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2. 发明授权

US5583123A Certain tetrazole derivatives 失效
标题翻译：某些四唑衍生物
公开(公告)号：US5583123A
公开(公告)日：1996-12-10
申请号：US361411
申请日：1994-12-22
申请人： St ephane De Lombaert
发明人： St ephane De Lombaert
IPC分类号： C07F9/6524 , C07F9/6558 , A61K31/675 , C07F9/58 , C07F9/653
CPC分类号： C07F9/6524 , C07F9/65583
摘要： The present invention relates to the phosphono-alkylamino-substituted tetrazole derivatives of formula I ##STR1## and tautomers thereof wherein R.sub.1 is (carbocyclic or heterocyclic) aryl-C.sub.1 -C.sub.4 -alkyl; X is phenylene, phenylene substituted by lower alkoxy, lower-alkyl, halogen or trifluoromethyl or X.sub.1 is ethynylene; R.sub.2 is carbocyclic or heterocyclic aryl; pharmaceutically acceptable mono- or di-ester derivatives thereof in which one or both of the acidic hydroxy groups of the phosphono functional group are esterified in form of a pharmaceutically acceptable mono- or di-ester, and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising said compounds; methods for preparation of said compounds and for the preparation of intermediates; and methods of treating disorders in mammals which are responsive to the inhibition of endothelin-converting enzyme by administration of said compounds to mammals in need of such treatment.
摘要翻译：本发明涉及式I的膦酰 - 烷基氨基取代的四唑衍生物（I）及其互变异构体，其中R 1是（碳环或杂环）芳基-C 1 -C 4 - 烷基; X是亚苯基，被低级烷氧基，低级烷基，卤素或三氟甲基取代的亚苯基，或X 1是亚乙炔基; R2是碳环或杂环芳基; 其中膦酰基官能团的酸性羟基中的一个或两个以药学上可接受的单酯或二酯的形式酯化的药学上可接受的单酯或二酯衍生物及其药学上可接受的盐; 包含该化合物的药物组合物制备所述化合物和制备中间体的方法; 以及通过将所述化合物施用于需要这种治疗的哺乳动物来治疗对内皮素转化酶的抑制有反应的哺乳动物疾病的方法。

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