Narrow SAR in odorant sensing Orco receptor agonists
摘要:
The systematic exploration of a series of triazole-based agonists of the cation channel insect odorant receptor is reported. The structure-activity relationships of independent sections of the molecules are examined. Very small changes to the compound structure were found to exert a large impact on compound activity. Optimal substitutions were combined using a 'mix-and-match' strategy to produce best-in-class compounds that are capable of potently agonizing odorant receptor activity and may form the basis for the identification of a new mode of insect behavior modification. (C) 2014 Elsevier Ltd. All rights reserved.
[EN] THIOPHENE DERIVATIVES FOR THE TREATMENT OF DISORDERS CAUSED BY IGE<br/>[FR] DÉRIVÉS DE THIOPHÈNE POUR LE TRAITEMENT DE TROUBLES PROVOQUÉS PAR IGE
申请人:UCB BIOPHARMA SRL
公开号:WO2019243550A1
公开(公告)日:2019-12-26
Thiophene derivatives of formula (I) and a pharmaceutically acceptable salt thereof are provided. These compounds have utility for the treatment or prevention of disorders caused by IgE, such as allergy, type 1 hypersensitivity or familiar sinus inflammation.
[EN] P2X3, RECEPTOR ANTAGONISTS FOR TREATMENT OF PAIN<br/>[FR] ANTAGONISTES DU RÉCEPTEUR P2X3 POUR LE TRAITEMENT DE LA DOULEUR
申请人:MERCK SHARP & DOHME
公开号:WO2010111058A1
公开(公告)日:2010-09-30
The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.
Azoxy compounds bearing a 2,5-disubstituted pyridine ring as a principal constituent and at least one alkyl group at a molecular end were synthesized and their mesomorphic (nematic) ranges were examined. As for azoxy compounds containing an alkyl and an alkoxy group at both ends, respectively, mesomorphic ranges appeared with lower alkyl groups than those for azo compounds, their precursors. The ranges were also lower than those with both alkoxy ends. As regards an azoxy compound containing alkyl groups at both ends, no mesomorphic phenomenon appeared within the scope of this study.
[EN] INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION<br/>[FR] INHIBITEURS DE LA RÉPLICATION DU VIRUS DE L'IMMUNODÉFICIENCE HUMAINE
申请人:BRISTOL MYERS SQUIBB CO
公开号:WO2016172424A1
公开(公告)日:2016-10-27
Compounds of Formula I, including pharmaceutically acceptable salts thereof, and compositions and methods for treating human immunodeficiency virus (HIV) infection are set forth: (I)
[EN] AZACYCLIC SPIRODERIVATIVES AS HSL INHIBITORS<br/>[FR] SPIRODÉRIVÉS AZACYCLIQUES EN TANT QU'INHIBITEURS DE LA HSL
申请人:HOFFMANN LA ROCHE
公开号:WO2010130665A1
公开(公告)日:2010-11-18
Compounds of formula (I) as well as pharmaceutically acceptable salts thereof can be used in the form of pharmaceutical compositions, wherein n, m, A, R1 and R2 have the significance given in claim 1. The compounds are useful as HSL inhibitors for the treatment of diabetes dyslipidemia, atherosclerosis and obesity.