Title:
コルチスタチン類縁体並びにその合成及び使用
Document Type and Number:
Japanese Patent JP6494631
Kind Code:
B2
Abstract:
Provided herein are compounds of Formula (), (), (), () and (), pharmaceutically acceptable salts, quaternary amine salts, and N-oxides thereof, and pharmaceutical compositions thereof.Compounds of Formula (), (), (), (), and () are contemplated useful as therapeutics for treating a wide variety of conditions,., including but not limited to, conditions associated with angiogenesis and with CDK8 and/or CDK19 kinase activity. Further provided are methods of inhibiting CDK8 and/or CDK19 kinase activity, methods of modulating the β-catenin pathway, methods of modulating STAT1 activity, methods of modulating the TGFβ/BMP pathway, methods of modulating HIF-1-alpha activity in a cell, and methods of increasing BIM expression to induce apoptosis, using a compound of Formula (), (), (), (), or (). Further provided are CDK8 and CDK19 point mutants and methods of use thereof.
Inventors:
Share Matthew Dee.
Ramhalter Juergen
Perish Henry Efflem
Riau Bryan Bo-Jen
Angelon
Ramhalter Juergen
Perish Henry Efflem
Riau Bryan Bo-Jen
Angelon
Application Number:
JP2016542733A
Publication Date:
April 03, 2019
Filing Date:
December 24, 2014
Export Citation:
Assignee:
PRESIDENT AND FELLOWS OFHARVARD COLLEGE
International Classes:
C07J71/00; A61K31/4725; A61K31/5377; A61P3/04; A61P3/10; A61P9/10; A61P27/02; A61P29/00; A61P35/00; A61P35/02; A61P43/00
Foreign References:
| WO2010024930A1 | ||||
| WO2009137335A1 | ||||
| WO2009137337A1 | ||||
| US20110060140 |
Attorney, Agent or Firm:
Patent Business Corporation Saegusa International Patent Office