected from (C1-C6)alkyl, (C2-C6)alkenyl, and (C2-C6)alkynyl, each of which may be optionally substituted with one or more groups selected from —C(═O)ORa, —C(═O)NRaRb, —C(═O)Ra, —C(═NORa)Rb, —C(═NRa)NRbRa, —NRaC(═O)NRbRa, —NRaC(═O)Rb, —NRaC(═NRb)NRaRb, —NRaC(═O)ORb, —OC(═O)NRaRb, —OC(═O)Ra, —OC(═O)ORa, —S(O)0-3Ra, —SO2NRaRb, —NRaSO2Rb, —NRaSO2NRbRa, and —P(═O)ORaORb, wherein each Ra and Rb are independently hydrogen or (C1-C6)alkyl;
- provided that the compound of Formula I is not 2-(8-(6-aminopyridin-3-yl)-1-methyl-6-(4-(trifluoromethyl)phenyl)-4H-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide, 2-(8-(6-aminopyridin-3-yl)-6-(4-chlorophenyl)-1-methyl-4H-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide, or 2-(8-(6-aminopyridin-3-yl)-6-(4-fluorophenyl)-1-methyl-4H-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide, or a pharmaceutically acceptable salt thereof.
A compound that is of the formula:
- or a pharmaceutically acceptable salt thereof.
A pharmaceutical composition comprising:
- i) a pharmaceutically acceptable carrier or diluent;
- and ii) a compound of the formula:
- or a pharmaceutically acceptable salt thereof.
A method of treating a human with a disorder modulated by a bromodomain-containing protein, comprising the step of administering to the human an effective amount of a compound of the formula:
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.