149597-89-7

Upstream product

• 149597-92-2 (S)-β,β-diphenyl-α-alanine 
• 75-36-5 acetyl chloride 

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.

Production method of optically active dephenylalanine compounds

Optically active diphenylalanine compounds may be conveniently prepared in a good yield by reacting a diphenylalanine compound represented by formula (1) with an optically active amine compound represented by formula (2) in the presence of an organic solvent to give a diastereomeric salt represented by formula (5) and then treating the diastereomeric salt under acidic conditions to give an optically active diphenylalanine compound represented by formula (3): wherein each symbol is as defined in the specification.

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.

Aromatic derivatives as HIV aspartyl protease inhibitors

The present invention provides HIV aspartyl protease inhibitors of the formula; and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein n is 3 or 4, wherein R1may be, for example,