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    • 1. 发明授权
    • Ketolide antibacterials
    • 酮内酯抗菌剂
    • US06590083B1
    • 2003-07-08
    • US09691540
    • 2000-10-18
    • Dennis HlastaTodd C. HenningerEugene B. GrantChaitin KhoslaDaniel T. W. ChuGary Ashley
    • Dennis HlastaTodd C. HenningerEugene B. GrantChaitin KhoslaDaniel T. W. ChuGary Ashley
    • C07H1708
    • C07H17/08Y02P20/55
    • The present invention includes compounds of the formula wherein: X is hydrogen or halide; R2 is hydrogen, acyl, or a hydroxy protecting group; R6 is hydrogen, hydroxyl, or —ORa wherein Ra is a substituted or unsubstituted moiety selected from the group consisting of C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl; R13 is hydrogen or a substituted or unsubstituted moiety wherein the moiety is selected from the group consisting of methyl; C3-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl; and, R is hydrogen or a substituted or unsubstituted moiety wherein the moiety is selected from the group consisting of C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl; and the pharmaceutically acceptable salts, esters and pro-drug forms thereof. These compounds possess anti-infective activity and are useful for the treatment of bacterial and protozoal infections.
    • 本发明包括糠醛的化合物:X是氢或卤化物; R 2是氢,酰基或羟基保护基; R 6是氢,羟基或-OR a,其中R a是选自以下的取代或未取代的部分: C 1 -C 10烷基,C 2 -C 10烯基,C 2 -C 10炔基,芳基,杂环基,芳基(C 1 -C 10)烷基,芳基(C 2 -C 10)烯基,芳基(C 2 -C 10)炔基,杂环(C 1 -C 10) ,杂环基(C 2 -C 10)烯基和杂环基(C 2 -C 10)炔基; R 13是氢或取代或未取代的部分,其中该部分选自甲基; C 1 -C 10烷基,C 2 -C 10烯基,C 2 -C 10炔基,芳基,杂环基,芳基(C 1 -C 10)烷基,芳基(C 2 -C 10) ,杂环基(C 2 -C 10)烯基和杂环基(C 2 -C 10)炔基; C 1 -C 10烷基,C 2 -C 10烯基,C 2 -C 10炔基,芳基,杂环基,芳基(C 1 -C 10)烷基,芳基(C 1 -C 10) C 2 -C 10)烯基,芳基(C 2 -C 10)炔基,杂环基(C 1 -C 10)烷基,杂环(C 2 -C 10)烯基和杂环(C 2 -C 10)炔基;及其药学上可接受的盐,酯和前药 形式。 这些化合物具有抗感染活性,可用于治疗细菌和原生动物感染。