摘要 |
The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts. |
申请人 |
MERCK & CO., INC.;COSFORD, NICHOLAS, D.;SEIDERS, THOMAS, J.;PAYNE, JOSEPH;ROPPE, JEFFREY, R.;HUANG, DEHUA;SMITH, NICHOLAS, D.;POON, STEVE, F.;KING, CHRIS;EASTMAN, BRIAN, W.;WANG, BOWEI;ARRUDA, JEANNIE, M.;VERNIER, JEAN-MICHEL;ZHAO, XIUMIN |
发明人 |
COSFORD, NICHOLAS, D.;SEIDERS, THOMAS, J.;PAYNE, JOSEPH;ROPPE, JEFFREY, R.;HUANG, DEHUA;SMITH, NICHOLAS, D.;POON, STEVE, F.;KING, CHRIS;EASTMAN, BRIAN, W.;WANG, BOWEI;ARRUDA, JEANNIE, M.;VERNIER, JEAN-MICHEL;ZHAO, XIUMIN |