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    3,6-disubstituted pyradazine derivatives
    2.
    发明授权
    3,6-disubstituted pyradazine derivatives 失效
    3,6-二取代的哒嗪衍生物

    公开(公告)号：US5462941A

    公开(公告)日：1995-10-31

    申请号：US215426

    申请日：1994-03-21

    申请人： Norimichi Iwase ,  Yasuhiro Morinaka ,  Yoshikuni Tamao ,  Toshiji Kanayama ,  Kumi Yamada

    发明人： Norimichi Iwase ,  Yasuhiro Morinaka ,  Yoshikuni Tamao ,  Toshiji Kanayama ,  Kumi Yamada

    IPC分类号： A61K31/50 ,  A61K31/502 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  C07D237/34 ,  C07D241/44 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D417/04 ,  C07D417/14 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04 ,  C07D521/00 ,  C07D247/02

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D237/34 ,  C07D249/08 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D417/04 ,  C07D491/04 ,  C07D495/04

    摘要： A 3,6-disubstituted pyridazine derivative having excellent platelet agglutination inhibitory effects. It is useful for a preventive medicine or a therapeutic medicine for a cerebrovascular disorder such as cerebral thrombosis and cerebral embolism, an ischemic heart disease such as myocardial infarction, and a circulation disorder such as peripheral circulation disorder. A pharmaceutical composition containing a compound of the present invention as an effective ingredient and a process for preparing the same are also disclosed. The compound has the formula (I) ##STR1## wherein A represents an alkyl group having 3 to 6 carbon atoms; a cycloalkyl group having 5 to 7 carbon atoms; a phenyl group, a thienyl group, a furyl group, a thiazolyl group, a phenoxy group, a phenylalkyl group having 7 to 9 carbon atoms, a phenylthio group, a 5-6 membered saturated heterocyclic group containing one or more nitrogen atoms, a pyridyl group or an imidazolyl group each of which may have at least one substituent selected from the group consisting of an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms and a halogen atom; B represents (a) --NH--D wherein D represents ##STR2## (4) --CH.sup.3 R.sup.4 ; or (5) an alkyl group having 3 to 8 carbon atoms; or ##STR3## and the ring C represents a benzene ring.

    摘要翻译： 具有优异的血小板凝集抑制作用的3,6-二取代哒嗪衍生物。 对脑血栓形成和脑栓塞，心肌梗死等缺血性心脏病，周围循环障碍等循环障碍的脑血管障碍的预防药或治疗药有用。 还公开了含有本发明化合物作为有效成分的药物组合物及其制备方法。 该化合物具有式（I）其中A表示具有3至6个碳原子的烷基; 具有5至7个碳原子的环烷基; 苯基，噻吩基，呋喃基，噻唑基，苯氧基，具有7〜9个碳原子的苯基烷基，苯硫基，含有一个或多个氮原子的5-6元饱和杂环基， 吡啶基或咪唑基，其各自可具有至少一个选自具有1至4个碳原子的烷基，具有1至4个碳原子的烷氧基和卤素原子的取代基; （A）-NH-D其中D表示（1）图像（2）图像（3）（4）-CH 3 R 4; 或（5）碳原子数为3〜8的烷基; 或（B），环C表示苯环。

    4-phenylphthalazine derivatives which inhibit platelet aggregation
    4.
    发明授权
    4-phenylphthalazine derivatives which inhibit platelet aggregation 失效
    抑制板聚集的4-苯基苯胺衍生物

    公开(公告)号：US5089494A

    公开(公告)日：1992-02-18

    申请号：US675259

    申请日：1991-03-27

    申请人： Norimichi Iwase ,  Yasuhiro Morinaka ,  Yoshikuni Tamao ,  Toshiji Kanayama

    发明人： Norimichi Iwase ,  Yasuhiro Morinaka ,  Yoshikuni Tamao ,  Toshiji Kanayama

    IPC分类号： C07D237/34

    CPC分类号： C07D237/34

    摘要： 4-Phenylphthalazine derivatives having platelet aggregation inhibitory activity of the formula: ##STR1## wherein R.sup.1 is an alkyl or hydroxyalkyl group of 1-5 carbon atoms; R.sup.2 is a hydrogen atom or an alkyl group of 1-5 carbon atoms; or R.sup.1 and R.sup.2, when taken together, may represent an alkylene group of 2-6 carbon atoms, said group optionally containing one or more oxygen atoms; R.sup.3 and R.sup.4 are independently a hydrogen or halogen atom, an alkyl or alkoxy group of 1-4 carbon atoms, or when two of R.sup.3 are adjacently positioned, (R.sup.3)l may represent a --O--(CH.sub.2).sub.p --O-- group and/or when two of R.sup.4 are adjacently positioned, (R.sup.4).sub.m may represent a --O--(CH.sub.2).sub.p --O-- group; R.sup.5 is a hydrogen or halogen atom, an alkyl or alkoxy group of 1-4 carbon atoms, a trifluoromethyl group or a hydroxy group, or when two of R.sup.5 are adjacently positioned, (R.sup.5).sub.n may represent a --O--(CH.sub.2).sub.p --O-- group; p is an integer of 1-3; l and m are independently an integer of 1-2; and n is an integer of 1-3, and optical isomers and pharmaceutically acceptable acid addition salts thereof.

    Fibrinolysis-enhancing agents
    5.
    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
    10.
    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.