79094-23-8

Upstream product

• 210115-50-7 [4-(2-methanesulfonylamino-ethyl)-phenyl]-acetic acid methyl ester 
• 683200-41-1 [4-(2-amino-ethyl)-phenyl]-acetic acid methyl ester 
• 7398-42-7 methyl 2-(4-(bromomethyl)phenyl)acetate 
• 13737-36-5 4-bromophenylacetic acid 

Relevant academic research and scientific papers

Arylacetamide κ opioid receptor agonists with reduced cytochrome P450 2D6 inhibitory activity

Some κ opioid receptor agonists of the arylacetamide class, for example, ICI 199441 (1), were found to strongly inhibit the activity of cytochrome P450 2D6 (CYP2D6) (1: CYP2D6 IC50 = 26 nM). Certain analogs bearing a substituted sulfonylamino group, for example, 13, were discovered to have significantly reduced CYP2D6 inhibitory activity (13: CYP2D6 IC50 > 10 μM) while displaying high affinity toward the cloned human κ opioid receptor, good κ/δ and κ/μ selectivity, and potent in vitro and in vivo agonist activity.

Sulfonylamino phenylacetamide derivatives and methods of their use

Sulfonylamino phenylacetamide derivatives of the general formula are disclosed. Pharmaceutical compositions containing the compounds and methods for their use are also disclosed. In certain embodiments, the compounds of the invention that, preferably: (1) bind with high affinity to κ opioid receptors; (2) display good opioid receptor selectivity of κ versus μ and κ versus δ; and (3) do not substantially inhibit cytochrome P450 enzymatic activity, in particular CYP2D6, CYP2C9 and CYP3A4.

Sulphonamidophenylcarboxylic acid compounds and pharmaceutical compositions containing them

The invention provides sulphonamides of the formula STR1 wherein R is a hydrogen atom or a lower alkyl radical; R1 is alkyl, aryl, aralkyl or aralkenyl, the aryl moiety of which in each case can be optionally substituted one or more times by hydroxyl, halogen, trifluoromethyl, lower alkyl or alkoxy or by acyl, carboxy or alkoxycarbonyl; n is 1, 2 or 3; and W is a valence bond or a divalent aliphatic hydrocarbon linkage and the physiologically acceptable salts, esters and amides of such compound. These compounds have excellent pharmacological lipid depressing activity and inhibit thrombocyte aggregation.