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

被引：17

作者：

Haginoya, N

Kobayashi, S

Komoriya, S

Hirokawa, Y

Furugori, B

Nagahara, T

机构：

[1] Daiichi Pharmaceut Co Ltd, Med Chem Res Lab, Edogawa Ku, Tokyo 1348630, Japan

[2] Daiichi Pharmaceut Co Ltd, New Prod Res Lab 2, Edogawa Ku, Tokyo 1348630, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 11期

关键词：

factor Xa inhibitor; 4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine;

D O I：

10.1016/j.bmcl.2004.03.036

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：2935 / 2939

页数：5

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