发明授权
- 专利标题: STEROID DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE AS ANTIBIOTICS OR DISINFECTANTS
- 专利标题(中): 甾类衍生物,药物组合物含幽及其作为抗生素或消毒剂
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申请号: EP94911470.6申请日: 1994-03-10
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公开(公告)号: EP0688333B1公开(公告)日: 1998-08-19
- 发明人: FRYE, Leah, L. , ZASLOFF, Michael, A. , KINNEY, William, A. , MORIARTY, Robert, M.
- 申请人: MAGAININ PHARMACEUTICALS INC.
- 申请人地址: 5110 Campus Drive Plymouth Meeting PA 19462 US
- 专利权人: MAGAININ PHARMACEUTICALS INC.
- 当前专利权人: MAGAININ PHARMACEUTICALS INC.
- 当前专利权人地址: 5110 Campus Drive Plymouth Meeting PA 19462 US
- 代理机构: Hansen, Bernd, Dr. Dipl.-Chem.
- 优先权: US29018 19930310
- 国际公布: WO9420520 19940915
- 主分类号: C07J41/00
- IPC分类号: C07J41/00 ; C07J51/00 ; C07J43/00
摘要:
Compounds having a broad range of antimicrobial activity generally have a structure including a steroid nucleus with a cationic, preferably polyamine, side chain (X) and an anionic side chain (Y). The invention is also directed to compounds of formula (III) preferably where the steroid ring nucleus is saturated; the steroid ring substituent Z5 is alpha -H; one Z7 is beta -H and the other is alpha -H or alpha -OH; both substituents Z12 are hydrogen; X' is a polyamine side chain of the formula -NH-(CH2)p-NH-(CH2)q-N(R )(R ) where p and q are each independently 3 or 4, and R and R are each independently hydrogen or methyl; R' is methyl; and Y' is (C1-C10)-alkyl substituted with a group such as -CO2H or -SO3H.
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