931105-37-2Relevant articles and documents
2-AMINO-N-PHENYL-NICOTINAMIDES AS NAV1.8 INHIBITORS
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Page/Page column 136-137, (2020/05/28)
Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of Nav1.8 channel activity and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by Nav1.8 channel activity. The compounds of the present invention may be useful in the treatment, prevention or management of pain disorders, cough disorders, acute itch disorders, and chronic itch disorders.
Structure-Based Design, Synthesis, and Biological Evaluation of Imidazo[4,5-b]Pyridin-2-one-Based p38 MAP Kinase Inhibitors: Part 2
Kaieda, Akira,Takahashi, Masashi,Fukuda, Hiromi,Okamoto, Rei,Morimoto, Shinji,Gotoh, Masayuki,Miyazaki, Takahiro,Hori, Yuri,Unno, Satoko,Kawamoto, Tomohiro,Tanaka, Toshimasa,Itono, Sachiko,Takagi, Terufumi,Sugimoto, Hiroshi,Okada, Kengo,Lane, Weston,Sang, Bi-Ching,Saikatendu, Kumar,Matsunaga, Shinichiro,Miwatashi, Seiji
supporting information, p. 2093 - 2101 (2019/11/16)
We identified novel potent inhibitors of p38 mitogen-activated protein (MAP) kinase using a structure-based design strategy, beginning with lead compound, 3-(butan-2-yl)-6-(2,4-difluoroanilino)-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-one (1). To enhance the inhibitory activity of 1 against production of tumor necrosis factor-α (TNF-α) in human whole blood (hWB) cell assays, we designed and synthesized hybrid compounds in which the imidazo[4,5-b]pyridin-2-one core was successfully linked with the p-methylbenzamide fragment. Among the compounds evaluated, 3-(3-tert-butyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-6-yl)-4-methyl-N-(1-methyl-1H-pyrazol-3-yl)benzamide (25) exhibited potent p38 inhibition, superior suppression of TNF-α production in hWB cells, and also significant in vivo efficacy in a rat model of collagen-induced arthritis (CIA). In this paper, we report the discovery of potent, selective, and orally bioavailable imidazo[4,5-b]pyridin-2-one-based p38 MAP kinase inhibitors.
SUBSTITUTED GUANIDINE DERIVATIVE
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Paragraph 1387; 1388, (2018/06/23)
The present invention provides a compound of general formula (I) (wherein, R1, X, p and q are as described in the present description and claims), or a pharmacologically acceptable salt thereof, and a pharmaceutical composition containing that compound.