发明公开
EP0508699A1 9-Deoxo-8a-aza-8a-homoerythromycin a derivatives modified at the 4"- and 8a-positions
失效
4“ - 和8A-Stellungen modifizierte 9-Deoxo-8a-Aza-8a-高红霉素-A衍生物。
- 专利标题： 9-Deoxo-8a-aza-8a-homoerythromycin a derivatives modified at the 4"- and 8a-positions
- 专利标题（中）： 4“ - 和8A-Stellungen modifizierte 9-Deoxo-8a-Aza-8a-高红霉素-A衍生物。
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申请号： EP92303003.5申请日： 1992-04-03
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公开(公告)号： EP0508699A1公开(公告)日： 1992-10-14
- 发明人: Heck, James V. , Leanza, William J. , Ratcliffe, Ronald W. , Salzmann, Thomas N. , Wilkening, Robert R. , Szymonifka, Michael J. , Shankaran, Kothandaraman
- 申请人： MERCK & CO. INC.
- 申请人地址： 126, East Lincoln Avenue P.O. Box 2000 Rahway New Jersey 07065-0900 US
- 专利权人： MERCK & CO. INC.
- 当前专利权人： MERCK & CO. INC.
- 当前专利权人地址： 126, East Lincoln Avenue P.O. Box 2000 Rahway New Jersey 07065-0900 US
- 代理机构： Thompson, John Dr.
- 优先权： US680217 19910404; US811161 19911219; US855242 19920326
- 主分类号： C07H17/08
- IPC分类号： C07H17/08 ; A61K31/70
摘要：
Compounds of the formula:
where R is hydrogen, hydroxyl, alkyl or acyl, R′ and R˝ together are oxo, hydroxyimino or alkoxyimino, and R′ and R˝ independently are hydrogen, hydroxyl, acyloxy, or amino substituted by any of hydrogen, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, alkoxycarbonyl, aralkoxycarbonyl, alkylsulfonyl or arylsulfonyl, and n is 0 or 1, and the pharmaceutically acceptable salts thereof. The compounds are macrolide antibiotics and are also useful as intermediates to the synthesis of other macrolide antibiotics. Pharmaceutical compositions and methods of their use are also provided for.
where R is hydrogen, hydroxyl, alkyl or acyl, R′ and R˝ together are oxo, hydroxyimino or alkoxyimino, and R′ and R˝ independently are hydrogen, hydroxyl, acyloxy, or amino substituted by any of hydrogen, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, alkoxycarbonyl, aralkoxycarbonyl, alkylsulfonyl or arylsulfonyl, and n is 0 or 1, and the pharmaceutically acceptable salts thereof. The compounds are macrolide antibiotics and are also useful as intermediates to the synthesis of other macrolide antibiotics. Pharmaceutical compositions and methods of their use are also provided for.
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