Orally active factor Xa inhibitors: 4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine derivatives |
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Authors: | Haginoya Noriyasu Kobayashi Syozo Komoriya Satoshi Hirokawa Yumiko Furugori Taketoshi Nagahara Takayasu |
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Institution: | Medicinal Chemistry Research Laboratory, Daiichi Pharmaceutical Co. Ltd, 1-16-13, Kita-Kasai, Edogawa-ku, Tokyo 134-8630, Japan. hagin9kg@daiichipharm.co.jp |
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Abstract: | In our investigation of factor Xa inhibitors, a series of 1-(6-chloronaphthalen-2-yl)sulfonyl-4-(4,5,6,7-tetrahydrothiazolo5,4-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. |
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