476194-45-3

Upstream product

• 1361235-53-1 ethyl 6-bromo-4-hydroxy-7-methoxyquinoline-3-carboxylate 
• 87-13-8 diethyl 2-ethoxymethylenemalonate 
• 19056-40-7 4-bromo-3-methoxyaniline 
• 1361235-53-1 ethyl 6-bromo-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylate 
• 953803-77-5 diethyl {[(4-bromo-3-methoxyphenyl)amino]methylene}malonate 

Downstream Products

• 953802-77-2 ethyl 6-bromo-4-[(2,4-difluorophenyl)amino]-7-methoxyquinoline-3-carboxylate 
• 953804-35-8 ethyl 6-bromo-4-[(2,4-dichlorophenyl)amino]-7-methoxyquinoline-3-carboxylate 
• 953801-10-0 ethyl 4-[(2,3-dichlorophenyl)amino]-7-methoxy-6-(4-methylpiperazin-1-yl)quinoline-3-carboxylate 
• 953804-36-9 ethyl 6-bromo-4-[(3,4-dichlorophenyl)amino]-7-methoxyquinoline-3-carboxylate 

Relevant academic research and scientific papers

COMPOUNDS FOR THE DEGRADATION OF BRD9 OR MTH1

Compounds that degrade BRD9 or MTH1 via the ubiquitin proteasome pathway in a subject in need thereof for therapeutic applications are provided. The compounds provided have an E3 Ubiquitin Ligase targeting moiety (Degron) that is linked to a Targeting Ligand for BRD9 or MTH1.

3-Amido-4-anilinoquinolines as CSF-1R kinase inhibitors 2: Optimization of the PK profile

The optimization of compounds from the 3-amido-4-anilinoquinolines series of CSF-1R kinase inhibitors is described. The series has excellent activity and kinase selectivity. Excellent physical properties and rodent PK profiles were achieved through the introduction of cyclic amines at the quinoline 6-position. Compounds with good activity in a mouse PD model measuring inhibition of pCSF-1R were identified.

Identification of 3-amido-4-anilinoquinolines as potent and selective inhibitors of CSF-1R kinase

3-Amido-4-anilinoquinolines are potent and highly selective inhibitors of CSF-1R. Their synthesis and SAR is reported, along with initial efforts to optimize the physical properties and PK through modifications at the quinoline 6- and 7-positions.

CHEMICAL COMPOUNDS

The invention relates to chemical compounds of formula (I): or pharmaceutically acceptable salts thereof which possess CSF 1R kinase inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the huma

4-ANILINOQUINOLINE-3-CARBOXAMIDES AS CSF-1R KINASE INHIBITORS

The invention relates to chemical compounds of formula IA or IB: formula IA IB or pharmaceutically acceptable salts thereof which possess CSF 1R kinase inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of tr