88982-82-5Relevant articles and documents
FORMAMIDE COMPOUND, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
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Paragraph 0196, (2021/05/14)
The present invention relates to a formamide compound, a preparation method therefor and an application thereof. The structure of the compound is shown in formula (I), and the definition of each variable in the formula is as provided in the description. The compound is capable of inhibiting the activity of ASK1 kinase. The compound of the present invention may be used in the treatment/prevention of diseases associated with ASK1 kinase, such as inflammatory diseases, metabolic diseases, autoimmune diseases, cardiovascular diseases, neurodegenerative diseases, cancers and other diseases.
AMINO HETEROCYCLIC COMPOUNDS AND USES THEREOF
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Paragraph 01327, (2020/08/22)
The present disclosure relates to compounds of Formula (I): and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inflammatory, autoinflammatory, and autoimmune diseases and cancers.
Synthesis and biological evaluation of picolinamides and thiazole-2-carboxamides as mGluR5 (metabotropic glutamate receptor 5) antagonists
Vu, Hoang Nam,Kim, Ji Young,Hassan, Ahmed H.E.,Choi, Kihang,Park, Jong-Hyun,Park, Ki Duk,Lee, Jae Kyun,Pae, Ae Nim,Choo, Hyunah,Min, Sun-Joon,Cho, Yong Seo
supporting information, p. 140 - 144 (2015/12/18)
We described here the synthesis and biological evaluation of picolinamides and thiazole-2-carboxamides as potential mGluR5 antagonists. We found that a series of thiazole derivatives 6 showed better inhibitory activity against mGluR5. Compounds 6bc and 6bj have been identified as potent antagonists (IC50 = 274 and 159 nM) showing excellent in vitro stability profile. Molecular docking study using the crystal structure of mGluR5 revealed that our compounds 6bc and 6bj fit the allosteric binding site of mavoglurant well.