Invention Grant
- Patent Title: Thiazolyl mglur5 antagonists and methods for their use
- Patent Title (中): 噻唑基mglur5拮抗剂及其使用方法
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Application No.: US11664902Application Date: 2005-10-06
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Publication No.: US07879882B2Publication Date: 2011-02-01
- Inventor: Nicholas D. Cosford , Thomas J. Seiders , Joseph E. 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
- Applicant: Nicholas D. Cosford , Thomas J. Seiders , Joseph E. 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
- Applicant Address: US NJ Rahway
- Assignee: Merck Sharp & Dohme Corp.
- Current Assignee: Merck Sharp & Dohme Corp.
- Current Assignee Address: US NJ Rahway
- Agent J. Eric Thies; Gerald M. Devlin
- International Application: PCT/US2005/035921 WO 20051006
- International Announcement: WO2007/050050 WO 20070503
- Main IPC: A61P25/00
- IPC: A61P25/00 ; A61K31/44 ; C07D417/14

Abstract:
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.
Public/Granted literature
- US20090203903A1 Thiazolyl mglur5 antagonists and methods for their use Public/Granted day:2009-08-13
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