Structure–activity relationship studies of 3-substituted pyrazoles as novel allosteric inhibitors of MALT1 protease
We report the discovery of a novel series of 1,5-bisphenylpyrazoles as potent MALT1 inhibitors. Structure–activity relationship exploration of a hit compound led to a potent MALT1 inhibitor. Compound 33 showed strong activity against MALT1 (IC50/sub
Asaba, Ken Nunettsu,Adachi, Yohei,Tokumaru, Kazuyuki,Watanabe, Akira,Goto, Yasufumi,Aoki, Takumi
(2021/04/27)
DIPHENYL PYRAZOLE DERIVATIVE AND PHARMACEUTICAL USE THEREOF
PROBLEM TO BE SOLVED: To provide a compound that functions to inhibit MALT1 protease activity and is useful as an agent for treating or for preventing autoimmune disease such as multiple sclerosis and psoriasis. SOLUTION: The present invention provides a diphenyl pyrazole derivative represented by the following formula or a pharmacologically acceptable salt thereof. SELECTED DRAWING: None COPYRIGHT: (C)2018,JPO&INPIT
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Paragraph 0123-0124
(2018/02/28)
Structural study of diarylazoles related to Rimonabant
The structures of three diarylazoles (two pyrazoles and one 1,2,4-triazole) related to Rimonabant have been determined by X-ray crystallography. The conformation of both aryl groups in the new structures is discussed with regard to other related compounds
Alkorta, Ibon,Alvarado, Mario,Elguero, José,García-Granda, Santiago,Goya, Pilar,Torre-Fernández, Laura,Menéndez-Taboada, Laura
experimental part
p. 82 - 89
(2009/06/27)
Antiobesity designed multiple ligands: Synthesis of pyrazole fatty acid amides and evaluation as hypophagic agents
Searching for new antiobesity agents, a new series of fatty acid amide derivatives of 1,5-diarylpyrazole have been synthesized as dual peroxisome proliferator activated receptor alpha (PPARα)/cannabinoid receptor ligands. The compounds have been evaluated in vivo and in vitro as PPARα activators and as cannabinoids in two tests of the mouse tetrad. In vivo, food intake studies have been performed with all the compounds. No significant cannabinoid activity has been found but some compounds behaved as potent PPARα activators. Several compounds showed anorexigenic properties reducing food intake in rats.
Alvarado, Mario,Goya, Pilar,Macias-Gonzalez, Manuel,Pavon, Francisco Javier,Serrano, Antonia,Jagerovic, Nadine,Elguero, Jose,Gutierrez-Rodriguez, Angel,Garcia-Granda, Santiago,Suardiaz, Margarita,Rodriguez de Fonseca, Fernando
experimental part
p. 10098 - 10105
(2009/04/06)
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