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    Method for the production of halogen-substituted 2-(aminomethylidene)-3-oxobutyric acid esters
    4.
    发明授权
    Method for the production of halogen-substituted 2-(aminomethylidene)-3-oxobutyric acid esters 有权
    卤素取代的2-（氨基亚甲基）-3-氧代丁酸酯的制备方法

    公开(公告)号：US08586750B2

    公开(公告)日：2013-11-19

    申请号：US12990364

    申请日：2009-04-30

    申请人： Thomas Zierke ,  Volker Maywald ,  Michael Rack ,  Sebastian Peer Smidt ,  Michael Keil ,  Bernd Wolf ,  Christopher Koradin

    发明人： Thomas Zierke ,  Volker Maywald ,  Michael Rack ,  Sebastian Peer Smidt ,  Michael Keil ,  Bernd Wolf ,  Christopher Koradin

    IPC分类号： C07D295/145 ,  C07D211/34 ,  C07D265/30

    CPC分类号： C07D295/145 ,  C07D231/14

    摘要： The present invention relates to a process for preparing 2-(aminomethylidene)-4,4-dihalo-3-oxobutyric esters of the formula (I), wherein R1, R2, R3 are C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C3-C10-cycloalkyl or benzyl, and/or R2 together with R3 and the nitrogen atom to which the two radicals are attached are a heterocyclic radical, in which a corresponding 3-aminoacrylic ester is reacted with a halogen-substituted acetyl fluoride in the presence of at least one alkali or alkaline earth metal fluoride; and the further conversion of halogen-substituted 2-(aminomethylidene)-3-oxobutyric esters of the formula (I) to halomethyl-substituted pyrazol-4-ylcarboxylic acids and their esters.

    摘要翻译： 本发明涉及制备式（I）的2-（氨基亚甲基）-4,4-二卤代-3-氧代丁酸酯的方法，其中R1，R2，R3是C1-C6-烷基，C1-C6-卤代烷基 ，C 2 -C 6 - 烯基，C 3 -C 10 - 环烷基或苄基，和/或R 2与R 3和两个基团所连接的氮原子是杂环基团，其中相应的3-氨基丙烯酸酯与 卤素取代的乙酰氟在至少一种碱金属或碱土金属氟化物的存在下; 以及将式（I）的卤素取代的2-（氨基亚甲基）-3-氧代丁酸酯进一步转化为卤代甲基取代的吡唑-4-基羧酸及其酯。

    Method for preparing 1,3,4-substituted pyrazol compounds
    6.
    发明申请
    Method for preparing 1,3,4-substituted pyrazol compounds 有权
    制备1,3,4-取代吡唑化合物的方法

    公开(公告)号：US20110172436A1

    公开(公告)日：2011-07-14

    申请号：US12990340

    申请日：2009-05-04

    申请人： Bernd Wolf ,  Volker Maywald ,  Michael Keil ,  Christopher Koradin ,  Michael Rack ,  Thomas Zierke ,  Martin Sukopp

    发明人： Bernd Wolf ,  Volker Maywald ,  Michael Keil ,  Christopher Koradin ,  Michael Rack ,  Thomas Zierke ,  Martin Sukopp

    IPC分类号： C07D231/14 ,  C07C243/10

    CPC分类号： C07D409/12 ,  C07C251/76 ,  C07C251/84 ,  C07C251/86 ,  C07D231/14

    摘要： The invention provides an Ethernet bridge or router comprising a network fabric adapted to provide interconnectivity to a plurality of Ethernet ports, each of the Ethernet ports being adapted to receive and/or transmit Ethernet frames, and wherein the Ethernet bridge or router further comprises an encapsulator connected to receive Ethernet Protocol Data Units from the Ethernet ports, wherein the encapsulator is operable to generate a Fabric Protocol Data Unit from a received Ethernet Protocol Data Unit, the Fabric Protocol Data Unit comprising a header portion, and a payload portion which comprises the Ethernet Protocol Data Unit concerned, and wherein the encapsulator is operable to transform Ethernet destination address information from the Ethernet Protocol Data Unit into a routing definition for the network fabric, and to include this routing definition in the header portion of the Fabric Protocol Data Unit. Also provided is a method of data delivery across a network.

    摘要翻译： 本发明提供了一种以太网桥或路由器，其包括适于提供与多个以太网端口的互连性的网络结构，每个以太网端口适于接收和/或发送以太网帧，并且其中所述以太网桥或路由器还包括封装器 连接以从以太网端口接收以太网协议数据单元，其中所述封装器可操作以从接收到的以太网协议数据单元生成结构协议数据单元，所述结构协议数据单元包括报头部分和包括以太网的有效载荷部分 协议数据单元，并且其中所述封装器可操作以将以太网目的地地址信息从以太网协议数据单元转换为所述网络结构的路由定义，并将所述路由定义包括在所述结构协议数据单元的报头部分中。 还提供了一种通过网络进行数据传送的方法。

    Method for Producing Difluoromethyl-Substituted Pyrazole Compounds
    7.
    发明申请
    Method for Producing Difluoromethyl-Substituted Pyrazole Compounds 有权
    二氟甲基取代吡唑化合物的制备方法

