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 i n a phase-specific manner and thus find use in treating diseases or conditions associated with the need for cell growth, division and/or proliferation. Thu s 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.
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申请人 |
SCHERING AKTIENGESELLSCHAFT |
发明人 |
LICHTNER, ROSEMARIE;HOFFMANN, JENS;BUCHMANN, BERND;SKUBALLA, WERNER;SCHWEDE, WOLFGANG;KLAR, ULRICH |