1394820-97-3

Upstream product

• 749922-34-7 7-(benzyloxy)quinolin-4-ol 
• 369-34-6 3,4-difluoronitrobenzene 
• 909345-85-3 5-((3-(benzyloxy)phenylamino)methylene)-2,2-dimethyl-1,3-dioxane-4,6-dione 
• 178984-56-0 7-(benzyloxy)-4-chloroquinoline 
• 403-19-0 2-fluoro-4-nitrophenol 
• 1484-26-0 3-(benzyloxy)aniline 

Downstream Products

• 1221443-46-4 N-(3-fluoro-4-(7-hydroxyquinolin-4-yloxy)phenyl)-1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide 
• 1394820-70-2 (R)-N-(3-fluoro-4-((7-(2-hydroxypropoxy)quinolin-4-yl)oxy)phenyl)-1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide 
• 1394820-91-7 N-(3-fluoro-4-((7-((1-hydroxy-2-methylpropan-2-yl)oxy)quinolin-4-yl)oxy)phenyl)-1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide 
• 1394821-10-3 2-((4-(2-fluoro-4-nitrophenoxy)quinolin-7-yl)oxy)-2-methylpropanoic acid 
• 1394821-11-4 methyl 2-((4-(2-fluoro-4-nitrophenoxy)quinolin-7-yl)oxy)-2-methylpropanoate 
• 1394821-12-5 2-((4-(2-fluoro-4-nitrophenoxy)quinolin-7-yl)oxy)-2-methylpropan-1-ol 
• 1394821-13-6 2-((4-(4-amino-2-fluorophenoxy)quinolin-7-yl)oxy)-2-methylpropan-1-ol 
• 1394821-01-2 4-(4-amino-2-fluorophenoxy)quinolin-7-ol 
• 1394821-00-1 1-((4-(4-amino-2-fluorophenoxy)quinolin-7-yl)oxy)-2-methylpropan-2-ol 
• 1394820-69-9 N-(3-fluoro-4-((7-(2-hydroxy-2-methylpropoxy)quinolin-4-yl)oxy)phenyl)-1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide 

Relevant academic research and scientific papers

Preparation method of quinoline compound

The present invention relates to a preparation method of a quinoline compound, the quinoline compound has a structure represented by a formula (I), and the preparation method comprises the following steps: providing a compound having a structure represented by a formula (I-1); and reacting the compound with the structure shown in the formula (I-1) with 3, 4-difluoro-nitrobenzene to prepare the quinoline compound with the structure shown in the formula (I). The preparation method of the quinoline compound is high in production safety, low in cost and suitable for large-scale industrial production.

Discovery of N-[4-(Quinolin-4-yloxy)phenyl]benzenesulfonamides as Novel AXL Kinase Inhibitors

The overexpression of AXL kinase has been described in many types of cancer. Due to its role in proliferation, survival, migration, and resistance, AXL represents a promising target in the treatment of the disease. In this study we present a novel compound family that successfully targets the AXL kinase. Through optimization and detailed SAR studies we developed low nanomolar inhibitors, and after further biological characterization we identified a potent AXL kinase inhibitor with favorable pharmacokinetic profile. The antitumor activity was determined in xenograft models, and the lead compounds reduced the tumor size by 40% with no observed toxicity as well as lung metastasis formation by 66% when compared to vehicle control.

SUBSTITUTED QUINOLINE COMPOUNDS AND METHODS OF USE

The present invention provides novel substituted quinoline compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.