申请人:SANKYO COMPANY, LIMITED
公开号:US20040147555A1
公开(公告)日:2004-07-29
A compound of a formula (1) and pharmacologically acceptable salts thereof:
1
wherein R
1
represents hydrogen, halogen, alkyl or hydroxyl; R
2
represents hydrogen or halogen; R
3
represents hydrogen, alkyl, hydroxyl, carboxyalkyl, alkoxycarbonylalkyl, alkylsulfonyl, alkoxycarbonylalkylsulfonyl, craboxyalkylsulfonyl or carboxyalkylcarbonyl; each of R
4
and R
5
represents hydrogen, halogen, alkyl, carbamoyl, alkoxy, carboxyl, alkoxycarbonyl, monoalkylcarbamoyl or dialkylcarbamoyl; R
6
represents a heterocycle, hydrogen, alkyl, cycloalkyl, aralkyl, carboxyalkyl, alkoxycarbonyalkyl, aliphatic or aromatic acyl, carbamoyl, alkylsulfonyl, aryl, formimidoyl, 1-iminoalkyl, N-alkylforminidoyl or iminoarylmethyl; each of R
7
and R
8
represents hydrogen or alkyl; n represents 0, 1 or 2. The compound exhibits excellent activated blood coagulation factor X inhibitory activity and prevents or treats blood coagulation-related diseases.
一个公式(1)的化合物及其药理学上可接受的盐:其中R1代表氢,卤素,烷基或羟基;R2代表氢或卤素;R3代表氢,烷基,羟基,羧基烷基,烷氧羰基烷基,烷基磺酰基,烷氧羰基磺酰基,羧基烷基磺酰基或羧基烷基羰基;R4和R5中的每一个代表氢,卤素,烷基,氨基酰基,烷氧基,羧基,烷氧羰基,单烷基氨基酰基或双烷基氨基酰基;R6代表杂环,氢,烷基,环烷基,芳基烷基,羧基烷基,烷氧羰基烷基,脂肪族或芳香族酰基,氨基酰基,烷基磺酰基,芳基,甲酰胺基,1-亚氨基烷基,N-烷基亚氨基甲酰基或亚氨基芳基甲基;R7和R8中的每一个代表氢或烷基;n代表0、1或2。该化合物表现出优异的激活血液凝血因子X抑制活性,可预防或治疗与血液凝固相关的疾病。