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BENZOPYRANO 4,3-C PYRAZOLES AND PYRAZOLO 4,3-C QUINOLINES

机译:苯并吡喃4,3-C吡咯和吡唑并4,3-C喹啉

摘要

This invention provides a benezene-fused heterocyclic compound of the formula: IMAGE wherein R1 is halogen, nitro, amino, hydroxy, lower alkyl, lower alkoxy substituted by carboxy or protected carboxy, acylamino which may have lower alkyl on the amino moiety, or aryloxy which may have halogen, R2 is hydrogen or halogen, X is -O- or IMAGE in which R3 is hydrogen, lower alkyl or acyl and A is a group of the formula: IMAGE in which R4 is hydrogen, lower alkenyl, lower alkynyl or alkyl which may have suitable substituent(s) selected from the groups consisting of hydroxy, acyl, lower alkoxy, di(lower)alkylamino, carboxy, protected carboxy and aryl; or R1 is hydrogen or lower alkoxy, R2 is hydrogen, X is IMAGE in which Ra3 is lower alkanoyl and A is a group of the formula: IMAGE and pharmaceutically acceptable salts thereof. This compound possesses diuretic activity, uricosuric activity and vasodilative activity and are useful as a diuretic agent, uricosuric agent and anti-hypertensive agent. The invention further relates to processes for the preparation of this compound and pharmaceutical composition comprising compound of the above formula.
机译:本发明提供下式的苯并稠合的杂环化合物:其中R 1为卤素,硝基,氨基,羟基,低级烷基,被羧基或被保护的羧基取代的低级烷氧基,在氨基部分上可能具有低级烷基的酰基氨基,或R 2为氢或卤素的芳氧基,X为-O-或,其中R3为氢,低级烷基或酰基,A为下式的基团:,其中R4为氢,可以具有选自羟基,酰基,低级烷氧基,二(低级)烷基氨基,羧基,受保护的羧基和芳基的合适的取代基的低级烯基,低级炔基或烷基;或R 1为氢或低级烷氧基,R 2为氢,X为,其中Ra 3为低级烷酰基,且A为下式的基团:及其药学上可接受的盐。该化合物具有利尿活性,尿酸尿酸活性和血管舒张活性,并且可用作利尿剂,尿酸尿酸剂和抗高血压药。本发明进一步涉及该化合物的制备方法和包含上式化合物的药物组合物。

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