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    4-phenylphthalazine derivatives which inhibit platelet aggregation
    2.
    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.

    Pharmaceuticals containing prostaglandin I.sub.2
    3.
    发明授权
    Pharmaceuticals containing prostaglandin I.sub.2 失效
    含有前列腺素I2的药物

    公开(公告)号：US4699921A

    公开(公告)日：1987-10-13

    申请号：US763618

    申请日：1985-08-08

    申请人： Masakatsu Shibasaki ,  Mikiko Sodeoka ,  Yuji Ogawa ,  Toshiaki Mase ,  Akira Ishibashi ,  Daijiro Horii ,  Toshiji Kanayama ,  Katsuhiko Iseki ,  Masaki Shinoda ,  Chiyoko Ishiyama ,  Yoshio Hayashi

    发明人： Masakatsu Shibasaki ,  Mikiko Sodeoka ,  Yuji Ogawa ,  Toshiaki Mase ,  Akira Ishibashi ,  Daijiro Horii ,  Toshiji Kanayama ,  Katsuhiko Iseki ,  Masaki Shinoda ,  Chiyoko Ishiyama ,  Yoshio Hayashi

    IPC分类号： C07C59/46 ,  A61K31/557 ,  A61P1/04 ,  A61P7/02 ,  A61P9/00 ,  A61P9/08 ,  A61P9/12 ,  C07C51/00 ,  C07C67/00 ,  C07C69/732 ,  C07C405/00

    CPC分类号： C07C405/0083 ,  A61K31/557 ,  Y02P20/55

    摘要： Disclosed is a pharmaceutical composition having circulation ameliorating effect and antiulcer effect containing a prostaglandin I.sub.2 analogue represented by the formula shown below or a non-toxic salt or a cyclodextrin inclusion compound thereof as the effective ingredient: ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl group having 1 to 12 carbon atoms, a cycloalkyl group having 4 to 7 carbon atoms or a phenyl group, A represents a pentyl group, a cyclopentyl group, a cyclohexyl group, a 1-methyl-3-hexynyl group, a 2-methyl-3-hexynyl group, a 1-methylhexyl group, a 2-phenethyl group, a 1,1-dimethylpentyl group, a 2-methylpentyl group, a 1-cyclohexylethyl group, a 2-methylhexyl group, a 1-methyl-3-pentynyl group or a 2,6-dimethyl-5-heptenyl group; the double bond between the carbon atoms at 4- and 5-positions is E or Z or a mixture thereof; the asymmetric center in the substituent represented by A is in the R-configuration or the S-configuration or a mixture thereof.Pharmaceutical compositions containing, as an active ingredient, prostaglandin I.sub.2 analogues of the present invention have potent platelet aggregation inhibiting effect, blood pressure depressing effect, vasodilative effect and antiulcer effect, and are also low in toxicity.

    摘要翻译： 本发明公开了一种具有循环改善作用和抗溃疡效果的药物组合物，其含有下述式表示的前列腺素I 2类似物或其无毒性盐或环糊精包合物作为有效成分：其中R 1表示氢原子， 碳原子数1〜12的烷基，碳原子数4〜7的环烷基或苯基，A表示戊基，环戊基，环己基，1-甲基-3-己炔基，2 1-甲基-3-己炔基，1-甲基己基，2-苯乙基，1,1-二甲基戊基，2-甲基戊基，1-环己基乙基，2-甲基己基，1-甲基 -3-戊炔基或2,6-二甲基-5-庚烯基; 4-和5-位的碳原子之间的双键是E或Z或它们的混合物; 由A表示的取代基中的不对称中心是R构型或S-构型或其混合物。 含有本发明的前列腺素I2类似物作为活性成分的药物组合物具有有效的血小板聚集抑制作用，降血压作用，血管扩张作用和抗溃疡作用，毒性也低。

    3,6-disubstituted pyradazine derivatives
    5.
    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。

    Pharmaceuticals containing prostaglandin I.sub.2
    6.
    发明授权
    Pharmaceuticals containing prostaglandin I.sub.2 失效
    含有前列腺素I2的药物

    公开(公告)号：US5053526A

    公开(公告)日：1991-10-01

    申请号：US511945

    申请日：1990-04-16

    申请人： Masakatsu Shibasaki ,  Mikiko Sodeoka ,  Yuji Ogawa ,  Toshiaki Mase ,  Akira Ishibashi ,  Daijiro Horii ,  Toshiji Kanayama ,  Katsuhiko Iseki ,  Masaki Shinoda ,  Chiyoko Ishiyama ,  Yoshio Hayashi

    发明人： Masakatsu Shibasaki ,  Mikiko Sodeoka ,  Yuji Ogawa ,  Toshiaki Mase ,  Akira Ishibashi ,  Daijiro Horii ,  Toshiji Kanayama ,  Katsuhiko Iseki ,  Masaki Shinoda ,  Chiyoko Ishiyama ,  Yoshio Hayashi

    IPC分类号： A61K31/557 ,  C07C405/00

    CPC分类号： C07C405/0083 ,  A61K31/557

    摘要： Disclosed is a pharmaceutical having circulation ameliorating effect and antiulcer effect containing a prostaglandin I.sub.2 analogue represented by the formula shown below or a non-toxic salt of its salt or a cyclodextrin inclusion compound thereof as the effective ingredient: ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl group having 1 to 12 carbon atoms, a cycloalkyl group having 4 to 7 carbon atoms or a phenyl group; A represents a pentyl group, a cyclopentyl group, a cyclohexyl group, a 1-methyl-3-hexynyl group, a 2-methyl-3-hexynyl group, a 1-methylhexyl group, a 2-phenethyl group, a 1,1-dimethylpentyl group, a 2-methylpentyl group, a 1-cyclohexylethyl group, a 2-methylhexyl group, a 1-methyl-3-pentynyl group or 1 2,6-dimethyl-5-heptenyl group; the double bond between the carbon atoms at 4- and 5-positions is E or Z or a mixture thereof, the asymmetric center in the substituent represented by A is R-configuration or S-configuration or a mixture thereof.The pharmaceuticals containing, as an active ingredient, prostaglandin I.sub.2 analogues of the present invention have potent platelet aggregation inhibiting effect, blood pressure depressing effect, vasodilative effect and antiulcer effect, and are also low in toxicity.

    摘要翻译： 本发明公开了一种具有循环改善作用和抗溃疡效果的药物，其含有下述式表示的前列腺素I2类似物或其盐的无毒性盐或其环糊精包合物作为有效成分：其中R1表示氢 原子，碳原子数1〜12的烷基，碳原子数4〜7的环烷基或苯基; A表示戊基，环戊基，环己基，1-甲基-3-己炔基，2-甲基-3-己炔基，1-甲基己基，2-苯乙基，1,1 2-甲基戊基，2-甲基戊基，1-环己基乙基，2-甲基己基，1-甲基-3-戊炔基或1,6-二甲基-5-庚烯基; 在4-和5-位碳原子之间的双键是E或Z或其混合物，由A表示的取代基中的不对称中心是R-构型或S-构型或其混合物。 含有本发明的前列腺素I2类似物作为活性成分的药物具有有效的血小板聚集抑制作用，降血压作用，血管扩张作用和抗溃疡作用，毒性也低。