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    Synthetic marcfortine derivatives useful as antiparasitic agents
    1.
    发明授权
    Synthetic marcfortine derivatives useful as antiparasitic agents 失效
    用作抗寄生虫剂的合成马可氟汀衍生物

    公开(公告)号：US4923867A

    公开(公告)日：1990-05-08

    申请号：US235418

    申请日：1988-08-24

    申请人： Timothy A. Blizzard ,  Helmut Mrozik

    发明人： Timothy A. Blizzard ,  Helmut Mrozik

    IPC分类号： A01N43/90 ,  C07D491/22

    CPC分类号： C07D491/22 ,  A01N43/90

    摘要： There are disclosed synthetic marcfortine derivatives of the natural products marcfortine A, marcfortine B, and marcfortine C. The synthetic derivatives are described in the following formula: ##STR1## wherein: n is 0 or 1R.sub.1 is hydrogen, loweralkyl, benzyl, lower alkanoyl, benzenesulfonyl in which the benzene ring is substituted with from 0 to 3 substituents selected from lower alkyl groups, lower alkoxy groups and halogen atoms, lower alkylamino-carbonyl, lower alkoxy-carbonyl;R.sub.24 is hydrogen, halogen or lower alkoxy (provided that R.sub.24 is other than hydrogen only if the broken line represents a single bond at the 24, 25-position),R.sub.25 is hydrogen or halogen (provided that R.sub.25 is other than hydrogen only if the broken line represents a single bond at the 24, 25-position);R.sub.29 is hydrogen, lower alkyl, alkoxyalkyl, haloalkyl, lower alkenyl, lower alkynyl, benzyl, lower alkanoyl, substituted benzenesulfonyl, lower alkylamino-carbonyl, not hydrogen or methyl if R.sub.1 is hydrogen; and the broken line represents a single or double bond between carbons 24 and 25.The compounds are active antiparasitic agents useful in particular against insect and nematode pests, and compositions for that use are disclosed.

    摘要翻译： 公开了天然产物马可氟汀A，马可氟汀B和马可氟汀C的合成马可氟汀衍生物。合成衍生物描述于下式中：其中：n为0或1，R1为氢，低级烷基，苄基，低级烷酰基 苯磺酰基，其中苯环被0-3个选自低级烷基，低级烷氧基和卤素原子的取代基取代，低级烷基氨基 - 羰基，低级烷氧羰基; R24是氢，卤素或低级烷氧基（只要虚线表示24,25位的单键，R24不是氢），R25是氢或卤素（只要R25不是氢，只要是 虚线代表24,25位的单键）; 如果R1是氢，R29是氢，低级烷基，烷氧基烷基，卤代烷基，低级烯基，低级炔基，苄基，低级烷酰基，取代的苯磺酰基，低级烷基氨基 - 羰基，不是氢或甲基; 并且虚线表示碳24和25之间的单键或双键。化合物是有效的抗寄生虫剂，特别适用于昆虫和线虫害虫，并且公开了该用途的组合物。

    24-and 25-substituted avermectin and milbemycin derivatives
    4.
    发明授权
    24-and 25-substituted avermectin and milbemycin derivatives 失效
    24-和25-取代的阿维菌素和米尔倍霉素衍生物

    公开(公告)号：US5830875A

    公开(公告)日：1998-11-03

    申请号：US429919

    申请日：1989-10-30

    申请人： Helmut Mrozik ,  Thomas L. Shih

    发明人： Helmut Mrozik ,  Thomas L. Shih

    IPC分类号： C12P17/18 ,  A01N43/90 ,  A61K31/365 ,  A61K31/70 ,  A61P33/10 ,  C07D493/22 ,  C07F7/18 ,  C07H19/01 ,  C12R1/465 ,  A61K31/335 ,  C07H17/08 ,  C07D300/00

    CPC分类号： C07H19/01

    摘要： Novel avermectin and milbemycin derivatives are disclosed, where the C-24 and C-25 carbon atoms are substituted by hydrogen, alkyl, alkenyl, substituted alkyl or substituted alkenyl groups. These compounds can be further substituted at the 4"-, 5-, 13-, and 23-positions. The new C-24 and C-25 substituted avermect prepared by cleavage of known and suitably protected avermectin and milbemycin compounds. The new compounds are potent anti-parasitic agents, in particular, the compounds are anthelmintic, insecticidal and acaricidal agents.

    摘要翻译： 公开了新的除虫菌素和米尔倍霉素衍生物，其中C-24和C-25碳原子被氢，烷基，烯基，取代的烷基或取代的烯基取代。 这些化合物可以在4“，5”，“13”和“23”位进一步取代。 通过裂解已知和适当保护的阿维菌素和米尔倍霉素化合物制备的新C-24和C-25取代的除虫剂。 新化合物是有效的抗寄生虫剂，特别是化合物是驱肠虫，杀虫剂和杀螨剂。

    Avermectin derivatives
    6.
    发明授权
    Avermectin derivatives 失效
    阿维菌素衍生物

    公开(公告)号：US4895837A

    公开(公告)日：1990-01-23

    申请号：US296172

    申请日：1989-01-13

    申请人： Helmut Mrozik ,  Frank S. Waksmunski

    发明人： Helmut Mrozik ,  Frank S. Waksmunski

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

    CPC分类号： C07H19/01 ,  A01N43/90

    摘要： There are disclosed novel avermectin .DELTA. 23,24-derivatives (also referred to as 23,24-dehydro compounds). The compounds are prepared by selective dehydration of avermectin A2 or B2 compounds. The avermectin compounds have utility as anti-parasitic agents and compositions for that use are also disclosed. The compounds are also highly potent insecticides against agricultural pests. The .DELTA. 23,24-avermectin compounds have increased activity relative to the A2 or B2 compounds.

    摘要翻译： 公开了新的除虫菌素DELTA 23,24衍生物（也称为23,24-脱氢化合物）。 通过阿维菌素A2或B2化合物的选择性脱水制备化合物。 除虫菌素化合物可用作抗寄生虫剂，并且还公开了用于该用途的组合物。 这些化合物对农业有害生物也是非常有效的杀虫剂。 DELTA 23,24-阿维菌素化合物相对于A2或B2化合物具有增加的活性。

    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。