1041852-97-4

Basic information

• Product Name: 4-[(2-fluoro-4-methylphenyl)amino]-6-{4-[(2R)-2-hydroxypropanoyl]piperazin-1-yl}-7-methoxycinnoline-3-carboxamide
• Synonyms: 4-[(2-fluoro-4-methylphenyl)amino]-6-{4-[(2R)-2-hydroxypropanoyl]piperazin-1-yl}-7-methoxycinnoline-3-carboxamide
• CAS NO: 1041852-97-4
• Molecular Weight: 482.515
• Mol File: 1041852-97-4.mol
• Article Data: 3

Chemical Properties

• CAS DataBase Reference: 4-[(2-fluoro-4-methylphenyl)amino]-6-{4-[(2R)-2-hydroxypropanoyl]piperazin-1-yl}-7-methoxycinnoline-3-carboxamide(CAS DataBase Reference)
• NIST Chemistry Reference: 4-[(2-fluoro-4-methylphenyl)amino]-6-{4-[(2R)-2-hydroxypropanoyl]piperazin-1-yl}-7-methoxycinnoline-3-carboxamide(1041852-97-4)
• EPA Substance Registry System: 4-[(2-fluoro-4-methylphenyl)amino]-6-{4-[(2R)-2-hydroxypropanoyl]piperazin-1-yl}-7-methoxycinnoline-3-carboxamide(1041852-97-4)

Safety Data

• Hazardous Substances Data: 1041852-97-4(Hazardous Substances Data)

Upstream product

• 1041853-91-1 4-(2-fluoro-4-methylphenylamino)-7-methioxy-6-(piperazin-1-yl)cinnoline-3-carbonitrile 
• 1041853-42-2 6-bromo-4-[(2-fluoro-4-methylphenyl)amino]-7-methoxycinnoline-3-carbonitrile 
• 10326-41-7 D-Lactic acid 
• 1041852-94-1 4-(2-fluoro-4-methylphenylamino)-7-methoxy-6-(piperazin-1-yl)cinnoline-3-carboxamide 

Relevant articles and documents

Mitigation of cardiovascular toxicity in a series of CSF-1R inhibitors, and the identification of AZD7507

The potent and selective 3-amido-4-anilinoquinoline CSF-1R inhibitor AZ683 suffered from cardiovascular liabilities, which were linked to the off-target activities of the compound and ion channel activity in particular. Less basic and less lipophilic examples from both the quinoline and cinnoline series demonstrated cleaner secondary pharmacology profiles. Cinnoline 31 retained the required potency and oral PK profile, and was progressed through the safety screening cascade to be nominated into development as AZD7507.

3 - CINNOLINECARBOXAMIDE DERIVATIVES AND THEIR USE FOR TREATING CANCER

The invention relates to chemical compounds of formula (I): 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 human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti cancer effect in a warm blooded animal such as man.