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    6-ALKENYL-, 6-ALKINYL- AND 6-EPOXY-EPOTHILONE DERIVATIVES, PROCESS FOR THEIR PRODUCTION, AND THEIR USE IN PHARMACEUTICAL PREPARATIONS
    6.
    发明申请
    6-ALKENYL-, 6-ALKINYL- AND 6-EPOXY-EPOTHILONE DERIVATIVES, PROCESS FOR THEIR PRODUCTION, AND THEIR USE IN PHARMACEUTICAL PREPARATIONS 审中-公开
    6-烷基 - ，6-烷基和6-环氧乙烯基酮衍生物，其生产方法及其在药物制备中的应用

    公开(公告)号：US20100168179A1

    公开(公告)日：2010-07-01

    申请号：US12721614

    申请日：2010-03-11

    申请人： Ulrich Klar ,  Wolfgang Schwede ,  Werner Skuballa ,  Bernd Buchmann ,  Jens Hoffmann ,  Rosemarie Lichtner

    发明人： Ulrich Klar ,  Wolfgang Schwede ,  Werner Skuballa ,  Bernd Buchmann ,  Jens Hoffmann ,  Rosemarie Lichtner

    IPC分类号： A61K31/4427 ,  A61K31/427 ,  A61K31/428 ,  A61K31/423 ,  C07D405/06 ,  C07D417/06 ,  C07D413/06 ,  A61P35/00

    CPC分类号： C07D493/04 ,  C07D405/04 ,  C07D405/06 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D417/14

    摘要： This invention describes the new 6-alkenyl- and 6-alkinyl-epothilone derivatives of general formula (I) in which R1a, R1b, R2a, R3a, R3b, R4, R5, R6, R7, A, Y, D, E, G, Y and Z have the meanings that are indicated in the description. The new compounds interact with tubulin by stabilizing microtubuli that are formed. They are able to influence the cell-splitting in a phase-specific manner and thus find use in treating diseases or conditions associated with the need for cell growth, division and/or proliferation. Thus the compounds are suitable for treating malignant tumors, for example, ovarian, stomach, colon, adeno-, breast, lung, head and neck carcinomas, malignant melanoma, acute lymphocytic and myelocytic leukemia. In addition, they are suitable for anti-angiogenesis therapy as well as for treatment of chronic inflammatory diseases (such as psoriasis, arthritis). Methods of use and preparation of the compounds are also described.

    摘要翻译： 本发明描述了通式（I）的新的6-烯基 - 和6-炔基 - 埃坡霉素衍生物，其中R1a，R1b，R2a，R3a，R3b，R4，R5，R6，R7，A，Y，D，E， G，Y和Z具有在说明书中指示的含义。 新化合物通过稳定形成的微管与微管蛋白相互作用。 它们能够以相位特异性方式影响细胞分裂，因此可用于治疗与细胞生长，分裂和/或增殖的需要相关的疾病或病症。 因此，该化合物适用于治疗恶性肿瘤，例如卵巢癌，胃癌，结肠癌，腺癌，乳腺癌，肺癌，头颈癌，恶性黑素瘤，急性淋巴细胞性白血病和骨髓性白血病。 此外，它们适用于抗血管生成治疗以及治疗慢性炎性疾病（如银屑病，关节炎）。 还描述了化合物的使用和制备方法。

    6-alkenyl-, 6-alkinyl- and 6-epoxy-epothilone derivatives, process for their production, and their use in pharmaceutical preparations
    8.
    发明授权
    6-alkenyl-, 6-alkinyl- and 6-epoxy-epothilone derivatives, process for their production, and their use in pharmaceutical preparations 失效
    6-烯基 - ，6-烷基 - 和6-环氧基 - 埃坡霉素衍生物，其制备方法及其在药物制剂中的用途

    公开(公告)号：US07645891B2

    公开(公告)日：2010-01-12

    申请号：US10965802

    申请日：2004-10-18

    申请人： Ulrich Klar ,  Wolfgang Schwede ,  Werner Skuballa ,  Bernd Buchmann ,  Jens Hoffmann ,  Rosemarie Lichtner

    发明人： Ulrich Klar ,  Wolfgang Schwede ,  Werner Skuballa ,  Bernd Buchmann ,  Jens Hoffmann ,  Rosemarie Lichtner

    IPC分类号： C07D319/06 ,  C07C49/20

    CPC分类号： C07D493/04 ,  C07D405/04 ,  C07D405/06 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D417/14

