Patent ID: 6387892
Filing Date: 2002-05-14
Classification: A61K,A61P,C07C,C07D

Abstract:
A method of inhibiting the enzyme cytochrome P450RAI in a mammal by administering to said mammal an effective dose of a pharmaceutical composition comprising a compound of the formula wherein A is heteroaryl selected from a group consisting of pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, oxazolyl, imidazolyl and pyrrazolyl, said heteroaryl groups being optionally substituted with one or two R2 groups; X is O, or S; Y is H, alkyl of 1 to 10 carbons, benzyl, lower alkyl or halogen substituted benzyl, fluoro-substituted alkyl of 1 to 10 carbons, cycloalkyl of 3 to 6 carbons, lower alkyl substituted cycloalkyl of 3 to 6 carbons, Cl, Br, or I; Z is â€”Câ‰¡Câ€”, â€”(CR1&boxH;CR1)n, where nâ€² is an integer having the value 1-5, â€”COâ€”NR1â€”, NR1â€”COâ€”; â€”COâ€”Oâ€”, â€”Oâ€”COâ€”, â€”CSâ€”NR1â€”, NR1â€”CSâ€”, â€”COâ€”Sâ€”, â€”Sâ€”COâ€”, â€”N&boxH;Nâ€”; R1 is independently H or alkyl of 1 to 6 carbons; p is an integer having the values of 0 to 4; R2 is independently H, alkyl of 1 to 6 carbons, F, Cl, Br, I, CF3, fluoro substituted alkyl of 1 to 6 carbons, alkoxy of 1 to 6 carbons, or alkylthio of 1 to 6 carbons; R3 is independently alkyl of 1 to 6 carbons, F, Cl, Br, I, fluoro substituted alkyl of 1 to 6 carbons, OH, SH, alkoxy of 1 to 6 carbons, alkylthio of 1 to 6 carbons or benzyl; m is an integer having the values 0 to 2; R4 is independently H, alkyl of 1 to 6 carbons, or F; fluorosubstituted alkyl of 1 to 6 carbons, or halogen; o is an integer having the values of 0 to 2; n is an integer having the values of 0 to 4, and R8 is H, alkyl of 1 to 6 carbons, â€”CH2O(C1-6-alkyl), or a cation of a pharmaceutically acceptable base.