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    Selective thrombin inhibitors
    5.
    发明授权
    Selective thrombin inhibitors 失效
    选择性凝血酶抑制剂

    公开(公告)号：US5985899A

    公开(公告)日：1999-11-16

    申请号：US967661

    申请日：1997-11-10

    申请人： Yeong Soo Oh ,  Sang Soo Kim ,  Sang Yeul Hwang ,  Mi Kyung Yun ,  Seong Ryul Hwang ,  Seong Won Hong ,  Yong Hee Lee ,  Yi Na Jeong ,  Koo Lee ,  You Seung Shin

    发明人： Yeong Soo Oh ,  Sang Soo Kim ,  Sang Yeul Hwang ,  Mi Kyung Yun ,  Seong Ryul Hwang ,  Seong Won Hong ,  Yong Hee Lee ,  Yi Na Jeong ,  Koo Lee ,  You Seung Shin

    IPC分类号： C07C257/22 ,  C07C311/19 ,  C07C311/29 ,  C07C311/42 ,  C07D211/60 ,  C07D295/185 ,  C07D295/205 ,  C07D295/26 ,  A61K31/445 ,  C07D211/34

    CPC分类号： C07C257/22 ,  C07C311/19 ,  C07C311/29 ,  C07C311/42 ,  C07D211/60 ,  C07D295/185 ,  C07D295/205 ,  C07D295/26 ,  C07C2101/02 ,  C07C2101/10 ,  C07C2101/14

    摘要： The present invention relates to a novel selective thrombin inhibitor having the following formula (I), which is also effective by oral administration: ##STR1## in which R.sup.1 represents acetyl substituted with aryl or aryloxy, or represents sulfonyl substituted with substituted or unsubstituted aryl or N-containing heterocyclic group,X represents a group of formula ##STR2## R.sup.2 and R.sup.3 independently of one another represent hydrogen; cycloalkyl substituted or unsubstituted with carboxyl or alkoxycarbonyl; arylalkyloxy; hydroxy; or lower alkyl substituted or unsubstituted with carboxyl, alkoxycarbonyl or hydroxy, orR.sup.2 and R.sup.3 together with nitrogen atom to which they are attached can form a piperidine group substituted with carboxyl or alkoxycarbonyl,R.sup.4 represents hydrogen, lower alkyl or lower alkoxy,R.sup.5 represents alkanesulfonyl; alkoxycarbonyl; alkylcarbonyl; formyl; lower alkyl; aryl substituted or unsubstituted with alkoxy or haloalkyl; or hydroxy-substituted lower alkyl, andR.sup.6 and R.sup.7 independently of one another represent hydrogen, lower alkyl or amino,and to a process for preparation thereof and a pharmaceutical composition for thrombin inhibition which comprises the compound of formula (I) as an active ingredient.

    摘要翻译： 本发明涉及一种新型的具有下列通式（I）的选择性凝血酶抑制剂，其也可通过口服给药有效：其中R1表示被芳基或芳氧基取代的乙酰基，或表示被取代或未取代的芳基或含N 杂环基，X表示式R 2的基团，R 3彼此独立地表示氢; 被羧基或烷氧基羰基取代或未取代的环烷基; 芳基烷氧基; 羟基; 或与羧基，烷氧基羰基或羟基取代或未取代的低级烷基，或R 2和R 3与它们所连接的氮原子一起形成被羧基或烷氧基羰基取代的哌啶基，R 4表示氢，低级烷基或低级烷氧基，R 5表示烷磺酰基 ; 烷氧基羰基 烷基羰基; 甲酰基 低级烷基 被烷氧基或卤代烷基取代或未取代的芳基; 或羟基取代的低级烷基，R 6和R 7彼此独立地表示氢，低级烷基或氨基，以及其制备方法和用于凝血酶抑制的药物组合物，其包含式（I）化合物作为活性成分 。

    Selective thrombin inhibitors
    6.
    发明授权
    Selective thrombin inhibitors 失效
    选择性凝血酶抑制剂

    公开(公告)号：US5977114A

    公开(公告)日：1999-11-02

    申请号：US967018

    申请日：1997-11-10

    申请人： Yeong Soo Oh ,  Sang Soo Kim ,  Sang Yeul Hwang ,  Mi Kyung Yun ,  Seong Ryul Hwang ,  Seong Won Hong ,  Yong Hee Lee ,  Yi Na Jeong ,  Koo Lee ,  You Seung Shin

    发明人： Yeong Soo Oh ,  Sang Soo Kim ,  Sang Yeul Hwang ,  Mi Kyung Yun ,  Seong Ryul Hwang ,  Seong Won Hong ,  Yong Hee Lee ,  Yi Na Jeong ,  Koo Lee ,  You Seung Shin

    IPC分类号： C07C257/22 ,  C07C311/19 ,  C07C311/29 ,  C07C311/42 ,  C07D211/60 ,  C07D295/185 ,  C07D295/205 ,  C07D295/26 ,  A61K31/495 ,  C07D241/04

    CPC分类号： C07C257/22 ,  C07C311/19 ,  C07C311/29 ,  C07C311/42 ,  C07D211/60 ,  C07D295/185 ,  C07D295/205 ,  C07D295/26 ,  C07C2101/02 ,  C07C2101/10 ,  C07C2101/14

    摘要： The present invention relates to a novel selective thrombin inhibitor having the following formula (I), which is also effective by oral administration: ##STR1## in which R.sup.1 represents acetyl substituted with aryl or aryloxy, or represents sulfonyl substituted with substituted or unsubstituted aryl or N-containing heterocyclic group,x represents a group of formula ##STR2## R.sup.2 and R.sup.3 independently of one another represent hydrogen; cycloalkyl substituted or unsubstituted with carboxyl or alkoxycarbonyl; arylalkyloxy; hydroxy; or lower alkyl substituted or unsubstituted with carboxyl, alkoxycarbonyl or hydroxy, orR.sup.2 and R.sup.3 together with nitrogen atom to which they are attached can form a piperidine group substituted with carboxyl or alkoxycarbonyl,R.sup.4 represents hydrogen, lower alkyl or lower alkoxy,R.sup.5 represents alkanesulfonyl; alkoxycarbonyl; alkylcarbonyl; formyl; lower alkyl; aryl substituted or unsubstituted with alkoxy or haloalkyl; or hydroxy-substituted lower alkyl, andR.sup.6 and R.sup.7 independently of one another represent hydrogen, lower alkyl or amino,and to a process for preparation thereof and a pharmaceutical composition for thrombin inhibition which comprises the compound of formula (I) as an active ingredient.

    摘要翻译： 本发明涉及一种新型的具有下列通式（I）的选择性凝血酶抑制剂，其也可通过口服给药有效：其中R1表示被芳基或芳氧基取代的乙酰基，或表示被取代或未取代的芳基或含N 杂环基，x代表式R2和R3彼此独立地表示氢; 被羧基或烷氧基羰基取代或未取代的环烷基; 芳基烷氧基; 羟基; 或与羧基，烷氧基羰基或羟基取代或未取代的低级烷基，或R 2和R 3与它们所连接的氮原子一起形成被羧基或烷氧羰基取代的哌啶基，R 4表示氢，低级烷基或低级烷氧基，R 5表示烷磺酰基 ; 烷氧基羰基 烷基羰基; 甲酰基 低级烷基 被烷氧基或卤代烷基取代或未取代的芳基; 或羟基取代的低级烷基，R 6和R 7彼此独立地表示氢，低级烷基或氨基，以及其制备方法和用于凝血酶抑制的药物组合物，其包含式（I）化合物作为活性成分 。