[EN] TASK CHANNEL ANTAGONISTS<br/>[FR] ANTAGONISTES DE CANAL TASK
申请人:MERCK SHARP & DOHME
公开号:WO2011103715A1
公开(公告)日:2011-09-01
This invention relates to TASK-1 and/or TASK-3 antagonists and/or their pharmaceutically acceptable salts, compositions and methods for treating and preventing disorders which are caused by activation or by an activated TASK-1 and/or TASK-3, and disorders which have TASK-1 and/or TASK-3-related damage as a secondary cause.
for mono-N-alkylation of aniline with di-iso-propylamine. The turnover frequency (TOF), defined as the reaction rate per number of surface Pt species, increases with sulfur loading. The catalyst with S/Pt ratio of 0.13 shows more than 5 times higher TOF than unmodified catalysts, and it acts as effective and recyclable catalyst for cross-coupling of various anilines and amines. Combined with kinetic
[EN] EFFICIENT METHODS FOR Z- OR CIS-SELECTIVE CROSS-METATHESIS<br/>[FR] PROCÉDÉS EFFICACES DE MÉTATHÈSE CROISÉE Z-SÉLECTIVE OU CIS-SÉLECTIVE
申请人:TRUSTEES BOSTON COLLEGE
公开号:WO2011097642A1
公开(公告)日:2011-08-11
The present invention generally relates to methods for performing metathesis reactions, including cross-metathesis reactions. Methods described herein exhibit enhanced activity and stereoselectivity, relative to known methods, and are useful in the synthesis of a large assortment of biologically and therapeutically significant agents.
POTENT ANALOGUES OF THE C-MYC INHIBITOR 10074-G5 WITH IMPROVED CELL PERMEABILITY
申请人:University of Maryland, Baltimore
公开号:US20140296307A1
公开(公告)日:2014-10-02
The present invention relates compounds and compositions for interfering with the association of Myc and Max. These compounds and compositions are useful in methods for inhibiting growth or proliferation of a cell. Methods of inhibiting growth or proliferation of a cell comprise contacting the cell with an amount of a compound that interferes with Myc and Max association effective to inhibit growth or proliferation of the cell. The compounds exhibit increased inhibitory activity against c-Myc relative to the known c-Myc inhibitor small-molecule benzofurazan N-([1,1′-biphenyl]-2-yl)-7-nitrobenzo[c][1,2,5]oxadiazol-4-amine (10074-G5).
Oxidative Pd(II)-Catalyzed C−H Bond Amination to Carbazole at Ambient Temperature
作者:James A. Jordan-Hore、Carin C. C. Johansson、Moises Gulias、Elizabeth M. Beck、Matthew J. Gaunt
DOI:10.1021/ja806543s
日期:2008.12.3
We report a new Pd(II)-catalyzed C-H bond amination reaction to form carbazoles, an important motif that is prevalent in a range of systems. The catalytic amination process operates under extremely mild conditions and produces carbazole products in good to excellent yields. Carbazoles possessing complex moleculararchitecture can also be formed using this reaction, highlighting its potential in natural