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60 条记录 (耗时 0.031 秒)

    Imidazole and 1,2,4-triazole derivatives with angiotensin II antagonist properties
    52.
    发明授权
    Imidazole and 1,2,4-triazole derivatives with angiotensin II antagonist properties 失效
    咪唑和1,2,4-三唑衍生物与血管紧张素II拮抗剂的性质

    公开(公告)号：US5389661A

    公开(公告)日：1995-02-14

    申请号：US194535

    申请日：1994-02-10

    申请人： Ila Sircar ,  Jagadish C. Sircar

    发明人： Ila Sircar ,  Jagadish C. Sircar

    IPC分类号： C07D401/06 ,  C07D403/06 ,  C07D403/14 ,  A61K31/41 ,  A61K31/415 ,  C07D257/04

    CPC分类号： C07D401/06 ,  C07D403/06 ,  C07D403/14

    摘要： This invention relates to novel substituted imidazole and triazole derivatives which antagonize the binding of angiotensin II to its receptors. The compounds are useful in the treatment of hypertension, heart failure, glaucoma, and hyperaldosteronism. Methods of making the compounds, novel intermediates useful in the preparation of the compounds, pharmaceutical compositions containing the compounds, and methods of using them are also covered.

    摘要翻译： 本发明涉及拮抗血管紧张素II与其受体的结合的新型取代的咪唑和三唑衍生物。 该化合物可用于治疗高血压，心力衰竭，青光眼和醛固酮增多症。 制备化合物的方法，可用于制备化合物的新中间体，含有该化合物的药物组合物，以及使用它们的方法也被覆盖。

    Imidazole with angiotensin II antagonist properties
    53.
    发明授权
    Imidazole with angiotensin II antagonist properties 失效
    咪唑与血管紧张素II拮抗剂的性质

    公开(公告)号：US5322950A

    公开(公告)日：1994-06-21

    申请号：US985395

    申请日：1992-12-04

    申请人： Ila Sircar ,  Jagadish C. Sircar

    发明人： Ila Sircar ,  Jagadish C. Sircar

    IPC分类号： C07D401/06 ,  C07D403/06 ,  C07D403/14

    CPC分类号： C07D401/06 ,  C07D403/06 ,  C07D403/14

    摘要： This invention relates to novel substituted imidazole and triazole derivatives which antagonize the binding of angiotensin II to its receptors. The compounds are useful in the treatment of hypertension, heart failure, glaucoma, and hyperaldosteronism. Methods of making the compounds, novel intermediates useful in the preparation of the compounds, pharmaceutical compositions containing the compounds, and methods of using them are also covered.

    摘要翻译： 本发明涉及拮抗血管紧张素II与其受体的结合的新型取代的咪唑和三唑衍生物。 该化合物可用于治疗高血压，心力衰竭，青光眼和醛固酮增多症。 制备化合物的方法，可用于制备化合物的新中间体，含有该化合物的药物组合物，以及使用它们的方法也被覆盖。

    Substituted 4,5-dihydro-6-(substituted)-phenyl-3(2H)-pyridazinones and 6-(substituted) phenyl-3(2H)-pyridazinones
    56.
    发明授权
    Substituted 4,5-dihydro-6-(substituted)-phenyl-3(2H)-pyridazinones and 6-(substituted) phenyl-3(2H)-pyridazinones 失效
    取代的4,5-二氢-6-（取代的） - 苯基-3（2H） - 哒嗪酮和6-（取代的）苯基-3（2H） - 哒嗪酮

