2-CYANO-4-AMINOPYRIMIDINE COMPOUNDS WITH INHIBITOR ACTION ON CATHEPSIN K, PHARMACEUTICAL COMPOUND AND METHODS OF OBTAINING THEM (ALTERNATIVES) Russian patent published in 2008 - IPC C07D239/42 C07D401/12 C07D403/12 A61K31/506 A61K31/505 A61P29/00 

FIELD: chemistry.

SUBSTANCE: invention pertains to compounds with formula II or IIa and their pharmaceutically acceptable salts or esters, with inhibitor action on cathepsin K, in which R2 is chosen respectively from H, 2-ethylbutyl, isobutyl or 2,2-dimethylpropyl; or C₃-C₆cycloalkyl, predominantly cyclopropyl, cyclopentyl or cyclohexyl, R5' represents 4-methoxyphenyl, 4-(1-propylpiperidine-4-yl)phenyl, 4-(4-methylpiperazin-1-yl)phenyl, 4-[1-(2-methoxyethyl)piperidine-4-yl]phenyl, 4-(4-propylpiperazin-1-yl)phenyl, 3-[4-(4-methylpiperazin-1-yl)phenyl]propionyl, 3-[3-(4-methylpiperazin-1-yl)phenyl]propionyl, 4-(4-ethylpiperazin-1-yl)phenyl, 4-(4-isoporylpiperazin-1-yl)phenyl, 4-[4-(2-ethoxyethyl)piperazin-1-yl]phenyl, 4-[4-(2-methoxyethyl)piperazin-1-yl]phenyl, 4-piperazin-1-yl phenyl, 4-[4-(tert-butyl ester of a carboxylic acid)piperazino-1-yl]phenyl, 3-(4-methylpiperazin-1-yl)phenyl, 3-(4-ethylpiperazin-1-yl)phenyl, 3-(4-isopropylpiperazin-1-yl)phenyl, 3-[4-(2-mthoxyethyl)piperazin-1-yl]phenyl, 3-[4-(2-ethoxyethyl)piperazin-1-yl]phenyl, 3-(2-pyrrolidine-1-yl ethoxy)phenyl, 3-(2-dimethylaminoethoxy)-4-methoxyphenyl, 4-dimethylaminomethylphenyl, 4-(4-methylpiperazin-1-yl methyl)phenyl, 4-[1-(2-methoxyethyl)piperazin-4-yl methyl]phenyl, 4-methoxy-3-(2-piperidine-1-yl ethoxy)phenyl, 3-[4-(4-ethylpiperazin-1-yl)phenyl]-2,2-dimethylpropionyl, 3-[4-(4-propylpiperazin-1-yl)phenyl]propionyl, 3-(4-pyrrolidine-1-yl phenyl)propionyl, 3-[3-(4-ethylpiperazin-1-yl)phenyl]-2,2-dimethylpropionyl, 3-{3-[4-(2-methoxyethyl)piperazin-1-yl]phenyl}-2,2-dimethylpropionyl, 3-(3-pyrrolidine-1-yl phenyl)propionyl, 2-[4-(4-methylpiperazin-1-yl)phenyl]isobutyl, 2-(4-methoxyphenyl)acetyl, 2-(3-methoxyphenyl)acetyl, 2-[4-(4-methylpiperazin-1-yl)phenyl]acetyl, 2-[4-(4-ethylpiperazin-1-yl)phenyl]acetyl, 2-[4-(4-isopropylpiperazin-1-yl)phenyl]acetyl, 2-(4-pyrrolidine-1-yl phenyl)acetyl, 2-[4-(2-diethylaminoethylamino)phenyl]isobutyl, 2-(4-pyrrolidine-1-yl phenyl)isobutyl. R5 "' and R6'" are respectively shown in the formula of invention.

EFFECT: cathepsin K inhibitor properties.

7 cl, 2 tbl, 109 ex