Patent ID: 6534544
Filing Date: 2003-03-18
Classification: A61K,A61P,G01N

Abstract:
A process of administering to a mammal a retinoid compound which binds specifically or selectively to a RAR&agr;, retinoid receptors in preference over RAR&bgr; and RAR&ggr; retinoid receptors, for the purpose of treating or preventing a disease or condition which is responsive to treatment by RAR&agr; specific or selective retinoid agonists, said disease or condition being premalignant and malignant hyperproliferative diseases and Kaposi sarcoma where the RAR&agr;, specific or selective retinoid compound has the formula (i) where X1 is (C(R1)2)n where n is an integer between 0 and 2; R1 is independently H or alkyl of 1 to 6 carbons; R2 is independently hydrogen, or lower alkyl of 1 to 6 carbons; R3 is hydrogen, lower alkyl of 1 to 6 carbons or F; m is an integer having the value of 0-5; o is an integer having the value of 0-4; p is an integer having the value of 0-2; r is an integer having the value 0-2; Y is a phenyl or naphthyl group, said phenyl or naphthyl groups being optionally substituted with one or two R2 groups; W1 is a substituent selected independently from the group consisting of F, Br, Cl, I, fluoro substituted C1-6 alkyl, NO2, and OH, with the provisos that: (i) when Z is O then the sum of p and r is at least 1 and W1 is not a fluoro, group in the 3 position of a tetrahydronaphthalene ring; (ii) when r is zero and p is 1 and W1 is OH then the OH group is positioned &agr; to the L group; W2 is a substituent selected independently from the group consisting of F, Br, Cl, I, fluoro substituted C1-6 alkyl, NO2, and OH; L is â€”(C&boxH;Z)â€”NHâ€” or â€”NHâ€”(C&boxH;Z)â€”Z is O or S, and B is COOH or a pharmaceutically acceptable salt thereof, or COOR8 where R8 is an alkyl group of 1 to 10 carbons or trimethylsilylalkyl where the alkyl group has 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons.