Transition-metal-free synthesis of primary to tertiary carboxamides: A quick access to prodrug-pyrazinecarboxamide
摘要:
One-pot expedient and direct carbamoylation of heterocyclics is described. The transformation is realized via direct dehydrogenative aminocarbonylation of heterocyclic compounds under transition-metal-free conditions. This method is regioselective and the protocol is proved to be scalable on a gram scale. Further, the therapeutically useful antitubercular agent pyrazinecarboxamide is successfully synthesized by employing this protocol. (C) 2017 Elsevier Ltd. All rights reserved.
[EN] IMIDAZO[1,2-A]PYRIDINE DERIVATIVES AS HISTONE DEMETHYLASE INHIBITORS<br/>[FR] DÉRIVÉS D'IMIDAZO[1,2-A]PYRIDINE UTILISÉS EN TANT QU'INHIBITEURS D'HISTONE DÉMÉTHYLASE
申请人:CHRYSALIS INC
公开号:WO2017214413A1
公开(公告)日:2017-12-14
This disclosure relates, inter alia, to compounds that inhibit histone demethylase activity. In particular, the disclosure relates to compounds that inhibit histone lysine demethylase KDM5B, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions disclosed herein.
[EN] FUSED TRICYCLIC AMIDE COMPOUNDS AS MULTIPLE KINASE INHIBITORS<br/>[FR] COMPOSÉS AMIDES TRICYCLIQUES CONDENSÉS COMME INHIBITEURS DE KINASES MULTIPLES
申请人:BEIGENE LTD
公开号:WO2014206344A1
公开(公告)日:2014-12-31
Provided are fused tricyclic amide compounds, pharmaceutical compositions comprising at least one such fused tricyclic compound, processes for the preparation thereof, and the use thereof in therapy. Disclosed herein are certain tricyclic amide compounds that can be useful for inhibiting multiple (specifically BRAF and/or EGFR-T790M) kinases and for treating disorders mediated thereby.
Phenethylamide derivatives with kinase inhibitory activity
申请人:Gould E. Alexandra
公开号:US20080064729A1
公开(公告)日:2008-03-13
The present invention provides novel phenethylamide compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
Compounds of Formula la, lb, or Ic, (Ia); (Ib); or (Ic), are described, where the various substituents are defined herein. The compounds can modulate a property or effect of Akt3 in vitro or in vivo, and can also be used, individually or in combination with other agents, in the prevention or treatment of a variety of conditions. Methods for synthesizing the compounds are described. Pharmaceutical compositions and methods of using these compounds or compositions, individually or in combination with other agents or compositions, in the prevention or treatment of a variety of conditions are also described.
The present invention relates to a compound which has a glucokinase-activating effect and is useful as a therapeutic agent for diabetes mellitus, being represented by a formula (I):
[wherein X
1
represents a nitrogen atom, sulfur atom, oxygen atom or the like; R
1
represents a 6- to 10-membered aryl group, 5- to 7-membered heteroaryl group or the like; D represents an oxygen atom or sulfur atom; R and R
3
are the same or different, each representing a hydrogen atom, lower alkyl group or the like; a formula (II)
represents an optionally substituted 5- to 7-membered heteroaryl group or the like; a formula (III)
represents a monocyclic or bicyclic heteroaryl group] or a pharmaceutically acceptable salt thereof.