Lysine based compounds

Details Lysine based compounds Lysine based compounds

C - Chemistry, Metallurgy

07

C

C07C 311/37 (2006.01) A61K 31/18 (2006.01) A61K 31/4164 (2006.01) A61K 31/44 (2006.01) A61K 31/445 (2006.01) A61K 31/47 (2006.01) A61K 31/498 (2006.01) A61K 31/5375 (2006.01) C07D 207/44 (2006.01) C07D 213/72 (2006.01) C07D 215/38 (2006.01) C07D 217/22 (2006.01) C07D 233/88 (2006.01) C07D 241/44 (2006.01) C07D 265/30 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01) C07D 405/12 (2006.01)

Patent

CA 2560071

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,

La présente invention concerne des composés à base de lysine de formule (I), et, lorsque le composé de formule (I) comprend un groupement aminé, les sels d~ammonium pharmaceutiquement acceptables de ceux-ci, dans laquelle Rl peut être, par exemple, (HO)2P(O)-, (NaO)2P(O)-, alkyl­CO- ou cycloalkyl-CO-, X pouvant être, par exemple, F, Cl, et Br, et R2 et R3 étant tels que définis dans ce texte. Ces composés à base de lysine possèdent un motif physiologiquement clivable, à savoir R1, permettant, lors du clivage du motif, la libération d~un inhibiteur de l~aspartyl-protéase du VIH,

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