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    Method for producing substituted-2-nitroguanidine derivatives
    72.
    发明授权
    Method for producing substituted-2-nitroguanidine derivatives 失效
    取代-2-硝基胍衍生物的制备方法

    公开(公告)号：US06462043B1

    公开(公告)日：2002-10-08

    申请号：US09485873

    申请日：2000-02-16

    申请人： Peter Maienfisch

    发明人： Peter Maienfisch

    IPC分类号： C07D25108

    CPC分类号： C07D213/40 ,  C07D213/61 ,  C07D213/89 ,  C07D251/08 ,  C07D261/08 ,  C07D277/28 ,  C07D277/32 ,  C07D307/14 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

    摘要： The invention relates to a method for producing an organic compound of formula (I) and optionally its E/Z-isomers, E/Z-isomer mixtures and/or tautomers, each in free or salt form, R1 representing hydrogen or C1-C4 alkyl, R2 representing hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl or a radical —CH2B, Het representing an unsubstituted or substituted heterocyclic radical and B representing phenyl, 3-pyridyl or thiazolyl, these being optionally substituted. The invention is characterized in that a compound of formula (IIa) Q—A—Q, wherein A represents a direct bond or an organic radical, or of formula (IIb), wherein U represents an organic radical, Q representing (1) in the compounds (IIa) and (IIb) and R1, R2 and Het having the meaning given above for formula (I), and optionally their E/Z-isomers, E/Z-isomer mixtures and/or tautomers, each in free or salt form are hydrolyzed. The invention also relates to a method for producing compounds of formulae (IIa), (IIb), (IIIa) and (IIIb), and to a method for combating pests with compounds of formulae (IIa) and (IIb).

    摘要翻译： 本发明涉及一种制备式（I）的有机化合物和任选的其E / Z-异构体，E / Z-异构体混合物和/或互变异构体的方法，各自为游离或盐形式，R1表示氢或C1-C4 烷基，R 2表示氢，C 1 -C 6烷基，C 3 -C 6环烷基或基团-CH 2 B，Het表示未取代或取代的杂环基，B表示苯基，3-吡啶基或噻唑基，它们任选被取代。 本发明的特征在于，式（IIa）QAQ的化合物，其中A表示直接键或有机基团，或式（IIb），其中U表示有机基团，Q表示化合物（IIa ）和（IIb），并且具有上述式（I）给出的含义的R1，R2和Het，以及任选的它们的E / Z-异构体，E / Z-异构体混合物和/或互变异构体，各自为游离或盐形式 。 本发明还涉及制备式（Ⅱa），（Ⅱb），（Ⅲa）和（Ⅲb）化合物的方法，以及用式（IIa）和（IIb）化合物防治害虫的方法。

    Oxadiazine derivatives
    73.
    发明授权
    Oxadiazine derivatives 有权
    恶二嗪衍生物

    公开(公告)号：US06376487B1

    公开(公告)日：2002-04-23

    申请号：US09136664

    申请日：1998-08-19

    申请人： Peter Maienfisch ,  Laurenz Gsell

    发明人： Peter Maienfisch ,  Laurenz Gsell

    IPC分类号： A01N4388

    CPC分类号： C07D413/06 ,  A01N47/40 ,  A01N51/00 ,  C07D273/00 ,  C07D273/04 ,  C07D417/06

    摘要： Compounds of the formula in which A is an unsubstituted or mono- to tetrasubstituted, aromatic or non-aromatic, monocyclic or bicyclic heterocyclic radical, where one to two of the substituents of A can be selected from the group consisting of halo-C1-C3alkyl, cyclopropyl, halocyclopropyl, C2-C3alkenyl, C2-C3alkynyl, halo-C2-C3alkenyl, halo-C2-C3alkynyl, halo-C1-C3alkoxy, C1-C3alkylthio, halo-C1-C3alkylthio, allyloxy, propargyloxy, allylthio, propargylthio, haloallyloxy, haloallylthio, cyano and nitro, and one to four of the substituents of A can be selected from the group consisting of C1-C3alkyl, C1-C3alkoxy and halogen; R is hydrogen, C1-C6alkyl, phenyl-C1-C4alkyl, C3-C6cycloalkyl, C2-C6alkenyl or C2-C6alkynyl; and X is N—NO2 or N—CN, and, if appropriate, tautomers thereof, in each case in free form or in salt form, can be used as agrochemical active ingredients and can be prepared in a manner known per se.

