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    • 10. 发明授权
    • Motilide compounds
    • 化合物
    • US06750205B2
    • 2004-06-15
    • US10409429
    • 2003-04-07
    • Gary AshleyMark BurlingameChristopher CarrerasDaniel Santi
    • Gary AshleyMark BurlingameChristopher CarrerasDaniel Santi
    • A61K3170
    • C07H17/08
    • 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.
    • 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。