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16 条记录 (耗时 0.016 秒)

    MOTILIDE COMPOUNDS
    1.
    发明公开
    MOTILIDE COMPOUNDS 审中-公开
    MOTILIDE化合物

    公开(公告)号：EP1255763A2

    公开(公告)日：2002-11-13

    申请号：EP01910921.4

    申请日：2001-02-15

    申请人： Kosan Biosciences, Inc.

    发明人： ASHLEY, Gary ,  BURLINGAME, Mark ,  CARRERAS, Christopher ,  SANTI, Daniel

    IPC分类号： C07H17/08 ,  A61K31/70

    CPC分类号： C07H17/08

    摘要： The present invention provides novel macrolide compounds of the formulas (I, II, III or IV) wherein: R is hydroxyl or methoxy; R1 is selected from the group consisting of hydrogen, hydroxyl, halide, NH¿2, OR?9, (a, b, c, and d) where R9 is C1-C10 alkenyl, C2-C10 alkynyl, aryl or heteroaryl and R?10 and R11¿ are each independently hydrogen, C¿1?-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, or aryl; R?2 and R3¿ are each independently selected from the group consisting of hydrogen, C¿1?-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, alkylaryl, alkenylaryl, alkynylaryl or R?2 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： 本发明提供了式（I，II，III或IV）的新的大环内酯化合物，其中：R是羟基或甲氧基; （a，b，c和d），其中R 9为C 1 -C 10烯基，C 2 -C 10炔基，芳基或杂芳基，R 1选自氢，羟基，卤素，NH 2，OR 9 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 2和R 3' 形成环烷基或环芳基部分; R4是氢或甲基; R5是氢，羟基，氧代或与R6和它们所连接的碳一起形成环状碳酸酯; R6为氢，羟基，OR12，其中R12为C1-C10烷基，C2-C10烯基，C2-C10炔基或与R5和它们所连接的碳一起形成环状碳酸酯; R7为甲基，C3-C10烷基，C2-C10烯基，C2-C10炔基，烷基芳基，烯基芳基，炔基芳基，酰氨基烷基芳基，酰氨基烷芳基或酰氨基烷芳基; R8为C1-C10烷基，C2-C10烯基，C2-C10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氨基炔基芳基; 并且，x是单键或双键。

    LAULIMALIDE DERIVATIVES
    5.
    发明公开
    LAULIMALIDE DERIVATIVES 审中-公开
    LAULIMALIDE衍生物

    公开(公告)号：EP1358186A1

    公开(公告)日：2003-11-05

    申请号：EP02703356.2

    申请日：2002-02-08

    申请人： Kosan Biosciences, Inc.

    发明人： ASHLEY, Gary ,  METCALF, Brian

    IPC分类号： C07D417/06 ,  C07D493/18 ,  C07D493/08 ,  A61K31/335

    CPC分类号： C07D493/08

    摘要： Laulimalide compounds, intermediates thereto and methods for their preparation and methods for their use in the treatment of diseases characterized by cellular hyperproliferation. Formula (I).

    摘要翻译： 劳拉米尔化合物，其中间体及其制备方法和它们用于治疗以细胞过度增殖为特征的疾病的方法。 公式（I）。

    KETOLIDE ANTIBACTERIALS
    8.
    发明公开
    KETOLIDE ANTIBACTERIALS 审中-公开
    酮内酯类作为抗菌剂

    公开(公告)号：EP1345953A2

    公开(公告)日：2003-09-24

    申请号：EP01981580.2

    申请日：2001-10-12

    申请人： Ortho-McNeil Pharmaceutical, Inc. ,  Kosan Biosciences, Inc.

    发明人： HLASTA, Dennis ,  HENNINGER, Todd, C. ,  GRANT, Eugene, B. ,  KHOSLA, Chaitin ,  CHU, Daniel, T., W. ,  ASHLEY, Gary

    IPC分类号： C07H17/08 ,  A61K31/7048 ,  A61P31/04

    CPC分类号： C07H17/08 ,  Y02P20/55

    摘要： 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 C¿1?-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; R?13¿ is hydrogen or a substituted or unsubstituted moiety wherein the moiety is selected from the group consisting of methyl; C¿3?-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.

    SYNTHESIS OF OLIGOKETIDES
    10.
    发明公开
    SYNTHESIS OF OLIGOKETIDES 审中-公开
    合成寡核苷酸

    公开(公告)号：EP1144375A2

    公开(公告)日：2001-10-17

    申请号：EP00911673.2

    申请日：2000-01-27

    申请人： Kosan Biosciences

    发明人： ASHLEY, Gary ,  CHAN-KAI, Isaac, Chu-Wah ,  BURLINGAME, Mark, Alma

    IPC分类号： C07C327/30 ,  C12P17/08 ,  C07D239/38

    CPC分类号： C07C327/30

    摘要： Facile methods for preparing diketide and triketide thioesters are disclosed. The resulting thioesters may be used as intermediates in the synthesis of desired polyketides, and may contain functional groups which ultimately reside in side chains on the resulting polyketide and thus can be used further to manipulate the polyketide so as to form derivatives. The polyketides produced may also be tailored by glycosylation, hydroxylation and the like. New polyketides and their derivatives and tailored forms are thereby produced.

    摘要翻译： 公开了用于制备双酮和三酮硫酯的简便方法。 所得硫酯可用作合成所需聚酮化合物的中间体，并可含有最终位于所得聚酮化合物侧链上的官能团，因此可进一步用于操纵聚酮化合物以形成衍生物。 产生的聚酮化合物也可以通过糖基化，羟基化等来调整。 由此产生新的聚酮化合物及其衍生物和定制形式。