Thiazolyl MGLUR5 antagonists and methods for their use

The identification of a unique series of 1,3 thiazoles 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 sel...

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Hauptverfasser: KING, CHRIS, HUANG, DEHUA, ROPPE, JEFFREY, R, POON, STEVE, F, PAYNE, JOSEPH, EASTMAN, BRIAN, W, ARRUDA, JEANNIE, M, SMITH, NICHOLAS, D, SEIDERS, THOMAS, J, COSFORD, NICHOLAS, D, VERNIER, JEAN-MICHEL, ZHAO, XIUMIN, WANG, BOWEI
Format: Patent
Sprache:eng ; fre ; ger
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Zusammenfassung:The identification of a unique series of 1,3 thiazoles 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.