Thiazolyl mGluR5 antagonists and methods for their use
View Patent ↗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.
1. A method for treating a mammalian patient having or at risk of having a condition selected from group consisting of anxiety, a mood disorder, depression, memory loss, cognitive impairment, and mental retardation which comprises administering to the patient in need thereof a therapeutically effective amount of a compound which is:
or a pharmaceutically acceptable salt thereof;
with the proviso that the compound does not comprise any radioisotopes at a level beyond their natural abundance.
2. The method of claim 1 werein the condition is anxiety.
3. The method of claim 1 werein the condition is a mood disorder.
4. The method of claim 1 werein the condition is depression.
5. The method of claim 1 werein the condition is memory loss.
6. The method of claim 1 werein the condition is cognitive impairment.
7. The method of claim 1 werein the condition is mental retardation.
8. The method of claim 1 werein the mammalian patient is a human.