VACHAL, Petr,RAHEEM, Izzat T.,GUO, Zhiqiang,HARTINGH, Timothy John
申请号:
PE0002162018
公开号:
PE10162018A1
申请日:
2016.08.08
申请国别(地区):
PE
年份:
2018
代理人:
摘要:
The present Invention relates to a compound of formula I, in which R1 and R2 are each independently selected from h, c1-c4 alkyl, phenyl - CH2 -,Among others R3 is C1 - C10 alkyl unsubstituted, - CH2 - unsubstituted aryl phenyl, not replaced, among others, ra is a rest of L - amino acid ester of formula I,A rest of D - amino acid ester of formula II, among others R4 is c1-c4 alkyl, aryl - CH2 - phenol R9 is C1 - C10 alkyl, aryl phenyl - CH2 -, not replaced, among others.Compounds are Favorites: N - [(S) - {[(1R) - 2 - (6 - amino - 9h purin - 9 - yl) methyl] - 1 - metiletoxi} {[(2S) - 2 - methyl - 3 - (1 - metiletoxi) - 3-oxopropyl] amino} fosforil l-alaninate] - 1 - metiletilico n - [(R) - {[(1R) - 2 - (6 - amino - 9H - slurry - 9 - yl) methyl] - 1 - metiletoxi} {[(2S) - 2 - methyl - 3 - (1 - metiletoxi) - 3-oxopropyl] amino} - 1] fosforil l-alaninate - metiletilico, among others.The present Invention also relates to a Pharmaceutical composition comprising an effective amount of one or more HIV antiviral agent such as abacavir, efavirenz,Among others, and a pharmaceutically acceptable vehicle.It is useful for the inhibition of HIV reverse transcriptase, both for its Prevention, Treatment and prophylaxis and \/ or delay the onset or progression of AIDS and \/ or ARC.La presente invencion refiere un compuesto de formula I, en la que R1 y R2 se seleccionan cada uno independientemente entre H, -alquilo C1-C4, -CH2-fenilo, entre otros R3 es -alquilo C1-C10 no sustituido, -CH2-fenilo no sustituido, arilo no sustituido, entre otros RA es un resto de ester de L-aminoacido de formula i, un resto de ester de D-aminoacido de formula ii, entre otros R4 es -alquilo C1-C4, -CH2-fenol, arilo R9 es -alquilo C1-C10, -CH2-fenilo, arilo no sustituido, entre otros. Son compuestos favoritos: N-[(S)-{[(1R)-2-(6-amino-9H-purin-9-il)-1-metiletoxi]metil}{[(2S)-2-metil-3-(1-metiletoxi)-3-oxopropil]amino}fosforil]-L-alaninato 1-metiletilico N-[(R)-{[(1R)-2-(6-amino-9H-purin-9-il)-1-metiletoxi