RAR.gamma.-specific retinobenzoic acid derivatives

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...

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A61K 31245

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active

057600848

ABSTRACT:
Retinoid-like activity is exhibited by compounds of the formula ##STR1## wherein X is F, Cl, OH or CH.sub.3, Y is H or F, R.sub.1 -R.sub.6 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl, n is an integer of 1 to 4 and R.sub.7 is hydrogen or a carboxyl-protecting group, and pharmaceutically acceptable salts thereof. The compounds of the formula I selectively interact with the retinoic acid subtype RAR.gamma. and have been found to lack the liver toxicity associated with systemic administration of non-relative retinoids.

REFERENCES:
Multiplicity generates diversity in the retinoic acid signalling pathways, Mark Leid et al, Trends in Biochemical Sciences, 17: 427-433, 1995.
Rudd, et al., Cancer Lett. (Shannon, Irel.) 73(1), 41-9, 1993.
Taylor J. of Craniofacial Genetics and developmental Biology 15 (1) 13 Abstract, 1995.

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