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US 5,919,970 AGranted
Substituted diaryl or diheteroaryl methanes, ethers and amines having retinoid agonist, antagonist or inverse agonist type biological activity
AssigneeAllergan Sales, Inc.
InventorsTae K. Song, Min Teng, Roshantha A. Chandraratna
Life of this patent
Estimating the term…
Abstract
Compounds of the formula Y.sub.3 (R.sub.4)--X--Y.sub.1 (R.sub.1 R.sub.2)--Z--Y.sub.2 (R.sub.2)--A--B where the symbols have the meaning defined in the specification, have retinoid, retinoid antagonist or retinoid inverse agonist type biological activity.
Claims19
A compound of the formula ##STR13## where R.sub.1 is C.sub.3-10 branch-chained alkyl, where alkyl has up to 6 carbons;
- R.sub.2 is lower alkyl of 1 to 6 carbons;
- m is an integer between 0 to 2;
- X is S, or O;
- Z is
- --C.tbd.C--,
- --CH.dbd.CH--,
- --CO--NH--,
- --COO--,
- Y.sub.2 is a phenyl or naphthyl group, said pheny or naphthyl groups being unsubstituted or substituted with one or two R.sub.2 groups;
- Y.sub.3 is phenyl or naphthyl, said pheny or naphthyl groups being unsubstituted or substituted with one to three R.sub.4 groups, where R.sub.4 is alkyl of 1 to 10 carbons;
- A is (CH.sub.2).sub.q where q is 0-5, and
- B is COOH or a pharmaceutically acceptable salt thereof or COOR.sub.8, where R.sub.8 is an alkyl group of 1 to 10 carbons or (trimethylsilyl)alkyl where the alkyl group has 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R.sub.8 is phenyl or lower alkylpheny.
9 more elements
A compound of the formula ##STR14## R.sub.2 is H;
- where R.sub.4 and R.sub.4 * are independently selected from H and C.sub.1-6 alkyl;
- Z is --C.tbd.C--, --CH.dbd.CH--, --CO--NH--, or --COO--;
- X.sub.3 is CH, and
- R.sub.8 is H, lower alkyl of 1 to 6 carbons, tri(lowerC.sub.1-6 alkyl)lsilyl-lowerC.sub.1-6 alkyl, benzyl, or a pharmaceutically acceptable salt of said compound.
1 more element
Dependencies are inferred from the claim text.