Thiazoles as nf-kb inhibitors (proteasome inhibitors)

Details Thiazoles as nf-kb inhibitors (proteasome inhibitors) Thiazoles as nf-kb inhibitors (proteasome inhibitors)

C - Chemistry, Metallurgy

07

D

C07D 417/14 (2006.01) A61K 31/427 (2006.01) A61P 35/00 (2006.01) C07D 471/04 (2006.01) C07D 491/04 (2006.01) C07D 495/04 (2006.01) C07D 519/00 (2006.01)

Patent

CA 2646516

The present invention relates to compounds of the general formula(Ig) or pharmaceutically acceptable salts thereof with an acid or a base, or pharmaceutically acceptable prodrugs or a stereoisomer thereof, (formula Ig) wherein R1 independently represents H, alkyl, cycloalkyl, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl, or heteroaryl; R2 independently represents NR3R5, (formula II) R3 independently represents H, COR6, CO2R6, SOR6, o SO2R6, SO3R6, alkyl, cycloalkyl, alkoxy, -NH2, alkylamine, -NR7COR6, halogen, -OH, -SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R5 independently represents H, COR6, CO2R6, SOR6, SO2R6, SO3R6, alkyl, cycloalkyl, alkoxy, -NH2, alkylamine, -NR7COR6, halogen, -OH, -SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R 6 independently represents H, alkyl, cycloalkyl, -NH2, alkylamine, aryl or heteroaryl; R7 independently represents H, alkyl, cycloalkyl, alkoxy, -OH, -SH, alkylthio, hydroxyalkyl, aryl, or heteroaryl; P is 0, or 1; q is 0, or 1; x is CO, CS, or SO2.

L'invention concerne des composés de formule générale (Ig) ou des sels pharmaceutiquement acceptables de ceux-ci associés à un acide ou à une base, ou des promédicaments pharmaceutiquement acceptables de ceux-ci ou un stéréoisomère de ceux-ci. Dans la formule (Ig), R1 représente indépendamment H, alkyle, cycloalkyle, hydroxyalkyle, haloalkyle, haloalkyloxy, aryle ou hétéroaryle; R2 représente indépendamment NR3R5, (formule II) R3 représente indépendamment H, COR6, CO2R6, SOR6, SO2R6, SO3R6, alkyle, cycloalkyle, alkoxy, -NH2, alkylamine, -NR7COR6, halogène, -OH, -SH, alkylthio, hydroxyalkyle, haloalkyle, haloalkyloxy, aryle ou hétéroaryle; R5 représente indépendamment H, COR6, CO2R6, SOR6, SO2R6, SO3R6, alkyle, cycloalkyle, alkoxy, -NH2, alkylamine, -NR7COR6, halogène, -OH, -SH, alkylthio, hydroxyalkyle, haloalkyle, haloalkyloxy, aryle ou hétéroaryle; R 6 représente indépendamment H, alkyle, cycloalkyle, -NH2, alkylamine, aryle ou hétéroaryle; R7 représente indépendamment H, alkyle, cycloalkyle, alkoxy, -OH, -SH, alkylthio, hydroxyalkyle, aryle, ou hétéroaryle; P désigne 0, ou 1; q désigne 0, ou 1; x désigne CO, CS, ou SO2.

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