发明名称 6-alkenyl-, 6-alkinyl- and 6-epoxy-epothilone derivatives, process for their production, and their use in pharmaceutical preparations
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.
申请公布号 AU4310300(A) 申请公布日期 2000.11.17
申请号 AU20000043103 申请日期 2000.05.01
申请人 SCHERING AKTIENGESELLSCHAFT 发明人 ULRICH KLAR;WOLFGANG SCHWEDE;WERNER SKUBALLA;BERND BUCHMANN;JENS HOFFMANN;ROSEMARIE LICHTNER
分类号 A61K31/335;A61K31/422;A61K31/429;A61K31/4427;A61K51/04;A61P35/00;A61P35/02;A61P43/00;C07D405/04;C07D405/06;C07D405/14;C07D413/04;C07D413/06;C07D413/14;C07D417/04;C07D417/06;C07D417/14;C07D493/04;C07D493/08 主分类号 A61K31/335
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