1426696-99-2Relevant academic research and scientific papers
INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3-Kinase Delta (PI3Kδ)
Yue, Eddy W.,Li, Yun-Long,Douty, Brent,He, Chunhong,Mei, Song,Wayland, Brian,Maduskuie, Thomas,Falahatpisheh, Nikoo,Sparks, Richard B.,Polam, Padmaja,Zhu, Wenyu,Glenn, Joseph,Feng, Hao,Zhang, Ke,Li, Yanlong,He, Xin,Katiyar, Kamna,Covington, Maryanne,Feldman, Patricia,Shin, Niu,Wang, Kathy He,Diamond, Sharon,Li, Yu,Koblish, Holly K.,Hall, Leslie,Scherle, Peggy,Yeleswaram, Swamy,Xue, Chu-Biao,Metcalf, Brian,Combs, Andrew P.,Yao, Wenqing
supporting information, p. 1554 - 1560 (2019/11/11)
A medicinal chemistry effort focused on identifying a structurally diverse candidate for phosphoinositide 3-kinase delta (PI3Kδ) led to the discovery of clinical candidate INCB050465 (20, parsaclisib). The unique structure of 20 contains a pyrazolopyrimidine hinge-binder in place of a purine motif that is present in other PI3Kδinhibitors, such as idelalisib (1), duvelisib (2), and INCB040093 (3, dezapelisib). Parsaclisib (20) is a potent and highly selective inhibitor of PI3Kδwith drug-like ADME properties that exhibited an excellent in vivo profile as demonstrated through pharmacokinetic studies in rats, dogs, and monkeys and through pharmacodynamic and efficacy studies in a mouse Pfeiffer xenograft model.
USE OF PYRAZOLOPYRIMIDINE DERIVATIVES FOR THE TREATMENT OF PI3K-DELTA RELATED DISORDERS
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Paragraph 0355; 0356; 0357; 0384, (2014/09/16)
The present application provides methods of treating PI3Kδ related disorders using compounds of Formula I: or pharmaceutically acceptable salts thereof.
HETEROCYCLYLAMINES AS PI3K INHIBITORS
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Paragraph 1079, (2013/03/26)
The present invention provides heterocyclylamine derivatives of Formula I: wherein the variables are defined herein, that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
