52574-79-5

Upstream product

• 25026-34-0 4-chlorophenacetyl chloride 
• 1878-66-6 4-chlorophenylacetic Acid 
• 3381-73-5 2-bromo-2-(4-chlorophenyl)acetic acid 
• 6212-33-5 2-(4-Chlorophenyl)glycine 

Downstream Products

• 116952-76-2 2-Brom-2-(4-chlorphenyl)-N'-tosylacetohydrazid 
• 873659-40-6 N-(4-amino-2-benzoylphenyl)-2-(4-chlorophenyl)-2-(4-methyl-1-piperazinyl)acetamide 
• 116952-88-6 N-<1-Chlor-2-(4-chlorphenyl)ethenyl>-N'-tosyldiazen 
• 116952-82-0 2-Brom-2-(4-chlorphenyl)-N-tosylacetohydrazonoylchlorid 
• 103807-49-4 Bromo-(4-chloro-phenyl)-acetic acid isopropyl ester 
• 101486-02-6 4-chlorophenyl-alpha-bromoacetic acid 3-iodopropargyl ester 
• 930779-79-6 (2S)-1-oxo-1-(pyrrolidin-1-yl)propan-2-yl 2-bromo-2-(4-chlorophenyl)acetate 
• 23953-39-1 (2R)-2-(4-chlorophenyl)-2-[3-(trifluoromethyl)phenoxy]acetic acid 

Relevant academic research and scientific papers

Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer

The bromodomain and extra-terminal proteins (BET) have emerged as promising therapeutic targets for the treatment of castration-resistant prostate cancer (CRPC). We report the design, synthesis and evaluation of a new series of benzoxazinone-containing 3,5-dimethylisoxazole derivatives as selective BET inhibitors. One of the new compounds, (R)-12 (Y02234), binds to BRD4(1) with a Kd value of 110 nM and blocks bromodomain and acetyl lysine interactions with an IC50 value of 100 nM. It also exhibits selectivity for BET over non-BET bromodomain proteins and demonstrates reasonable anti-proliferation and colony formation inhibition effect in prostate cancer cell lines such as 22Rv1 and C4-2B. The BRD4 inhibitor (R)-12 also significantly suppresses the expression of ERG, Myc and AR target gene PSA at the mRNA level in prostate cancer cells. Treatment with (R)-12 significantly suppresses the tumor growth of prostate cancer (TGI = 70%) in a 22Rv1-derived xenograft model. These data suggest that compound (R)-12 is a promising lead compound for the development of a new class of therapeutics for the treatment of CRPC.

COMPOSITIONS AND METHODS FOR THE TREATMENT OF METABOLIC SYNDROME

The invention relates to the compounds of formula (I) or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula (I), and methods for the treatment of metabolic syndrome may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of hyperuricemia, gout; dyslipidemia, obesity, urea cycle disorders, hyperglycemia, insulin resistance, diabetes mellitus, diabetes insipidus, type 1 diabetes, type 2 diabetes, microvascular complications,.macrovascular complications, lipid disorders, prediabetes., obesity, arrhythmia, myocardial infarction, stroke, neuropathy, renal complications, hypertriglyceridemia, cardiovascular complications, and post prandial hyperglycemia.

RESOLUTION OF α-(PHENOXY)PHENYLACETIC ACID DERIVATIVES

The present invention provides a method for producing an enantiomerically enriched alpha-(phenoxy)phenylacetic acid compound of the formula (I): from its enantiomeric mixture, where R1 is alkyl or haloalkyl and X is halide.

N-phenyl-n-alkoxycarbonylalkyl glycinamides, their preparation and the medicaments containing them

This invention relates to compounds of formula: STR1 in which R1 represents a hydrogen atom or an alkyl or alkoxycarbonyl radical or an unsubstituted or substituted phenyl radical, R2 represents an alkyl (1-8 C) or polyfluoroalkyl ra

Synthesis of Substituted Ethenyldiazenes

N-(1-Chloroethenyl)-N'-tosyldiazenes 5 are potential precursors to obtaine alkyne diazonium salts 6.Their multistep synthesis starts with substituted acetic acids.The aromatic diazenes 5 are crystalline, intensively orange compounds, which melt above 100