[EN] 1-(DIHYDRONAPHTHALENYL)PYRIDONES AS MELANIN-CONCENTRATING HORMONE RECEPTOR 1 ANTAGONISTS [FR] 1-(DIHYDRONAPHTALÉNYL)PYRIDONES EN TANT QU'ANTAGONISTES DU RÉCEPTEUR 1 DE L'HORMONE DE CONCENTRATION DE LA MÉLANINE
[EN] THIAZOLE SULFONAMIDE AND OXAZOLE SULFONAMIDE KINASE INHIBITORS<br/>[FR] INHIBITEURS DE THIAZOLE SULFONAMIDE ET OXAZOLE SULFONAMIDE KINASES
申请人:GLAXOSMITHKLINE LLC
公开号:WO2010104899A1
公开(公告)日:2010-09-16
The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents
There are presented compounds of the formula
or pharmaceutically acceptable salts thereof,
wherein Y
1
, Y
2
, X
1
, X
2
, X
3
and R are as described in this application. These compounds are believed to inhibit MDM2-p53 interaction and as such the compounds will have anti-hyperproliferative cellular activity.
The present invention relates to compounds of the formula (I), and the pharmaceutically acceptable salts and esters thereof, a process for their manufacture, medicaments containing them as well as the use of these compounds as pharmaceutically active agents. The compounds show antiproliferative activity and may be especially useful for the treatment of cancer.
The present invention provides imidazopyridine compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.
本发明提供了咪唑并吡啶化合物、含有该化合物的组合物,以及它们的制备方法和作为药物的使用方法。
CYCLIC AMINES AS BROMODOMAIN INHIBITORS
申请人:Fairfax David John
公开号:US20140142102A1
公开(公告)日:2014-05-22
The present disclosure relates to compounds, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.