1276122-67-8

Basic information

• Product Name: {2-[2-tert-butylmalonyl-Arg(Pbf)]aminoethyl}methylcarbamic acid benzyl ester
• Synonyms: {2-[2-tert-butylmalonyl-Arg(Pbf)]aminoethyl}methylcarbamic acid benzyl ester
• CAS NO: 1276122-67-8
• Molecular Weight: 758.937
• Mol File: 1276122-67-8.mol
• Article Data: 8

Chemical Properties

• CAS DataBase Reference: {2-[2-tert-butylmalonyl-Arg(Pbf)]aminoethyl}methylcarbamic acid benzyl ester(CAS DataBase Reference)
• NIST Chemistry Reference: {2-[2-tert-butylmalonyl-Arg(Pbf)]aminoethyl}methylcarbamic acid benzyl ester(1276122-67-8)
• EPA Substance Registry System: {2-[2-tert-butylmalonyl-Arg(Pbf)]aminoethyl}methylcarbamic acid benzyl ester(1276122-67-8)

Safety Data

• Hazardous Substances Data: 1276122-67-8(Hazardous Substances Data)

Upstream product

• 1048360-18-4 {(S)-4-({amino-[(E)-2,2,4,6,7-pentamethyl-2,3-dihydro-benzofuran-5-sulfonylimino]-methyl}-amino)-1-[2-(benzyloxycarbonyl-methyl-amino)-ethyl carbamoyl]-butyl}-carbamic acid tert-butyl ester 
• 186698-61-3 (S)-2-(tert-butoxycarbonylamino)-5-(3-(2,2,4,6,7-pentamethyl-2,3-dihydrobenzofuran-5-ylsulfonyl)guanidino)pentanoic acid 
• 1048360-18-4 {2-[boc-Arg(Pbf)]-aminoethyl}methylcarbamic acid benzyl ester 
• 200124-22-7 Boc-Arg-(Pbf)-OH 
• 1221593-52-7 methyl-[2-(2,2,2-trifluoro-acetylamino)-ethyl]carbamic acid benzyl ester 
• 40052-13-9 mono-tert-butyl malonate 
• 1048360-17-3 {2-[H-Arg(Pbf)]aminoethyl}methylcarbamic acid benzyl ester 
• 162576-01-4 2-(aminoethyl)methylcarbamic acid benzyl ester hydrochloride 

Downstream Products

• 1345532-66-2 N-[(S)-1-(2-([3-((1R,2R)-3-dimethylamino-1-ethyl-2-methyl-propyl)-phenoxycarbonyl]-methyl-amino)-ethylcarbamoyl)-4-guanidino-butyl]-malonamic acid trifluoroacetate 
• 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 

Relevant articles and documents

An enzyme and its optional [...] modified ketone and inhibitor composition comprising (by machine translation)

PROBLEM TO BE SOLVED: ketone-containing acrylic misuse, abuse or overload is prevented for a new takable amt. provitamin drag pain. SOLUTION: a compound represented by the following formula is represented, in which the drag oxystyrene provitamin hydrocodone ketone-containing acrylic. Pre-selected drug profile is modified and the ketone and schisandrin [...] holding hung contg. compsn. method for administration to a patient. Selected drawing: no (by machine translation)

Compositions Comprising Enzyme-Cleavable Oxycodone Prodrug

The embodiments provide Compound KC-8, N-1-[3-(oxycodone-6-enol-carbonyl-methyl-amino)-2,2-dimethyl-propylamine]-arginine-glycine-malonic acid, or acceptable salts, solvates, and hydrates thereof. The present disclosure also provides compositions, and their methods of use, where the compositions comprise a prodrug, Compound KC-8, that provides controlled release of oxycodone. Such compositions can optionally provide a trypsin inhibitor that interacts with the enzyme that mediates the controlled release of oxycodone from the prodrug so as to attenuate enzymatic cleavage of the prodrug.

COMPOSITIONS COMPRISING ENZYME-CLEAVABLE OPIOID PRODRUGS AND INHIBITORS THEREOF

The present disclosure provides pharmaceutical compositions, and their methods of use, where the pharmaceutical compositions comprise a prodrug that provides enzymatically-controlled release of a drug and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the drug from the prodrug so as to attenuate enzymatic cleavage of the prodrug. The disclosure provides pharmaceutical compositions which comprise an enzyme inhibitor and a prodrug that contains an enzyme-cleavable moiety that, when cleaved, facilitates release of the drug.