Back to results
US 4,537,892 AGranted
Spiro-tricyclicaromatic succinimide derivatives as inhibitors of aldose reductase
AssigneeAlcon Laboratories, Inc.
InventorBillie M. York, Jr.
Life of this patent
Estimating the term…
Abstract
Disclosed are substituted or unsubstituted planar tricyclic fluorene or nuclear analogs thereof, spiro-coupled to a five-membered ring containing a secondary amide, and the pharmaceutically acceptable salts thereof. These compounds are useful, inter alia, in the treatment of diabetes. Also disclosed are processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when indicated for, inter alia, long term, prophylactic treatment of the diabetes syndrome.
Claims72
A compound of the formula:
- ##STR182## and the pharmaceutically acceptable salts thereof, wherein A and B are aromatic rings connected through two adjacent positions to a central five-membered ring, and are independently selected from the group consisting of:
- ##STR183## U is selected from the group consisting of O, S, and NR.sup.1 ;
- X is selected from the group consisting of H, F, lower alkyl sulfide, and lower alkylsulfinyl;
- Y is selected from H, --OH, --OCOR.sup.3, F, Cl, lower alkyl, lower alkoxy, lower alkylsulfide, lower alkylsulfinyl, lower alkylsulfonyl, --CF.sub.3, --S--CF.sub.3, --SO.sub.2 CF.sub.3, CO--N(R.sup.1)--R.sup.2, lower alkyl alcohol, lower alkyl ether, nitro, lower alkyl sulfide lower alkyl, lower alkylamine, lower alkyl esters, --COOH and lower alkyl ester, lower alkyl carboxylic acids and lower alkyl esters, and cycloalkyl of six or less carbons, provided that when both of Rings A and B are phenyl, and one of X or Y is H or F, the other of X or Y must be other than H or F;
- and
- R.sup.1 and R.sup.2 are selected from the group consisting of hydrogen and lower alkyl;
- R.sup.3 is lower alkyl;
- Z is selected from the group consisting of hydrogen, lower alkyl, and halogen;
- t is selected from the group consisting of CHR.sup.1, NH, O, and S.
6 more elements
Dependencies are inferred from the claim text.