公开(公告)号：US08003787B2

公开(公告)日：2011-08-23

申请号：US12126437

申请日：2008-05-23

Applicant: Knut Eis ,  Olaf Prien ,  Ulrich Lücking ,  Judith Günther ,  Dieter Zopf ,  Dirk Brohm ,  Verena Vöhringer ,  Elisabeth Woltering ,  Hartmut Beck ,  Mario Lobell ,  Volkhart Min-Jian Li ,  Susanne Greschat

Inventor： Knut Eis ,  Olaf Prien ,  Ulrich Lücking ,  Judith Günther ,  Dieter Zopf ,  Dirk Brohm ,  Verena Vöhringer ,  Elisabeth Woltering ,  Hartmut Beck ,  Mario Lobell ,  Volkhart Min-Jian Li ,  Susanne Greschat

IPC: C07D239/86

CPC classification number: C07D239/86 ,  C07D215/44 ,  C07D409/04

Abstract: The present invention relates to a quinoline or quinazoline derivative having the general formula (A): in which R3, R4, W, Y and Q are indicated in the description and the claims, the use of the compounds of the general formula (A) for the treatment of various disorders, and the preparation of compounds of the general formula (A).

Abstract translation: 本发明涉及具有通式（A）的喹啉或喹唑啉衍生物：其中R3，R4，W，Y和Q在说明书和权利要求中表示，通式（A）的化合物的用途， 用于治疗各种疾病，以及制备通式（A）的化合物。

公开(公告)号：US20100048891A1

公开(公告)日：2010-02-25

申请号：US12432213

申请日：2009-04-29

Applicant: Klause SCHULZE ,  Knut Eis ,  Lars Wortmann ,  Dirk Kosemund ,  Olaf Prien ,  Gerhard Siemeister ,  Holger Hess-Stumpp ,  Uwe Eberspaecher ,  Dominic E.A. Brittain ,  Imadul Islam

Inventor： Klause SCHULZE ,  Knut Eis ,  Lars Wortmann ,  Dirk Kosemund ,  Olaf Prien ,  Gerhard Siemeister ,  Holger Hess-Stumpp ,  Uwe Eberspaecher ,  Dominic E.A. Brittain ,  Imadul Islam

IPC: C07D417/02 ,  C07D277/04 ,  C07D413/02 ,  C07D239/02

CPC classification number: C07D277/14 ,  C07D277/20 ,  C07D417/12 ,  C07D417/14

Abstract: Thiazolidinones of general formula (I) production thereof and use as inhibitors of polo like kinase (PLK) for the treatment of various diseases.

Abstract translation: 通式（I）的噻唑烷酮的制备，用作马球激酶（PLK）抑制剂用于治疗各种疾病。

公开(公告)号：US20080019922A1

公开(公告)日：2008-01-24

申请号：US11766232

申请日：2007-06-21

Applicant: Olaf Prien ,  Knut Eis ,  Wolfgang Schwede ,  Judith Guenther ,  Dieter Zopf ,  Dominic Brittain

Inventor： Olaf Prien ,  Knut Eis ,  Wolfgang Schwede ,  Judith Guenther ,  Dieter Zopf ,  Dominic Brittain

IPC: A61K49/04 ,  A61K31/495 ,  A61P9/00 ,  C07D239/72

CPC classification number: C07D513/04 ,  C07D239/70 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04

Abstract: The present invention relates to a quinazoline derivative having the general formula (A): in which R1, R2, X, Y and Z are indicated in the description and the claims, the use of the compounds of the general formula (A) for the treatment of various disorders, and the preparation of compounds of the general formula (A).

Abstract translation: 本发明涉及具有通式（A）的喹唑啉衍生物：其中R 1，R 2，X，Y和Z在说明书中表示， 权利要求书中，使用通式（A）的化合物治疗各种病症，以及制备通式（A）的化合物。

公开(公告)号：US20070010566A1

公开(公告)日：2007-01-11

申请号：US11410285

申请日：2006-04-25

Applicant: Olaf Prien ,  Volker Schulze ,  Knut Eis ,  Lars Wortmann ,  Dirk Kosemund ,  Gerhard Siemeister ,  Uwe Eberspaecher ,  Judith Guenther ,  Dominic Brittain

Inventor： Olaf Prien ,  Volker Schulze ,  Knut Eis ,  Lars Wortmann ,  Dirk Kosemund ,  Gerhard Siemeister ,  Uwe Eberspaecher ,  Judith Guenther ,  Dominic Brittain

IPC: A61K31/427 ,  C07D417/02

CPC classification number: C07D277/34 ,  C07D417/06

Abstract: The invention relates to thiazolidones of general formula (I) as welt as to their production and to their use as inhibitors of the polo-like kinase (Plk) for treating various diseases, as welt as to intermediate products for the production of the compounds according to the invention.

