Low Catalyst Loadings for Ligand-Free Copper(I)-Oxide-Catalyzed<i>N</i>-Arylation of Methanesulfonamide in Water
作者:Bryan Yong-Hao Tan、Yong-Chua Teo、Ai-Hua Seow
DOI:10.1002/ejoc.201301561
日期:2014.3
A simple and practical protocol for the cross-coupling of methanesulfonamide and aryl iodides under ligand-freecopper(I)-oxide-catalyzed conditions in water is reported. The method allows the preparation of a wide variety of synthetically useful N-arylated methanesulfonamides in good to excellent yields (up to 90 %) under the optimized conditions.
The present invention relates to substituted heterocyclic derivative compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of cancer and neoplastic disease.
[EN] 1,3,4-OXADIAZOLE SULFONAMIDE DERIVATIVE COMPOUNDS AS HISTONE DEACETYLASE 6 INHIBITOR, AND THE PHARMACEUTICAL COMPOSITION COMPRISING THE SAME<br/>[FR] COMPOSÉS DÉRIVÉS DE 1,3,4-OXADIAZOLE SULFONAMIDE SERVANT D'INHIBITEUR DE L'HISTONE DÉSACÉTYLASE 6, ET COMPOSITION PHARMACEUTIQUE COMPRENANT CEUX-CI
申请人:CHONG KUN DANG PHARMACEUTICAL CORP
公开号:WO2017018803A1
公开(公告)日:2017-02-02
The present invention relates to novel compounds represented by the formula I having histone deacetylase 6 (HDAC6) inhibitory activity, stereoisomers thereof or pharmaceutically acceptable salts thereof, the use thereof for the preparation of therapeutic medicaments, pharmaceutical compositions containing the same, a method for treating diseases using the composition, and methods for preparing the novel compounds. (I) The novel compounds, stereoisomers thereof or pharmaceutically acceptable salts thereof according to the present invention have histone deacetylase (HDAC) inhibitory activity and are effective for the prevention or treatment of HDAC6-mediated diseases.
[EN] NOVEL COMPOUNDS AND COMPOSITIONS FOR INHIBITION OF FASN<br/>[FR] NOUVEAUX COMPOSÉS ET COMPOSITIONS POUR L'INHIBITION DE FASN
申请人:FORMA THERAPEUTICS INC
公开号:WO2014164749A1
公开(公告)日:2014-10-09
The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below:
本发明涉及用于抑制FASN的化合物和组合物,其合成、应用和解毒剂。本发明的一个示例化合物如下所示:
[EN] NOVEL COMPOUNDS AND COMPOSITIONS FOR THE INHIBITION OF NAMPT<br/>[FR] NOUVEAUX COMPOSÉS ET COMPOSITIONS POUR L'INHIBITION DE NAMPT
申请人:FORMA THERAPEUTICS INC
公开号:WO2012031197A1
公开(公告)日:2012-03-08
The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below: