HETEROCYCLIC AMIDE DERIVATIVE AND PHARMACEUTICAL PRODUCT CONTAINING SAME
申请人:Ajinomoto Co., Inc.
公开号:US20140329796A1
公开(公告)日:2014-11-06
The present invention aims to provide a novel compound having a TRPA1 antagonist activity, and a medicament containing the compound. Moreover, the present invention aims to provide a TRPA1 antagonist and a medicament useful for the prophylaxis or treatment of diseases involving TRPA1.
A medicament containing a compound represented by the formula (I):
wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof, and the like.
(Hetero)aryl substituted thiazol-2,4-yl scaffold as human carbonic anhydrase I, II, VII and XIV activators
作者:Marouan Rami、Jean-Yves Winum、Claudiu T. Supuran、Patricia Melnyk、Saïd Yous
DOI:10.1080/14756366.2018.1543292
日期:2019.1.1
Abstract Using histamine as lead molecule, a library of (hetero)aryl substituted thiazol-2,4-yl derivatives incorporating pyridine as proton shuttling moiety were obtained and investigated as activators of human carbonic anhydrase (CA, EC 4.2.1.1) isoforms I, II, VII and XIV. Somederivatives displayed good activating and selectivity profiles. This study provides an interesting opportunity to study
Tetrahydroquinoline derivatives as P2X7 receptor antagonists
申请人:RaQualia Pharma Inc.
公开号:US11077100B2
公开(公告)日:2021-08-03
The present invention relates to tetrahydroquinoline derivatives of the present invention or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the P2X7 receptor.
Bis(2,2,2-trifluoroethyl) Carbonate as a Condensing Agent in One-Pot Parallel Synthesis of Unsymmetrical Aliphatic Ureas
作者:Andrey V. Bogolubsky、Yurii S. Moroz、Pavel K. Mykhailiuk、Dmitry S. Granat、Sergey E. Pipko、Anzhelika I. Konovets、Roman Doroschuk、Andrey Tolmachev
DOI:10.1021/co500025f
日期:2014.6.9
One-pot parallel synthesis of unsymmetrical aliphatic ureas was achieved with bis(2,2,2-trifluoroethyl) carbonate. The procedure worked well for both the monosubstituted and functionalized alkyl amines and required no special conditions (temperature control, order, or rate of addition). A library of 96 diverse ureas was easily synthesized.