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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| creator | 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 |
| description | 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. |
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| subjects | CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS |
| title | Thiazolyl MGLUR5 antagonists and methods for their use |
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