2942-40-7Relevant articles and documents
AMIDE DERIVATIVES COMPRISING HETEROCYCLOALKYL RING
-
Paragraph 0259-0261, (2020/05/20)
PROBLEM TO BE SOLVED: To provide compounds or pharmacologically acceptable salts thereof that have excellent EP300 and/or CREBBP histone acetyltransferase inhibitory activity. SOLUTION: The invention provides compounds represented by the formula (1) in the figure or pharmacologically acceptable salts thereof. (In the formula (1), ring Q1, ring Q2, ring Q3, X and L are as defined in the specification.) SELECTED DRAWING: None COPYRIGHT: (C)2020,JPO&INPIT
Discovery of 1-(1H-indazol-4-yl)-3-((1-phenyl-1H-pyrazol-5-yl)methyl) ureas as potent and thermoneutral TRPV1 antagonists
Kang, Jin Mi,Kwon, Sun Ok,Ann, Jihyae,Blumberg, Peter M.,Ha, Heejin,Yoo, Young Dong,Frank-Foltyn, Robert,Lesch, Bernhard,Bahrenberg, Gregor,Stockhausen, Hannelore,Christoph, Thomas,Lee, Jeewoo
, (2020/10/06)
A series of 1-indazol-3-(1-phenylpyrazol-5-yl)methyl ureas were investigated as hTRPV1 antagonists. The structure–activity relationship study was conducted systematically for both the indazole A-region and the 3-trifluoromethyl/t-butyl pyrazole C-region to optimize the antagonism toward the activation by capsaicin. Among them, the antagonists 26, 50 and 51 displayed highly potent antagonism with Ki(CAP) = 0.4–0.5 nM. Further, in vivo studies in mice indicated that these derivatives both antagonized capsaicin induced hypothermia, consistent with their in vitro activity, and themselves did not induce hyperthermia. In the formalin model, 51 showed anti-nociceptive activity in a dose-dependent manner.
Indazole compounds containing nitrogen substituents, and application of same as IDO inhibitors
-
Paragraph 0048; 0054; 0055; 0057; 0058; 0061, (2018/11/03)
The invention discloses nitrogen substituent-containing indazole compounds as shown in a formula (I) which is described in the specification, a preparation method for the compounds, and application ofthe compounds as IDO inhibitors. The compounds provided by the invention can be used for preventing and/or treating a plurality of diseases, such as Alzheimer's disease, cataract, infections relatedto cellular immune activation, autoimmune diseases, AIDS, cancers, depression, the metabolic disorder of tryptophan or the like.