    摘要翻译： 其中A是未取代或单取代或单取代的芳香族或非芳香族单环或双环杂环基的化合物，其中A的一个至两个取代基可以选自卤代-C 1 -C 3烷基，环丙基 卤代环丙基，C 2 -C 3烯基，C 2 -C 3炔基，卤代-C 2 -C 3烯基，卤代-C 2 -C 3炔基，卤代-C 1 -C 3烷氧基，C 1 -C 3烷硫基，卤代C 1 -C 3烷硫基，烯丙氧基，炔丙氧基，烯丙硫基，炔丙硫基，卤代烯氧基，卤代烯硫基 ，氰基和硝基，A至1-4个取代基可以选自C 1 -C 3烷基，C 1 -C 3烷氧基和卤素; R是氢，C 1 -C 6烷基，苯基-C 1 -C 4烷基，C 3 -C 6环烷基，C 2 -C 6烯基或C 2 -C 6炔基; 且X是N-NO 2或N-CN，并且如果合适，其互变异构体在各种情况下以游离形式或盐形式可用作农业化学活性成分，并且可以以本身已知的方式制备。

    2-nitromethylidene/2-cyanimino/2-nitro-imino-pyrrolidines and piperidines, intermediates, and their use as pesticides
    74.
    发明授权
    2-nitromethylidene/2-cyanimino/2-nitro-imino-pyrrolidines and piperidines, intermediates, and their use as pesticides 失效
    2-硝基亚甲基/ 2-氰基亚氨基/ 2-硝基 - 亚氨基 - 吡咯烷酮和哌啶，中间体及其作为农药的用途

    公开(公告)号：US06353001B1

    公开(公告)日：2002-03-05

    申请号：US09501464

    申请日：2000-02-09

    申请人： Peter Maienfisch ,  Jozef Gonda ,  Olivier Jacob ,  Laurenz Gsell

    发明人： Peter Maienfisch ,  Jozef Gonda ,  Olivier Jacob ,  Laurenz Gsell

    IPC分类号： A61K3144

    CPC分类号： C07D401/06 ,  A01N43/40 ,  A01N47/38 ,  A01N51/00 ,  C07D417/06

    摘要： Compounds of formula: wherein A is an unsubstituted or substituted aromatic or non-aromatic, monocyclic or bicyclic heterocyclic radical wherein a ring nitrogen atom may have been replaced by a group R1 is hydrogen or C1-C3alkyl; R2 is hydrogen or C1-C3alkyl; R3 is hydrogen, an unsubstituted or substituted C1-C6alkyl, C3-C6cycloalkyl, C2-C6alkenyl or C2-C6alkynyl group, or C(═O)—R5, R5 is C1-C4alkyl, C1-C4alkoxy, an unsubstituted or substituted phenyl, phenoxy or benzyloxy group, or N(R6)2, each R6, independently of the other, is hydrogen, C1-C4alkyl or unsubstituted or substituted phenyl, X is CH—NO2, N—CN or N—NO2 and n is from 1 to 3, in free form or in salt form, and, where appropriate, tautomers of those compounds and the salts thereof, can be used as agrochemical active ingredients and can be prepared in a manner known per se.

