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    • 86. 发明申请
    • 4-AMINO-3-HYDROXYCARBOXYLIC ACID DERIVATIVES
    • 4-氨基-3-羟基羧酸衍生物
    • WO1993001166A1
    • 1993-01-21
    • PCT/EP1992001471
    • 1992-06-30
    • SANDOZ LTD.SANDOZ-PATENT-GMBHBILLICH, AndreasCHARPIOT, BrigitteLEHR, PhilipSCHOLZ, Dieter
    • SANDOZ LTD.SANDOZ-PATENT-GMBH
    • C07C271/22
    • C07D213/30A61K38/00C07C271/22C07C323/59C07C323/60C07D209/16C07D209/20C07D213/38C07D213/40C07D215/36C07D233/64C07D235/12C07D235/14C07K5/0205Y02P20/55
    • The invention concerns the compounds of formula (I) wherein A and B independently are a bond or optionally substituted aminoacyl; R1 is hydrogen; an amino protecting group; or a group of formula R6Y- wherein R6 is hydrogen or an optionally substituted alkyl, alkenyl, alkinyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl or heterocyclylalkyl group; and Y is -CO-; -NHCO-; NHCS-; -SO2-; -O-CO-; or -O-CS-; R2 is the side chain of a natural amino acid; an alkyl, arylalkyl, heteroarylalkyl or cycloalkylalkyl group; or trimethylsilylmethyl, 2-thienylmethyl or styrylmethyl; R3 is an optionally substituted alkyl, alkenyl, alkinyl, cyloalkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl group; R4 is a group of formula -OR7 or -NHR7 wherein R7 has the significance indicated above for R6; and X is -S- or -NR5- wherein R5 is hydrogen, methyl, formyl or acetyl; in free form and, where such forms exist, in salt form. They can be obtained by a process comprising epoxide ring opening, appropriate substitution and/or deprotection or saponification. They have antiviral activity, particularly HIV-1 proteinase inhibiting activity, and are thus indicated for use in the treatment of retroviral diseases.
    • 本发明涉及式(I)的化合物,其中A和B独立地是一个键或任选取代的氨酰基; R1是氢; 氨基保护基; 烯基,炔基,芳基,芳基烷基,杂芳基,杂芳基烷基,杂环基或杂环基烷基;或其中R 6为氢或任选取代的烷基,烯基,炔基,芳基, Y为-CO-; -NHCO-; NHCS-; -SO2-; -O-CO-; 或-O-CS-; R2是天然氨基酸的侧链; 烷基,芳基烷基,杂芳基烷基或环烷基烷基; 或三甲基甲硅烷基甲基,2-噻吩基甲基或苯乙烯基甲基; 链烯基,炔基,环烷基,芳基,芳基烷基,杂芳基或杂芳基烷基; R4是式-OR7或-NHR7的基团,其中R7具有上面对R6表示的含义; 并且X是-S-或-NR 5 - ,其中R 5是氢,甲基,甲酰基或乙酰基; 以形式存在,且以盐形式存在。 它们可以通过包括环氧化物开环,适当取代和/或去保护或皂化的方法获得。 它们具有抗病毒活性,特别是HIV-1蛋白酶抑制活性,因此被指示用于治疗逆转录病毒疾病。