1361031-47-1

Upstream product

• 479690-03-4 7-benzyloxy-4-(2-fluoro-4-nitro-phenoxy)-6-methyloxyquinoline 
• 286371-49-1 7-(benzyloxy)-4-chloro-6-methoxyquinoline 
• 403-19-0 2-fluoro-4-nitrophenol 
• 479690-08-9 1-(2-fluoro-4-nitrophenyl)-6-hydroxy-7-methoxy-quinoline 
• 83948-53-2 3-bromopropylamine tert-butylcarbamate 

Downstream Products

• 1290538-60-1 {3-[4-(4-amino-2-fluorophenoxy)-6-methoxyquinolin-7-yloxy]propyl}carbamic acid tert-butyl ester 
• 1293291-39-0 (3-{4-[4-(2,5-difluorobenzenesulfonylamino)-2-fluorophenoxy]-6-methoxyquinolin-7-yloxy}propyl)carbamic acid tert-butyl ester 
• 1293291-38-9 (3-{4-[2-fluoro-4-(2-trifluoromethylbenzenesulfonylamino)phenoxy]-6-methoxyquinolin-7-yloxy}propyl)carbamic acid tert-butyl ester 

Relevant academic research and scientific papers

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.

PHARMACEUTICALLY ACTIVE COMPOUNDS AS AXL INHIBITORS

The present invention relates to 1-nitrogen-heterocyclic-2-carboxamides of general formula (I): and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the treatment and/or prevention of Axl receptor tyrosine kinase subfamily induced disorders, including cancer and primary tumor metastases, and pharmaceutical compositions containing at least one of said 1-nitrogen-heterocyclic-2-carboxamide derivatives and/or pharmaceutically acceptable salts thereof.

Pharmaceutically active compounds as Axl inhibitors

The present invention relates to 1-nitrogen-heterocyclic-2-carboxamides of general formula (I): and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the treatment and/or prevention of Axl receptor tyrosine kinase subfamily induced disorders, including cancer and primary tumor metastases, and pharmaceutical compositions containing at least one of said 1-nitrogen-heterocyclic-2-carboxamide derivatives and/or pharmaceutically acceptable salts thereof.