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    Motilide compounds
    10.
    发明授权
    Motilide compounds 有权
    化合物

    公开(公告)号：US06750205B2

    公开(公告)日：2004-06-15

    申请号：US10409429

    申请日：2003-04-07

    申请人： Gary Ashley ,  Mark Burlingame ,  Christopher Carreras ,  Daniel Santi

    发明人： Gary Ashley ,  Mark Burlingame ,  Christopher Carreras ,  Daniel Santi

    IPC分类号： A61K3170

    CPC分类号： C07H17/08

    摘要： The present invention provides novel macrolide compounds of the formulas wherein: R is hydroxyl or methoxy; R1 is selected from the group consisting of hydrogen, hydroxyl, halide, NH2, OR9, where R9 is C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl or heteroaryl and R10 and R11 are each independently hydrogen, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, or aryl; R2 and R3 are each independently selected from the group consisting of hydrogen, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, alkylaryl, alkenylaryl alkynylaryl or R2 and R3 together form a cycloalkyl or a cycloaryl moiety; R4 is hydrogen or methyl; R5 is hydrogen, hydroxyl, oxo, or together with R6 and the carbons to which they are attached form a cyclic carbonate; R6 is hydrogen, hydroxyl, OR12 where R12 is C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, or together with R5 and the carbons to which they are attached form a cyclic carbonate; R7 is methyl, C3-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, alkylaryl, alkenylaryl, alkynylaryl, amidoalkylaryl, amidoalkenylaryl, or amidoalkynylaryl; R8 is C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, alkylaryl, alkenylaryl, alkynylaryl, amidoalkylaryl, amidoalkenylaryl, or amidoalkynylaryl; and, x is a single or a double bond.

    摘要翻译： 本发明提供下式的新型大环内酯化合物，其中R是羟基或甲氧基; R 1选自氢，羟基，卤素，NH 2，OR 9，其中R 9是C 1 -C 10 烷基，C 2 -C 10烯基，C 2 -C 10炔基，芳基或杂芳基，R 10和R 11各自独立地为氢，C 1 -C 10烷基，C 2 -C 10烯基，C 2 -C 10炔基或芳基; R 2和R 3各自独立地选自氢，C 1 -C 10烷基，C 2 -C 10烯基，C 2 -C 10炔基，芳基，烷基芳基，烯基芳基炔基芳基或R 2和R 3一起 形成环烷基或环芳基部分; R 4是氢或甲基; R 5是氢，羟基，氧代或与R 6一起，并且它们连接的碳形成环状碳酸酯; 其中R 12是C 1 -C 10烷基，C 2 -C 10烯基，C 2 -C 10炔基，或与R 5一起形成的碳原子和它们所连接的碳原子形成环状 碳酸酯; R 7是甲基，C 3 -C 10烷基，C 2 -C 10烯基，C 2 -C 10 炔基，烷基芳基，烯基芳基，炔基芳基，酰氨基烷基芳基，酰氨基烯基芳基或酰胺基炔基芳基; R 8是C 1 -C 10烷基，C 2 -C 10烯基，C 2 -C 10炔基，烷基芳基，链烯基芳基，炔基芳基，酰氨基烷基芳基，酰胺基烯基芳基或酰胺基炔基芳基; x是单键或双键。