首页> 外国专利> (R)-N-(1,1-dimethylethyl)-3-(2S,3S)-2-hydroxy-3-(R)-2-(5-isoquinolyloxyacetyl)amino-3-methylthiopropanoyl amino-4-phenylbutanoyl-1,3-thiazolidine-4-carboxyamide (KNI-272) an another agent for the treatment of AIDS

(R)-N-(1,1-dimethylethyl)-3-(2S,3S)-2-hydroxy-3-(R)-2-(5-isoquinolyloxyacetyl)amino-3-methylthiopropanoyl amino-4-phenylbutanoyl-1,3-thiazolidine-4-carboxyamide (KNI-272) an another agent for the treatment of AIDS

机译:(R)-N-(1,1-二甲基乙基)-3-[(2S,3S)-2-羟基-3-[(R)-2-(5-异喹啉基氧基乙酰基)氨基-3-甲基硫代丙酰基]氨基-4 -苯基丁酰基] -1,3-噻唑烷-4-羧酰胺(KNI-272)是另一种治疗艾滋病的药物

摘要

An AIDS therapeutic composition comprising, as essential effective components which bring about a human immunodeficiency virus protease inhibition action, (R)-N-(1,1-dimethylethyl)-3-[(2S,3S)-2-hydroxy-3-[(R)-2-(5-isoquinolyloxyacetyl)amino-3-methylthiopropanoyl] amino-4-phenylbutanoyl]-1,3-thiazolidine-4-carboxyamide (KNI-272) and a compound selected from the group consisting of N-(1,1-dimethylethyl)-decahydro-2-[2(R)-hydroxy-4-phenyl-3(S)-{[N-(2-quinolylcarbonyl)-L-asparaginyl]amino}butyl]-(4aS, 8aS)-isoquinoline-3(S)-carboxyamide (Saquinavir), 5S-(5R*, 8R*, 10R*,11R*)-10-hydroxy-2-methyl-5-(1-methylethyl)-1-[2-(1-methylethyl)-4-thiazolyl]-3,6-dioxo-8,11-bis(phenyl methyl)-2,4,7,12-tetrazatridecane-13-hydroxy acid, 5-thiazolylmethyl ester (Ritonavir), [1(1S, 2R),5(S)]-2,3,5-trideoxy-N-(2,3-dihydro-2-hydroxy-1H-inden-1-yl)-5-[2-{[(1,1-dimethylethyl) amino]carbonyl}-4-(3-pyridinylmethyl)-1-p iperazinyl]-2-(phenylmethyl)-D-erythropentonamide (Indinavir), and [3S-2(2S*, 3S*), 3 alpha , 4a beta , 8a beta ]]-N-(1,1-dimethylethyl)-decahydro-2-[2-hydroxy-3-(3-hydroxy-2-methylbenzoyl)amino]-4-(phenylthio)butyl]-3-isoquinolinecarboxamide (Nelfinavir), in an amount and proportion in which a synergistic treatment effect can be exhibited.
机译:一种艾滋病治疗组合物,其包含(R)-N-(1,1-二甲基乙基)-3-[(2S,3S)-2-羟基-3-作为必需的有效成分来实现人类免疫缺陷病毒蛋白酶的抑制作用。 [(R)-2-(5-异喹啉基氧基乙酰基)氨基-3-甲基硫代丙酰基]氨基-4-苯基丁酰基] -1,3-噻唑烷-4-羧酰胺(KNI-272)和选自N-的化合物(1,1-二甲基乙基)-十氢-2- [2(R)-羟基-4-苯基-3(S)-{[N-(2-喹啉基羰基)-L-天冬酰胺基]氨基}丁基]-(4aS ,8aS)-异喹啉-3(S)-羧酰胺(沙奎那韦),5S-(5R *,8R *,10R *,11R *)-10-羟基-2-甲基-5-(1-甲基乙基)-1- [2-(1-甲基乙基)-4-噻唑基] -3,6-二氧-8,11-双(苯基甲基)-2,4,7,12-十四碳三烷-13-羟基酸,5-噻唑基甲基酯(利托那韦),[1(1S,2R),5(S)]-2,3,5-三苯氧基-N-(2,3-二氢-2-羟基-1H-茚满-1-基)-5- [ 2-{[((1,1-二甲基乙基)氨基]羰基} -4-(3-吡啶基甲基)-1-p哌嗪基] -2-(苯基甲基)-D-赤藓糖酰胺(Indinavir)和[3S-2(2S) *,3S *),3 alpha,4 a beta,8a beta]]-N-(1,1-二甲基乙基)-十氢-2- [2-羟基-3-(3-羟基-2-甲基苯甲酰基)氨基] -4-(苯硫基)丁基] -3 -异喹啉甲酰胺(Nelfinavir),其量和比例可显示出协同治疗作用。

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