132691-38-4

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 754959-55-2 methyl 2-(3-(aminomethyl)phenyl)acetate 
• 150529-73-0 methyl 2-(3-bromophenyl)acetatee 
• 52798-00-2 (3-cyano-phenyl)-acetic acid methyl ester 
• 1878-67-7 3-Bromophenylacetic acid 

Downstream Products

• 71420-95-6 2-(3-(((tertbutoxycarbonyl)amino)methyl)phenyl)acetic acid 
• 808753-16-4 [3-({methyl-[1-(S)-phenyl-2-pyrrolidin-1-yl-ethyl]-carbamoyl}-methyl)-benzyl]-carbamic acid tert-butyl ester 
• 808753-19-7 2-(3-aminomethyl-phenyl)-N-methyl-N-(1-phenyl-2-pyrrolidin-1-yl-ethyl)-acetamide 

Relevant academic research and scientific papers

COMPOUNDS AND THEIR METHODS OF USE

Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.

COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USES AS GLUTAMINASE INHIBITORS FOR TREATING CANCERS THEREOF

Provided are compounds of formula (I), wherein X, Y, Z, W, m, n, o, p, R1, R2 and R6 are defined as in the description. Pharmaceutical compositions and uses as glutaminase inhibitors for treating cancers thereof are also provided.

COMPOUNDS AND THEIR METHODS OF USE

Provided are compounds of formula (I), which can inhibit glutaminase. Pharmaceutical compositions comprising these compounds and uses as glutaminase inhibitors for treating cancers thereof are also provided.

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.