摘要 |
The invention relates to new epothilone derivatives of the general formula (I), in which the substituents Y, Z, R<2a>, R<2b>, R<4a>, R<4b>, D-E, R<5>, R<6>, R<7>, R<8> and X have the meanings assigned to them in the description. The new compounds interact with tubulin by stabilizing formed microtubuli. They are capable of influencing cell division in a phase-specific manner and are suitable for the treatment of malignant tumours, such as ovarian, gastric, colon, breast, lung, head and neck carcinoma, adenocarcinoma, malignant melanoma, and acute lymphocytic and myelocytic leukaemia. They are also suited for anti-angiogenesis therapy and for the treatment of chronic inflammatory diseases (psoriasis, arthritis). To prevent uncontrolled cell growth on, and for better tolerability of, medical implants, the derivatives can be introduced into or applied to polymeric materials. The compounds provided for in the invention can be used alone or, to achieve additive or synergistic effects, in combination with other principles and substance categories used in tumour therapy. |
申请人 |
SCHERING AKTIENGESELLSCHAFT;KLAR, ULRICH;SCHWEDE, WOLFGANG;SKUBALLA, WERNER;BUCHMANN, BERND;SCHIRNER, MICHAEL |
发明人 |
KLAR, ULRICH;SCHWEDE, WOLFGANG;SKUBALLA, WERNER;BUCHMANN, BERND;SCHIRNER, MICHAEL |