Abstract translation: 本发明涉及通式（I）的噻唑烷酮，其生产方式及其用作治疗各种疾病的polo样激酶（Plk）的抑制剂的用途，如用于生产化合物的中间产物 涉及本发明。

公开(公告)号：US20060079503A1

公开(公告)日：2006-04-13

申请号：US10513368

申请日：2003-04-29

Applicant: Wolfgang Schwede ,  Volker Schulze ,  Knut Eis ,  Bernd Buchmann ,  Hans Briem ,  Gerhard Siemeister ,  Ulf Boemer ,  Karsten Parczyk

Inventor： Wolfgang Schwede ,  Volker Schulze ,  Knut Eis ,  Bernd Buchmann ,  Hans Briem ,  Gerhard Siemeister ,  Ulf Boemer ,  Karsten Parczyk

IPC: A61K31/55 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/454 ,  A61K31/426 ,  C07D417/02

CPC classification number: C07D277/20 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D277/34 ,  C07D277/82 ,  C07D417/12 ,  C07D451/06 ,  C07D487/04

Abstract: Thiazolidones of general formula I in which R1, R2, R3, X and Y have the meanings that are indicated in the description, their production and use as inhibitors of polo-like kinases (PLK) for treating various diseases as well as intermediate products for the production of thiazolidones are described.

Abstract translation: 其中R 1，R 2，R 3，X和Y的通式I的噻唑烷酮具有说明书中指出的含义， 描述了它们作为用于治疗各种疾病的polo样激酶（PLK）抑制剂的生产和用途以及用于生产噻唑烷酮的中间产物。

公开(公告)号：US09284319B2

公开(公告)日：2016-03-15

申请号：US14129043

申请日：2012-06-21

Applicant: Knut Eis ,  Florian Pühler ,  Ludwig Zorn ,  Arne Scholz ,  Philip Lienau ,  Mark Jean Gnoth ,  Ulf Bömer ,  Judith Günther ,  Jörg Fanghänel ,  Daniel Korr

Inventor： Knut Eis ,  Florian Pühler ,  Ludwig Zorn ,  Arne Scholz ,  Philip Lienau ,  Mark Jean Gnoth ,  Ulf Bömer ,  Judith Günther ,  Jörg Fanghänel ,  Daniel Korr

IPC: A61K31/5025 ,  C07D487/04

CPC classification number: C07D487/04

Abstract: The present invention relates to heterocyclyl aminoimidazopyridazine compounds of general formula (I): in which A, R1, R2, R3 and R4 are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.

Abstract translation: 本发明涉及通式（I）的杂环基氨基咪唑并哒嗪化合物：其中A，R1，R2，R3和R4如权利要求中所定义，涉及制备所述化合物的方法，药物组合物和包含所述化合物的组合， 所述化合物用于制备用于治疗或预防疾病，特别是高增殖和/或血管生成障碍的药物组合物作为唯一试剂或与其它活性成分组合的用途。

公开(公告)号：US20140288069A1

公开(公告)日：2014-09-25

申请号：US14118519

申请日：2012-05-14

Applicant: Knut Eis ,  Florian Pühler ,  Ludwig Zorn ,  Arne Scholz ,  Philip Lienau ,  Mark Jean Gnoth ,  Ulf Bömer ,  Judith Günther ,  Jörg Fanghänel ,  Daniel Korr

Inventor： Knut Eis ,  Florian Pühler ,  Ludwig Zorn ,  Arne Scholz ,  Philip Lienau ,  Mark Jean Gnoth ,  Ulf Bömer ,  Judith Günther ,  Jörg Fanghänel ,  Daniel Korr

IPC: C07D487/04 ,  A61K31/5377 ,  A61K31/5025

CPC classification number: C07D487/04 ,  A61K31/5025 ,  A61K31/5377 ,  C07D519/00

Abstract: The present invention relates to amino imidazopyridazine compounds of general formula (I): in which A, R1, R2, R3 and R4 are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said 10 compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.

