| 摘要 |
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 cycl ic 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, C 1- 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(OR7)2, -(CH2)pOR5, -(CH2)q-CH=CH-CN, -(CH2)q- CH=CH-CO2H, -(CH2)p-CH=CH-CONHR5R6, -(CH2)pNHCOR8 or -(CH2)pNR9R10; R5 and R 6 are independently hydrogen or C1-6alkyl; R7 is C1-6alkyl;R8 is C1-7alkyl, or optionally substituted aryl, heteroaryl, arylC1-6alkyl or heteroaryl C1- 6alkyl; R9 and R10 are independently selected from hydrogen, C1-6alkyl, aryl and arylC1-6alkyl; p is 0-4; and q is 1-4 and salts and solvates thereof, ar e disclosed, as are methods for their preparation, pharmaceutical compositions containing them and their use in medicine.
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