The present invention is concerned with novel isoxazole derivatives of formula (I) wherein X, R1, R2, R3 and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the present invention have affinity and selectivity for GABA A α5 receptor. Further the present invention is concerned with the manufacture of the active compounds of formula (I), pharmaceutical compositions containing them and their use as medicaments.
本发明涉及具有以下式(I)的新
异恶唑衍
生物,其中X、R1、R2、R3和R4如本文所述,以及其药学上可接受的盐和酯。本发明的活性化合物具有对
GABA A α5受体的亲和力和选择性。此外,本发明涉及制备具有式(I)的活性化合物、含有它们的药物组合物以及它们作为药物的用途。