US 6,603,012 B2 · RAR selective retinoid agonists

Abstract

New compounds containing bicyclic fused rings, one of which being a phenyl moiety connected by an aliphatic chain to a cycloalkyl or aryl moiety, and pharmaceutically active salts thereof are useful as RAR selective retinoid agonists. Furthermore, such retinoic acid receptor agonists, particularly retinoic acid receptor γ (RARγ) selective agonists, are useful for the treatment of emphysema and associated pulmonary diseases, as well as for the therapy and prophylaxis of dermatological disorders, for the therapy and prophylaxis of malignant and premalignant epithelial lesions, tumors and precancerous changes of the mucous membrane in the mouth, tongue, larynx, esophagus, bladder, cervix and colon.

Claims25

Dependent claims

A compound selected from the group consisting of compounds of formula I

wherein
R1 and R2 independently of each other are hydrogen or lower alkyl;
A is C(R5R6),
n is an integer 1,2 or 3,
B is C(R3R4);
X is —CR7′—;
R3, R4, R5 and R6 independently of each other are hydrogen or lower alkyl;
R7 and R7′ independently of each other are hydrogen, alkyl, alkenyl, alkoxy, alkoxyalkyl, substituted alkyl, phenyloxy or substituted phenyloxy, or R7 and R7′ together are —(CH2)p—, where p is 2-6,
Z is —CH2O—;
Ar is phenyl;
and
R8 is hydrogen, lower alkyl or benzyl;
and pharmaceutically acceptable salts of carboxylic acids of formula I.

10 more elements

Dependencies are inferred from the claim text.

RAR selective retinoid agonists

Life of this patent

RAR selective retinoid agonists

Life of this patent

Abstract

Claims25