39959-99-4Relevant academic research and scientific papers
Pyrazolopyrimidine derivatives as PI3 kinase inhibitors
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, (2015/09/22)
PI3Kβ selective compounds having the structure
3a,4-Dihydropyrazolo[1,5 a]pyrimidines: Novel, Potent, and Selective Phosphatidylinositol-3-kinase β Inhibitors
Yu, Hongyi,Moore, Michael L.,Erhard, Karl,Hardwicke, Mary Ann,Lin, Hong,Luengo, Juan I.,McSurdy-Freed, Jeanelle,Plant, Ramona,Qu, Junya,Raha, Kaushik,Rominger, Cynthia M.,Schaber, Michael D.,Spengler, Michael D.,Rivero, Ralph A.
, p. 230 - 234 (2013/03/28)
A series of novel [3a,4]dihydropyrazolo[1,5a]pyrimidines were identified, which were highly potent and selective inhibitors of PI3Kβ. The template afforded the opportunity to develop novel SAR for both the hinge-binding (R 3) and back-pocket (R4) substitutents. While cellular potency was relatively modest due to high protein binding, the series displayed low clearance in rat, mouse, and monkey.
PYRAZOLOPYRIMIDINE DERIVATIVES AS PI3 KINASE INHIBITORS
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, (2013/03/26)
The present invention relates to compounds of formula (I) in which R1, R2, R3 and n have the meaning given in the specification and also relates to the use of these pyrazolopyrimidine derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3'OΗ kinase family (hereinafter PI3 kinases), wherein the compounds of formula (I) are described as selective inhibitors of PI3K[beta] activity.
