abstract |
3-ARYL-ISOXAZOL-4-CARBONYL-BENZOFURAN DERIVATIVES. The present invention relates to 3-arylisoxazole-4-carbonylbenzofuran derivatives of formula (I), wherein R4 is hydrogen or halogen; R 2 R 2 is hydrogen, halogen, hydroxy, lower alkoxy, OCF 3 -, -OCH 2 R 2, R 3 is hydrogen or lower alkoxy; or R 2, R 2 and R 4 form together with the atom to which they are attached a ring with -CH = CH-CH = -CH-; R is aryl or heteroaryl, optionally substituted by halogen or lower alkyl, or is C (O) NH-lower alkyl, or is -C (O) -heteroaryl, wherein the heteroaryl group is optionally substituted by lower alkyl or phenyl and with pharmaceutically acceptable acid addition salts thereof. It has been found that this class of compounds has high affinity and selectivity for GABA A cc5 receptor binding sites and could be useful as a cognition enhancer or for the treatment of cognitive disorders such as Alzheimer's disease. |