Pyridylacrylamide derivatives and nephritis remedies and...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 213/57 (2006.01) A61K 31/44 (2006.01) A61K 31/535 (2006.01) C07D 213/56 (2006.01) C07D 213/59 (2006.01) C07D 213/61 (2006.01) C07D 213/66 (2006.01) C07D 213/80 (2006.01) C07D 401/12 (2006.01)

Patent

CA 2298480

Compounds represented by general formula (I), and nephritis remedies and TGF- .beta. inhibitors containing the same, wherein Ar1 is (substituted) pyridyl; Ar2 is (substituted) phenyl; R1 is H, alkyl or aryl; R2 is H, alkyl, cyano or alkoxycarbonyl; R3 is H or (substituted) alkyl; X is O or S; A and B are each H, OH, alkoxy or alkylthio, or alternatively they together form oxo, thioxo, =N-Y (wherein Y is dialkylamino, OH, aralkyloxy or alkoxy) or -Z1-M-Z2- (wherein Z1 and Z2 are each O, S or optionally alkyl-substituted imino; and M is alkylene or phenylene), or B may be 1-alkylimidazol-2-yl with A being OH; and n is an integer of 1 to 3.

L'invention concerne des composés de la formule (I), des remèdes contre la néphrite et des inhibiteurs de TGF-bêta contenant lesdits éléments. Dans ladite formule, Ar?1¿ est pyridyle (substitué); Ar?2¿ est phényle (substitué); R?1¿ est H, alkyle ou aryle; R?2¿ est H, alkyle, cyano ou alcoxycarbonyle; R?3¿ est H ou alkyle (substitué); X est O ou S; A et B sont l'un et l'autre H, OH, alcoxy ou alkylthio, ou forment, dans une composition différente, oxo, thioxo, =N-Y (Y étant dialkylamino, OH, aralkyloxy ou alcoxy) ou -Z?1¿-M-Z?2¿- (Z?1¿ et Z?2¿ étant l'un et l'autre O, S ou éventuellement imino alkyle-substitué; et M est alkylène ou phénylène), ou B peut être 1-alkylimidazole-2-yle, A étant OH; et n est un entier compris entre 1 et 3.

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