The invention is an algorithm and method for designing an inhibitor that covalently binds a target polypeptide. The algorithm and method can be used to rapidly and efficiently convert reversible inhibitors into irreversible inhibitors.
[EN] HETEROARYL COMPOUNDS AND USES THEREOF<br/>[FR] COMPOSÉS HÉTÉROARYLES ET LEURS UTILISATIONS
申请人:AVILA THERAPEUTICS INC
公开号:WO2009051822A1
公开(公告)日:2009-04-23
The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
本发明提供了化合物、药学上可接受的组合物以及使用它们的方法。
Protein Kinase Conjugates and Inhibitors
申请人:Celgene Avilomics Research, Inc.
公开号:US20170174691A1
公开(公告)日:2017-06-22
The invention relates to protein conjugates that contain a protein kinase containing a cysteine residue in the ATP binding site and an inhibitor that is covalently and irreversibly bonded to said cysteine residue, such that the activity of the protein kinase is irreversibly inhibited. The invention also relates to compounds that irreversibly inhibit protein kinases.
A novel enantioselective protonation protocol that is triggered by reductive cross coupling of olefins is reported. When under cooperative photoredox and chiral hydrogen-bonding catalytic conditions and using a terminal reductant, various α-branched vinylketones with diverse vinylazaarenes could provide important enantioenriched azaarene derivatives containing tertiary stereocenters at their remote