公开(公告)号：US20090170125A1

公开(公告)日：2009-07-02

申请号：US11919178

申请日：2006-04-27

Applicant: Isabelle Heit ,  Monika Baudler ,  Sascha Dammeier ,  Michaela Schäfer ,  Hubert Paul ,  Gottfried Baier ,  Stephen Shaw

Inventor： Isabelle Heit ,  Monika Baudler ,  Sascha Dammeier ,  Michaela Schäfer ,  Hubert Paul ,  Gottfried Baier ,  Stephen Shaw

IPC: C12Q1/48 ,  G01N33/573 ,  C07K16/40

CPC classification number: G01N33/5041 ,  C07K16/40 ,  C07K16/44 ,  G01N2333/9121

Abstract: The invention relates to a method for investigating the modulating effect of a test substance on a PKCθ-dependent signal transduction pathway or for finding a PKCθ modulator in a human or animal cell, including the steps (a) contacting the cell with the test substance or with the PKCθ modulator; (b) where appropriate inducing the kinase activity of PKCθ; (c) incubating the cell under conditions which bring about phosphorylation at least of a serine or threonine residue of PKCθ; (d) where appropriate lysing the cell; and (e) determining the phosphorylation content of the at least one serine or threonine residue of PKCθ.

Abstract translation: 本发明涉及一种用于研究测试物质对PKCθ依赖性信号转导途径或在人或动物细胞中发现PKCθ调节剂的调节作用的方法，包括步骤（a）使细胞与测试物质接触或 与PKCtheta调制器; （b）适当诱导PKCθ的激酶活性; （c）在至少引起PKCθ的丝氨酸或苏氨酸残基的磷酸化的条件下孵育细胞; （d）适当时裂解细胞; 和（e）确定PKCθ的至少一个丝氨酸或苏氨酸残基的磷酸化含量。

公开(公告)号：US20080242681A1

公开(公告)日：2008-10-02

申请号：US10586121

申请日：2005-01-19

Applicant: Johannes Barsig ,  Monika Baudler ,  Daniela Bundschuh ,  Florian Gantner ,  Ulrich Graedler ,  Isabelle Heit ,  Thomas Martin ,  Michaela Schaefer ,  Imre Schlemminger ,  Josef Stadlwieser ,  Wolf-Ruediger Ulrich

Inventor： Johannes Barsig ,  Monika Baudler ,  Daniela Bundschuh ,  Florian Gantner ,  Ulrich Graedler ,  Isabelle Heit ,  Thomas Martin ,  Michaela Schaefer ,  Imre Schlemminger ,  Josef Stadlwieser ,  Wolf-Ruediger Ulrich

IPC: A61K31/505 ,  C07D239/42 ,  A61P31/00 ,  A61P35/00 ,  A61P25/28 ,  A61P3/10 ,  A61P9/10 ,  A61P19/02 ,  A61P29/00 ,  A61P17/00 ,  A61P27/02

CPC classification number: C07D239/42 ,  C07D403/04 ,  C07D405/04 ,  C07D409/14

Abstract: Compounds of a certain formula 1 in which R1 and R2 have the meanings indicated in the description are novel kinase inhibitors. Formula (1), in which R1 is phenyl, phenyl substituted by R3 and/or R4, naphthalenyl, naphthalenyl substituted by and/or R6, aryl1, aryl1 substituted by R7 and/or R8, R9, R10 or R11, R2 is phenyl, phenyl substituted by R12 and/or R13, naphthalenyl, naphthalenyl substituted by R14 and/or R15, aryl2, aryl2 substituted by R16 and/or R17 or a radical selected from Formula (2).

Abstract translation: 其中R1和R2具有说明书所述含义的某种式1的化合物是新的激酶抑制剂。 式（1）其中R 1为苯基，被R 3和/或R 4取代的苯基，被R 1和/或R 6取代的萘基，萘基，芳基，被R 7和/或R 8，R 9，R 10或R 11取代的芳基， 被R 12和/或R 13取代的苯基，被R 14和/或R 15取代的萘基，萘基，芳基2，被R 16和/或R 17取代的芳基2或选自式（2）的基团。