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77 条记录 (耗时 0.041 秒)

    Method for the Production of N-Substituted (3-Dihalomethyl-1-Methyl-Pyrazole-4-yl) Carboxamides
    51.
    发明申请
    Method for the Production of N-Substituted (3-Dihalomethyl-1-Methyl-Pyrazole-4-yl) Carboxamides 有权
    N-取代的（3-二卤代甲基-1-甲基 - 吡唑-4-基）羧酰胺的制备方法

    公开(公告)号：US20100174094A1

    公开(公告)日：2010-07-08

    申请号：US12601966

    申请日：2008-05-30

    申请人： Thomas Zierke ,  Joachim Rheinheimer ,  Michael Rack ,  Sebastian Peer Smidt ,  Ansgar Gereon Altenhoff ,  Joachim Schmidt-Leithoff ,  Nina Challand

    发明人： Thomas Zierke ,  Joachim Rheinheimer ,  Michael Rack ,  Sebastian Peer Smidt ,  Ansgar Gereon Altenhoff ,  Joachim Schmidt-Leithoff ,  Nina Challand

    IPC分类号： C07D231/18 ,  C07D231/12

    CPC分类号： C07D231/14

    摘要： The present invention relates to a process for preparing N-substituted (3-dihalomethylpyrazol-4-yl)carboxamides of the formula (I) in which R1 is optionally substituted phenyl or C3-C7-cycloalkyl, R1a is hydrogen or fluorine, or R1a together with R1 is optionally substituted C3-C5-alkanediyl or C5-C7-cycloalkanediyl, R2 is C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl or C1-C4-alkoxy-C1-C2-alkyl, X is F or Cl and n is 0, 1, 2 or 3; which comprises A) providing a compound of the formula (II) in which X is F or Cl, Y is Cl or Br and R2 has one of the meanings given above and B) reacting a compound of the formula (II) with carbon monoxide and a compound of the formula (III) in which R1, R1a and n have one of the meanings given above; in the presence of a palladium catalyst; to intermediates used for the preparation according to the process according to the invention, and also to processes for their preparation.

    摘要翻译： 本发明涉及式（I）的N-取代的（3-二卤代甲基吡唑-4-基）甲酰胺的制备方法，其中R 1为任选取代的苯基或C 3 -C 7 - 环烷基，R 1a为氢或氟，或R 1a R 1是C 1 -C 6 - 烷基，C 2 -C 6 - 烯基，C 2 -C 6炔基或C 1 -C 4 - 烷氧基-C 1 -C 2 - 烷基，其中R 1是任选取代的C 3 -C 5 - 烷二基或C 5 -C 7 - 环烷二基， X是F或Cl，n是0,1,2或3; 其包括A）提供其中X为F或Cl，Y为Cl或Br的式（II）化合物，R 2具有上述含义之一，B）使式（II）化合物与一氧化碳 和其中R1，R1a和n具有上述含义之一的式（III）化合物; 在钯催化剂的存在下; 用于根据本发明的方法制备的中间体，以及其制备方法。

    Process for Preparing Fluoromethyl-Substituted Heterocyclic Compounds
    52.
    发明申请
    Process for Preparing Fluoromethyl-Substituted Heterocyclic Compounds 失效
    制备氟甲基取代的杂环化合物的方法

    公开(公告)号：US20100022782A1

    公开(公告)日：2010-01-28

    申请号：US12519032

    申请日：2007-12-20

    申请人： Thomas Zierke ,  Michael Rack

    发明人： Thomas Zierke ,  Michael Rack

    IPC分类号： C07D231/10

    CPC分类号： C07D231/14

    摘要： The present invention relates to a process for preparing fluoromethyl-substituted heterocyclic compounds of the general formula (I) in which R1 is H or F; R2 is an -[A-O]m—R3 group in which A is C2-C4-alkanediyl, R3 is C1-C4-alkyl and m is 1 or 2; by converting the corresponding chloromethyl-substituted compounds (II) in the presence of fluorinating agents, to processes for preparing the chloromethyl-substituted compounds (II), to processes for preparing amides of the general formula (IV) and to compounds of the general formulae (I) and (II).