    摘要翻译： 下式的化合物：其中A是未取代或取代的芳环或非芳族单环或双环杂环基，其中环氮原子可以被基团R 1取代为氢或C 1 -C 3烷基; R 2是氢或C 1 -C 3烷基; R 3是 氢，未取代或取代的C1-C6烷基，C3-C6环烷基，C2-C6链烯基或C2-C6炔基，或C（= O）-R5，R5是C1-C4烷基，C1-C4烷氧基，未取代或取代的苯基，苯氧基或 苄基氧基或N（R6）2，各自独立地为氢，C1-C4烷基或未取代或取代的苯基，X为CH-NO2，N-CN或N-NO2，n为1至3， 游离形式或盐形式，并且在适当时，这些化合物及其盐的互变异构体可用作农业化学活性成分，并且可以以本身已知的方式制备。

    Anthelmintics
    76.
    发明授权
    Anthelmintics 失效
    ANTHELMINTICS

    公开(公告)号：US5077300A

    公开(公告)日：1991-12-31

    申请号：US586096

    申请日：1990-09-19

    申请人： Peter Maienfisch ,  Christof Hildenbrand ,  Jean-Claude Gehret

    发明人： Peter Maienfisch ,  Christof Hildenbrand ,  Jean-Claude Gehret

    IPC分类号： A61K31/425 ,  A61K31/428 ,  A61P33/10 ,  C07D277/68 ,  C07D513/04

    CPC分类号： C07D277/68 ,  C07D513/04

    摘要： Anthelmintically active compounds of formula I are described ##STR1## in which R.sub.1 is hydrogen, halogen, C.sub.1 -C.sub.2 alkyl, C.sub.1 -C.sub.2 haloalkyl, nitro, C.sub.1 -C.sub.2 alkoxy, or the group SO.sub.n R in which R is C.sub.1 -C.sub.2 alkyl or phenyl and n is 0, 1 or 2;R.sub.2 is hydrogen, halogen, C.sub.1 -C.sub.2 alkyl, C.sub.1 -C.sub.2 haloalkyl, C.sub.1 -C.sub.2 haloalkoxy or C.sub.1 -C.sub.2 alkoxy;R.sub.3 is hydrogen or C.sub.1 -C.sub.2 alkyl;R.sub.4 is hydrogen or C.sub.1 -C.sub.2 alkyl;R.sub.5 is hydrogen, halogen or C.sub.1 -C.sub.5 alkyl;R.sub.6 is hydrogen, halogen or C.sub.1 -C.sub.5 alkyl;R.sub.7 is hydrogen, halogen, or C.sub.1 -C.sub.2 alkyl, nitro, C.sub.1 -C.sub.2 haloalkyl, C.sub.1 -C.sub.2 haloalkoxy or C.sub.1 -C.sub.2 alkoxy;R.sub.8 is hydrogen, halogen, C.sub.1 -C.sub.2 alkyl, C.sub.1 -C.sub.2 haloalkyl, C.sub.1 -C.sub.2 haloalkoxy or C.sub.1 -C.sub.2 alkoxy;R.sub.9 is hydrogen, halogen, C.sub.1 -C.sub.2 alkyl, C.sub.1 -C.sub.2 haloalkyl, C.sub.1 -C.sub.2 haloalkoxy or C.sub.1 -C.sub.2 alkoxy;R.sub.10 is hydrogen, halogen, nitro, NCS, OCF.sub.3, C.sub.1 -C.sub.2 alkyl or C.sub.1 -alkoxy;R.sub.11 is hydrogen, halogen, nitro, NCS, OCF.sub.3, C.sub.1 -C.sub.2 alkyl or C.sub.1 -C.sub.2 alkoxy; orR.sub.10 and R.sub.11 together form a --O(CH.sub.2).sub.m O-- bridge in which m is 1, 2 or 3, including the physiologically tolerable acid addition salts thereof, and also the preparation and use thereof and novel intermediates.

