Patent ID: 6541503
Filing Date: 2003-04-01
Classification: A61P,C07D

Abstract:
A compound of formula (I): whereinX is N, CH or CCH3; R1 is hydrogen, nitro, carboxamide, isopropyl, hydroxymethyl, pyridin-4-ylethyl, ethoxycarbonyl, iodo, isobutyl, 2-methyl-propenyl, 2-methyl-1-butenyl, 2-methyl-2-butenyl, 2-methylbutyl, cyclobutyl-methyl, cyclobutylidenemethyl, 4-hydroxyphenyl-ethyl, 4-hydroxyphenyl-vinyl, phenoxy, isopropoxy, pyrazol-3-yl, methyl or chloro; R2 is hydrogen, oxazol-5-yl, pentafluorophenoxycarbonyl, nitro, hydroxy, methoxy, methyl, triazol-1-yl, sulfonate, carboxamide, methoxycarbonyl, bromo, iodo, aminosulfonyl, methylsulfonyl, methylaminosulfonyl, methyloxime, phenyl, N,N-dimethylaminocarbonyl, N-furan-2-ylmethylaminocarbonyl, N-(N-morpholino)ethylaminocarbonyl, N-(1,5-dimethoxybenzyl)aminocarbonyl, N-(imidazol-1-yl)ethylaminocarbonyl, N-(imidazol-1-yl)propylaminocarbonyl, N-(methoxyethyl)aminocarbonyl, N-(hydroxyethyl)aminocarbonyl, N-(hydroxypropyl)aminocarbonyl, N-(3-hydroxy-2,2-dimethylpropyl)aminocarbonyl, N-(pyrid-3-ylmethyl)aminocarbonyl, quaternary ammonium, methylcarbonylamino or isobutoxycarbonyl; R3 is hydrogen, bromo, chloro, methyl, ethyl, isopropyl, hydroxy, hydroxymethyl, phenoxy, or ethoxy; R4 is in the para-position of the phenyl ring relative to the NH group, and is selected from aminosulfonyl, N-methylaminosulfonyl, methylsulfonyl, N,N-dimethylaminosulfonyl, aminosulfonylamino, N-hydroxyethoxyethylaminosulfonyl, N-hydroxyethylaminosulfonyl, N-(3-hydroxy-2,2-dimethyl-propyl)aminosulfonyl-methyl, N-methylaminosulfonyl-methyl, indazol-6-ylaminosulfonyl, thiazol-2-ylaminosulfonyl, N-amino-iminomethyl-aminosulfonyl, N-pyrid-2-ylaminosulfonyl, aminosulfonyl-methyl, N-allylaminosulfonyl-methyl, methylsulfonylmethyl, N-(3-hydroxy-2,2-dimethyl-propyl)aminosulfonyl, N-(3-trifluoromethylphenyl)aminosulfonyl, N-pyrimidin-2-ylaminosulfonyl, N-(5-methyl-thiadiazol-2-yl)aminosulfonyl, N-methylcarbonylaminosulfonyl, N-phenylcarbonylaminosulfonyl, N-hydroxyethoxyethyl-N-methylaminosulfonyl, N-methoxyethoxyethoxyethoxyethyl-aminosulfonyl and N-(pyridin-4-yl-methyl)aminosulfonyl; R5 is hydrogen; with the proviso that R1, R2 and R3 cannot simultaneously each represent hydrogen; and the pharmaceutically acceptable salts, biohydrolyzable esters, biohydrolyzable amides, biohydrolyzable carbamates, solvates, hydrates, affinity reagents or prodrugs thereof in either crystalline or amorphous form.