Orally active factor Xa inhibitors: 4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine derivatives.

Abstract In our investigation of factor Xa inhibitors, a series of 1-(6-chloronaphthalen-2-yl)sulfonyl-4-(4,5,6,7-tetrahydrothiazolo[5,4- c ]pyridine-2-carbonyl)piperazines 3a – i were synthesized. In vitro inhibitory activities of the compounds against factor Xa and coagulation are summarized. Among the compounds, 3c and 3d , possessing a carbamoyl or N -methylcarbamoyl moiety, showed potent inhibitory activities when administered orally to rats.