公开(公告)号：US20080171747A1

公开(公告)日：2008-07-17

申请号：US11941463

申请日：2007-11-16

Applicant: Matthias Hoffman ,  Matthias Grauert ,  Trixi Brandl ,  Steffen Breitfelder ,  Christian Eickmeier ,  Martin Steegmaier ,  Gisela Schnapp ,  Anke Baum ,  Jens Juergen Quant ,  Flavio Solca ,  Florian Colbatzky

Inventor： Matthias Hoffman ,  Matthias Grauert ,  Trixi Brandl ,  Steffen Breitfelder ,  Christian Eickmeier ,  Martin Steegmaier ,  Gisela Schnapp ,  Anke Baum ,  Jens Juergen Quant ,  Flavio Solca ,  Florian Colbatzky

IPC: A61K31/525 ,  C07D475/02

CPC classification number: C07D295/073 ,  C07D475/00

Abstract: Disclosed are new dihydropteridinones of general formula (I) wherein the groups L and R1-R5 have the meanings given in the claims and specification, the isomers thereof, intermediates and processes for preparing these dihydropteridinones and the use thereof as pharmaceutical compositions.

Abstract translation: 公开了通式（I）的新的二氢蝶啶酮，其中基团L和R 1 -R 5具有权利要求和说明书中给出的含义，其异构体，中间体和 制备这些二氢蝶啶酮的方法及其作为药物组合物的用途。

公开(公告)号：US20060148800A1

公开(公告)日：2006-07-06

申请号：US11206703

申请日：2005-08-17

Applicant: Heinz Stadtmueller ,  Harald Engelhardt ,  Martin Steegmaier ,  Anke Baum ,  Ulrich Guertler ,  Andreas Schoop ,  Jen Quant ,  Flavio Solca ,  Rudolf Hauptmann ,  Ulrich Reiser ,  Stephan Zahn ,  Lars Herfurth

Inventor： Heinz Stadtmueller ,  Harald Engelhardt ,  Martin Steegmaier ,  Anke Baum ,  Ulrich Guertler ,  Andreas Schoop ,  Jen Quant ,  Flavio Solca ,  Rudolf Hauptmann ,  Ulrich Reiser ,  Stephan Zahn ,  Lars Herfurth

IPC: A61K31/53

CPC classification number: C07D239/42 ,  C07D239/48 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D453/02 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08 ,  C07D491/08 ,  C07D491/10

Abstract: The present invention encompasses compounds of general formula (1), wherein A, W, X, Y, Z, Ra, Rb, Rc, R1 and R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.

公开(公告)号：US20060100254A1

公开(公告)日：2006-05-11

申请号：US11243796

申请日：2005-10-05

Applicant: Bodo Betzemeier ,  Trixi Brandl ,  Steffen Breitfelder ,  Ralph Brueckner ,  Thomas Gerstberger ,  Michael Gmachl ,  Matthias Grauert ,  Frank Hilberg ,  Christoph Hoenke ,  Matthias Hoffmann ,  Maria Impagnatiello ,  Dirk Kessler ,  Christian Klein ,  Bernd Krist ,  Udo Maier ,  Darryl McConnell ,  Charlotte Reither ,  Stefan Scheuerer ,  Andreas Schoop ,  Norbert Schweifer ,  Oliver Simon ,  Martin Steegmaier ,  Steffen Steurer ,  Irene Waizenegger ,  Ulrike Weyer-Czernilofsky ,  Andreas Zoephel

Inventor： Bodo Betzemeier ,  Trixi Brandl ,  Steffen Breitfelder ,  Ralph Brueckner ,  Thomas Gerstberger ,  Michael Gmachl ,  Matthias Grauert ,  Frank Hilberg ,  Christoph Hoenke ,  Matthias Hoffmann ,  Maria Impagnatiello ,  Dirk Kessler ,  Christian Klein ,  Bernd Krist ,  Udo Maier ,  Darryl McConnell ,  Charlotte Reither ,  Stefan Scheuerer ,  Andreas Schoop ,  Norbert Schweifer ,  Oliver Simon ,  Martin Steegmaier ,  Steffen Steurer ,  Irene Waizenegger ,  Ulrike Weyer-Czernilofsky ,  Andreas Zoephel

IPC: A61K31/429 ,  C07D513/02

CPC classification number: C07D513/04 ,  C07D277/84

Abstract: The present invention encompasses compounds of the general formula (1) in which R1 to R3 are defined as in Claim 1, which are suitable for treating diseases which are characterized by excessive or anomalous cell proliferation, and their use for producing a pharmaceutical having the abovementioned properties.

Abstract translation: 本发明包括通式（1）的化合物，其中R 1至R 3定义如权利要求1，其适用于治疗以下特征的疾病： 过度或异常细胞增殖，以及它们用于制备具有上述性质的药物。

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：US20060052383A1

公开(公告)日：2006-03-09

申请号：US11210951

申请日：2005-08-24

Applicant: Matthias Grauert ,  Matthias Hoffmann ,  Martin Steegmaier ,  Christian Eickmeier ,  Gisela Schnapp ,  Norbert Redemann ,  Flavio Solca ,  Jens Quant

Inventor： Matthias Grauert ,  Matthias Hoffmann ,  Martin Steegmaier ,  Christian Eickmeier ,  Gisela Schnapp ,  Norbert Redemann ,  Flavio Solca ,  Jens Quant

IPC: A61K31/525 ,  C07D475/02

CPC classification number: C07D487/04 ,  C07D475/00 ,  Y02P20/55

Abstract: Disclosed are new dihydropteridinones of general formula (I) whereby the groups L, R1, R2, R3, R4 and R5 have the meanings given in the claims and specification, the isomers thereof, processes for preparing these dihydropteridinones and their use as pharmaceutical compositions.

