公开(公告)号：US20060100211A1

公开(公告)日：2006-05-11

申请号：US11313380

申请日：2005-12-21

Applicant: Georg Dahmann ,  Frank Himmelsbach ,  Bernd Krist ,  Martin Lenter ,  Alexander Pautsch ,  Gisela Schnapp ,  Martin Steegmaier ,  Helmut Wittneben ,  Anthony Prokopowicz ,  Walter Spevak ,  Andreas Schoop ,  Steffen Steurer

Inventor： Georg Dahmann ,  Frank Himmelsbach ,  Bernd Krist ,  Martin Lenter ,  Alexander Pautsch ,  Gisela Schnapp ,  Martin Steegmaier ,  Helmut Wittneben ,  Anthony Prokopowicz ,  Walter Spevak ,  Andreas Schoop ,  Steffen Steurer

IPC: C07D403/02 ,  A61K31/501 ,  A61K31/506

CPC classification number: C07D239/48 ,  C07D231/12 ,  C07D233/56 ,  C07D239/50 ,  C07D239/80 ,  C07D249/08 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D451/04 ,  C07D451/06 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10

Abstract: The present invention relates to trisubstituted pyrimidines of formula (I) wherein 0Ra to Re are defined as in claim 1, which are suitable for the treatment of illnesses characterised by excessive or abnormal cell proliferation, the use thereof for preparing a pharmaceutical composition with the abovementioned properties, and processes for the preparation thereof.

Abstract translation: 本发明涉及如权利要求1所定义的式（I）的三取代嘧啶，其中R 1和R 2定义如权利要求1所述，其适用于治疗以过量为特征的疾病 或异常细胞增殖，其用于制备具有上述性质的药物组合物的用途及其制备方法。

公开(公告)号：US20060263841A1

公开(公告)日：2006-11-23

申请号：US11492654

申请日：2006-07-25

Applicant: Anthony Prokopowicz ,  Martha Brown ,  Jessi Wildeson ,  Scott Jakes ,  Mark Labadia

Inventor： Anthony Prokopowicz ,  Martha Brown ,  Jessi Wildeson ,  Scott Jakes ,  Mark Labadia

IPC: C12Q1/48 ,  C07D405/02

CPC classification number: C07D405/12 ,  C09B11/24 ,  C09B55/003 ,  C12Q1/485 ,  G01N33/533 ,  G01N33/573 ,  G01N33/582 ,  G01N2500/02

Abstract: The invention provides methods relating to a novel screening assay format that can be applied to broad members of the protein kinase gene family. The assay uses a series of labeled, active site probes described herein that can be displaced by an inhibitor agent. The Kd for the inhibitor compound is derived based on the Kd of the probe for the kinase and the dose response of the inhibitor agent. The invention also provides novel active site probes suitable for use with the screening method.

Abstract translation: 本发明提供了可应用于蛋白激酶基因家族的广泛成员的新型筛选测定形式的方法。 该测定使用本文所述的一系列标记的可被抑制剂代替的活性位点探针。 用于抑制剂化合物的K 基于用于激酶的探针的KⅢ和抑制剂的剂量反应而衍生。 本发明还提供适用于筛选方法的新型活性位点探针。

公开(公告)号：US20050100978A1

公开(公告)日：2005-05-12

申请号：US10955129

申请日：2004-09-30

Applicant: Anthony Prokopowicz ,  Martha Brown ,  Jessi Wildeson ,  Scott Jakes ,  Mark Labadia

Inventor： Anthony Prokopowicz ,  Martha Brown ,  Jessi Wildeson ,  Scott Jakes ,  Mark Labadia

IPC: C07D405/12 ,  C09B11/24 ,  C12Q1/48 ,  G01N33/533 ,  G01N33/542 ,  G01N33/573 ,  G01N33/58

CPC classification number: C07D405/12 ,  C09B11/24 ,  C09B55/003 ,  C12Q1/485 ,  G01N33/533 ,  G01N33/573 ,  G01N33/582 ,  G01N2500/02

Abstract: The invention provides methods relating to a novel screening assay format that can be applied to broad members of the protein kinase gene family. The assay uses a series of labeled, active site probes described herein that can be displaced by an inhibitor agent. The Kd for the inhibitor compound is derived based on the Kd of the probe for the kinase and the dose response of the inhibitor agent. The invention also provides novel active site probes suitable for use with the screening method.

Abstract translation: 本发明提供了可应用于蛋白激酶基因家族的广泛成员的新型筛选测定形式的方法。 该测定使用本文所述的一系列标记的可被抑制剂代替的活性位点探针。 用于抑制剂化合物的K 基于用于激酶的探针的KⅢ和抑制剂的剂量反应而衍生。 本发明还提供适用于筛选方法的新型活性位点探针。

公开(公告)号：US20050124640A1

公开(公告)日：2005-06-09

申请号：US10933635

申请日：2004-09-03

Applicant: Mario Cardozo ,  Derek Cogan ,  Charles Cywin ,  George Dahmann ,  Darren DiSalvo ,  John Ginn ,  Anthony Prokopowicz ,  Denice Spero ,  Erick Young

Inventor： Mario Cardozo ,  Derek Cogan ,  Charles Cywin ,  George Dahmann ,  Darren DiSalvo ,  John Ginn ,  Anthony Prokopowicz ,  Denice Spero ,  Erick Young

IPC: A61K31/505 ,  A61K31/506 ,  A61P3/10 ,  A61P37/00 ,  C07D239/48 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D471/04 ,  H01L51/00 ,  C07D43/02

CPC classification number: C07D239/48 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D471/04 ,  H01L51/0089

Abstract: Disclosed are novel compounds of formula (I): wherein R1, R2 and R3 are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC-theta, including immunological disorders and type II diabetes. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

Abstract translation: 公开了式（I）的新化合物：其中R 1，R 2和R 3 3如本文所定义，其可用作抑制剂 的PKC-θ，因此可用于治疗通过PKC-θ的活性介导或持续的各种疾病和病症，包括免疫学障碍和II型糖尿病。 本发明还涉及包含这些化合物的药物组合物，使用这些化合物治疗各种疾病和病症的方法，制备这些化合物的方法和可用于这些方法的中间体。