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17 条记录 (耗时 0.047 秒)

    Epothilone derivatives and their synthesis and use
    1.
    发明授权
    Epothilone derivatives and their synthesis and use 失效
    埃坡霉素衍生物及其合成和用途

    公开(公告)号：US06531497B1

    公开(公告)日：2003-03-11

    申请号：US09720070

    申请日：2001-04-19

    申请人： Kyriacos Costa Nicolaou ,  Nigel Paul King ,  Maruice Raymond Verschoyle Finlay ,  Yun He ,  Frank Roschangar ,  Dionisios Vourloumis ,  Hans Vallberg ,  Antony Bigot

    发明人： Kyriacos Costa Nicolaou ,  Nigel Paul King ,  Maruice Raymond Verschoyle Finlay ,  Yun He ,  Frank Roschangar ,  Dionisios Vourloumis ,  Hans Vallberg ,  Antony Bigot

    IPC分类号： A61K31425

    CPC分类号： C07D313/00 ,  C07D417/06 ,  C07D493/04 ,  Y02P20/55

    摘要： The invention relates to epothilone analog represented by formula (I) wherein (i) R2 is absent or oxygen; “a” can be either a single or double bond; “b” can be either absent or a single bond; and “c” can be either absent or a single bond, with the proviso that if R2 is oxygen then “b” and “c” are both a single bond and “a” is a single bond; if R2 is absent then “b” and “c” are absent and “a” is a double bond; and if “a” is a double bond, then R2, “b” and “c” are absent; R3 is a radical selected from the group consisting of hydrogen; lower alkyl; —CH═CH2; —C≡CH; —CH2F; —CH2Cl; —CH2—OH; —CH2—O—(C1-C6-alkyl); and —CH2—S—(C1-C6-alkyl); R4 and R5 are independently selected from hydrogen, methyl or a protecting group; and R1 is as defined in the specification, or a salt of a compound of formula (I) where a salt-forming group is present. A further aspect of the invention is related to the synthesis of epothilone E. These compounds have inter alia microtubuli depolymerization inhibiting activity and are e.g. useful against proliferative diseases

    摘要翻译： 本发明涉及由式（I）表示的埃坡霉素类似物，其中（i）R2不存在或氧; “a”可以是单键或双键; “b”可以是缺席或单一债券; 和“c”可以不存在或单键，条件是如果R2是氧，则“b”和“c”都是单键，“a”是单键; 如果R2不存在，则“b”和“c”不存在，“a”是双键; 如果“a”是双键，那么R2，“b”和“c”不存在; R3是选自氢的基团; 低级烷基 -CH = CH 2; -C = CH -CH2F; -CH2Cl; -CH 2 -OH; -CH 2 -O-（C 1 -C 6 - 烷基）; 和-CH 2 -S-（C 1 -C 6 - 烷基）; R 4和R 5独立地选自氢，甲基或保护基; 和R1如说明书中所定义，或其中存在成盐基团的式（I）化合物的盐。 本发明的另一方面涉及埃坡霉素E的合成。这些化合物尤其具有微管解聚抑制活性，例如。 对增殖性疾病有用

    Epothilone derivatives and their synthesis and use
    2.
    发明授权
    Epothilone derivatives and their synthesis and use 失效
    埃坡霉素衍生物及其合成和用途

    公开(公告)号：US07579366B2

    公开(公告)日：2009-08-25

    申请号：US10386999

    申请日：2003-03-11

    申请人： Kyriacos C. Nicolaou ,  Nigel Paul King ,  Maurice Raymond Verschoyle Finlay ,  Yun He ,  Frank Roschangar ,  Dionisios Vourloumis ,  Hans Vallberg ,  Antony Bigot

    发明人： Kyriacos C. Nicolaou ,  Nigel Paul King ,  Maurice Raymond Verschoyle Finlay ,  Yun He ,  Frank Roschangar ,  Dionisios Vourloumis ,  Hans Vallberg ,  Antony Bigot

    IPC分类号： A61K31/44 ,  C07D277/04

    CPC分类号： C07D313/00 ,  C07D417/06 ,  C07D493/04 ,  Y02P20/55

    摘要： The invention relates to epothilone analog represented by the formula I wherein (i) R2 is absent or oxygen; “a” can be either a single or double bond; “b” can be either absent or a single bond; and “c” can be either absent or a single bond, with the proviso that if R2 is oxygen then “b” and “c” are both a single bond and “a” is a single bond; if R2 is absent then “b” and “c” are absent and “a” is a double bond; and if “a” is a double bond, then R2, “b” and “c” are absent; R3 is a radical selected from the group consisting of hydrogen; lower alkyl; —CH═CH2; —C≡CH; —CH2F; —CH2Cl; —CH2—OH; —CH2—O—(C1-C6-alkyl); and —CH2—S—(C1-C6-alkyl); R4 and R5 are independently selected from hydrogen, methyl or a protecting group; and R1 is as defined in the specification, or a salt of a compound of the formula I where a salt-forming group is present. A further aspect of the invention is related to the synthesis of epothilone E. These compounds have inter alia microtubuli depolymerisation inhibiting activity and are e.g. useful against proliferative diseases.

    摘要翻译： 本发明涉及由式I表示的埃坡霉素类似物，其中（i）R2不存在或氧; “a”可以是单键或双键; “b”可以是缺席或单一债券; 和“c”可以不存在或单键，条件是如果R2是氧，则“b”和“c”都是单键，“a”是单键; 如果R2不存在，则“b”和“c”不存在，“a”是双键; 如果“a”是双键，那么R2，“b”和“c”不存在; R3是选自氢的基团; 低级烷基 -CH-CH 2; -C≡CH; -CH2F; -CH2Cl; -CH 2 -OH; -CH 2 -O-（C 1 -C 6 - 烷基）; 和-CH 2 -S-（C 1 -C 6 - 烷基）; R 4和R 5独立地选自氢，甲基或保护基; R1如本说明书中所定义，或其中存在成盐基团的式I化合物的盐。 本发明的另一方面涉及埃坡霉素E的合成。这些化合物尤其具有微管解聚抑制活性， 对增殖性疾病有用。

    Process for preparing camptothecin
    10.
    发明授权
    Process for preparing camptothecin 有权
    制备喜树碱的方法

    公开(公告)号：US06218540B1

    公开(公告)日：2001-04-17

    申请号：US09230683

    申请日：1999-05-04

    申请人： Marco Ciufolini ,  Frank Roschangar

    发明人： Marco Ciufolini ,  Frank Roschangar

    IPC分类号： C07D49122

    CPC分类号： C07D491/22 ,  C12N15/52 ,  C12P13/08

    摘要： A process for preparing the anti-cancer drug camptothecin (CPT) and certain derivatives thereof. The process includes the reacting of three base reagents and a five-step process for synthesizing optically pure CPT in high overall yield from inexpensive starting materials.

    摘要翻译： 制备抗癌药物喜树碱（CPT）及其某些衍生物的方法。 该方法包括三种碱试剂的反应和用于从廉价起始原料以高总产率合成光学纯CPT的五步法。