1300031-63-3

Upstream product

• 3886-69-9 (R)-1-phenyl-ethyl-amine 
• 1300031-62-2 3,5-dimethyl-4-[2-(methyloxy)-5-nitrophenyl]isoxazole 
• 5399-03-1 2-iodo-1-methoxy-4-nitrobenzene 
• 1300031-61-1 [3-(3,5-dimethyl-4-isoxazolyl)-4-(methyloxy)phenyl]amine 
• 16114-47-9 3,5-dimethylisoxazole-4-boronic acid 
• 1300031-64-4 7-(3,5-dimethylisoxazol-4-yl)-6-methoxy-3-nitro-N-((R)-1-phenylethyl)quinolin-4-amine 
• 1300031-65-5 4-chloro-7-(3,5-dimethyl-1,2-oxazol-4-yl)-6-methoxy-3-nitroquinoline 
• 1300031-66-6 7-(3,5-dimethyl-4-isoxazolyl)-6-(methyloxy)-3-nitro-4-quinolinol 
• 1300031-67-7 7-(3,5-dimethylisoxazol-4-yl)-6-methoxyquinolin-4-ol 
• 1300031-68-8 7-iodo-6-methoxy-quinolin-4-ol 
• 1300031-69-9 5-{[(3-iodo-4-methoxyphenyl)amino]methylene}-2,2-dimethyl-1,3-dioxane-4,6-dione 
• 74587-12-5 3-iodo-4-methoxyaniline 

Downstream Products

• 1300031-50-8 7-(3,5-dimethyl-4-isoxazolyl)-8-(methoxy)-1-[(1R)-1-phenylethyl]-2-(tetrahydro-2H-pyran-4-yl)-1H-imidazo[4,5-c]quinoline 
• 1300735-35-6 7-(3,5-dimethyl-4-isoxazolyl)-8-(methoxy)-1-[(1R)-1-phenylethyl]-1H-[1,2,3]triazolo[4,5-c]quinoline 
• 1300736-25-7 7-(3,5-dimethylisoxazol-4-yl)-8-methoxy-1-((R)-1-phenylethyl)-1H-imidazo[4,5-c]quinoline-2(3H)-thione 

Relevant academic research and scientific papers

Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N-Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype

The bromodomain and extraterminal domain (BET) family of epigenetic regulators comprises four proteins (BRD2, BRD3, BRD4, BRDT), each containing tandem bromodomains. To date, small molecule inhibitors of these proteins typically bind all eight bromodomains of the family with similar affinity, resulting in a diverse range of biological effects. To enable further understanding of the broad phenotype characteristic of pan-BET inhibition, the development of inhibitors selective for individual, or sets of, bromodomains within the family is required. In this regard, we report the discovery of a potent probe molecule possessing up to 150-fold selectivity for the N-terminal bromodomains (BD1s) over the C-terminal bromodomains (BD2s) of the BETs. Guided by structural information, a specific amino acid difference between BD1 and BD2 domains was targeted for selective interaction with chemical functionality appended to the previously developed I-BET151 scaffold. Data presented herein demonstrate that selective inhibition of BD1 domains is sufficient to drive anti-inflammatory and antiproliferative effects.

QUINOLINE DERIVATIVES AS BROMODOMAIN INHIBITORS

Provided is a novel quinoline derivative inhibiting the bromodomain and extra terminal domain (BET) proteins, and a pharmaceutical composition comprising the same which can be useful for prevention or treatment of a precancerous transformation or a cancer.

IMIDAZOQUINOLINE COMPOUNDS AS BROMODOMAIN INHIBITORS

The present invention provides compound of formula (I), or an isotopic form, a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a solvate, a polymorph, a prodrug, N-oxide or S-oxide thereof; and processes for their preparation. The invention further relates to pharmaceutical compositions containing said compounds and their use in the treatment of diseases or disorders mediated by bromodomain containing proteins, particularly cancer.

Imidazo [4, 5-C] Quinoline Derivatives As Bromodomain Inhibitors

Novel compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and their use in therapy.

IMIDAZO [4, 5-C] QUINOLINE DERIVATES AS BROMODOMAIN INHIBITORS

Novel compounds of Formula (I) and salts thereof, pharmaceutical compositions containing such compounds and their use in therapy.