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    Cellular RhoGTPase activation assay
    4.
    发明申请
    Cellular RhoGTPase activation assay 审中-公开
    细胞RhoGTPase活化测定

    公开(公告)号：US20060177816A1

    公开(公告)日：2006-08-10

    申请号：US11332680

    申请日：2006-01-13

    申请人： Nicole Teusch ,  Mario Mezler

    发明人： Nicole Teusch ,  Mario Mezler

    IPC分类号： C12Q1/00 ,  C12N5/08

    CPC分类号： C12Q1/42

    摘要： The invention relates to a cellular RhoGTPase activation assay based on the determination of changes in the actin cytoskeleton (actin cytoskeletal rearrangement assay); to the recombinant cell lines used to carry out this assay; to the constructs required to produce these cell lines; to the use of these recombinant cell lines for detecting effectors of Nogo receptor (NgR)-dependent signal transduction involving RhoGTPase, in particular for determining effectors of neuronal regeneration; and to assay methods using these recombinant cell lines.

    摘要翻译： 本发明涉及基于测定肌动蛋白细胞骨架（肌动蛋白细胞骨架重排测定）变化的细胞RhoGTPase活化测定法; 用于进行该测定的重组细胞系; 生产这些细胞系所需的构建体; 使用这些重组细胞系检测涉及RhoGTPase的Nogo受体（NgR）依赖性信号转导的影响因子，特别是用于确定神经元再生的作用者; 并使用这些重组细胞系测定方法。

    Azetidin compounds suitable for treating disorders that respond to modulation of the serotonin 5-HT6 receptor
    8.
    发明授权
    Azetidin compounds suitable for treating disorders that respond to modulation of the serotonin 5-HT6 receptor 有权
    适用于治疗对5-羟色胺5-HT 6受体的调节作用的疾病的氮杂环丁啶化合物

    公开(公告)号：US08507469B2

    公开(公告)日：2013-08-13

    申请号：US12532406

    申请日：2008-03-20

    申请人： Thomas Schultz ,  Wilfried Braje ,  Sean Colm Turner ,  Andreas Haupt ,  Udo Lange ,  Karla Drescher ,  Karsten Wicke ,  Liliane Unger ,  Mario Mezler ,  Matthias Mayrer

    发明人： Thomas Schultz ,  Wilfried Braje ,  Sean Colm Turner ,  Andreas Haupt ,  Udo Lange ,  Karla Drescher ,  Karsten Wicke ,  Liliane Unger ,  Mario Mezler ,  Matthias Mayrer

    IPC分类号： A61K31/397 ,  C07D403/04 ,  C07D471/04

    CPC分类号： C07D471/04 ,  C07D403/04

    摘要： The present invention relates to compounds of formula (I) wherein A is C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-hydroxyalkyl, C2-C6-alkenyl, C2-C6-halo-alkenyl, C3-C6-cycloalkyl, aryl-C1-C4-alkyl, aryl-C2-C4-alkenyl, aryl or hetaryl; is a single or double bond; X1 and X2 are N, CRx1, NRx2 or CRx3Rx4; Rx1, Rx3 and Rx4 are H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylcarbonyl, etc. or two geminal radicals Rx3 and Rx4 together with the carbon atom to which they are bound may form a carbonyl group or a 3- to 6-membered carbocyclic or heterocyclic spiro-annulated ring; Rx2 is hydrogen, C1-C6-alkyl, C1-C6-alkylcarbonyl, C1-C6-haloalkyl, etc.; or two vicinal radicals Rx1, Rx2, Rx3 or Rx4 together with X1 and X2 form a five- or six-membered carbocyclic or heterocyclic fused ring; Y1, Y2 and Y3 are N or CRy; Ry is H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylcarbonyl, C1-C6-haloalkyl, etc.; wherein a maximum of 3 of the radicals X1, X2, Y1, Y2 and Y3 are selected from NRx1 and N; R1 is hydrogen, C1-C6-alkyl, C1-C6-hydroxyalkyl, C1-C6-haloalkyl, etc.; R2 is C1-C4-alkyl or C1-C4-haloalkyl; n is 0, 1 or 2; physiologically tolerated acid addition salts and the N-oxides thereof, pharmaceutical composition comprising them, a method for treating medical disorders selected from diseases of the central nervous system, addiction diseases or obesity, said method comprising administering an effective amount of such compounds to a subject in need and the use of such a compound for preparing a pharmaceutical compositions.

    摘要翻译： 本发明涉及式（I）化合物，其中A为C 1 -C 6 - 烷基，C 1 -C 6 - 卤代烷基，C 1 -C 6羟基烷基，C 2 -C 6 - 烯基，C 2 -C 6 - 卤代烯基，C 3 -C 6 - 芳基-C 1 -C 4 - 烷基，芳基-C 2 -C 4 - 烯基，芳基或杂芳基; 是单键或双键; X1和X2是N，CRx1，NRx2或CRx3Rx4; Rx1，Rx3和Rx4是H，卤素，CN，NO2，C1-C6-烷基，C1-C6-烷氧基，C1-C6-烷基羰基等，或两个偕根基Rx3和Rx4与它们所在的碳原子一起 结合可形成羰基或3-至6-元碳环或杂环螺环状环; Rx2是氢，C1-C6-烷基，C1-C6-烷基羰基，C1-C6-卤代烷基等; 或两个连位基Rx1，Rx2，Rx3或Rx4与X1和X2一起形成五元或六元碳环或杂环稠环; Y1，Y2和Y3为N或CRy; Ry是H，卤素，CN，NO 2，C 1 -C 6 - 烷基，C 1 -C 6 - 烷氧基，C 1 -C 6 - 烷基羰基，C 1 -C 6 - 卤代烷基等; 其中基团X1，X2，Y1，Y2和Y3中的最多3个选自NRx1和N; R1是氢，C1-C6-烷基，C1-C6-羟基烷基，C1-C6-卤代烷基等; R2是C1-C4-烷基或C1-C4卤代烷基; n为0,1或2; 生理耐受的酸加成盐及其N-氧化物，包含它们的药物组合物，治疗选自中枢神经系统疾病，成瘾疾病或肥胖症的医学病症的方法，所述方法包括向受试者施用有效量的这些化合物 并且使用这种化合物来制备药物组合物。