    摘要翻译： 式Ⅰ的驱虫活性化合物描述为其中R 1是氢，卤素，C 1 -C 2烷基，C 1 -C 2卤代烷基，硝基，C 1 -C 2烷氧基或其中R是C 1 -C 2烷基或苯基的基团SO n R和 n为0,1或2; R 2是氢，卤素，C 1 -C 2烷基，C 1 -C 2卤代烷基，C 1 -C 2卤代烷氧基或C 1 -C 2烷氧基; R3是氢或C1-C2烷基; R4是氢或C1-C2烷基; R5是氢，卤素或C1-C5烷基; R6是氢，卤素或C1-C5烷基; R 7是氢，卤素或C 1 -C 2烷基，硝基，C 1 -C 2卤代烷基，C 1 -C 2卤代烷氧基或C 1 -C 2烷氧基; R 8是氢，卤素，C 1 -C 2烷基，C 1 -C 2卤代烷基，C 1 -C 2卤代烷氧基或C 1 -C 2烷氧基; R 9是氢，卤素，C 1 -C 2烷基，C 1 -C 2卤代烷基，C 1 -C 2卤代烷氧基或C 1 -C 2烷氧基; R 10是氢，卤素，硝基，NCS，OCF 3，C 1 -C 2烷基或C 1 - 烷氧基; R 11是氢，卤素，硝基，NCS，OCF 3，C 1 -C 2烷基或C 1 -C 2烷氧基; 或R 10和R 11一起形成其中m为1,2或3的-O（CH 2）m O-桥，包括其生理上可耐受的酸加成盐，以及其制备和用途以及新型中间体。

    Composition for controlling parasites in productive livestock
    77.
    发明授权
    Composition for controlling parasites in productive livestock 失效

    公开(公告)号：US4871719A

    公开(公告)日：1989-10-03

    申请号：US168766

    申请日：1988-03-16

    申请人： Peter Maienfisch

    发明人： Peter Maienfisch

    IPC分类号： C07D493/22 ,  A01N43/16 ,  A01N43/90 ,  A61K31/365 ,  A61P33/00 ,  C07H19/01

    CPC分类号： C07H19/01 ,  A01N43/90 ,  Y02P20/55

    摘要： Novel 13-spiro-2'-[tetrahydrofuran]-milbemycins of the formula I ##STR1## in which X represents one of the groups --CH(OR.sub.1)--, --C(.dbd.O)-- or --C(.dbd.N--OH)--;R.sub.1 represents hydrogen or a OH-protecting group;R.sub.2 represents methyl, ethyl, isopropyl or sec.-butyl or the group --C(CH.sub.3).dbd.CH--A in which A represents methyl, ethyl or isopropyl; andR.sub.3 represents hydrogen; C.sub.1 -C.sub.10 -alkyl; C.sub.1 -C.sub.10 -alkyl substituted by at least one substituent selected from the group consisting of halogen, C.sub.1 -C.sub.6 -alkoxy, C.sub.2 -C.sub.6 -alkoxyalkoxy C.sub.3 -C.sub.9 -alkoxyalkoxyalkoxy, C.sub.1 -C.sub.6 -alkylthio, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.1 -C.sub.3 -alkyl-substituted C.sub.3 -C.sub.7 -cycloalkyl, hydroxy, benzyloxy, C.sub.1 -C.sub.6 -acyl and C.sub.1 -C.sub.6 -acyloxy, it being possible for each of the above-mentioned radicals representing or containing an alkoxy group to be terminally substituted at a terminal alkoxy group by hydroxy, halogen, C.sub.1 -C.sub.6 -acyl or by C.sub.1 -C.sub.6 -acyloxy; C.sub.3 -C.sub.7 -cycloalkyl; C.sub.3 -C.sub.7 -cycloalkyl substituted by at least one substituent selected from the group consisting of halogen and C.sub.1 -C.sub.3 -alkyl; C.sub.3 -C.sub.7 -cycloalkenyl; C.sub.2 -C.sub.10 -alkenyl; C.sub.2 -C.sub.10 -alkynyl; a radical selected from the group consisting of C.sub.2 -C.sub.10 -alkenyl and C.sub.2 -C.sub.10 -alkynyl, which radical is substituted by halogen, C.sub.1 -C.sub.6 -alkoxy or by C.sub.1 -C.sub.6 -acyloxy; 1-adamantylmethyl; menthyl; carveyl; phenyl; benzyl; napthyl; a radical selected from the group consisting of phenyl, benzyl and naphthyl, which radical is substituted by at least one substituent selected from the group consisting of halogen, C.sub.1 -C.sub.3 -alkyl, C.sub.1 -C.sub.3 -haloalkyl, C.sub.1 -C.sub.3 -alkoxy, C.sub.1 -C.sub.3 -haloalkoxy, C.sub.1 -C.sub.3 -alkylthio, nitro and cyano; benzyl substituted by a phenoxy group; or a four- to six-membered heterocyclic radical that has from one to three hetero atoms selected from the group consisting of oxygen, sulphur and nitrogen and that is unsubstituted or is substituted by at least one substituent selected from the group consisting of halogen, C.sub.1 -C.sub.3 -alkyl, C.sub.1 -C.sub.3 -haloalkyl, C.sub.1 -C.sub.3 -alkoxy, C.sub.1 -C.sub.3 -haloalkoxy, C.sub.1 -C.sub.3 -alkylthio, nitro and cyano, it being possible for the said heterocyclic radical also to be bonded via a C.sub.1 -C.sub.6 -alkylene bridge to the oxygen atom in the 5'-position of the tetrahydrofuran ring,their preparation and their use against parasites in productive livestock and against insect pests, are described.

