428817-45-2

Upstream product

• 768-60-5 4-methoxyphenylacetylen 
• 5315-25-3 2-bromo-6-methylpyridine 
• 428817-57-6 2-(4-methoxy-phenylethynyl)-6-methyl-pyridine 

Downstream Products

• 710947-01-6 4-[4-(4-methoxy-phenyl)-5-(6-methyl-pyridin-2-yl)-[1,2,3]triazol-2-ylmethyl]-benzonitrile 
• 710947-12-9 4-[4-(4-methoxy-phenyl)-5-(6-methyl-pyridin-2-yl)-[1,2,3]triazol-2-yl]-benzonitrile 

Relevant academic research and scientific papers

Synthesis and biological evaluation of novel 2-pyridinyl-[1,2,3]triazoles as inhibitors of transforming growth factor β1 type 1 receptor

A series of 2-pyridinyl-[1,2,3]triazoles have been synthesized and evaluated for their ALK5 inhibitory activity in the luciferase reporter assays. Compound 8d showed significant ALK5 inhibition (SBE-luciferase activity, 25%; p3TP-luciferase activity, 17%) at a concentration of 5μM that is comparable to that of SB-431542 (SBE-luciferase activity, 21%; p3TP-luciferase activity, 12%), but weak p38α MAP kinase inhibition (13%) at a concentration of 10μM that is much lower than that of SB-431542 (54%).

Pyridyl-substituted triazoles as tgf inhibitors

Pyridyl substituted triazoles of formula (I) wherein R1 is naphthyl or phenyl optionally substituted with one or more substituents selected from the group consisting of 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 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; R2 is H, C1-6alkyl, C1-6alkoxy, phenyl, NH(CH2)n-Ph, NH—C1-6alkyl, halo, CN, NO2, CONHR and SO2NHR; two of X1, X2 and X3 are N and the other is NR3 wherein R3 is hydrogen, C1-6alkyl, C3-7cycloalkyl, —(CH2)p—CN, —(CH2)p—CO2H, —(CH2)p—CONHR4R5, —(CH2)pCOR4, —(CH2)q(OR6)2, —(CH2)pOR4, —(CH2)q—CH═CH—CN, —(CH2)q—CH═CH—CO2H, —(CH2)p—CH═CH—CONHR4R5, (CH2)pNHCOR7 or (CH2)pNR8R9; R4 and R5 are independently hydrogen or C1-6alkyl; R6 is C1-6alkyl; R7 is C1-7alkyl, or optionally substituted aryl, heteroaryl, arylC1-6alkyl or heteroarylC1-6alkyl; R8 and R9 are independently selected from hydrogen, C1-6alkyl, aryl and arylC1-6alkyl; p is 04; and q is 1-4. and salts and solvates thereof, are disclosed, as are methods for their preparation, pharmaceutical compositions containing them and their use in medicine.