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Antiviral compounds of fosfodiamida beta amino acid ester

机译:大叶双孢菌β氨基酸酯的抗病毒化合物

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.
机译:本发明涉及式I化合物,其中R 1和R 2各自独立地选自h,c 1 -c 4烷基,苯基-CH 2-,以及其他。 R 3是未被取代的C 1 -C 10烷基,-CH 2-未被取代的芳基苯基,其中,ra是其余的-式I的L-氨基酸酯,其余是D-的式II的氨基酸酯,等等。 R4是C1-C4烷基,芳基-CH2-苯酚; R9是C1-C10烷基,芳基苯基-CH2-(未取代)等。化合物是最喜欢的:N-[(S)-{[((R)-2-(6--氨基-9h嘌呤-9-yl))甲基]-1-甲氧} {[((2S)-2-甲基-3-(1-甲氧))-3-氧代丙基]氨基} fosforil l-alaninate]-1-甲铁; n-[(R)-{[((R)-2-(6-氨基-9H-浆液-9-yl)甲基)]-1-甲毒素} {[((2S)-2-甲基-3-(1- (Metiletoxi)-3-氧代丙基]氨基}-1] fosforil 1-丙氨酸盐-metiletilico等。它可用于抑制HIV逆转录酶,可用于其预防,治疗和预防和/或延缓AIDS和/或ARC的发作或发展。

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