65487-32-3Relevant articles and documents
2-(Halogenated Phenyl) acetamides and propanamides as potent TRPV1 antagonists
Ann, Jihyae,Bahrenberg, Gregor,Blumberg, Peter M.,Choi, Sun,Christoph, Thomas,Do, Nayeon,Frank-Foltyn, Robert,Ha, Heejin,Jeong, Jin Ju,Kang, Jin Mi,Kim, Changhoon,Kwon, Sun Ok,Lee, Jeewoo,Lee, Sunho,Lesch, Bernhard,Stockhausen, Hannelore,Vu, Thi Ngoc Lan,Yoon, Sanghee
, (2021/07/28)
A series consisting of 117 2-(halogenated phenyl) acetamide and propanamide analogs were investigated as TRPV1 antagonists. The structure–activity analysis targeting their three pharmacophoric regions indicated that halogenated phenyl A-region analogs exhibited a broad functional profile ranging from agonism to antagonism. Among the compounds, antagonists 28 and 92 exhibited potent antagonism toward capsaicin for hTRPV1 with Ki[CAP] = 2.6 and 6.9 nM, respectively. Further, antagonist 92 displayed promising analgesic activity in vivo in both phases of the formalin mouse pain model. A molecular modeling study of 92 indicated that the two fluoro groups in the A-region made hydrophobic interactions with the receptor.
Flurbiprofen synthesis method
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Paragraph 0042-0046; 0054-0058; 0066-0070; 0078-0082; 0090, (2017/08/28)
The invention relates to a flurbiprofen synthesis method and belongs to the technical field of pharmaceutical synthesis. According to the flurbiprofen synthesis method, Suzuki coupling reaction is utilized, the flurbiprofen can be obtained from 2-(3-fluoro-4-bromophenyl) propionic acid and phenyl boron reagent in organic solvent in the alkali condition through palladium catalytic Suzuki coupling reaction; the mole ratio between the 2-(3-fluoro-4-bromophenyl) propionic acid and the phenyl boron reagent is 1: (0.9 to 1.1). The synthesis method is simple, and the obtained flurbiprofen is high in yield and high in purity.
GAMMA SECRETASE MODULATORS
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Page/Page column 100-101, (2009/07/17)
The present invention provides compounds that are gamma secretase modulators and are therefore useful for the treatment of diseases treatable by modulation of gamma secretase such as Alzheimer's disease. Also provided are pharmaceutical compositions conta