This invention provides a series of novel heterocyclic aliphatic carboxamides of formula I in which the group >Z--Y--X< is selected from >C.dbd.CH--N<, >N--CH.dbd.C<, >C.dbd.N--N< and >N--N.dbd.C< and the other radicals have the meanings defined in the following specification. The compounds of formula I are leukotriene antagonists. The invention also provides pharmaceutically acceptable salts of the formula I compounds; pharmaceutical compositions containing the formula I compound, or their salts, for use in the treatment of, for example, allergic or inflammatory diseases, or endotoxic or traumatic shock conditions; and processes for the manufacture of the formula I compounds, as well as intermediates for use in such manufacture.
[EN] PYRAZOLE DERIVATIVES AS BROMODOMAIN INHIBITORS<br/>[FR] DÉRIVÉS DE PYRAZOLE UTILISÉS EN TANT QU'INHIBITEURS DE BROMODOMAINE
申请人:GLAXOSMITHKLINE IP NO 2 LTD
公开号:WO2018158212A1
公开(公告)日:2018-09-07
The present invention is directed to pyrazole derivatives, pharmaceutical compositions comprising the compounds and the use of the compounds or the compositions in the treatment of various diseases
Detosylative (Deutero)alkylation of Indoles and Phenols with (Deutero)alkoxides
作者:Ming-Hui Zhu、Cheng-Long Yu、Ya-Lan Feng、Muhammad Usman、Dayou Zhong、Xin Wang、Nasri Nesnas、Wen-Bo Liu
DOI:10.1021/acs.orglett.9b02639
日期:2019.9.6
An efficient strategy for N/O-(deutero)alkylation of indoles and phenols with alkoxides/alcohols as the alkylation reagents is described. The consecutive detosylation/alkylation transformations feature mild reaction conditions, high ipso-selectivity, and good functional group tolerance (>50 examples). A one-pot selective N-alkylation of unprotected indoles with alcohols and TsCl is also realized. The
Iodine-Mediated Electrochemical C(sp<sup>2</sup>)–H Amination: Switchable Synthesis of Indolines and Indoles
作者:Kangfei Hu、Yan Zhang、Zhenghong Zhou、Yu Yang、Zhenggen Zha、Zhiyong Wang
DOI:10.1021/acs.orglett.0c01821
日期:2020.8.7
A metal-free electrochemical intramolecular C(sp2)–Hamination using iodine as a mediator was developed. This method enables a switchable synthesis of indoline and indole derivatives, respectively, from easily available 2-vinyl anilines.
Design, synthesis and antiviral efficacy of a series of potent chloropyridyl ester-derived SARS-CoV 3CLpro inhibitors
作者:Arun K. Ghosh、Gangli Gong、Valerie Grum-Tokars、Debbie C. Mulhearn、Susan C. Baker、Melissa Coughlin、Bellur S. Prabhakar、Katrina Sleeman、Michael E. Johnson、Andrew D. Mesecar
DOI:10.1016/j.bmcl.2008.08.082
日期:2008.10
Design, synthesis and biological evaluation of a series of 5-chloropyridine ester-derived severe acute respiratory syndrome-coronavirus chymotrypsin-like protease inhibitors is described. Position of the carboxylate functionality is critical to potency. Inhibitor 10 with a 5-chloropyridinyl ester at position 4 of the indole ring is the most potent inhibitor with a SARS-CoV 3CLpro IC(50) value of 30