[EN] PREPARATION METHOD FOR NITROGEN-CONTAINING HETEROCYCLIC COMPOUND AS UBIQUITIN-SPECIFIC PROTEASE 1 INHIBITOR, AND APPLICATION AND USE THEREOF [FR] PROCÉDÉ DE PRÉPARATION D'UN COMPOSÉ HÉTÉROCYCLIQUE CONTENANT DE L'AZOTE EN TANT QU'INHIBITEUR DE LA PROTÉASE 1 SPÉCIFIQUE DE L'UBIQUITINE, AINSI QUE APPLICATION ET UTILISATION DE CELUI-CI [ZH] 含氮杂环化合物作为泛素-特异性蛋白酶1抑制剂的制备方法、应用及其用途
[EN] SUBSTITUTED IMIDAZOPYRIDINES, THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS [FR] IMIDAZOPYRIDINES SUBSTITUÉES, LEUR PRÉPARATION ET LEUR UTILISATION COMME MÉDICAMENTS
Synthesis and SAR of Benzisothiazole- and Indolizine-β-<scp>d</scp>-glucopyranoside Inhibitors of SGLT2
作者:Huiqiang Zhou、Dana P. Danger、Steven T. Dock、Lora Hawley、Shane G. Roller、Chari D. Smith、Anthony L. Handlon
DOI:10.1021/ml900010b
日期:2010.4.8
A series of benzisothiazole- and indolizine-beta-D-glucopyranoside inhibitors of human SGLT2 are described. The synthesis of the Clinked heterocyclic glucosides took advantage of a palladium-catalyzed cross-coupling reaction between a glucal boronate and the corresponding bromo heterocycle. The compounds have been evaluated for their human SGLT2 inhibition potential using cell-based functional transporter assays, and their structure activity relationships have been described Benzisothiazole-C-glucoside 16d was found to be an inhibitor of SGLT2 with an IC50 of 10 nM
SUBSTITUTED IMIDAZOPYRIDINES, THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS
申请人:NEOMED Institute
公开号:US20180312504A1
公开(公告)日:2018-11-01
This application relates to substituted imidazopyridines, compositions comprising them and their uses in the treatment of diseases and conditions in which inhibition of a bromodomain is indicated. For example, the application relates to substituted imidazopyridines and to their use as bromodomain inhibitors. The present application is also related to the treatment or prevention of proliferative disorders, auto-immune disorders, inflammatory disorders, dermal disorders, and neoplasms, including tumors and/or cancers.