发明授权
- 专利标题: Thiazolyl mGluR5 antagonists and methods for their use
- 专利标题(中): 噻唑基mGluR5拮抗剂及其使用方法
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申请号: US13016304申请日: 2011-01-28
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公开(公告)号: US08242143B2公开(公告)日: 2012-08-14
- 发明人: Nicholas D. Cosford , Thomas J. Seiders , Joseph Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
- 申请人: Nicholas D. Cosford , Thomas J. Seiders , Joseph Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
- 申请人地址: US NJ Rahway
- 专利权人: Merck Sharp & Dohme Corp.
- 当前专利权人: Merck Sharp & Dohme Corp.
- 当前专利权人地址: US NJ Rahway
- 代理商 J. Eric Thies; Gerard M. Devlin
- 主分类号: A61P25/00
- IPC分类号: A61P25/00 ; A61K31/44 ; C07D417/00
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.
公开/授权文献
- US20110230526A1 Thiazolyl Mglur5 Antagonists and Methods for Their Use 公开/授权日:2011-09-22
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