865451-01-0Relevant articles and documents
METHODS OF CANCER TREATMENT USING ANTI-OX40 ANTIBODIES IN COMBINATION WITH PI3 KINASE DELTA INHIBITORS
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Paragraph 0131-0132; 0160-0161, (2021/05/29)
Provided are methods of treating cancer with non-competitive, agonist anti-OX40 antibodies and antigen-binding fragments thereof that bind to human OX40 (ACT35, CD134, or TNFRSF4), in combination with a PI3K (phosphatidylinositol-4, 5-bisphosphate 3-kinas
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.
IMIDAZO [1,5-A] PYRAZINE DERIVATIVES AS PI3Kdelta INHIBITORS
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Paragraph 0188; 0189; 0317; 0318; 0596; 0597; 0620; 0621, (2018/06/30)
Disclosed is a compound of Formula (I), or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions comprising thereof. Also disclosed is a method of treating PI3Kδ related disorders or diseases by using the c