Abstract translation: 本发明涉及通式（I）的氨基咪唑并哒嗪化合物：其中A，R 1，R 2，R 3和R 4如权利要求中所定义，涉及制备所述化合物的方法，药物组合物和包含所述10种化合物和 涉及用于制造用于治疗或预防疾病，特别是高增殖和/或血管生成障碍的药物组合物作为唯一试剂或与其它活性成分组合的用途。

公开(公告)号：US07741333B2

公开(公告)日：2010-06-22

申请号：US11766232

申请日：2007-06-21

Applicant: Olaf Prien ,  Knut Eis ,  Wolfgang Schwede ,  Judith Guenther ,  Dieter Zopf ,  Dominic E. A. Brittain

Inventor： Olaf Prien ,  Knut Eis ,  Wolfgang Schwede ,  Judith Guenther ,  Dieter Zopf ,  Dominic E. A. Brittain

IPC: A61K31/505 ,  C07D239/00 ,  C07D471/00 ,  C07D487/00 ,  C07D491/00

CPC classification number: C07D513/04 ,  C07D239/70 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04

Abstract: The present invention relates to a quinazoline derivative having the general formula (A): in which R1, R2, X, Y and Z are indicated in the description and the claims, the use of the compounds of the general formula (A) for the treatment of various disorders, and the preparation of compounds of the general formula (A).

Abstract translation: 本发明涉及具有通式（A）的喹唑啉衍生物：其中R1，R2，X，Y和Z在说明书和权利要求中表示，通式（A）的化合物用于 各种病症的治疗，以及通式（A）的化合物的制备。

公开(公告)号：US20060223833A1

公开(公告)日：2006-10-05

申请号：US11345666

申请日：2006-02-02

Applicant: Volker Schulze ,  Knut Eis ,  Lars Wortmann ,  Dirk Kosemund ,  Olaf Prien ,  Gerhard Siemeister ,  Holger Hess-Stumpp ,  Uwe Eberspaecher ,  Damian Arnaiz

Inventor： Volker Schulze ,  Knut Eis ,  Lars Wortmann ,  Dirk Kosemund ,  Olaf Prien ,  Gerhard Siemeister ,  Holger Hess-Stumpp ,  Uwe Eberspaecher ,  Damian Arnaiz

IPC: A61K31/506 ,  A61K31/4709 ,  A61K31/4439 ,  A61K31/427 ,  C07D417/02

CPC classification number: C07D277/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

Abstract: The invention relates to thiazolidinones of general formula (I) their production and use as inhibitors of polo-like kinases (Plk) for treating various diseases.

公开(公告)号：US20150038485A1

公开(公告)日：2015-02-05

申请号：US14129043

申请日：2012-06-21

Applicant: Knut Eis ,  Florian Pühler ,  Ludwig Zorn ,  Arne Scholz ,  Philip Lienau ,  Mark Jean Gnoth ,  Ulf Bömer ,  Judith Günther ,  Jörg Fanghänel ,  Daniel Korr

Inventor： Knut Eis ,  Florian Pühler ,  Ludwig Zorn ,  Arne Scholz ,  Philip Lienau ,  Mark Jean Gnoth ,  Ulf Bömer ,  Judith Günther ,  Jörg Fanghänel ,  Daniel Korr

IPC: C07D487/04

CPC classification number: C07D487/04

Abstract: The present invention relates to heterocyclyl aminoimidazopyridazine compounds of general formula (I): in which A, R1, R2, R3 and R4 are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.

Abstract translation: 本发明涉及通式（I）的杂环基氨基咪唑并哒嗪化合物：其中A，R1，R2，R3和R4如权利要求中所定义，涉及制备所述化合物的方法，药物组合物和包含所述化合物的组合， 所述化合物用于制备用于治疗或预防疾病，特别是高增殖和/或血管生成障碍的药物组合物作为唯一试剂或与其它活性成分组合的用途。