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Oxyphthalazinyleddikesyre heterocyclic compounds and pharmaceutical compositions for the inhibition of aldose reductase activity

机译:用于抑制醛糖还原酶活性的羟基邻苯二甲酰二乙酮杂环化合物和药物组合物

摘要

A heterocyclic oxophthalazinyl acetic acid having aldose reductase inhibitory activity has the formula CHEM wherein X is oxygen or sulfur, Z is a covalent bond, O, S, NH or CH2; R1 is hydroxy, or a prodrug group; R2 is a heterocyclic group, R3 and R4 are hydrogen or the same or a different substituent, and R5 is hydrogen or methyl. The pharmaceutically acceptable acid addition salts of the above compounds wherein R1 is di(C1-C4)alkylamino or (C1-C4)alkoxy substituted by N-morpholino or di(C1-C4)alkylamino and the pharmaceutically active base addition salts of the above compounds wherein R1 is hydroxy are also aldose reductase inhibitors.
机译:具有醛糖还原酶抑制活性的杂环氧代邻苯二甲酰基乙酸具有式,其中X是氧或硫,Z是共价键,O,S,NH或CH 2; R1是羟基或前药基团; R 2为杂环基,R 3和R 4为氢或相同或不同的取代基,且R 5为氢或甲基。上述化合物的药学上可接受的酸加成盐,其中R1是被N-吗啉代或二(C1-C4)烷基氨基取代的二(C1-C4)烷基氨基或(C1-C4)烷氧基,以及上述药学上有效的碱加成盐R 1为羟基的化合物也是醛糖还原酶抑制剂。

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