885693-15-2

Basic information

• Product Name: 4-cyano-1-(2-trimethylsilanylethoxymethyl)-1H-imidazole-2-carboxylic acid (2-cyclohex-1-enyl-4-piperidin-4-ylphenyl)amide trifluoroacetic acid salt
• Synonyms: 4-cyano-1-(2-trimethylsilanylethoxymethyl)-1H-imidazole-2-carboxylic acid (2-cyclohex-1-enyl-4-piperidin-4-ylphenyl)amide trifluoroacetic acid salt
• CAS NO: 885693-15-2
• Molecular Weight: 619.759
• Mol File: 885693-15-2.mol
• Article Data: 5

Chemical Properties

• CAS DataBase Reference: 4-cyano-1-(2-trimethylsilanylethoxymethyl)-1H-imidazole-2-carboxylic acid (2-cyclohex-1-enyl-4-piperidin-4-ylphenyl)amide trifluoroacetic acid salt(CAS DataBase Reference)
• NIST Chemistry Reference: 4-cyano-1-(2-trimethylsilanylethoxymethyl)-1H-imidazole-2-carboxylic acid (2-cyclohex-1-enyl-4-piperidin-4-ylphenyl)amide trifluoroacetic acid salt(885693-15-2)
• EPA Substance Registry System: 4-cyano-1-(2-trimethylsilanylethoxymethyl)-1H-imidazole-2-carboxylic acid (2-cyclohex-1-enyl-4-piperidin-4-ylphenyl)amide trifluoroacetic acid salt(885693-15-2)

Safety Data

• Hazardous Substances Data: 885693-15-2(Hazardous Substances Data)

Upstream product

• 214360-73-3 4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)aniline 
• 138647-49-1 4-Trifluoromethanesulfonyloxy-3,6-dihydro-2H-pyridine-1-carboxylic acid tert-butyl ester 
• 885693-01-6 4-(4-amino-3-cyclohex-1-enyl-phenyl)-piperidine-1-carboxylic acid tert-butyl ester 
• 885693-00-5 4-(4-amino-3-bromophenyl)piperidine-1-carboxylic acid tert-butyl ester 
• 170011-57-1 tert-butyl 4-(4-aminophenyl)piperidin-1-carboxylate 
• 873454-43-4 4-(4-aminophenyl)-3,6-dihydro-2H-pyridine-1-carboxylic acid tert-butyl ester 
• 885693-02-7 (4-{[4-cyano-1-(2-trimethylsilanyl-ethoxymethyl)-1H-imidazole-2-carbon-yl]-amino}-3-cyclohex-1-enyl-phenyl)-piperidine-1-carboxylic acid tert-butyl ester 
• 76-05-1 trifluoroacetic acid 

Downstream Products

• 885693-16-3 4-(4-{[4-cyano-1-(2-trimethylsilanylethoxymethyl)-1H-imidazole-2-carbonyl]amino}-3-cyclohex-1-enylphenyl)piperidine-1-carboxylic acid (2-hydroxyethyl)amide 
• 885693-03-8 4-cyano-1-(2-trimethylsilanylethoxymethyl)-1H-imidazole-2-carboxylic acid {2-cyclohex-1-enyl-4-[1-(2-morpholin-4-yl-ethyl)piperidin-4-yl]phenyl}amide 

Relevant articles and documents

Optimization of a potent class of arylamide colony-stimulating factor-1 receptor inhibitors leading to anti-inflammatory clinical candidate 4-cyano-N -[2-(1-cyclohexen-1-yl)-4-[1-[(dimethylamino)acetyl]-4-piperidinyl]phenyl]-1 H -imidazole-2-carboxamide (JNJ-28312141)

A class of potent inhibitors of colony-stimulating factor-1 receptor (CSF-1R or FMS), as exemplified by 8 and 21, was optimized to improve pharmacokinetic and pharmacodynamic properties and potential toxicological liabilities. Early stage absorption, distribution, metabolism, and excretion assays were employed to ensure the incorporation of druglike properties resulting in the selection of several compounds with good activity in a pharmacodynamic screening assay in mice. Further investigation, utilizing the type II collagen-induced arthritis model in mice, culminated in the selection of anti-inflammatory development candidate JNJ-28312141 (23, FMS IC50 = 0.69 nM, cell assay IC50 = 2.6 nM). Compound 23 also demonstrated efficacy in rat adjuvant and streptococcal cell wall-induced models of arthritis and has entered phase I clinical trials.

METHOD OF INHIBITING FLT3 KINASE

A method of reducing or inhibiting kinase activity of FLT3 in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to FLT3 using a compound of the present invention (I), or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof. The present invention is further directed to methods for treating conditions such as cancers and other cell proliferative disorders.

SYNERGISTIC MODULATION OF FLT3 KINASE USING A FLT3 INHIBITOR AND A FARNESYL TRANSFERASE INHIBITOR

The invention is directed to a method of inhibiting FLT3 tyrosine kinase activity or expression or reducing FLT3 kinase activity or expression in a cell or a subject comprising the administration of a farnesyl transferase inhibitor and a FLT3 kinase inhibitor selected from compounds of Formula I′: Included within the present invention is both prophylactic and therapeutic methods for treating a subject at risk of (or susceptible to) developing a cell proliferative disorder or a disorder related to FLT3.