Patent ID: 6576645
Filing Date: 2003-06-10
Classification: A61P,C07C,C07D

Abstract:
A compound of the formula: wherein R1 is H, halogen, OCH3, or OH; R2 is selected from the group consisting of â€”Yâ€”(CH2)nCH2â€”Oâ€”R6, 2,3-dihydroxypropoxy, 2-methylsulfamylethoxy, 2-chloroethoxy, 1-ethyl-2-hydroxyethoxy, 2,2-diethyl-2-hydroxyethoxy, and carboxymethoxy; where X is NH or S; n is an integer from 1 to 4; R4 and R5, which are the same or different, are a 1 to 4 carbon alkyl, H, â€”CH2Câ‰¡CH or â€”CH2CH2OH; or R4 and R5 form an N-containing five- or six-membered ring or heteroaromatic ring selected from the group consisting of an imidazole ring and a piperidine ring; Y is O, NH or S; and R6 is H, â€”CH2CH2OH, or â€”CH2CH2Cl; and R3 is H, halogen, OH or â€”OCH3; or a stereoisomer; or a non-toxic pharmaceutically acceptable salt or ester thereof or mixtures thereof,provided that when R2 is â€”Oâ€”CH2CH2â€”OH or â€”Oâ€”CH2COOH in the 4-position of the phenyl, then R1 and R3, cannot simultaneously be H, or OH in the 4-position of the phenyl; and if R1 is OH in the 4-position of the phenyl, R3 cannot be H.