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    Fibrinolysis-enhancing agents
    1.
    发明授权
    Fibrinolysis-enhancing agents 失效
    纤维蛋白溶解增强剂

    公开(公告)号：US5141947A

    公开(公告)日：1992-08-25

    申请号：US758208

    申请日：1991-09-12

    申请人： Yoshikuni Tamao ,  Ryoji Kikumoto

    发明人： Yoshikuni Tamao ,  Ryoji Kikumoto

    IPC分类号： C07D211/60 ,  A61K31/18 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/455 ,  A61K31/47 ,  A61K31/63 ,  A61K31/635 ,  A61K38/00 ,  A61K38/49 ,  A61P7/02 ,  C07D215/36 ,  C07D401/12

    CPC分类号： A61K31/635 ,  A61K31/18 ,  A61K31/445 ,  A61K31/47 ,  A61K31/63 ,  A61K38/49

    摘要： Disclosed herein is a fibrinolysis-enhancing agent comprising, as an effective ingredient, an N.sup.2 -arylsulfonyl-L-arginine amide represented by the general formula (I): ##STR1## wherein R.sup.1 is a group of the formula: ##STR2## where R.sup.3 is an alkyl group having 3 to 5 carbon atoms or an alkoxyalkyl group having 2 to 4 carbon atoms and R.sup.4 is an alkyl group having 1 to 3 carbon atoms; and R.sup.2 is a group of the formula: ##STR3## where R.sup.5 and R.sup.6 are independently hydrogen atom, methyl group or methoxy group provided that they cannot be hydrogen atoms simultaneously, and R.sup.7 is an alkyl group having 1 to 3 carbon atoms; or a salt thereof. The agent is used in combination with a plasminogen activator.

    摘要翻译： 本文公开了一种纤维蛋白溶解增强剂，其包含作为有效成分的由通式（I）表示的N 2 - 芳基磺酰基-L-精氨酸酰胺：其中R1是下式基团：IMAGE >其中R3是具有3至5个碳原子的烷基或具有2至4个碳原子的烷氧基烷基，R4是具有1至3个碳原子的烷基; 并且R 2是下式的基团：其中R 5和R 6独立地为氢原子，甲基或甲氧基，条件是它们不能同时为氢原子，且R 7为具有1至3个碳原子的烷基; 或其盐。 该试剂与纤溶酶原激活剂组合使用。

    N.sup.2 -naphthalenesulfonyl-L-arginine derivatives, and the pharmaceutically acceptable acid addition salts thereof
    6.
    发明授权
    N.sup.2 -naphthalenesulfonyl-L-arginine derivatives, and the pharmaceutically acceptable acid addition salts thereof 失效

    公开(公告)号：US4066758A

    公开(公告)日：1978-01-03

    申请号：US671436

    申请日：1976-03-29

    申请人： Shosuke Okamoto ,  Ryoji Kikumoto ,  Kazuo Ohkubo ,  Shinji Tonomura ,  Yoshikuni Tamao ,  Tohru Tezuka ,  Akiko Hijikata

    发明人： Shosuke Okamoto ,  Ryoji Kikumoto ,  Kazuo Ohkubo ,  Shinji Tonomura ,  Yoshikuni Tamao ,  Tohru Tezuka ,  Akiko Hijikata

    IPC分类号： A61K38/00 ,  C07D211/16 ,  C07D211/32 ,  C07D211/46 ,  C07D211/60 ,  C07D211/90 ,  C07D295/185 ,  A61K31/445

    CPC分类号： C07D295/185 ,  C07D211/16 ,  C07D211/32 ,  C07D211/46 ,  C07D211/60 ,  C07D211/90 ,  A61K38/00 ,  Y10S514/822

    摘要： N.sup.2 -naphthalenesulfonyl-L-arginine esters and amides having the formula ##STR1## or the acid addition salts thereof with a pharmaceutically acceptable acid, wherein R is selected from the class consisting of (1) alkoxy, alkenyloxy, cycloalkoxy and halogenated alkoxy, respectively containing not more than 10 carbon atoms, aralkyloxy of not more than 15 carbon atoms, and alkoxy of not more than 10 carbon atoms substitured with an alkoxy group of not more than 10 carbon atoms; ##STR2## wherein R.sub.1 and R.sub.2 are members selected from the class consisting of hydrogen, alkyl, aryl, alkenyl and cycloalkyl, respectively containing not more than 10 carbon atoms, and aralkyl and cycloalkylalkyl, respectively containing not more than 15 carbon atoms, and substituted alkyl containing not more than 20 carbon atoms, said substituent being selected from the class consisting of alkoxy, alkoxycarbonyl, acyl, acyloxy, arylcarbamoyl and N,N-polymethylenecarbamoyl, respectively containing not more than 10 carbon atoms, and carboxy; and ##STR3## wherein Z is a divalent group containing up to 10 carbons atoms, which consists of more than one group selected from the class consisting of methylene --CH.sub.2 --, monosubstituted methylene ##STR4## wherein R.sub.3 is selected from the class consisting of alkyl, acyl, alkoxy, and alkoxycarbonyl, respectively containing not more than 10 carbon atoms, and carbamoyl; and disubstituted methylene ##STR5## wherein R.sub.4 and R.sub.5 are alkyl groups of not more than 10 carbon atoms, and which may further contain at least one member selected from the class consisting of oxy--O--, thio --S--, cycloalkylene of not more than 10 carbon atoms, imino ##STR6## alkyl-substituted imino ##STR7## wherein R.sub.6 is an alkyl group of not more than 10 carbon atoms, acyl-substituted imino ##STR8## wherein R.sub.7 is an alkyl group of not more than 10 carbon atoms, and phenylene ##STR9## which may be arranged in any order and complete the ##STR10## ring together with the said methylene, monosubstituted methylene or disubstituted methylene; and R' is a member selected from the class consisting of 1-naphthyl substituted alkoxy or alkoxycarbonyloxy, respectively containing not more than 10 carbon atoms; and 2-naphthyl substituted with alkoxy or alkoxycarbonyloxy, respectively containing not more than 10 carbon atoms.