发明名称 NEW EPOTHIOLONE DERIVATIVES, PROCESS FOR THEIR PRODUCTION, AND THEIR PHARMACEUTICAL USE
摘要 This invention relates to the new epothilone derivatives of general formula I, in which substituents Y, Z, R2a, R2b, R3, R4a, R4b, D-E, R5, R6, R7, R8 and X 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 are suitable for treating malignant tumors, for example, ovarian, stomach, colon, adeno-, breast, lung, head and neck carcinomas, malignant melanomas, acute lymphocytic and myelocytic leukemia. In addition, they are suitable for anti-angiogenesis therapy as well as for treatment of chronic inflammatory diseases (psoriasis, arthritis). To avoid uncontrolled proliferation of cells and for better compatibility of medical implants, they can be applied or introduced into polymer materials. The compounds according to the invention can be used alone or to achieve additive or synergistic actions in combination with other principles and classes of substances that can be used in tumor therapy.
申请公布号 US2009018342(A1) 申请公布日期 2009.01.15
申请号 US20080178039 申请日期 2008.07.23
申请人 KLAR ULRICH;SCHWEDE WOLFGANG;SKUBALLA WERNER;BUCHMANN BERND 发明人 KLAR ULRICH;SCHWEDE WOLFGANG;SKUBALLA WERNER;BUCHMANN BERND
分类号 C07D313/00;C07D417/06;A61K31/335;A61K31/427;A61K31/4427;A61K31/443;A61P35/00;A61P43/00;C07C43/04;C07C45/29;C07C45/56;C07C45/67;C07C49/185;C07C49/337;C07C49/355;C07C51/31;C07C59/185;C07D213/50;C07D213/55;C07D263/22;C07D277/22;C07D277/24;C07D307/33;C07D309/12;C07D319/06;C07D319/08;C07D319/14;C07D405/06;C07D405/12;C07D405/14;C07D407/04;C07D407/12;C07D417/12;C07D417/14;C07D493/04;C07F7/18 主分类号 C07D313/00
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