MACROLIDE ANTIINFECTIVE AGENTS
    72.
    发明公开

    公开(公告)号:EP1171448A2

    公开(公告)日:2002-01-16

    申请号:EP00925966.4

    申请日:2000-04-14

    IPC分类号: C07H17/08 A61K31/70

    CPC分类号: Y02P20/55

    摘要: Compounds of formula (1), (2) or (3) or the 10,11-anhydro forms thereof, wherein Ra is H or OH; Rb is H or halogen; Rc is H or a protecting group; Rd is methyl; unsubstituted alkyl(3-10C); substituted alkyl(1-10C); substituted or unsubstituted alkenyl(2-10C) or substituted or unsubstituted alkynyl(2-10C); substituted or unsubstituted aryl(4-14C); substituted or unsubstituted arylalkyl(5-20C); substituted or unsubstituted arylalkenyl(5-20C); substituted or unsubstituted arylalkynyl(5-20C); substituted or unsubstituted amidoarylalkyl(5-20C); substituted or unsubstituted amidoarylalkenyl(5-20C); or substituted or unsubstituted amidoarylalkynyl(5-20C); Re is H or a protecting group or is mono- or disubstituted amino carbonyl; Rf is H; substituted or unsubstituted alkyl(1-10C), substituted or unsubstituted alkenyl(1-10C); substituted or unsubstituted alkynyl(1-10C); substituted or unsubstituted aryl(4-14C); substituted or unsubstituted arylalkyl(5-20C); or -ORf may be replaced by -H; one of Z and Y is H and the other is OH or protected OH, or is amino, mono- or dialkyl-amino, protected amino, or an aminoheterocycle or Z and Y together are =O, =NOH or a derivatized oxime; including any pharmaceutically acceptable salts thereof and any stereoisomeric forms and mixtures of stereoisomeric forms thereof, are antimicrobial agents.

    摘要翻译: 式(1),(2)或(3)的化合物或其10,11-脱水形式,其中Ra是H或OH; Rb是H或卤素; Rc是H或保护基团; Rd是甲基; 未取代的烷基(3-10C); 取代的烷基(1-10C); 取代或未取代的烯基(2-10C)或取代或未取代的炔基(2-10C); 取代或未取代的芳基(4-14C); 取代或未取代的芳基烷基(5-20​​C); 取代或未取代的芳基链烯基(5-20​​℃); 取代或未取代的芳基炔基(5-20​​C); 取代或未取代的酰氨基芳烷基(5-20​​C); 取代或未取代的酰胺基链烯基(5-20​​℃); 或取代或未取代的酰胺基芳炔基(5-20​​C); Re是H或保护基团或者是单取代或二取代的氨基羰基; Rf是H; 取代或未取代的烷基(1-10C),取代或未取代的链烯基(1-10C); 取代或未取代的炔基(1-10C); 取代或未取代的芳基(4-14C); 取代或未取代的芳基烷基(5-20​​C); 或-ORf可以被-H取代; Z和Y中的一个是H,另一个是OH或被保护的OH,或者是氨基,单或二烷基氨基,被保护的氨基或氨基杂环,或者Z和Y一起是= O,= NOH或衍生的肟; 包括其任何药学上可接受的盐和任何立体异构体形式及其立体异构体形式的混合物是抗微生物剂。