286371-63-9

Upstream product

• 13790-39-1 6,7-dimethoxy-4-chloroquinazoline 
• 52671-64-4 4-Amino-3-chlorophenol hydrochloride 
• 13794-72-4 3H-6,7-dimethoxyquinazolin-4-one 
• 26759-46-6 methyl 2-amino-4,5-dimethoxybenzoate 

Downstream Products

• 1356835-75-0 N-(3-bromophenyl)-N'-{4-[(6,7-dimethoxyquinazolin-4-yl)oxy]-2-chlorophenyl}urea 
• 1356835-76-1 N-(3-chloro-4-fluorophenyl)-N'-{4-[(6,7-dimethoxyquinazolin-4-yl)oxy]-2-chlorophenyl}urea 
• 1622396-57-9 C₂₉H₃₀Cl₂N₆O₄ 
• 1622396-56-8 C₂₇H₂₈ClN₅O₅ 
• 1622396-55-7 C₂₈H₃₀ClN₅O₅ 
• 1622396-53-5 C₂₉H₃₁ClN₆O₄ 
• 1622396-52-4 C₂₈H₂₈ClN₅O₅ 
• 1622396-51-3 C₂₈H₂₈ClN₅O₅ 
• 286370-69-2 N-Butyl-N'-{2-chloro-4-[(6,7-dimethoxy-4-quinazolinyl)oxy]phenyl}-N-methylurea 
• 286370-67-0 N'-{2-Chloro-4-[(6,7-dimethoxy-4-quinazolinyl)oxy]phenyl}-N-ethyl-N-propylurea 
• 286370-33-0 N-{2-Chloro-4-[(6,7-dimethoxy-4-quinazolinyl)oxy]phenyl}-N'-(2,4-difluorobenzyl)urea 

Relevant academic research and scientific papers

THERAPEUTIC COMPOUNDS AND USES THEREOF

Described herein are compounds of Formula (I) or Formula (VI), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I) or Formula (VI) and pharmaceutical compositions thereof that are mucus penetrating. Methods of using the compounds or pharmaceutical compositions thereof for treating diseases are also provided.

Synthesis and structure-activity relationships of (aryloxy)quinazoline ureas as novel, potent, and selective vascular endothelial growth factor receptor-2 inhibitors

In our continuing search for medicinal agents to treat proliferative diseases, quinazoline derivatives were synthesized and evaluated pharmacologically as epithelial growth factor receptor and vascular endothelial growth factor receptor 2 (VEGFR-2) tyrosine kinase inhibitors. A quantitative structure-activity relationship analysis was conducted to rationalize the structure-activity relationship and to predict how similar the inhibitor-binding profiles of two protein kinases are likely to be on the basis of the docking of lead coumpounds into the ATP-binding site. This model was used to direct the synthesis of new compounds. A series of N-(aromatic)-N′-{4-[(6,7- dimethoxyquinazolin-4-yl)oxy]phenyl}urea were identified as potent and selective inhibitors of the tyrosine kinase activity of VEGFR-2 (fetal liver kinase 1, kinase insert domain-containing receptor). An efficient route was developed that enabled the synthesis of a wide variety of analogues with substitution on several positions of the template. Substitution of diarylurea, competitive with ATP, afforded several analogues with low nanomolar inhibition of enzymatic activity of VEGFR-2. In this paper, we describe the synthesis, structure-activity relationships, and pharmacological characterization of the series.

QUINOLINE DERIVATIVES AND QUINAZOLINE DERIVATIVES

An object of the present invention is to provide compounds which have antitumor activity and do not change cytomorphosis. Disclosed are compounds represented by formula (I) and a pharmaceutically acceptable salts and solvates thereof and pharmaceutical compositions comprising said compounds: wherein X and Z each independently represent CH or N; R1 to R3 represent H, substituted alkoxy, unsubstituted alkoxy or the like; R4 represents H; R5 to R8 represent H, halogen, alkyl, alkoxy, alkylthio, nitro, or amino, provided that R5 to R8 do not simultaneously represent H; R9 and R10 represent H, alkyl, or alkylcarbonyl; and R11 represents alkyl, alkenyl, alkynyl, or aralkyl.