1396007-91-2

Upstream product

• 912358-41-9 3-(4-bromo-phenylamino)-but-2-enoic acid methylester 
• 105-45-3 acetoacetic acid methyl ester 
• 106-40-1 4-bromo-aniline 
• 2101-88-4 1-azido-4-bromobenzene 
• 23326-27-4 Methyl 2-butynoate 
• 5467-74-3 4-Bromophenylboronic acid 

Downstream Products

• 1396007-52-5 {3-[4'-(1-methanesulfonylaminocarbonyl-cyclopropyl)-biphenyl-4-yl]-5-methyl-3H-[1,2,3]triazol-4-yl}-carbamic acid (R)-1-phenyl-ethyl ester 
• 1396007-92-3 3-(4-bromo-phenyl)-5-methyl-3H-[1,2,3]triazole-4-carboxylic acid 
• 1396007-93-4 [3-(4-bromo-phenyl)-5-methyl-3H-[1,2,3]triazol-4-yl]-carbamic acid (R)-1-phenyl-ethyl ester 
• 1396007-94-5 1-{4'-[4-methyl-5-((R)-1-phenyl-ethoxycarbonylamino)-1H-[1,2,3]triazol-1-yl]biphenyl-4-yl}cyclopropanecarboxylic acid methyl ester 
• 1396006-71-5 1-[4’-[4-methyl-5-[[(1R)-1-phenylethoxy]carbonylamino]-1H-1,2,3-triazol-1-yl][1,1′-biphenyl]-4-yl]cyclo-propanecarboxylic acid 
• 1396007-95-6 {4'-[4-methyl-5-((R)-1-phenyl-ethoxycarbonylamino)-[1,2,3]triazol-1-yl]-biphenyl-4-yl}-acetic acid ethyl ester 
• 1396007-29-6 {4'-[4-methyl-5-((R)-1-phenyl-ethoxycarbonylamino)-[1,2,3]triazol-1-yl]-biphenyl-4-yl}-acetic acid 
• 1396007-33-2 1-(4'-{5-[(R)-1-(2-fluoro-phenyl)-ethoxycarbonylamino]-4-methyl-[1,2,3]triazol-1-yl}-biphenyl-4-yl)-cyclopropanecarboxylic acid 
• 1396007-37-6 1-(4'-{5-[(R)-1-(2-trifluoromethyl-phenyl)-ethoxycarbonylamino]-4-methyl-[1,2,3]triazol-1-yl}-biphenyl-4-yl)-cyclopropanecarboxylic acid 
• 1396007-40-1 1-(4'-{4-methyl-5-[(R)-1-(3-trifluoromethyl-phenyl)-ethoxycarbonylamino]-[1,2,3]triazol-1-yl}-biphenyl-4-yl)-cyclopropanecarboxylic acid 

Relevant academic research and scientific papers

TBAI or KI-Promoted Oxidative Coupling of Enamines and N-Tosylhydrazine: An Unconventional Method toward 1,5- and 1,4,5-Substituted 1,2,3-Triazoles

A novel method for the synthesis of 1,5- and 1,4,5-substituted 1,2,3-triazoles has been reported. This approach is promoted by iodine-TBHP oxidation system using enamines and N-tosylhydrazine as materials, which avoid the dependence of traditional methods on azides and transition metals. Through this approach, various 1,5- and 1,4,5-substituted 1,2,3-triazoles were delivered in moderate to high yields. The mechanistic study indicated that an amino exchange would be involved in the reaction process. Moreover, the product methyl 1-(2-methoxyphenyl)-4-methyl-1H-1,2,3-triazole-5-carboxylate is a useful precursor to anti-influenza A agent, and further application research was conducted. (Figure presented.).

N-ARYLTRIAZOLE COMPOUNDS AS LPAR ANTAGONISTS

Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, pulmonary fibrosis

Discovery of highly selective and orally active lysophosphatidic acid receptor-1 antagonists with potent activity on human lung fibroblasts

Lysophosphatidic acid is a class of bioactive phospholipid that mediates most of its biological effects through LPA receptors, of which six isoforms have been identified. The recent results from LPA1 knockout mice suggested that blocking LPA1 signaling could provide a potential novel approach for the treatment of idiopathic pulmonary fibrosis. Here, we report the design and synthesis of pyrazole- and triazole-derived carbamates as LPA1-selective and LPA1/3 dual antagonists. In particular, compound 2, the most selective LPA1 antagonist reported, inhibited proliferation and contraction of normal human lung fibroblasts (NHLF) following LPA stimulation. Oral dosing of compound 2 to mice resulted in a dose-dependent reduction of plasma histamine levels in a murine LPA challenge model. Furthermore, we applied our novel antagonists as chemistry probes and investigated the contribution of LPA1/2/3 in mediating the pro-fibrotic responses. Our results suggest LPA1 as the major receptor subtype mediating LPA-induced proliferation and contraction of NHLF.