865451-01-0

Usage

Preparation

Obtained by reaction of acetyl chloride with 4-chloro-3- fluorophenol in the presence of aluminium chloride in toluene, first at 40° for 1 h, then at 80° for 3 h (61%).

Upstream product

• 348-60-7 4-chloro-3-fluorophenol 
• 75-36-5 acetyl chloride 
• 1481-27-2 4-Fluoro-2-hydroxyacetophenone 

Downstream Products

• 937817-43-1 (2-acetyl-4-chloro-5-fluorophenoxy)acetic acid ethyl ester 

Relevant academic research and scientific papers

METHODS OF CANCER TREATMENT USING ANTI-OX40 ANTIBODIES IN COMBINATION WITH PI3 KINASE DELTA INHIBITORS

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

SALTS AND SOLID FORMS AND PROCESSES OF PREPARING A PI3K INHIBITOR

The present disclosure provides processes for preparing (R)-4-(3-((S)-1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-5-chloro-2-ethoxy-6-fluorophenyl)pyrrolidin-2-one, which is useful as an inhibitor phosphoinositide 3-kinase-delta (PI3Kδ), a

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.

IMIDAZO[1,5-A]PYRAZINE DERIVATIVES AS PI3Kdelta INHIBITORS

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

IMIDAZO [1,5-A] PYRAZINE DERIVATIVES AS PI3Kdelta INHIBITORS

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

SALTS OF PI3K INHIBITOR AND PROCESSES FOR THEIR PREPARATION

The present application provides processes for preparing (R)-4-(3-((S)-1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-5-chloro-2-ethoxy-6-fluorophenyl)pyrrolidin-2-one, which is useful as an inhibitor phosphoinositide 3-kinase-delta (PI3Kδ),

USE OF PYRAZOLOPYRIMIDINE DERIVATIVES FOR THE TREATMENT OF PI3K-DELTA RELATED DISORDERS

The present application provides methods of treating PI3Kδ related disorders using compounds of Formula I: or pharmaceutically acceptable salts thereof.

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.

BICYCLIC AZAHETEROCYCLOBENZYLAMINES AS PI3K INHIBITORS

The present invention provides bicyclic azaheterocyclobenzylamines 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

PYRIMIDINE-4,6-DIAMINE DERIVATIVES AS PI3K INHIBITORS

The present invention provides pyrimidine-4,6-diamine 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 activit