    公开(公告)号：US4734415A

    公开(公告)日：1988-03-29

    申请号：US477695

    申请日：1983-03-22

    申请人： Ila Sircar ,  James A. Bristol

    发明人： Ila Sircar ,  James A. Bristol

    IPC分类号： C07D403/10 ,  C07D521/00 ,  C07D237/04 ,  A61K31/50

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D403/10

    摘要： Substituted 4,5-dihydro-6-(substituted)phenyl-3(2H)-pyridazinone compounds and 6-(substituted)phenyl-3(2H)-pyridazinone compounds and pharmaceutically acceptable salts thereof are useful as cardiotonic and antihypertensive agents.Said compounds cause a significant increase in myocardial contractility in the dog. Said compounds also cause a decrease in blood pressure in the spontaneously hypertensive rat. Said compounds are produced by reacting substituted .gamma.-oxobenzenebutanoic acids with suitably substituted hydrazines to provide 4,5-dihydro-6-(substituted)phenyl-3(2H)-pyridazinones which are dehydrogenated to 6-(substituted)phenyl-3(2H)-pyridazinones.Both the intermediate 4,5-dihydro-6-(substituted)phenyl-3(2H)-pyridazinones and the 6-(substituted)phenyl-3(2H)-pyridazinones are useful as cardiotonic and antihypertensive agents.

    摘要翻译： 取代的4,5-二氢-6-（取代的）苯基-3（2H） - 哒嗪酮化合物和6-（取代的）苯基-3（2H） - 哒嗪酮化合物及其药学上可接受的盐可用作强心剂和抗高血压剂。 所述化合物引起狗中心肌收缩力的显着增加。 所述化合物还引起自发性高血压大鼠血压降低。 所述化合物通过使取代的γ-氧代苯丁酸与适当取代的肼反应制得，得到4,5-二氢-6-（取代的）苯基-3（2H） - 哒嗪酮，将其脱氢为6-（取代的）苯基-3（2H ） - 哒嗪酮。 中间体4,5-二氢-6-（取代的）苯基-3（2H） - 哒嗪酮和6-（取代的）苯基-3（2H） - 哒嗪酮均可用作强心剂和抗高血压剂。

    4,5-dihydro-6-[2-[4-(1H-imidazol-1-yl)phenyl]-ethenyl]-3(2H)- pyridazinones and related compounds
    58.
    发明授权
    4,5-dihydro-6-[2-[4-(1H-imidazol-1-yl)phenyl]-ethenyl]-3(2H)- pyridazinones and related compounds 失效
    -4,5-二氢-6- [2- [4-（1H-咪唑-1-基）苯基] - 乙烯基] -3（2H） - 哒嗪酮和相关化合物

    公开(公告)号：US4599332A

    公开(公告)日：1986-07-08

    申请号：US669323

    申请日：1984-11-09

    申请人： Ila Sircar

    发明人： Ila Sircar

    IPC分类号： C07D403/10 ,  C07D521/00 ,  A61K31/50

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D403/10

    摘要： 4,5-Dihydro-6-[2-[4-(1H -imidazol-1-yl)phenyl]alkylenyl or alkylene-3(2H)-pyridazinones and related compounds and pharmaceutically acceptable acid addition salts thereof are useful as cardiotonic and antihypertensive agents.The above compounds cause a significant increase in myocardial contractility in the dog and also cause a decrease in blood pressure in the spontaneously hypertensive rat. The compounds are produced by reacting the appropriate .gamma.-oxobutanoic acid with a suitably substituted hydrazine to provide 4,5-dihydro-6-[4-[imidazolylphenyl]-alkenylene or alkylene-3(2H)-pyridazinones which may be oxidized to 6-[4-[imidazolylphenyl]alkenylene or alkylene-3(2H)-pyridazinones.

    摘要翻译： 4,5-二氢-6- [2- [4-（1H-咪唑-1-基）苯基]亚烷基或亚烷基-3（2H） - 哒嗪酮及其相关化合物及其药学上可接受的酸加成盐可用作强心剂和 抗高血压药。 上述化合物引起狗中心肌收缩力的显着增加，并引起自发性高血压大鼠血压降低。 通过使合适的γ-氧代丁酸与适当取代的肼反应制得化合物，得到4,5-二氢-6- [4- [咪唑基苯基] - 亚烯基或亚烷基-3（2H） - 哒嗪酮，其可被氧化成6 - [4- [咪唑基苯基]亚烯基或亚烷基-3（2H） - 哒嗪酮。