PYRIDOPYRIMIDINONE INHIBITORS OF VIRUSES

摘要

Provided herein are novel small molecule pyridomyrimidone viral inhibitor agents of Formula (I), such as 4-acetyl-2,3,7,8-tetrahydro-3-phenylpyrido[1,2-f]pyrimidin-1-one, and methods of using pharmaceutical or therapeutic compositions comprising such viral inhibitor agents of Formula (I) in inhibiting and treating viral infections including orthopox and retroviral infections. Methods of synthesizing such agents are also provided herein.;

主权项

1. A pharmaceutical composition comprising a pyridopyrimidinone viral inhibitor of Formula (I): wherein: R1, R2 and R4 are independently, H, alkyl, alkenyl, alkynyl, aryl, heteroaryl, cyclyl, heterocyclyl, acyl, amino, hydroxyl, alkoxy, C(O)OR8, or C(O)N(R8)2, each of which can be optionally substituted; R3 is H, alkyl, alkenyl, alkynyl, aryl, heteroaryl, cyclyl, heterocyclyl, acyl, amino, or alkyl silane (e.g., trialkylsilane), each of which can be optionally substituted; R5 is H, alkyl, alkenyl, alkynyl, aryl, heteroaryl, cyclyl, heterocyclyl, acyl, amino, hydroxyl, alkoxy, mercapato, thioalkoxy, sulfinyl, sulfonyl, C(O)OR8, or C(O)N(R8)2, each of which can be optionally substituted; R6 is H, alkyl, alkenyl, alkynyl, aryl, heteroaryl, cyclyl, heterocyclyl, or acyl, each of which can be optionally substituted; R7 is independently for each occurrence H, halo, cyano, amino, nitro, hydroxyl, mercapto, thioalkoxy, sulfinyl, sulfonyl, alkyl, alkenyl, alkynyl, alkoxy, acyl, aryl, heteroaryl, cyclyl, heterocyclyl, C(O)OR8, or C(O)N(R8)2, each of which can be optionally substituted; R8 is H, alkyl, alkenyl, alkynyl, aryl, heteroaryl, cyclyl, or heterocyclyl, each of which can be optionally substituted; n is 0, 1, 2, 3, 4, or 5; and pharmaceutically acceptable salts thereof in a pharmaceutically acceptable carrier.