1382995-22-3

Upstream product

• 28480-70-8 5'-chloro-2'-hydroxy-4'-methyl acetophenone 
• 1382994-99-1 1-(3-bromo-5-chloro-2-methoxy-4-methylphenyl)ethanone 
• 1025373-45-8 trifluoromethanesulfonic acid anhydride 
• 358-23-6 trifluoromethylsulfonic anhydride 

Downstream Products

• 1382992-95-1 N-{1-[4-chloro-6-(2,6-difluoropyridin-4-yl)-5-methylbiphenyl-2-yl]ethyl}-9H-purin-6-amine 
• 1382995-24-5 1-[4-chloro-6-(2,6-difluoropyridin-4-yl)-5-methylbiphenyl-2-yl]ethanone 
• 1382995-25-6 1-[4-chloro-6-(2,6-difluoropyridin-4-yl)-5-methylbiphenyl-2-yl]ethanamine 
• 1382993-55-6 N-{1-[4-chloro-3'-fluoro-5-methyl-6-(1-methyl-1H-pyrazol-4-yl)biphenyl-2-yl]ethyl}-9H-purin-6-amine 
• 1382995-52-9 1-{4-chloro-6-[1-(1-ethoxyethyl)-1H-pyrazol-4-yl]-3'-fluoro-5-methylbiphenyl-2-yl}ethanamine 
• 1382995-51-8 1-{4-chloro-6-[1-(1-ethoxyethyl)-1H-pyrazol-4-yl]-3'-fluoro-5-methylbiphenyl-2-yl}ethanone 
• 1382995-57-4 N-{1-[4-Chloro-3'-fluoro-5-methyl-6-(1H-pyrazol-4-yl)biphenyl-2-yl]ethyl}-9H-purin-6-amine trifluoroacetate 
• 1382995-49-4 1-[4-chloro-6-(3,5-dimethylisoxazol-4-yl)-3'-fluoro-5-methylbiphenyl-2-yl]ethanone 
• 1382995-50-7 1-[4-chloro-6-(3,5-dimethylisoxazol-4-yl)-3'-fluoro-5-methylbiphenyl-2-yl]ethanamine 
• 1382995-56-3 N-{1-[4-chloro-6-(3,5-dimethylisoxazol-4-yl)-3'-fluoro-5-methylbiphenyl-2-yl]ethyl}-9H-purin-6-amine trifluoroacetate 

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.

N-(1-(SUBSTITUTED-PHENYL)ETHYL)-9H-PURIN-6-AMINES AS PI3K INHIBITORS

The present invention provides N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines derivatives 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 examp