1141894-75-8

Upstream product

• 261952-06-1 4-methyl-3-(trifluoromethyl)benzonitrile 
• 853368-32-8 4?(bromomethyl)?3?(trifluoromethyl)benzonitrile 

Downstream Products

• 1141895-96-6 N-{[4-cyano-2-(trifluoromethyl)phenyl]methyl}-1-[4-methyl-6-(methylamino)-1,3,5-triazin-2-yl]-4-piperidinecarboxamide 
• 1142090-23-0 (cis)-N-{[4-cyano-2-(trifluoromethyl)phenyl]methyl}-3-{[4-methyl-6-(methylamino)-1,3,5-triazin-2-yl]amino}cyclohexanecarboxamide 

Relevant academic research and scientific papers

Multigram-scale?synthesis?of GSK 2,256,294, an inhibitor of soluble epoxide hydrolase in clinical evaluation

This paper described the development of an improved, practical and efficient protocol method for the multigram-scale synthesis of GSK 2,256,294, an orally bioavailable potent and selective inhibitor of sEH. The key to this optimization was the design and development of a novel synthetic strategy, which involved the preparation of 4-(aminomethyl)-3-(trifluoromethyl)benzonitrile (3) and 4-chloro-N,6-dimethyl-1,3,5-triazin-2-amine (6). The developed process provided an overall yield of 26.8%, which enabled us to rapidly synthesize large quantities of GSK 2,256,294 in 99% purity. Graphical abstract: [Figure not available: see fulltext.].

NOVEL SEH INHIBITORS AND THEIR USE

The invention is directed to novel sEH inhibitors and their use in the treatment of diseases mediated by the sEH enzyme. Specifically, the invention is directed to compounds according to Formula I: (I) wherein R1, R2, R3, R5a, R6a A, B, Y, x, and m are defined below, and to pharmaceutically-acceptable salts thereof. The compounds of the invention are sEH inhibitors and can be used in the treatment of diseases mediated by the sEH enzyme, such as hypertension. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting sEH and treatment of conditions associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

NOVEL SEH INHIBITORS AND THEIR USE

The invention is directed to novel sEH inhibitors and their use in the treatment of diseases mediated by the sEH enzyme. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, R4, R5, R6, A, B, Y, Z, n, and m are defined below, and to pharmaceutically-acceptable salts thereof. The compounds of the invention are sEH inhibitors and can be used in the treatment of diseases mediated by the sEH enzyme, such as hypertension. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting sEH and treatment of conditions associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.