Inhibitors of Akt activity
View Patent ↗The present invention is directed to compounds comprising a 2,3-diphenylquinoxaline moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention
1. A compound of the formula A:
wherein
R 1 independently represents amino-C 1-6 alkyl, C 1-4 alkylamino-(C 1-6 )alkyl or di(C 1-4 alkyl)amino-(C 1-6 )alkyl;
R 2 independently represents hydrogen, amino-C 1-6 alkyl, C 1-4 alkylamino-(C 1-6 )alkyl or di(C 1-4 alkyl)amino-(C 1-6 )alkyl;
r is 1 to 3;
s is 1 to 3;
or a pharmaceutically acceptable salt or a stereoisomer thereof.
2. The compound according to claim 1 of the formula A-1:
wherein
R 1 independently represents amino-C 1-6 alkyl, C 1-4 alkylamino-(C 1-6 )alkyl or di(C 1-4 alkyl)amino-(C 1-6 )alkyl; or the pharmaceutically acceptable salts thereof.
3. The compound according to claim 1 which is:
2-[4-(2-aminoprop-2-yl)phenyl]-3-phenylquinoxaline
or a pharmaceutically acceptable salt thereof.
4. A pharmaceutical composition comprising a pharmaceutical carrier, and dispersed therein, a therapeutically effective amount of a compound of claim 1 .
5. A pharmaceutical composition comprising a pharmaceutical carrier, and dispersed therein, a therapeutically effective amount of a compound of claim 3 .
6. A method for treating ovarian, pancreatic and breast cancer which comprises administering to a mammal in need thereof a therapeutically effective amount of a compound of claim 1 .
7. A method for treating ovarian, pancreatic and breast cancer which comprises administering to a mammal in need thereof a therapeutically effective amount of a compound of claim 3 .
8. A method for treating ovarian, pancreatic and breast cancer which comprises administering to a mammal in need thereof a therapeutically effective amount of a composition of claim 4 .
9. A method for treating ovarian, pancreatic and breast cancer which comprises administering to a mammal in need thereof a therapeutically effective amount of a composition of claim 5 .
10. A pharmaceutical composition made by combining a compound of claim 1 and a pharmaceutically acceptable carrier.
11. A process for making a pharmaceutical composition comprising combining a compound of claim 1 and a pharmaceutically acceptable carrier.