发明名称 6-Alkenyl-, 6-alkynyl- and 6-epoxyepothilone derivatives, process of their preparation and use in pharmaceutical preparations
摘要 <p>This invention describes the new 6-alkenyl- and 6-alkinyl- epothilone derivatives of general formula (I) in which R<1a>, R<1b>, R<2a>, R<3a>, R<3b>, R<4>, R<5>, R<6>, R<7>, 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.</p>
申请公布号 CZ20013885(A3) 申请公布日期 2002.04.17
申请号 CZ20010003885 申请日期 2000.05.01
申请人 SCHERING AKTIENGESELLSCHAFT 发明人 KLAR ULRICH;SCHWEDE WOLFGANG;SKUBALLA WERNER;BUCHMANN BERND;HOFFMANN JENS;LICHTNER ROSEMARIE
分类号 A61K31/335;A61K31/422;A61K31/429;A61K31/4427;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;(IPC1-7):C07D493/04;A61P29/00 主分类号 A61K31/335
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