Novel five-membered heterocyclic amidines, their preparation and use as competitive inhibitors of trypsin-like serine proteases, especially thrombin and kininogenases such as kallikrein. Pharmaceutical compositions which contain the compounds as active ingredients, and use of the compounds as thrombin inhibitors, anticoagulants and antiinflammatory agents.
Facile, diversity-orientated one-pot synthesis of ethyl 1,5-disubstituted-1H-1,2,4-triazole-3-carboxylates
作者:Sébastien Degorce、Bénédicte Delouvrié、Paul R.J. Davey、Myriam Didelot、Hervé Germain、Craig S. Harris、Christine Lambert-van der Brempt、Honorine Lebraud、Gilles Ouvry
DOI:10.1016/j.tetlet.2012.08.130
日期:2012.11
Access to the 1,5-disubstituted-1H-1,2,4-triazole-3-carboxamide motif is quite laborious and requires forcing conditions to effect the cyclocondensation step. Herein, we report an efficient and mild one-pot protocol to access this substructure in good chemical yields with high regiocontrol. (C) 2012 Elsevier Ltd. All rights reserved.
WO2008/74991
申请人:——
公开号:——
公开(公告)日:——
INHIBITORS OF MPTP
申请人:[en]NRG THERAPEUTICS LTD
公开号:WO2024153946A1
公开(公告)日:2024-07-25
The invention relates to compounds of formula (I), and related aspects.