NOVEL 6-6 BICYCLIC AROMATIC RING SUBSTITUTED NUCLEOSIDE ANALOGUES FOR USE AS PRMT5 INHIBITORS
The present invention relates novel 6-6 bicyclic aromatic ring substituted nucleoside analogues of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as PRMT5 inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
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(2017/03/14)
Novel Mps1 kinase inhibitors: From purine to pyrrolopyrimidine and quinazoline leads
Mps1, also known as TTK, is a mitotic checkpoint protein kinase that has become a promising new target of cancer research. In an effort to improve the lead-likeness of our recent Mps1 purine lead compounds, a scaffold hopping exercise has been undertaken.
Bursavich, Matthew G.,Dastrup, David,Shenderovich, Mark,Yager, Kraig M.,Cimbora, Daniel M.,Williams, Brandi,Kumar, D. Vijay
p. 6829 - 6833
(2014/01/06)
QUINAZOLINES FOR PDK1 INHIBITION
The invention provides novel quinazoline compounds that are inhibitors of PDK1. Also provided are pharmaceutical compositions including the compounds, and methods of treating proliferative diseases, such as cancers, with the compounds or compositions.
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(2008/06/13)
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