612547-11-2

Usage

Uses

Used in Pharmaceutical Industry:
PL-100 is used as an antiretroviral agent for the treatment and prevention of HIV/AIDS. It is effective in blocking the action of HIV protease, which is crucial for the virus's replication process, thus helping to control the disease's progression in patients.
Used in Clinical Research:
PL-100 is used as a research compound for studying the mechanisms of HIV resistance and the development of new antiretroviral therapies. Its high potency against a wide range of HIV strains, including those resistant to other protease inhibitors, makes it a valuable tool in the ongoing search for more effective treatments for HIV/AIDS.

Upstream product

• 900187-22-6 (1-S)-{4-[(5-tert-butoxycarbonylamino-1-hydroxymethyl-pentyl)-isobutyl-sulfamoyl]-phenyl}-carbamic acid tert-butyl ester 
• 874339-75-0 (3S)-3-{[4-(acetyl-tert-butoxycarbonyl-amino)-benzenesulfonyl]-isobutyl-amino}-2-oxo-azepane-1-carboxylic acid tert-butyl ester 
• 21568-87-6 2-aminocaprolactam 
• 121-60-8 p-acetylaminobenzenesulfonyl chloride 
• 149597-92-2 (S)-β,β-diphenyl-α-alanine 
• 161869-03-0 (S)-2-((methoxycarbonyl)amino)-3,3-diphenylpropanoic acid 
• 449806-99-9 (1S)-4-amino-N-(5-amino-1-hydroxymethyl-pentyl)-N-isobutyl-benzenesulfonamide 
• 449806-97-7 Nα-isobutyl-Nα-(4-acetamidobenzenesulfonyl)-L-α-amino-ε-caprolactam 
• 359782-00-6 (3S)-3-isobutylamino-azepan-2-one 

Downstream Products

• 874339-76-1 (1S,5S)-{1-[5-[(4-amino-benzenesulfonyl)-isobutyl-amino]-6-(diethoxy-phosphoryloxy)-hexylcarbamoyl]-2,2-diphenyl-ethyl}-carbamic acid methyl ester 

Relevant academic research and scientific papers

LYSINE-BASED PRODRUGS OF ASPARTYL PROTEASE INHIBITORS AND PROCESSES FOR THEIR PREPARATION

The present invention provides processes for synthesizing lysine based compounds of the Formula (I); wherein R1 may be, for example, (HO)2P(O)-, (NaO)2P(O)-, wherein X may be, for example, NH2, Y may be H, F, Cl, or Br, and wherein n, X', Y', R2, R3, R4, R5 and R6 are as defined herein.

Lysine sulfonamides as novel HIV-protease inhibitors: Nε-Acyl aromatic α-amino acids

A series of lysine sulfonamide analogues bearing Nε-acyl aromatic amino acids were synthesized using an efficient synthetic route. Evaluation of these novel protease inhibitors revealed compounds with high potency against wild-type and multiple-protease inhibitor-resistant HIV viruses.

LYSINE BASED COMPOUNDS

The present invention provides lysine based compounds of the formula (I); and when the compound of formula (I) comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein Rl may be, for example, (HO)2P(O)-, (NaO)2P(O)-, alkyl-CO- or cycloalkyl-CO-, wherein X may be, for example, F, Cl, and Br, and wherein R2 and R3 are as defined herein. These lysine based compounds have a physiologically cleavable unit, namely R1 , whereby upon cleavage of the unit, an HIV aspartyl protease inhibitor is released,

Lysine based compounds

The present invention provides lysine based compounds of the formula; and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein R1 may be, for example, (HO)2P(O)—, (NaO)2P(O)—, alkyl-CO— or cycloalkyl-CO—, wherein X may be, for example, F, Cl, and Br, and wherein R2 and R3 are as defined herein.

METHOD FOR IMPROVING PHARMACOKINETICS OF PROTEASE INHIBITORS AND PROTEASE INHIBITOR PRECURSORS

The present invention provides methods for improving the pharmacokinetics of protease inhibitors and protease inhibitor precursors and pharmaceutical composition comprising protease inhibitors or protease inhibitor precursors of formula I and a cytochrome P450 monooxigenase inhibitor; Formula (I) when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein R1 may be, for example, (HO)2P(O)-, (NaO)2P(O)-, alkyl- CO- or cycloalkyl-CO-, wherein X may be, for example, F, CI, and Br, and wherein R2 and R3 are as defined herein.