Preparation of 1-(3-aminobenzo(d)isoxazol-5-yl)-1H-pyrazolo(4,3-d)pyrimidin-7(6H)-ones as potent, selective, and efficacious inhibitors of coagulation factor Xa.

摘要

Previously, potent factor Xa inhibitors were described based on the 1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one bicyclic core and a 4-methoxyphenyl P1 moiety. This manuscript describes 1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one and related bicyclic cores with the 3-aminobenzisoxazole P1 moiety. Many of these compounds are potent, selective, and efficacious inhibitors of coagulation factor Xa.