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N-ISOXAZOLYL-SULFONAMIDE DERIVATIVES, PHARMACEUTICAL PREPARATIONS CONTAINING THEM AND PROCESS FOR THEIR PREPARATION

机译:N-异恶唑基-磺酰胺衍生物,包含它们的药物制剂及其制备方法

摘要

The present invention relates to novel N-isoxazolylnaphthalenesulfonamide derivatives of formula (I) and their pharmaceutically acceptable salts, to pharmaceutical compositions containing them, and to the preparation of such compounds and pharmaceutical compositions. In the formula, one of X and Y is nitrogen and the other is oxygen; R 2 is halogen or hydroxy, carboxy, amino, C 1 -C 7 alkoxy, C 2 -C 7 alkenyl, C 1 -C 7 hydroxyalkyl, (C 1 -C 7 alkoxy) carbonyl, mono- or di- C 7 -C 7 alkylamino, mono- or di (C 1 -C 7 alkyl) amino (C 1 -C 7 alkyl), phenyl (C 1 -C 7 alkyl) amino, (C 1 -C 7 alkoxy) - carbonyl (C1 -C7 alkyl) amino, C1 -C7 alkanoylamino, phenyl (C1 -C7 alkyl) carbonylamino, [di (phenyl) (C1 -C7 alkyl)] -amino, (di (phenyl) - (C 1 -C 7) alkyl, carbonyl-amino, carboxy (C 1 -C 7) -alkylamino, 3-phenyl (thio-ureido) or optionally naphthyl optionally substituted by oxo-substituted, 5-7-membered saturated mono- nitrogen-containing heterocyclyl attached to its nitrogen atom, R4 and R5 are hydrogen, ornitro, phenyl, C1-7 alkyl, phenyl (C1-7 alkyl) or (1-7 hay alkoxy) carbonyl or R4 and R5 taken together form - (CH2) 4. The compounds of the formula I are endothelial antagonists and are useful inter alia for the treatment of hypertension. ŕ
机译:本发明涉及式(I)的新的N-异恶唑基萘磺酰胺衍生物及其药学上可接受的盐,涉及包含它们的药物组合物,以及此类化​​合物和药物组合物的制备。式中,X和Y之一为氮,另一个为氧。 R 2是卤素或羟基,羧基,氨基,C 1 -C 7烷氧基,C 2 -C 7烯基,C 1 -C 7羟烷基,(C 1 -C 7烷氧基)羰基,单或二C 7- C 7烷基氨基,单或二(C 1 -C 7烷基)氨基(C 1 -C 7烷基),苯基(C 1 -C 7烷基)氨基,(C 1 -C 7烷氧基)-羰基(C1- C 7烷基)氨基,C 1 -C 7烷酰基氨基,苯基(C 1 -C 7烷基)羰基氨基,[二(苯基)(C 1 -C 7烷基)]-氨基,(二(苯基)-(C 1 -C 7)烷基,羰基-氨基,羧基(C 1 -C 7)-烷基氨基,3-苯基(硫代-脲基)或任选地萘基,其任选地被与其氮原子相连的氧代取代的5-7元饱和单氮杂环基取代, R4和R5是氢,硝基,苯基,C1-7烷基,苯基(C1-7烷基)或(1-7干草烷氧基)羰基或R4和R5一起形成-(CH2)4。式I化合物是内皮拮抗剂,尤其可用于治疗高血压。

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