    摘要： This invention describes the new 6-alkenyl- and 6-alkinyl-epothilone derivatives of general formula (I) in which R1a, R1b, R2b, R3a, R3b, R4, R5, R6, R7, A, Y, D, E, G, Y and Z have the meanings that are indicated in the description. The new compounds interact with tubulin by stabilizing microtubuli that are formed. They are able to influence the cell-splitting in a phase-specific manner and thus find use in treating diseases or conditions associated with the need for cell growth, division and/or proliferation. Thus the compounds are suitable for treating malignant tumors, for example, ovarian, stomach, colon, adeno-, breast, lung, head and neck carcinomas, malignant melanoma, acute lymphocytic and myelocytic leukemia. In addition, they are suitable for anti-angiogenesis therapy as well as for treatment of chronic inflammatory diseases (such as psoriasis, arthritis). Methods of use and preparation of the compounds are also described.

    摘要翻译： 本发明描述了通式（I）的新的6-烯基 - 和6-炔基 - 埃坡霉素衍生物，其中R1a，R1b，R2a，R3a，R3b，R4，R5，R6，R7，A，Y，D，E， G，Y和Z具有在说明书中指示的含义。 新化合物通过稳定形成的微管与微管蛋白相互作用。 它们能够以相位特异性方式影响细胞分裂，因此可用于治疗与细胞生长，分裂和/或增殖的需要相关的疾病或病症。 因此，该化合物适用于治疗恶性肿瘤，例如卵巢癌，胃癌，结肠癌，腺癌，乳腺癌，肺癌，头颈癌，恶性黑素瘤，急性淋巴细胞性白血病和骨髓性白血病。 此外，它们适用于抗血管生成治疗以及治疗慢性炎性疾病（如银屑病，关节炎）。 还描述了化合物的使用和制备方法。

    6-Alkenyl -, 6-alkinyl- and 6-epoxy-epothilone derivatives, process for their production, and their use in pharmaceutical preparations
    10.
    发明申请
    6-Alkenyl -, 6-alkinyl- and 6-epoxy-epothilone derivatives, process for their production, and their use in pharmaceutical preparations 失效
    6-烯基 - ，6-炔基和6-环氧基 - 埃坡霉素衍生物，其制备方法及其在药物制剂中的用途

    公开(公告)号：US20060046997A1

    公开(公告)日：2006-03-02

    申请号：US11214988

    申请日：2005-08-31

    申请人： Ulrich Klar ,  Wolfgang Schwede ,  Werner Skuballa ,  Bernd Buchmann ,  Jens Hoffmann ,  Rosemarie Lichtner

    发明人： Ulrich Klar ,  Wolfgang Schwede ,  Werner Skuballa ,  Bernd Buchmann ,  Jens Hoffmann ,  Rosemarie Lichtner

    IPC分类号： A61K31/4709 ,  A61K31/427 ,  C07D417/02

    CPC分类号： C07D493/04 ,  C07D405/04 ,  C07D405/06 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D417/14

    摘要： This invention describes the new 6-alkenyl- and 6-alkinyl-epothilone derivatives of general formula (I) in which R1a, R1b, R2a, R3a, R3b, R4, R5, R6, R7, A, Y, D, E, G, Y and Z have the meanings that are indicated in the description. The new compounds interact with tubulin by stabilizing microtubuli that are formed. They are able to influence the cell-splitting in a phase-specific manner and thus find use in treating diseases or conditions associated with the need for cell growth, division and/or proliferation. Thus the compounds are suitable for treating malignant tumors, for example, ovarian, stomach, colon, adeno-, breast, lung, head and neck carcinomas, malignant melanoma, acute lymphocytic and myelocytic leukemia. In addition, they are suitable for anti-angiogenesis therapy as well as for treatment of chronic inflammatory diseases (such as psoriasis, arthritis). Methods of use and preparation of the compounds are also described.

    摘要翻译： 本发明描述了通式（I）的新的6-烯基 - 和6-炔基 - 埃坡霉素衍生物，其中R 1a，R 1b，R 2b， R 3，R 3b，R 4，R 4，R 5，R 6， 其中，R 7，A，Y，D，E，G，Y和Z具有说明书中所示的含义。 新化合物通过稳定形成的微管与微管蛋白相互作用。 它们能够以相位特异性方式影响细胞分裂，因此可用于治疗与细胞生长，分裂和/或增殖的需要相关的疾病或病症。 因此，该化合物适用于治疗恶性肿瘤，例如卵巢癌，胃癌，结肠癌，腺癌，乳腺癌，肺癌，头颈癌，恶性黑素瘤，急性淋巴细胞性白血病和骨髓性白血病。 此外，它们适用于抗血管生成治疗以及治疗慢性炎性疾病（如银屑病，关节炎）。 还描述了化合物的使用和制备方法。