    摘要翻译： 本发明涉及制备通式（I）的氟甲基取代的杂环化合物的方法，其中R 1为H或F; R2是其中A是C 2 -C 4烷二基，R 3是C 1 -C 4烷基，m是1或2的 - [A-O] m -R 3基团; 通过在氟化剂的存在下将相应的氯甲基取代的化合物（II）转化为制备氯甲基取代的化合物（II）的方法，制备通式（IV）的酰胺的方法和通式 （I）和（II）。

    Crystalline Modification of N-Ethyl-2,2-Dichloro-1-Methylcyclopropane-Carboxamide-2-(2,6-Dichloro-Alpha, Alpha, Alpha-Trifluoro-P-Tolyl)Hydrazone
    54.
    发明申请
    Crystalline Modification of N-Ethyl-2,2-Dichloro-1-Methylcyclopropane-Carboxamide-2-(2,6-Dichloro-Alpha, Alpha, Alpha-Trifluoro-P-Tolyl)Hydrazone 审中-公开
    N-乙基-2,2-二氯-1-甲基环丙烷 - 甲酰胺-2-（2,6-二氯-α，α，α-三氟对甲苯基）腙的结晶改性

    公开(公告)号：US20080249182A1

    公开(公告)日：2008-10-09

    申请号：US12090733

    申请日：2006-10-26

    申请人： Thomas Zierke

    发明人： Thomas Zierke

    IPC分类号： A01N37/18 ,  C07C233/00 ,  A01N25/34 ,  A01P7/04

    CPC分类号： A01N53/00 ,  C07C257/22 ,  C07C2601/02

    摘要： The present invention relates to a novel crystalline modification of N-ethyl-2,2-dichloro-1-methylcyclopropane-carboxamide-2-(2,6-dichloro-α,α,α-trifluoro-p-tolyl)hydrazone, to a process for its preparation and to its use for combating pests and parasites. Further, the invention relates to pesticidal and parasiticidal mixtures and compositions comprising said crystalline modification.

    摘要翻译： 本发明涉及N-乙基-2,2-二氯-1-甲基环丙烷 - 甲酰胺-2-（2,6-二氯-α，α，α-三氟 - 对甲苯基）腙的新结晶改性， 其制备过程及其用于防治害虫和寄生虫的过程。 此外，本发明涉及包含所述结晶改性的杀虫剂和杀虫剂混合物和组合物。

    Dolastatin 15 derivatives
    57.
    发明授权
    Dolastatin 15 derivatives 失效
    Dolastatin 15衍生物

    公开(公告)号：US6143721A

    公开(公告)日：2000-11-07

    申请号：US896394

    申请日：1997-07-18

    申请人： Bernd Janssen ,  Teresa Barlozzari ,  Andreas Haupt ,  Thomas Zierke ,  Andreas Kling

    发明人： Bernd Janssen ,  Teresa Barlozzari ,  Andreas Haupt ,  Thomas Zierke ,  Andreas Kling

    IPC分类号： A61K38/00 ,  A61K38/08 ,  A61P35/00 ,  C07K7/06 ,  C12P19/34

    CPC分类号： C07K7/06 ,  C12P19/34 ,  A61K38/00

    摘要： Compounds of the present invention include cell growth inhibitors which are peptides of Formula I,A-B-D-E-F-(G).sub.r -(K).sub.s -L (I),and acid salts thereof, wherein A, B, D, E, F, G and K are .alpha.-amino acid residues, and s and r are each, independently, 0 or 1. L is a monovalent radical, such as, for example, an amino group, an N-substituted amino group, a .beta.-hydroxylamino group, a hydrazido group, an alkoxy group, a thioalkoxy group, an aminoxy group, or an oximato group. The present invention also includes a method for treating cancer in a mammal, such as a human, comprising administering to the mammal an effective amount of a compound of Formula I in a pharmaceutically acceptable composition.

    摘要翻译： 本发明的化合物包括作为式I的肽，ABDEF-（G）r-（K）sL（I）及其酸式盐的细胞生长抑制剂，其中A，B，D，E，F，G和K 是α-氨基酸残基，s和r各自独立地为0或1.L为单价基团，例如氨基，N-取代氨基，β-羟基氨基， 酰肼基，烷氧基，硫代烷氧基，氨氧基或肟基。 本发明还包括用于治疗哺乳动物（例如人）中的癌症的方法，包括向所述哺乳动物施用有效量的药学上可接受的组合物中的式I化合物。