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HALOGEN-SUBSTITUTED BENZOPYRAN- AND BENZOTHIOPYRAN-4-CARBOXYLIC ACIDS, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME

申请公布号:DE2965755(D1)

申请号:DE19792965755

申请日期:1979.11.06

申请公布日期:1983.07.28

申请人:
PFIZER INC.

发明人:BELLETIRE, JOHN L.

分类号:A61K31/35;A61K31/352;A61K31/38;A61K31/382;A61P3/08;A61P3/10;A61P25/00;A61P27/02;A61P27/12;C07D311/04;C07D311/22;C07D311/58;C07D311/92;C07D335/06;C07F7/18;(IPC1-7):07D311/58;61K31/38;61K31/35;07D335/06;07D311/92

主分类号:A61K31/35

摘要:Benzopyran- and benzothiopyran-4 -carboxylic acid aldose reductase inhibitors of the formula: <CHEM> or a pharmaceutically acceptable salt thereof, wherein x is 0, S, S = O or <CHEM> n is zero or one; R is hydrogen or alkyl of 1 to 4 carbon atoms; R1 is hydrogen, chloro, bromo, fluoro or phenyl; R2 and R3 when taken individually, are each hydrogen, alkyl of 1 to 3 carbon atoms, chloro, bromo or fluoro; and when taken together, R2, R3 and the carbon atoms to which they are connected form a fused benzene ring; with the proviso that at least one of R1, R2 and R3 is chloro, bromo or fluoro. The compounds are useful in the treatment of diabetic-associated complications, such as cataracts, neuropathy or retinopathy, in a diabetic host. Also disclosed are methods for preparing the compounds of the formula (I) and their salts, and pharmaceutical compositions containing them.

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