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    • 12. 发明授权
    • Macrolide antiinfective agents
    • 大环内酯类抗感染药
    • US06593302B2
    • 2003-07-15
    • US10075466
    • 2002-02-13
    • Daniel ChuGary Ashley
    • Daniel ChuGary Ashley
    • A61K3170
    • C07H17/08Y02P20/55
    • Compounds of the formula wherein Ra is H; substituted or unsubstituted alkyl (1-10C); substituted or unsubstituted alkenyl (2-10C); substituted or unsubstituted alkynyl (2-10C); substituted or unsubstituted aryl (4-14C); substituted or unsubstituted arylalkyl (5-20C); or ORa is replaced by H; 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 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; L is methylene or carbonyl; T is —O—, —N(R)—, —N(OR)—, —N(NHCOR)—, —N(N═CHR)—, or —N(NHR)— wherein R is H or Ra as defined above, with the proviso that when L is methylene, T is —O—; one of Z and Y is H and the other is OH, protected OH, or amino, mono- or dialkylamino, protected amino, or an amino heterocycle 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.
    • 化学式R a的化合物是H; 取代或未取代的烷基(1-10C); 取代或未取代的烯基(2-10C); 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​​℃); 或ORa被H代替; Rb是H或卤素; Rc是H或保护基; 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​​℃); 取代或未取代的芳基烯基(5-20​​℃); 取代或未取代的芳基炔基(5-20​​℃); 取代或未取代的酰氨基芳基烷基(5-20​​℃); 取代或未取代的酰氨基芳基烯基(5-20​​℃); 或取代或未取代的酰氨基芳基炔基(5-20​​℃); Re是H或保护基; L是亚甲基或羰基; T是-O-,-N(R) - , - N(OR) - , - N(NHCOR) - ,-N(N = CHR) - 或-N(NHR) - ,其中R是如上定义的H或Ra,条件是当L是亚甲基时,T是-O-; Z和Y之一是H 另一个是OH,保护的OH或氨基,单或二烷基氨基,保护的氨基或氨基杂环,或Z和Y一起为= 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形式, 其立体异构形式的混合物是抗微生物剂。