1033809-85-6

Usage

Uses

Used in Pharmaceutical Industry:
1H-Isoindol-1-one, 2,3-dihydro-7-hydroxyis used as a chemical intermediate for the synthesis of various drugs. Its unique chemical structure, including the ring system and hydroxy group, makes it a promising candidate for the development of new pharmaceutical compounds with potential therapeutic applications.

Upstream product

• 808127-81-3 4-bromo-7-hydroxy-2,3-dihydro-1H-isoindol-1-one 
• 808127-82-4 4-bromo-7-methoxy-2,3-dihydro-1H-isoindol-1-one 
• 6520-83-8 ethyl 2-methoxy-6-methylbenzoate 
• 133379-05-2 ethyl 3-bromo-2-(bromomethyl)-6-methoxybenzoate 

Downstream Products

• 1033809-87-8 7-(4-amino-2-chlorophenoxy)-2,3-dihydro-1H-isoindol-1-one 
• 1033809-86-7 7-(2-chloro-4-nitrophenoxy)-2,3-dihydro-1H-isoindol-1-one 

Relevant academic research and scientific papers

Design and synthesis of pyrrolo[3,2- d ]pyrimidine human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors: Exploration of novel back-pocket binders

To develop novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) kinase inhibitors, we explored pyrrolo[3,2-d]pyrimidine derivatives bearing bicyclic fused rings designed to fit the back pocket of the HER2/EGFR proteins. Among them, the 1,2-benzisothiazole (42m) ring was selected as a suitable back pocket binder because of its potent HER2/EGFR binding and cell growth inhibitory (GI) activities and pseudoirreversibility (PI) profile as well as good bioavailability (BA). Ultimately, we arrived at our preclinical candidate 51m by optimization of the N-5 side chain to improve CYP inhibition and metabolic stability profiles without a loss of potency (HER2/EGFR inhibitory activity, IC50, 0.98/2.5 nM; and GI activity BT-474 cells, GI50, 2.0 nM). Reflecting the strong in vitro activities, 51m exhibited potent tumor regressive efficacy against both HER2- and EGFR-overexpressing tumor (4-1ST and CAL27) xenograft models in mice at oral doses of 50 mg/kg and 100 mg/kg.

FUSED HETEROCYCLIC COMPOUND

The present invention provides a fused heterocyclic compound having a tyrosine kinase inhibitory action, which is represented by the formula: wherein R1 is a hydrogen atom, a halogen atom, or an optionally substituted group bonded via a carbon atom, a nitrogen atom or an oxygen atom; R2 is a hydrogen atom, or an optionally substituted group bonded via a carbon atom or a sulfur atom, or R1 and R2, or R2 and R3 are optionally bonded to each other to form an optionally substituted ring structure; R3 is a hydrogen atom or an optionally substituted aliphatic hydrocarbon group, or R3 is optionally bonded to the carbon atom on ring A to form an optionally substituted ring structure; ring A is an optionally substituted benzene ring; and ring B is (i) an optionally substituted fused ring, or (ii) a pyridine ring having optionally substituted carbamoyl (the pyridine ring is optionally further substituted).