    公开(公告)号：US20100184994A1

    公开(公告)日：2010-07-22

    申请号：US12664448

    申请日：2008-06-13

    申请人： Markus Nett ,  Thomas Grote ,  Jan Klaas Lohmann ,  Jochen Dietz ,  Sebastian Peer Smidt ,  Michael Rack ,  Thomas Zierke

    发明人： Markus Nett ,  Thomas Grote ,  Jan Klaas Lohmann ,  Jochen Dietz ,  Sebastian Peer Smidt ,  Michael Rack ,  Thomas Zierke

    IPC分类号： C07D231/14 ,  C07C229/06

    CPC分类号： C07D231/12 ,  C07D231/14

    摘要： The present invention relates to a process for preparing 3-difluoromethyl-substituted pyrazole compounds of the formula (I) in which R1 is H, halogen, nitro, C1-C8-alkyl, C1-C8-haloalkyl, C3-C8-cycloalkyl, phenyl, naphthyl, hetaryl, cyano, —C(═O)—OR1a, —C(═O)—NR1bR1c, —C(═O)—SR1d or —C(═S)—SR1e; R2 is H, C1-C4-alkyl, benzyl or phenyl; R3 is H, halogen, C1-C8-alkoxy, C1-C8-haloalkoxy, C3-C8-cycloalkoxy, C2-C8-alkenyloxy, C1-C8-alkylthio, C1-C8-haloalkylthio, C3-C8-cyclo-alkylthio or C2-C8-alkenylthio; compounds of the formula (II.a) or (II.b), in which R1 and R3 each have one of the definitions given above; R4 is halogen, —OR4a, —SR4a, —O—SO2—R4a or an —NR4bR4c group; R5 and R6 are each C1-C8-alkyl, C1-C8-haloalkyl, C3-C8-cycloalkyl, benzyl or phenyl, or, together with the nitrogen atom to which they are bonded, are a 3- to 8-membered heterocycle; Lewis acid adducts of compounds of the formula (II.b); the use of compounds of the formula (II.a) or (II.b) and of the Lewis acid adducts for preparing compounds of the formula (I) or (VI); and to a process for converting such compounds to the corresponding 3-difluoro-pyrazol-4-ylcarboxylic acids.

    摘要翻译： 本发明涉及制备式（I）的3-二氟甲基取代的吡唑化合物的方法，其中R 1是H，卤素，硝基，C 1 -C 8 - 烷基，C 1 -C 8 - 卤代烷基，C 3 -C 8 - 环烷基， 苯基，萘基，杂芳基，氰基，-C（= O）-OR1a，-C（= O）-NR1bR1c，-C（= O）-SR1d或-C（= S）-SR1e; R2是H，C1-C4-烷基，苄基或苯基; R 3是H，卤素，C 1 -C 8 - 烷氧基，C 1 -C 8 - 卤代烷氧基，C 3 -C 8 - 环烷氧基，C 2 -C 8 - 烯氧基，C 1 -C 8 - 烷硫基，C 1 -C 8 - 卤代烷硫基，C 3 -C 8环 - C 2 -C 8 - 烯硫基; 式（II.a）或（II.b）化合物，其中R 1和R 3各自具有上述定义之一; R4是卤素，-OR4a，-SR4a，-O-SO2-R4a或-NR4bR4c基团; R 5和R 6各自为C 1 -C 8 - 烷基，C 1 -C 8 - 卤代烷基，C 3 -C 8 - 环烷基，苄基或苯基，或与它们所键合的氮原子一起为3-至8-元杂环; 式（II.b）化合物的路易斯酸加合物; 使用式（II.a）或（II.b）化合物和路易斯酸加成物制备式（I）或（VI）化合物的方法; 以及将这些化合物转化为相应的3-二氟 - 吡唑-4-基羧酸的方法。

    Dolastatin 15 derivatives
    8.
    发明授权
    Dolastatin 15 derivatives 有权
    Dolastatin 15衍生物

    公开(公告)号：US07662786B2

    公开(公告)日：2010-02-16

    申请号：US11406512

    申请日：2006-04-18

    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

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

    摘要： Compounds of the present invention include cell growth inhibitors which are peptides of Formula I, A-B-D-E-F-(G)r-(K)s-L   (I), and acid salts thereof, wherein A, B, D, E, F, G and K are α-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 β-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。

    Process For Preparing Substituted Phenylhydrazines
    9.
    发明申请
    Process For Preparing Substituted Phenylhydrazines 审中-公开
    制备取代苯肼的方法

    公开(公告)号：US20100010263A1

    公开(公告)日：2010-01-14

    申请号：US12529066

    申请日：2008-02-27

    申请人： Thomas Zierke ,  Michael Rack

    发明人： Thomas Zierke ,  Michael Rack

    IPC分类号： C07C241/02

    CPC分类号： C07C319/20 ,  C07C241/02 ,  C07C323/48 ,  C07C243/22

    摘要： This invention relates to a process for preparing substituted phenylhydrazines of the formula I wherein R has the meaning as indicated in the description, comprising reacting a dichlorofluorobenzene of the formula II with a hydrazine source selected from hydrazine, hydrazine hydrate and acid addition salts of hydrazine and optionally being carried out in the presence of at least one organic solvent.

    摘要翻译： 本发明涉及一种制备式I取代苯肼的方法，其中R具有如说明书所述的含义，包括使式II的二氯氟苯与选自肼，水合肼和肼的酸加成盐的肼源和 任选地在至少一种有机溶剂的存在下进行。