1426699-24-2

Upstream product

• 1382996-38-4 1-(3-bromo-5-chloro-2-methoxy-4-methylphenyl)ethanol 
• 1426699-19-5 4-[3-chloro-5-(1-hydroxyethyl)-6-methoxy-2-methylphenyl]pyridine-2-carbonitrile 
• 28478-40-2 1-(5-chloro-2-methoxy-4-methylphenyl)ethanone 
• 1382994-99-1 1-(3-bromo-5-chloro-2-methoxy-4-methylphenyl)ethanone 
• 1426699-23-1 3-bromo-1-chloro-5-(1-chloroethyl)-4-methoxy-2-methylbenzene 
• 5399-44-0 3-methyl-4-amino-1H-pyrazolo[3,4-d]pyrimidine 

Downstream Products

• 1426700-09-5 1-[1-(3-bromo-5-chloro-2-methoxy-4-methylphenyl)ethyl]-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine 
• 1426700-10-8 1-[1-(3-bromo-5-chloro-2-methoxy-4-methylphenyl)ethyl]-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine 

Relevant academic research and scientific papers

INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3-Kinase Delta (PI3Kδ)

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.

HETEROCYCLYLAMINES AS PI3K INHIBITORS

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.