フェニル置換トリアゾール類およびALK5キナーゼの選択的阻害剤としてのその使用

Japanese Patent JP2005518352

A

Phenyl substituted triazoles of formula (I) wherein R1 is naphthyl or phenyl optionally substituted with one or more substituents selected from halo, -O-C1-6alkyl, -S-C1-6alkyl, C1-6alkyl, C1-6haloalkyl, -O-(CH2)n-Ph, -S-(CH2)n-Ph, cyano, phenyl, and CO2R, wherein R is hydrogen or C1-6alkyl, and n is 0, 1, 2 or 3; or R1 is phenyl or pyridyl fused with an aromatic or non-aromatic cyclic ring of 5-7 members wherein said cyclic ring optionally contains up to three heteroatoms, independently selected from N, O and S, and N may be further optionally substituted by C1-6 alkyl, and wherein the cyclic ring may be optionally substituted by =O; R2 and R3 are independently selected from H, C1-6alkyl, C1-6alkoxy, phenyl, NH(CH2)n-Ph, NH-C1-6alkyl, halo, alkoxy, CN, NO2, CONHR and SO2NHR; two of X1, X2 and X3 are N and the other is NR4 wherein R4 is hydrogen, C1-6alkyl, C3-7cycloalkyl, -(CH2)p-CN, -(CH2)p-CO2H, -(CH2)p-CONHR5R6, -(CH2)pCOR5, -(CH2)q(CR7)2, -(CH2)pOR5, (CH2)qCH=CH-CN, -(CH2)q-CH=CH-CO2H, -(CH2)p-CH=CH-CONHR5R6, -(CH2)pNHCOR8 or -(CH2)p