Potent 2′-aminoanilide inhibitors of cFMS as potential anti-inflammatory agents
摘要:
A series of 2 '-aminoanilides have been identified which exhibit potent and selective inhibitory activity against the cFMS tyrosine kinase. Initial SAR studies within this series are described which examine aroyl and amino group substitutions, as well as the introduction of hydrophilic substituents on the benzene core. Compound 47 inhibits the isolated enzyme (IC50 = 0.027 mu M) and blocks CSF-1-induced proliferation of bone marrow-derived macrophages (IC50 = 0.11 mu M) and as such, serves as a lead candidate for further optimization studies. (C) 2007 Elsevier Ltd. All rights reserved.
Potent 2′-aminoanilide inhibitors of cFMS as potential anti-inflammatory agents
摘要:
A series of 2 '-aminoanilides have been identified which exhibit potent and selective inhibitory activity against the cFMS tyrosine kinase. Initial SAR studies within this series are described which examine aroyl and amino group substitutions, as well as the introduction of hydrophilic substituents on the benzene core. Compound 47 inhibits the isolated enzyme (IC50 = 0.027 mu M) and blocks CSF-1-induced proliferation of bone marrow-derived macrophages (IC50 = 0.11 mu M) and as such, serves as a lead candidate for further optimization studies. (C) 2007 Elsevier Ltd. All rights reserved.
Provided is an agent for treating or preventing urinary frequency, urinary urgency and urinary, incontinence which are associated with overactive bladder, a lower urinary tract disease such as interstitial cystitis and chronic prostatitis accompanied by lower urinary tract pain, and various diseases accompanied by pain. A novel azolecarboxamide derivative in which an azole ring such as thioazole or oxazole is bonded to a benzene ring, pyridine ring or pyrimidine ring through carboxamide was confirmed to have a potent trkA receptor-inhibitory activity and found to be an agent for treating or preventing lower urinary tract disease and various diseases accompanied by pain, which is excellent in efficacy and safety, and thus the present invention was accomplished.
Methods for Using Carboxamide, Sulfonamide and Amine Compounds
申请人:RIGEL PHARMACEUTICALS, INC.
公开号:US20140323460A1
公开(公告)日:2014-10-30
Disclosed are uses of carboxamide, sulfonamide and amine compounds for the treatment and amelioration of disorders and conditions related to oxidative stress, mitochondrial dysfunction, free radical damage and metabolic inefficiency, among others. Also described are methods for increasing exercise endurance, exercise efficiency and aerobic workload using the compounds described herein.
US8163746B2
申请人:——
公开号:US8163746B2
公开(公告)日:2012-04-24
[EN] COSMETIC COMPOSITION FOR KERATIN FIBERS<br/>[FR] COMPOSITION COSMÉTIQUE POUR DES FIBRES KÉRATINIQUES
申请人:OREAL
公开号:WO2013069166A1
公开(公告)日:2013-05-16
The present invention relates to a cosmetic composition for keratin fibers, in a mousse form, comprising: (a) at least one fatty material; (b) at least one glucoside type surfactant; (c) at least one non-volatile alkaline agent; and (d) at least one oxidizing agent, and (e) at least one foam stabilizer wherein the amount of the (a) fatty material (s) is 20% by weight or more, preferably 30% by weight or more, and more preferably 40% by weight or more, relative to the total weight of the composition. The present invention is useful, because the cosmetic composition according to the present invention can have good foamability as well as good bleaching or coloring ability, without offensive odor from ammonia.
Potent 2′-aminoanilide inhibitors of cFMS as potential anti-inflammatory agents
作者:Raymond J. Patch、Benjamin M. Brandt、Davoud Asgari、Nand Baindur、Naresh K. Chadha、Taxiarchis Georgiadis、Wing S. Cheung、Ioanna P. Petrounia、Robert R. Donatelli、Margery A. Chaikin、Mark R. Player
DOI:10.1016/j.bmcl.2007.09.057
日期:2007.11
A series of 2 '-aminoanilides have been identified which exhibit potent and selective inhibitory activity against the cFMS tyrosine kinase. Initial SAR studies within this series are described which examine aroyl and amino group substitutions, as well as the introduction of hydrophilic substituents on the benzene core. Compound 47 inhibits the isolated enzyme (IC50 = 0.027 mu M) and blocks CSF-1-induced proliferation of bone marrow-derived macrophages (IC50 = 0.11 mu M) and as such, serves as a lead candidate for further optimization studies. (C) 2007 Elsevier Ltd. All rights reserved.