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15 条记录 (耗时 0.025 秒)

    2'-protected 3'-dimethylamine, 9-etheroxime erythromycin A derivatives
    1.
    发明授权
    2'-protected 3'-dimethylamine, 9-etheroxime erythromycin A derivatives 失效
    2'-保护的3'-二甲胺，9-乙酰肟红霉素A衍生物

    公开(公告)号：US5719272A

    公开(公告)日：1998-02-17

    申请号：US627795

    申请日：1996-04-02

    申请人： Chengxi Yang ,  Hemantkumar H. Patel ,  Yi-Yin Ku ,  Jih-Hua Liu

    发明人： Chengxi Yang ,  Hemantkumar H. Patel ,  Yi-Yin Ku ,  Jih-Hua Liu

    IPC分类号： C07H17/08 ,  C07H1/00

    CPC分类号： C07H17/08 ,  Y02P20/55

    摘要： A process of preparing a 6-O-methyl erythromycin A derivative using a 2'-protected, 9-etheroxime erythromycin A intermediate is provided. A preferred protecting group for the 2'-position is acetyl. 2'-protected, 9-etheroxime erythromycin A derivatives are also provided. Also disclosed is a method for inhibiting quaternary salt formation at the 3' amine without the need for 3'N-protecting groups.

    摘要翻译： 提供了使用2'-保护的9-乙烯基肟红霉素A中间体制备6-O-甲基红霉素A衍生物的方法。 2位的优选保护基是乙酰基。 还提供了2'-保护的9-乙酰肟红霉素A衍生物。 还公开了抑制在3'胺上形成季盐的方法，而不需要3'N保护基团。

    Process for preparing 6-O-alkyl-9-oxime erythromycin B
    2.
    发明授权
    Process for preparing 6-O-alkyl-9-oxime erythromycin B 失效
    制备6-O-烷基-9-肟红霉素B的方法

    公开(公告)号：US5932710A

    公开(公告)日：1999-08-03

    申请号：US980918

    申请日：1997-12-01

    申请人： Jih-Hua Liu ,  Stephen H. Montgomery

    发明人： Jih-Hua Liu ,  Stephen H. Montgomery

    IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/08 ,  C07H5/04 ,  A61K31/71

    CPC分类号： C07H17/08

    摘要： A process of preparing a 6-O-alkyl derivative of 9-oxime erythromycin B is provided. Intermediates used in the preparation of a 6-O-alkyl 9-oxime erythromycin B are also provided. Pharmaceutical compositions containing a 6-O-alkyl derivative of 9-oxime erythromycin B and the use of those compositions to treat bacterial infections are also provided.

    摘要翻译： 提供了制备9-肟红霉素B的6-O-烷基衍生物的方法。 还提供了用于制备6-O-烷基9-肟红霉素B的中间体。 还提供了含有9-肟红霉素B的6-O-烷基衍生物的药物组合物以及这些组合物用于治疗细菌感染的用途。

    6-O-aklyl erythromycin B oxime
    5.
    发明授权
    6-O-aklyl erythromycin B oxime 有权
    6-O-甲酰红霉素B肟

    公开(公告)号：US06194387B1

    公开(公告)日：2001-02-27

    申请号：US09301773

    申请日：1999-04-29

    申请人： Jih-Hua Liu ,  Stephen H. Montgomery

    发明人： Jih-Hua Liu ,  Stephen H. Montgomery

    IPC分类号： A61K3170

    CPC分类号： C07H17/08

    摘要： A process of preparing a 6-O-alkyl derivative of 9-oxime erythromycin B is provided. Intermediates used in the preparation of a 6-O-alkyl 9-oxime erythromycin B are also provided. Pharmaceutical compositions containing a 6-O-alkyl derivative of 9-oxime erythromycin B and the use of those compositions to treat bacterial infections are also provided.

