Invention Grant
US07645891B2 6-alkenyl-, 6-alkinyl- and 6-epoxy-epothilone derivatives, process for their production, and their use in pharmaceutical preparations
失效
6-烯基 - ,6-烷基 - 和6-环氧基 - 埃坡霉素衍生物,其制备方法及其在药物制剂中的用途
- Patent Title: 6-alkenyl-, 6-alkinyl- and 6-epoxy-epothilone derivatives, process for their production, and their use in pharmaceutical preparations
- Patent Title (中): 6-烯基 - ,6-烷基 - 和6-环氧基 - 埃坡霉素衍生物,其制备方法及其在药物制剂中的用途
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Application No.: US10965802Application Date: 2004-10-18
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Publication No.: US07645891B2Publication Date: 2010-01-12
- Inventor: Ulrich Klar , Wolfgang Schwede , Werner Skuballa , Bernd Buchmann , Jens Hoffmann , Rosemarie Lichtner
- Applicant: Ulrich Klar , Wolfgang Schwede , Werner Skuballa , Bernd Buchmann , Jens Hoffmann , Rosemarie Lichtner
- Applicant Address: DE Berlin
- Assignee: Bayer Schering Pharma Aktiengesellschaft
- Current Assignee: Bayer Schering Pharma Aktiengesellschaft
- Current Assignee Address: DE Berlin
- Agency: Millen, White, Zelano & Branigan, P.C.
- Main IPC: C07D319/06
- IPC: C07D319/06 ; C07C49/20

Abstract:
This invention describes the new 6-alkenyl- and 6-alkinyl-epothilone derivatives of general formula (I) in which R1a, R1b, R2b, 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.
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