    5-esters of milbemycins for controlling parasitic pests
    78.
    发明授权
    5-esters of milbemycins for controlling parasitic pests 失效
    用于控制寄生虫害的米尔倍霉素的5-酯

    公开(公告)号：US4778809A

    公开(公告)日：1988-10-18

    申请号：US895979

    申请日：1986-08-13

    申请人： Peter Maienfisch ,  Elmar Sturm

    发明人： Peter Maienfisch ,  Elmar Sturm

    IPC分类号： C07D493/22 ,  A01N43/90 ,  A23K20/195 ,  A61K31/365 ,  A61P33/10 ,  C07H19/01

    CPC分类号： C07H19/01 ,  A01N43/90 ,  A23K20/195

    摘要： The invention relates to ecto- and endoparasitic milbemycins of formula I ##STR1## wherein R is methyl, ethyl, isopropyl or sec-butyl;R.sub.1 is hydrogen, fluorine or C.sub.1 -C.sub.4 alkyl;R.sub.2 is one of the groups ##STR2## in which formulaeis a value from 2 to 6;X is oxygen or sulfur;R.sub.3 is halogen; andR.sub.4 is hydrogen, C.sub.1 -C.sub.12 alkoxy, C.sub.3 -C.sub.7 cycloalkoxy or C.sub.2 -C.sub.6 alkenyloxy; or C.sub.1 -C.sub.18 alkyl which is unsubstituted or substituted by halogen, C.sub.1 -C.sub.4 alkoxy, hydroxy and/or COOG, G being hydrogen, an alkali metal cation or an alkaline earth metal cation; or R.sub.4 is C.sub.3 -C.sub.7 cycloalkyl which is unsubstituted or substituted by halogen and/or C.sub.1 -C.sub.4 alkyl;C.sub.2 -C.sub.18 alkenyl which is unsubstituted or substituted by halogen;C.sub.2 -C.sub.18 alkynyl which is unsubstituted or substituted by halogen;phenyl which is unsubstituted or substituted by halogen, C.sub.1 -C.sub.4 alkyl C.sub.1 -C.sub.4 alkoxy, nitro, cyano and/or C.sub.1 -C.sub.4 haloalkyl; or a 5- or 6-membered unsaturated or saturated heterocyclic ring system which contains one to three hetero atoms selected from the series consisting of nitrogen, oxygen and sulfur and which is unsubstituted or substituted by oxo and/or by one to three substituents selected from halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy and/or C.sub.1 -C.sub.4 haloalkyl;to the use thereof in agriculture and to the preparation thereof by esterifying the 5-OH-milbemycins on which they are based.

