[EN] AZOLE COMPOUNDS AS PIM INHIBITORS<br/>[FR] COMPOSÉS D'AZOLE UTILISÉS EN TANT QU'INHIBITEURS DES PIM
申请人:AMGEN INC
公开号:WO2012129338A1
公开(公告)日:2012-09-27
The invention relates to bicyclic compounds of formulas I and Ia, and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.
[EN] SUBSTITUTED PYRIDINE AND PYRAZINE BMI-1 INHIBITORS<br/>[FR] INHIBITEURS DE BMI-1 À BASE DE PYRIDINE ET DE PYRAZINE SUBSTITUÉES
申请人:PTC THERAPEUTICS INC
公开号:WO2015076800A1
公开(公告)日:2015-05-28
Amine substituted pyridine and pyrazine compounds and forms thereof that inhibit the function and reduce the level of B -cell specific Moloney murine leukemia virus integration site 1 (Bmi-1) protein and methods for their use to inhibit Bmi-1 function and reduce the level of Bmi-1 to treat a cancer mediated by Bmi-1 are described herein.
paper, we describe the synthesis of a wide range of new rod-like conjugated molecules with a pyrazine or a bipyrazine core connected to electron acceptor (A) or donor (D) groups through π-conjugated bridges as transmitters for the internal charge transfer (ICT). The key steps of the synthesis involve metallation and subsequent transmetallation of 2-chloropyrazine derivatives followed by Sonogashira
Herein, we report the development of a palladium-catalyzed cross-coupling reaction that focuses on the preparation of aromatic ketones. Aroyl chlorides react quickly at 120 °C with aryl stannanes in the presence of Pd(PPh3)4 and Et3SiH to efficiently give the corresponding ketones without the formation of significant decarbonylated byproducts. In other words, the decarbonylative side reaction is practically
Regioselective metalation of pyrazines and cross-coupling reactions provides an easy access to botryllazines A and B and to an isomer of botryllazine A with good yields from chloropyrazine.