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    O-alkyl macrolide and azalide derivatives and regioselective process for their preparation
    1.
    发明授权
    O-alkyl macrolide and azalide derivatives and regioselective process for their preparation 失效
    O-烷基大环内酯和azalide衍生物及其制备方法

    公开(公告)号：US07435805B2

    公开(公告)日：2008-10-14

    申请号：US10851768

    申请日：2004-05-21

    申请人： Davor Kidemet ,  Gorjana Lazarevski ,  Marko Derek ,  Marija Leljak

    发明人： Davor Kidemet ,  Gorjana Lazarevski ,  Marko Derek ,  Marija Leljak

    IPC分类号： C07H17/08

    CPC分类号： C07H17/00 ,  C07H17/08

    摘要： The present disclosure relates to new 11-O-alkyl macrolides and azalides and pharmaceutically acceptable salts and solvates thereof, and to pharmaceutical compositions thereof. The disclosure also relates to a process for the preparation of 11-O-alkyl macrolides and azalides by regioselective 11-O-alkylation of macrolides and azalides having a vicinal diol system, using diazoalkanes in the presence of transition-metal halides or boric acid as catalysts. In another aspect, the disclosure relates to uses of the 11-O-alkyl macrolides and azalides as antibacterial agents or intermediates for the synthesis of other antibacterial agents.

    摘要翻译： 本公开内容涉及新的11-O-烷基大环内酯和氮杂ides啶及其药学上可接受的盐和溶剂合物，以及其药物组合物。 本公开还涉及通过在过渡金属卤化物或硼酸的存在下使用重氮烷烃在具有邻位二醇体系的大环内酯和氮杂环丙烷的区域选择性11-O-烷基化作用下制备11-O-烷基大环内酯和氮杂环丁烷的方法， 催化剂。 在另一方面，本公开涉及11-O-烷基大环内酯和氮杂环丁烷作为抗细菌剂或中间体用于合成其它抗菌剂的用途。

    O-alkyl macrolide and azalide derivatives and regioselective process for their preparation
    2.
    发明申请
    O-alkyl macrolide and azalide derivatives and regioselective process for their preparation 失效
    O-烷基大环内酯和azalide衍生物及其制备方法

    公开(公告)号：US20050164958A1

    公开(公告)日：2005-07-28

    申请号：US10851768

    申请日：2004-05-21

    申请人： Davor Kidemet ,  Gorjana Lazarevski ,  Marko Derek ,  Marija Leljak

    发明人： Davor Kidemet ,  Gorjana Lazarevski ,  Marko Derek ,  Marija Leljak

    IPC分类号： A61K31/7052 ,  C07H17/00 ,  C07H17/08

    CPC分类号： C07H17/00 ,  C07H17/08

    摘要： The present disclsoure relates to new 11-O-alkyl macrolides and azalides and pharmaceutically acceptable salts and solvates thereof, and to pharmaceutical compositions thereof. The disclosure also relates to a process for the preparation of 11-O-alkyl macrolides and azalides by regioselective 11-O-alkylation of macrolides and azalides having a vicinal diol system, using diazoalkanes in the presence of transition-metal halides or boric acid as catalysts. In another aspect, the disclosure relates to uses of the 11-O-alkyl macrolides and azalides as antibacterial agents or intermediates for the synthesis of other antibacterial agents.

    摘要翻译： 本发明涉及新的11-O-烷基大环内酯和氮杂环丁烷及其药学上可接受的盐和溶剂合物，以及其药物组合物。 本公开还涉及通过在过渡金属卤化物或硼酸的存在下使用重氮烷烃在具有邻位二醇体系的大环内酯和氮杂环丙烷的区域选择性11-O-烷基化作用下制备11-O-烷基大环内酯和氮杂环丁烷的方法， 催化剂。 在另一方面，本公开涉及11-O-烷基大环内酯和氮杂环丁烷作为抗细菌剂或中间体用于合成其它抗菌剂的用途。