    摘要翻译： 本发明涉及式I的异位和内寄生米尔倍霉素（I），其中R是甲基，乙基，异丙基或仲丁基; R1是氢，氟或C1-C4烷基; R2是其中公式为2至6的值之一之一; X是氧或硫; R3是卤素; 和R 4是氢，C 1 -C 12烷氧基，C 3 -C 7环烷氧基或C 2 -C 6烯氧基; 或未取代或被卤素取代的C 1 -C 18烷基，C 1 -C 4烷氧基，羟基和/或COOG，G为氢，碱金属阳离子或碱土金属阳离子; 或R 4为未被取代或被卤素和/或C 1 -C 4烷基取代的C 3 -C 7环烷基; 未被取代或被卤素取代的C 2 -C 18烯基; 未被取代或被卤素取代的C 2 -C 18炔基; 未被取代或被卤素取代的苯基，C 1 -C 4烷基C 1 -C 4烷氧基，硝基，氰基和/或C 1 -C 4卤代烷基; 或含有一至三个选自氮，氧和硫的杂原子的5-或6-元不饱和或饱和杂环体系，其未被取代或被氧代和/或被1-3个选自以下的取代基取代： 卤素，C 1 -C 4烷基，C 1 -C 4烷氧基和/或C 1 -C 4卤代烷基; 在农业中的用途以及通过酯化其所基于的5-OH- milbemycins来制备它们。

    5-azolylacetoxymilbemycins as ecto- and endoparasites
    79.
    发明授权
    5-azolylacetoxymilbemycins as ecto- and endoparasites 失效
    5-azolylaceoxymilbemycins as ecto-和endoparasites

    公开(公告)号：US4696922A

    公开(公告)日：1987-09-29

    申请号：US799373

    申请日：1985-11-18

    申请人： Elmar Sturm ,  Peter Maienfisch

    发明人： Elmar Sturm ,  Peter Maienfisch

    IPC分类号： A01N43/90 ,  A61K31/365 ,  A61P33/10 ,  C07D493/22 ,  C07H19/01 ,  C07D249/08

    CPC分类号： C07H19/01

    摘要： The present invention relates to milbemycin derivatives of the formula I ##STR1## wherein X is hydrogen or .beta.-halogen, R is methyl, ethyl, isopropyl or sec-butyl and Az is a 5 membered heterocyclic aromatic ring which contains 2-4 nitrogen atoms and is attached in the 1-position and which is unsubstituted or substituted by one or two C.sub.1 -C.sub.6 alkyl groups. These compounds, and the acid addition salts and metal complexes thereof, are effective pesticides for controlling endo-and ectoparasites, especially for controlling neamatodes which are parasites of animals. The may be obtained by appropriate esterification in 5-position of milbemycin derivatives. The selective .beta.-halogenation of 14,15-epoxymilbemycin derivatives can be effected via the intermediate .DELTA..sup.13,14 -15-hydroxymilbemycins with appropriate halogenating agents.

    摘要翻译： 本发明涉及式I（I）的密尔伯霉素衍生物，其中X是氢或β-卤素，R是甲基，乙基，异丙基或仲丁基，而Az是含有2- 4个氮原子并且连接在1-位且未被取代或被一个或两个C 1 -C 6烷基取代。 这些化合物及其酸加成盐和金属络合物是用于控制内寄生虫和外寄生虫的有效农药，特别是用于控制作为动物寄生虫的寄生虫。 可以通过在密尔伯霉素衍生物的5-位合适的酯化获得。 14,15-环氧米尔伯霉素衍生物的选择性β-卤代化可以通过中间体DELTA 13,14-15-羟吗啉霉素与适当的卤化剂进行。