发明名称 |
Thiazolyl mGluR5 antagonists and methods for their use |
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. |
申请公布号 |
US8242143(B2) |
申请公布日期 |
2012.08.14 |
申请号 |
US201113016304 |
申请日期 |
2011.01.28 |
申请人 |
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;MERCK SHARP & DOHME CORP. |
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 |
分类号 |
A61P25/00;A61K31/44;C07D417/00 |
主分类号 |
A61P25/00 |
代理机构 |
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地址 |
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