    摘要翻译： 提供了制备9-肟红霉素B的6-O-烷基衍生物的方法。 还提供了用于制备6-O-烷基9-肟红霉素B的中间体。 还提供了含有9-肟红霉素B的6-O-烷基衍生物的药物组合物以及这些组合物用于治疗细菌感染的用途。

    Process for 6-O-alkylation of erythromycin derivatives
    8.
    再颁专利
    Process for 6-O-alkylation of erythromycin derivatives 有权
    红霉素衍生物6-O-烷基化方法

    公开(公告)号：USRE39383E1

    公开(公告)日：2006-11-07

    申请号：US10806089

    申请日：2004-03-22

    申请人： Jih-Hua Liu ,  George A. Foster, Jr. ,  Stephen H. Montgomery

    发明人： Jih-Hua Liu ,  George A. Foster, Jr. ,  Stephen H. Montgomery

    IPC分类号： C07H1/00

    CPC分类号： C07H17/08 ,  Y02P20/55

    摘要： A procedure for preparing 6-O-alkyl erythromycin compounds having the formula: wherein R1 is a loweralkyl group, R2 and R3 an independently hydrogen or a hydroxy-protecting group, except that R2 and R3 may not both be hydrogen simultaneously; Y is oxygen or a specifically substituted oxime; and Z is hydrogen, hydroxy or protected-hydroxy; by reaction of the compound wherein R1 is hydrogen with an alkylating reagent, is the presence of a strong alkali metal base and also in the presence of a weak organic amino base, in a suitable stirred or agitated polar aprotic solvent, or a mixture of such polar aprotic solvents maintained at a reaction temperature and for a period of time sufficient to effect alkyation.

    摘要翻译： 制备具有下式的6-O-烷基红霉素化合物的方法：其中R 1是低级烷基，R 2和R 3 独立地是氢或羟基保护基，不同之处在于R 2和R 3不能同时是氢; Y是氧或特定取代的肟; Z是氢，羟基或被保护的羟基; 通过其中R 1是氢的化合物与烷基化试剂的反应，是在合适的搅拌或搅拌的极性中存在强碱金属碱，并且在弱有机氨基的存在下 非质子溶剂或这些极性非质子溶剂的混合物保持在反应温度下并持续足以实现烷基化的时间。

    Process for 6-O-alkylation of erythromycin derivatives
    9.
    发明授权
    Process for 6-O-alkylation of erythromycin derivatives 失效
    红霉素衍生物6-O-烷基化方法

    公开(公告)号：US5872229A

    公开(公告)日：1999-02-16

    申请号：US560752

    申请日：1995-11-21

    申请人： Jih-Hua Liu ,  George A. Foster, Jr. ,  Stephen H. Montgomery

    发明人： Jih-Hua Liu ,  George A. Foster, Jr. ,  Stephen H. Montgomery

    IPC分类号： C07H17/08 ,  C07H1/00

    CPC分类号： C07H17/08 ,  Y02P20/55

    摘要： A procedure for preparing 6-O-alkyl erythromycin compounds having the formula: ##STR1## wherein R.sup.1 is a loweralkyl group, R.sup.2 and R.sup.3 are independently hydrogen or a hydroxy-protecting group, except that R.sup.2 and R.sup.3 may not both be hydrogen simultaneously; Y is oxygen or a specifically substituted oxime; and Z is hydrogen, hydroxy or protected-hydroxy; by reaction of the compound wherein R.sup.1 is hydrogen with an alkylating reagent, in the presence of a strong alkali metal base and also in the presence of a weak organic amine base, in a suitable stirred or agitated polar aprotic solvent, or a mixture of such polar aprotic solvents maintained at a reaction temperature and for a period of time sufficient to effect alkyation.

    摘要翻译： 制备具有下式的6-O-烷基红霉素化合物的方法：其中R 1是低级烷基，R 2和R 3独立地是氢或羟基保护基，不同之处在于R 2和R 3可不同时同时为氢; Y是氧或特定取代的肟; Z是氢，羟基或被保护的羟基; 通过其中R 1为氢的化合物与烷基化试剂在强碱金属碱存在下还在弱有机胺碱的存在下，在合适的搅拌或搅拌的极性非质子溶剂或其混合物中反应 极性非质子溶剂保持在反应温度和足以进行烷基化的一段时间。