855198-27-5

Upstream product

• 64-67-5 diethyl sulfate 
• 140472-69-1 3-bromo-5-hydroxy-benzoic acid 
• 1229442-68-5 ethyl 3-bromo-5-ethoxybenzoate 
• 1180016-48-1 3-bromo-5-ethoxy-benzonitrile 

Downstream Products

• 1333896-50-6 1-(3-bromo-5-ethoxyphenyl)ethanone 
• 1333896-53-9 1-(3-(3,5-dimethylisoxazol-4-yl)-5-ethoxyphenyl)ethanone 
• 1333896-54-0 (RS)-1-(3-(3,5-dimethylisoxazol-4-yl)-5-ethoxyphenyl)ethanol 
• 1180016-49-2 3-bromo-5-ethoxy-N-methoxy-N-methylbenzamide 

Relevant academic research and scientific papers

HYDROXY FORMAMIDE DERIVATIVES AND THEIR USE

Disclosed are compounds having the formula: (I) wherein R1, R2 and R3 are as defined herein, and methods of making and using the same, including use as inhibitors of BMP1, TLL1 and/or TLL2 and in treatment of diseases associated with BMP1, TLL1 and/or TLL2 activity.

3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands

Histone-lysine acetylation is a vital chromatin post-translational modification involved in the epigenetic regulation of gene transcription. Bromodomains bind acetylated lysines, acting as readers of the histone-acetylation code. Competitive inhibitors of this interaction have antiproliferative and anti-inflammatory properties. With 57 distinct bromodomains known, the discovery of subtype-selective inhibitors of the histone-bromodomain interaction is of great importance. We have identified the 3,5-dimethylisoxazole moiety as a novel acetyl-lysine bioisostere, which displaces acetylated histone-mimicking peptides from bromodomains. Using X-ray crystallographic analysis, we have determined the interactions responsible for the activity and selectivity of 4-substituted 3,5-dimethylisoxazoles against a selection of phylogenetically diverse bromodomains. By exploiting these interactions, we have developed compound 4d, which has IC50 values of 5 μM for the bromodomain-containing proteins BRD2(1) and BRD4(1). These compounds are promising leads for the further development of selective probes for the bromodomain and extra C-terminal domain (BET) family and CREBBP bromodomains.

4,5-DIHYDRO-OXAZOL-2-YL AMINE DERIVATIVES

The present invention relates to a compounds of formula I wherein R1, R1′, R2, R3, R4, X, Ar, and m are as defined in the specification and claims and pharmaceutically active acid addition salts thereof. Compounds of the invention have Asp2 (β-secretase, BACE 1 or Memapsin-2) inhibitory activity and are useful for the treatment of diseases characterized by elevated β-amyloid levels or β-amyloid deposits, particularly Alzheimer's disease.