1345532-66-2

Upstream product

• 1276121-61-9 N-{2-[2-tert-butylmalonyl-Arg(Pfb)]}-N'-methylethane-1,2-diamine 
• 1276122-67-8 {2-[2-tert-butylmalonyl-Arg(Pbf)]aminoethyl}methylcarbamic acid benzyl ester 
• 1048360-17-3 {2-[H-Arg(Pbf)]aminoethyl}methylcarbamic acid benzyl ester 
• 1048360-18-4 {2-[boc-Arg(Pbf)]-aminoethyl}methylcarbamic acid benzyl ester 
• 1345532-64-0 N-((S)-1-(2-([3-((1R,2R)-3-dimethylamino-1-ethyl-2-methyl-propyl)-phenoxycarbonyl]-methyl-amino)-ethylcarbamoyl)-4-(2,2,4,6,7-pentamethyldihydrobenzofuran-5-sulfonyl-guanidino)-butyl)-malonamic acid tert-butyl ester 
• 76-05-1 trifluoroacetic acid 

Relevant academic research and scientific papers

COMPOSITIONS COMPRISING ENZYME-CLEAVABLE PHENOL-MODIFIED TAPENTADOL PRODRUG

A method of providing a patient with controlled release of tapentadol using a prodrug capable, upon enzymatic activation and intramolecular cyclization, of releasing tapentadol is disclosed. The disclosure also provides such prodrug compounds and pharmaceutical compositions comprising such compounds. Such pharmaceutical compositions can optionally include an enzyme inhibitor that interacts with the enzyme(s) to mediate the enzymatically-controlled release of tapentadol from the prodrug so as to modify enzymatic cleavage of the prodrug. Also included are methods to use such compounds and pharmaceutical compositions.