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

N Haginoya, S Kobayashi, S Komoriya…

Index: Haginoya, Noriyasu; Kobayashi, Syozo; Komoriya, Satoshi; Hirokawa, Yumiko; Furugori, Taketoshi; Nagahara, Takayasu Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 11 p. 2935 - 2939

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Citation Number: 15

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 ...