利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

33 条记录 (耗时 0.014 秒)

    24- and 25-substituted avermectin and milbemycin derivatives
    1.
    发明公开
    24- and 25-substituted avermectin and milbemycin derivatives 失效
    24-和25-取代的阿维菌素和米氏霉素衍生物

    公开(公告)号：EP0428286A3

    公开(公告)日：1991-10-23

    申请号：EP90311809.9

    申请日：1990-10-29

    申请人： MERCK & CO. INC.

    发明人： Mrozik, Helmut ,  Shih, Thomas L.

    IPC分类号： C07H17/08 ,  C07D493/22 ,  A61K31/70 ,  A61K31/365 ,  A01N43/90

    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 avermectin and milbemycin derivatives are 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.

    Synthetic derivative of paraherquamide
    2.
    发明公开
    Synthetic derivative of paraherquamide 失效
    合成衍生物冯Paraherquamid。

    公开(公告)号：EP0354615A1

    公开(公告)日：1990-02-14

    申请号：EP89202026.4

    申请日：1989-08-03

    申请人： Merck & Co., Inc.

    发明人： Blizzard, Timothy A. ,  Marino, Gaye ,  Sinclair, Peter J. ,  Mrozik, Helmut

    IPC分类号： C07D491/22 ,  C07D471/22 ,  A61K31/435 ,  A01N43/90

    CPC分类号： C07D491/22 ,  A01N43/90 ,  C07D498/22 ,  C07F7/1856 ,  C07F9/6561

    摘要： There are disclosed synthetic derivatives of the natural product paraherquamide. The synthetic derivatives are prepared by reactions at the parahe­quamide A, B, E, F and G rings, that is at carbon atoms 14 to 16, the lactam ring and carbon atoms 24 to 26 as well as carbon atoms 5 and 12. The compounds are active antiparasitic agents and compositions for that use are also disclosed.

    摘要翻译： 公开了天然产物对苯二甲酰胺的合成衍生物。 合成的衍生物通过在二价酰胺A，B，E，F和G环，即14至16碳原子，内酰胺环和碳原子24至26以及碳原子5和12的反应制备。化合物 还是公开了活性抗寄生虫剂和用于该用途的组合物。

    Fluoroavermectin and fluoromilbemycin derivatives with antiparasitic and pesticidal properties
    3.
    发明公开
    Fluoroavermectin and fluoromilbemycin derivatives with antiparasitic and pesticidal properties 失效
    氟维他米嗪和氟莫米菌素衍生的抗真菌药物和杀虫剂Wirkung。

    公开(公告)号：EP0340849A2

    公开(公告)日：1989-11-08

    申请号：EP89201079.4

    申请日：1989-04-25

    申请人： MERCK & CO. INC.

    发明人： Eskola, Philip ,  Fisher, Michael H. ,  Mrozik, Helmut

    IPC分类号： C07D493/22 ,  C07H19/01 ,  A61K31/365 ,  A61K31/70 ,  A01N43/90

    CPC分类号： C07H19/01 ,  A01N43/90

    摘要： Novel avermectin and milbemycin compounds, wherein at least one of the 4a, 5 or 4˝ positions are substituted with a fluoro groups, are prepared by replacement of hydroxy or other suitable leaving group of avermectin and milbemycin compounds with fluorine. The fluoroavermectin and fluoromilbemycin compounds have utility as anti-parasitic agents and as highly potent insecticides against agricultural pests.

    摘要翻译： 通过用氟取代除虫菌素和米尔倍霉素化合物的羟基或其它合适的离去基团，制备其中至少一个4a，5或4秒位置被氟基团取代的新的除虫菌素和米尔倍霉素化合物。 氟维菌素和氟米尔贝霉素化合物具有抗寄生虫作用和作为高效杀虫剂的作用。

    13-beta-O-methoxymethyl-22,23-dihydro avermectin B1A/B1B aglycone
    6.
    发明公开
    13-beta-O-methoxymethyl-22,23-dihydro avermectin B1A/B1B aglycone 失效
    13-β-O-甲氧基甲基-22,23-二氢阿维菌素B1A / B1B Aglykone。

    公开(公告)号：EP0530901A1

    公开(公告)日：1993-03-10

    申请号：EP92202603.4

    申请日：1992-08-27

    申请人： MERCK & CO. INC.

    发明人： Linn, Bruce O. ,  Mrozik, Helmut

    IPC分类号： C07D493/22 ,  A01N43/90 ,  A61K31/365

    CPC分类号： C07H19/01 ,  A01N43/90

    摘要： The novel compound 13β-O-methoxymethyl-22,23-dihydro avermectin B1a/B1b aglycone is useful as an anthelmintic and antiparasitic agent and has been discovered to be unexpectedly superior to the corresponding 13α-compound. The compound is also useful as a pesticide and insecticide against agricultural pests. Compositions containing said compound and methods of administering said compositions are also disclosed.

    摘要翻译： 新化合物13β-O-甲氧基甲基-22,23-二氢阿凡曼菌素B1a / B1b糖苷配基用作驱虫剂和抗寄生虫剂，已被发现意外地优于相应的13α-化合物。 该化合物还可用作农药和农药杀虫剂。 还公开了含有所述化合物的组合物和施用所述组合物的方法。

    4a-Substituted avermectin derivatives
    7.
    发明公开
    4a-Substituted avermectin derivatives 失效
    4-a-Substantierte Avermectinderivate。

    公开(公告)号：EP0519731A1

    公开(公告)日：1992-12-23

    申请号：EP92305633.7

    申请日：1992-06-19

    申请人： MERCK & CO. INC.

    发明人： Chu, Lin ,  Jones, Todd K. ,  Mrozik, Helmut

    IPC分类号： C07H17/08 ,  C07D493/22 ,  A61K31/70 ,  A61K31/365 ,  A01N43/90

    CPC分类号： C07H19/01

    摘要： Avermectin compounds are substituted at the 4a-position: the 4a-methyl group is first derivatized with a hydroxy group which is then substituted with a variety of alkyl, alkoxy alkyl, or polyalkoxy alkyl groups and derivatives thereof. The compounds are potent antiparasitic and anthelmintic agents and compositions for such uses are also disclosed.

    摘要翻译： 阿维菌素化合物在4a位被取代：4a-甲基首先用羟基衍生化，然后羟基被多种烷基，烷氧基烷基或聚烷氧基烷基及其衍生物取代。 这些化合物是有效的抗寄生虫和驱虫剂，并且还公开了用于这些用途的组合物。