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33 条记录 (耗时 0.037 秒)

    Avermectin difluoro derivatives
    5.
    发明授权
    Avermectin difluoro derivatives 失效
    阿维菌素二氟衍生物

    公开(公告)号：US5350742A

    公开(公告)日：1994-09-27

    申请号：US74763

    申请日：1993-06-10

    申请人： Peter T. Meinke ,  Helmut Mrozik ,  Michael H. Fisher

    发明人： Peter T. Meinke ,  Helmut Mrozik ,  Michael H. Fisher

    IPC分类号： C07H17/08 ,  A01N43/90 ,  A61K31/365 ,  A61K31/366 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P33/00 ,  A61P33/10 ,  C07D493/22 ,  C07H19/01

    CPC分类号： C07H19/01 ,  A01N43/90

    摘要： Avermectin derivatives are disclosed which incorporate two fluorine atoms at the 4' monosaccharide position, the 4" disaccharide position or the 23 position. Avermectin aglycone derivatives are also disclosed which incorporate two fluorine atoms at position 13 or 23. These difluoro avermectin analogs are derived from corresponding ketones and enones which in turn are prepared by chemical modification of naturally occurring avermectins. These compounds are used as antiparisitic, insecticidal and antihelmintic agents in humans and animals and compositions containing such compounds as the active ingredient thereof are also disclosed.

    摘要翻译： 公开了阿维菌素衍生物，其在4'单糖位置，4“二糖位置或23位置引入两个氟原子。 还公开了阿维菌素糖苷配基衍生物，其在13或23位上引入两个氟原子。这些二氟阿维菌素类似物衍生自相应的酮和烯酮，其又通过天然存在的阿凡曼菌素的化学修饰来制备。 这些化合物在人和动物中用作止痛药，杀虫剂和抗脑炎药，还公开了含有其活性成分的化合物的组合物。

    Avermectin difluoro derivatives
    6.
    发明授权
    Avermectin difluoro derivatives 失效
    阿维菌素二氟衍生物

    公开(公告)号：US5229416A

    公开(公告)日：1993-07-20

    申请号：US875486

    申请日：1992-04-29

    申请人： Peter T. Meinke ,  Helmut Mrozik ,  Michael H. Fisher

    发明人： Peter T. Meinke ,  Helmut Mrozik ,  Michael H. Fisher

    IPC分类号： C07H17/08 ,  A01N43/90 ,  A61K31/365 ,  A61K31/366 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P33/00 ,  A61P33/10 ,  C07D493/22 ,  C07H19/01

    CPC分类号： C07H19/01 ,  A01N43/90

    摘要： Avermectin derivatives are disclosed which incorporate two fluorine atoms at the 4' monosaccharide position, the 4" disaccharide position or the 23 position. Avermectin aglycone derivatives are also disclosed which incorporate two fluorine atoms at position 13 or 23. These difluoro avermectin analogs are derived from corresponding ketones and enones which in turn are prepared by chemical modification of naturally occurring avermectins. These compounds are used as antiparisitic, insecticidal and antihelmintic agents in humans and animals and compositions containing such compounds as the active ingredient thereof are also disclosed.

    摘要翻译： 公开了阿维菌素衍生物，其在4'单糖位置，4“二糖位置或23位置引入两个氟原子。 还公开了阿维菌素糖苷配基衍生物，其在13或23位上引入两个氟原子。这些二氟阿维菌素类似物衍生自相应的酮和烯酮，其又通过天然存在的阿凡曼菌素的化学修饰来制备。 这些化合物在人和动物中用作止痛药，杀虫剂和抗脑炎药，还公开了含有其活性成分的化合物的组合物。

    23-nor-23-oxa avermectin analogs are active anthelmintic agents
    10.
    发明授权
    23-nor-23-oxa avermectin analogs are active anthelmintic agents 失效
    23-nor-23-oxa阿维菌素类似物是活性的驱肠剂

    公开(公告)号：US5244879A

    公开(公告)日：1993-09-14

    申请号：US853452

    申请日：1992-03-18

    申请人： Peter T. Meinke ,  Helmut Mrozik

    发明人： Peter T. Meinke ,  Helmut Mrozik

    IPC分类号： C07H19/01

    CPC分类号： C07H19/01

    摘要： Avermectin analogs are prepared where the 23-position ring carbon atom is deleted and replaced by an oxygen atom. The compounds are prepared by opening the outer spiroketal ring to gain access to the 23-position atom, substituting the ring-opened compounds with a substituent containing the oxygen atom in the appropriate position and closing the ring to prepare the desired compounds. The compounds are potent anthelmintic agents and methods and compositions including such 23-nor-23-oxa compounds are also disclosed.

    摘要翻译： 制备阿维菌素类似物，其中23位环碳原子被缺失并被氧原子代替。 通过打开外螺旋酮环以获得进入23位原子，用含有氧原子的取代基取代开环化合物在适当位置并封闭环以制备所需化合物来制备化合物。 这些化合物是有效的驱肠剂，并且还公开了包括这种23-降-23-氧杂化合物的方法和组合物。