Benzimidazoles as potent and orally active mGlu5 receptor antagonists with an improved pk profile
A focused chemical optimization effort of compound 1 based on metabolite elucidation is described, resulting in 15i, a highly potent and selective mGlu5 receptor antagonist with an improved pharmacokinetic profile compared to 1. Characterization of 15i in
The present invention relates to novel benzimidazole derivatives, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them, wherein the compounds have the formula (I): in which the substitutents are as defined in claim 1 and salts, solvates, hydrates and N-oxides thereof.
-
Page/Page column 21
(2009/05/29)
NICOTINIC ACID DERIVATIVES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTOR-5
The present invention relates to novel benzimidazole derivatives, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them, wherein the compounds have the Formula (I): in which the substitutents are as defined in claim 1 and and salts, solvates, hydrates and N- oxides thereof.
-
Page/Page column 49
(2008/12/08)
More Articles about upstream products of 1072929-03-3