Discovery of potent, selective small molecule inhibitors of α-subtype of type III phosphatidylinositol-4-kinase (PI4KIIIα)
摘要:
The discovery and optimisation of novel, potent and selective small molecule inhibitors of the alpha-isoform of type III phosphatidylinositol-4-kinase (PI4K alpha) are described. Lead compounds show cellular activity consistent with their PI4K alpha potency inhibiting the accumulation of IP1 after PDGF stimulation and reducing cellular PIP, PIP2 and PIP3 levels. Hence, these compounds are useful in vitro tools to delineate the complex biological pathways involved in signalling through PI4Ka. (C) 2015 Elsevier Ltd. All rights reserved.
Discovery of potent, selective small molecule inhibitors of α-subtype of type III phosphatidylinositol-4-kinase (PI4KIIIα)
摘要:
The discovery and optimisation of novel, potent and selective small molecule inhibitors of the alpha-isoform of type III phosphatidylinositol-4-kinase (PI4K alpha) are described. Lead compounds show cellular activity consistent with their PI4K alpha potency inhibiting the accumulation of IP1 after PDGF stimulation and reducing cellular PIP, PIP2 and PIP3 levels. Hence, these compounds are useful in vitro tools to delineate the complex biological pathways involved in signalling through PI4Ka. (C) 2015 Elsevier Ltd. All rights reserved.
The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of us ing the same in the treatment or prevention of diseases mediated by the activation of β3-adrenoceptor.
[EN] TRICYCLIC CARBOXAMIDE DERIVATIVES AS PRMT5 INHIBITORS<br/>[FR] DÉRIVÉS DE CARBOXAMIDE TRICYCLIQUES EN TANT QU'INHIBITEURS DE PRMT5
申请人:AMGEN INC
公开号:WO2022115377A1
公开(公告)日:2022-06-02
Described herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity and may have use in treating proliferative, such as cancer, metabolic and blood disorders. Compounds of Formula (I) have the following structure of Formule (I).
[EN] PREPARATION OF SUBSTITUTED 1,2-DIAMINOHETEROCYCLIC COMPOUND DERIVATIVES AND THEIR USE AS PHARMACEUTICAL AGENTS<br/>[FR] PRÉPARATION DE DÉRIVÉS DE COMPOSÉS 1,2-DIAMINOHÉTÉROCYCLIQUES SUBSTITUÉS ET LEUR UTILISATION EN TANT QU'AGENTS PHARMACEUTIQUES
申请人:AVELOS THERAPEUTICS INC
公开号:WO2022260441A1
公开(公告)日:2022-12-15
This invention relates to compounds which are microtubule associated serine/threonine-like kinase (MASTL) inhibitors and the use of the compounds in the treatment of diseases and medical conditions mediated by MASTL, for example in the treatment of cancer and other target related diseases.
PYRAZOLO(3,4-B)PYRIDINE COMPOUNDS, AND THEIR USE AS PHOSPHODIESTERASE INHIBITORS
申请人:GLAXO GROUP LIMITED
公开号:EP1539753B1
公开(公告)日:2009-09-09
PRO-SURVIVAL COMPOUNDS
申请人:University Court of The University of Glasgow
公开号:US20170362184A1
公开(公告)日:2017-12-21
Disclosed herein are a class of compounds useful in cell culture, in particular, the in vitro culture of stem cells. The compounds have been found to promote the survival and/or maintenance of stem cells in (or during) culture and/or throughout passage.