Substituted triazoles as angiotensin II inhibitors
    4.
    发明公开
    Substituted triazoles as angiotensin II inhibitors 失效
    取代三唑仑als血管紧张素II抑制剂。

    公开(公告)号:EP0554107A1

    公开(公告)日:1993-08-04

    申请号:EP93300661.1

    申请日:1993-01-29

    CPC分类号: C07D403/10 C07D249/12

    摘要: This invention relates to novel bis-biphenyl substituted 3-mercapto-1,2,4-tetrazoles and to pharmaceutically acceptable salts thereof.
    The compounds are angiotensin II receptor antagonists, and are useful in treating hypertension (lowering high blood pressure), congestive heart failure, elevated ocular pressure, cerebral stroke, angina, cardiac insufficiency, myocardial infarction or diabetic nephropathy.
    The invention also relates to a pharmaceutical composition comprising a compound of the invention, a method of treating a physiological condition in a mammal that is mediated by angiotensin 11 which comprises administering to the mammal an effective amount of a compound of the invention, and novel processes for preparing the compounds of the invention.

    摘要翻译: 本发明涉及新的双联苯基取代的3-巯基-1,2,4-四唑及其药学上可接受的盐。 这些化合物是血管紧张素II受体拮抗剂,可用于治疗高血压(降低高血压),充血性心力衰竭,眼压升高,脑中风,心绞痛,心功能不全,心肌梗塞或糖尿病肾病。 本发明还涉及包含本发明化合物的药物组合物,治疗由血管紧张素11介导的哺乳动物中的生理状况的方法,其包括给予哺乳动物有效量的本发明化合物和新方法 用于制备本发明的化合物。

    Substituted N-biphenylyl lactams
    5.
    发明公开
    Substituted N-biphenylyl lactams 失效
    取代基N-二苯基甲酰胺。

    公开(公告)号:EP0542554A1

    公开(公告)日:1993-05-19

    申请号:EP92310353.5

    申请日:1992-11-12

    摘要: This invention relates to novel N-biphenylyl lactam compounds having a substituted methylidene or methyl moiety adjacent to the lactam nitrogen, and pharmaceutically acceptable salts thereof.
    The compounds are angiotensin II receptor antagonists, and are useful in treating hypertension (lowering high blood pressure), congestive heart failure, elevated ocular pressure, cerebral stroke, angina, cardiac insufficiency, myocardial infarction or diabetic nephropathy.
    The invention also relates to a pharmaceutical composition comprising a compound of the invention, a method of treating a physiological condition in a mammal that is mediated by angiotensin II which comprises administering to the mammal an effective amount of a compound of the invention, and novel processes for preparing the compounds of the invention.

    摘要翻译: 本发明涉及具有邻近内酰胺氮的取代亚甲基或甲基部分的新型N-联苯酰基内酰胺化合物及其药学上可接受的盐。 这些化合物是血管紧张素II受体拮抗剂,可用于治疗高血压(降低高血压),充血性心力衰竭,眼压升高,脑中风,心绞痛,心功能不全,心肌梗塞或糖尿病肾病。 本发明还涉及包含本发明化合物的药物组合物,一种治疗由血管紧张素II介导的哺乳动物的生理状态的方法,其包括向哺乳动物施用有效量的本发明化合物和新方法 用于制备本发明的化合物。

    Regioselective synthesis of 1,5-diaryl pyrazole anti-inflammatory agents
    7.
    发明公开
    Regioselective synthesis of 1,5-diaryl pyrazole anti-inflammatory agents 失效
    Regioselektive Synthese von 1,5-Diaryl-Pyrazole,verwendbar alsentzündungshemmendeMittel。

    公开(公告)号:EP0534800A2

    公开(公告)日:1993-03-31

    申请号:EP92308811.6

    申请日:1992-09-28

    摘要: The invention provides a process for preparing 1,5-diaryl pyrazole anti-inflammatory agents. A 6-aryl-4,6-dioxohexanoic acid is treated with acetic anhydride or acetyl chloride to produce an enol lactone, which is added to methylhydroxylamine to generate the dione hydroxamic acid. This dione hydroxamic acid is then treated with 4-methoxyphenylhydrazine hydrochloride to yield the 1,5-diaryl pyrazole. Novel intermediate compounds in the synthetic pathway are also disclosed.

    摘要翻译: 本发明提供了制备1,5-二芳基吡唑抗炎剂的方法。 将6-芳基-4,6-二氧代己酸用乙酸酐或乙酰氯处理以产生烯醇内酯,将其加入到甲基羟胺中以产生二酮异羟肟酸。 然后用4-甲氧基苯肼盐酸盐处理该二酮异羟肟酸,得到1,5-二芳基吡唑。 还公开了合成途径中的新型中间体化合物。