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
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