Abstract translation: 公开了通式（I）的新的二氢蝶啶酮，

公开(公告)号：US20050261295A1

公开(公告)日：2005-11-24

申请号：US11132091

申请日：2005-05-18

Applicant: Heinz Stadtmueller ,  Harald Engelhardt ,  Ulrich Reiser ,  Stephan Zahn ,  Rudolf Hauptmann ,  Martin Steegmaier ,  Ulrich Guertler ,  Matthias Hoffmann ,  Matthias Grauert

Inventor： Heinz Stadtmueller ,  Harald Engelhardt ,  Ulrich Reiser ,  Stephan Zahn ,  Rudolf Hauptmann ,  Martin Steegmaier ,  Ulrich Guertler ,  Matthias Hoffmann ,  Matthias Grauert

IPC: C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D253/08 ,  A61K31/506 ,  A61K31/53 ,  C07D43/02

CPC classification number: C07D239/48 ,  C07D401/12 ,  C07D403/12

Abstract: The present invention comprises compounds of general formula (1) wherein A, X, Y, Z, Ra, Rb, Rc, R1, R2 and R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or anomalous cell proliferation, and the use thereof for preparing a pharmaceutical composition with the above-mentioned properties.

Abstract translation: 本发明包括通式（1）的化合物，其中A，X，Y，Z，R a，O，R b，R c， R 1，R 2和R 3定义如权利要求1所述，其适用于治疗以过度或异常细胞为特征的疾病 增殖及其用于制备具有上述性质的药物组合物的用途。

公开(公告)号：US08591895B2

公开(公告)日：2013-11-26

申请号：US13342507

申请日：2012-01-03

Applicant: Gerd Munzert ,  Martin Steegmaier ,  Anke Baum

Inventor： Gerd Munzert ,  Martin Steegmaier ,  Anke Baum

IPC: A61K39/395 ,  A61K33/24 ,  A61K31/535 ,  A01N43/50 ,  A01N43/00

CPC classification number: A61K31/4985 ,  A61K31/435 ,  A61K31/4409 ,  A61K31/519

Abstract: Disclosed are pharmaceutical compositions for the treatment of diseases which involve cell proliferation. Also disclosed are methods for the treatment of said diseases, comprising co-administration of a compound 1 of Formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings given herein and of an effective amount of an active compound 2 and/or co-treatment with radiation therapy, in a ratio which provides an additive and synergistic effect, and to the combined use of a compound 1 of Formula (I) and of an effective amount of an active compound 2 and/or radiotherapy for the manufacture of corresponding pharmaceutical combination preparations.

Abstract translation: 公开了用于治疗涉及细胞增殖的疾病的药物组合物。 还公开了治疗所述疾病的方法，包括共同给予式（I）的化合物1，其中基团L，R 1，R 2，R 3，R 4和R 5具有本文给出的含义和有效量的 活性化合物2和/或以放射疗法共同治疗，以提供添加剂和协同效应的比例，以及组合使用式（I）化合物1和有效量的活性化合物2和/ 或放射治疗用于制造相应的药物组合制剂。

公开(公告)号：US08420630B2

公开(公告)日：2013-04-16

申请号：US12711364

申请日：2010-02-24

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

IPC: C07D239/48 ,  C07D403/12 ,  C07D401/12 ,  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 characterized 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: 本发明涉及式（I）的三取代嘧啶，其中0Ra至Re如权利要求1所定义，其适用于治疗以细胞增殖过度或异常为特征的疾病，其用于制备具有上述药物组合物的用途 性质及其制备方法。

公开(公告)号：US08003786B2

公开(公告)日：2011-08-23

申请号：US12873687

申请日：2010-09-01

Applicant: Matthias Hoffmann ,  Matthias Grauert ,  Martin Steegmaier ,  Anke Baum ,  Jens Juergen Quant ,  Flavio Solca ,  Florian Colbatzky ,  Gisela Schnapp

Inventor： Matthias Hoffmann ,  Matthias Grauert ,  Martin Steegmaier ,  Anke Baum ,  Jens Juergen Quant ,  Flavio Solca ,  Florian Colbatzky ,  Gisela Schnapp

IPC: C07D475/00

CPC classification number: C07D295/073 ,  C07D475/00

Abstract: Disclosed are new dihydropteridinones of general formula (I) wherein the groups L and R1-R5 have the meanings given in the claims and specification, the isomers thereof, intermediates and processes for preparing these dihydropteridinones and the use thereof as pharmaceutical compositions.

Abstract translation: 公开了通式（I）的新的二氢蝶啶酮，其中基团L和R 1 -R 5具有权利要求书和说明书中给出的含义，其异构体，制备这些二氢蝶啶烷的中间体和方法及其作为药物组合物的用途。

公开(公告)号：US20100240657A1

公开(公告)日：2010-09-23

申请号：US12665776

申请日：2008-07-01

Applicant: Ioannis Sapountzis ,  Peter Ettmayer ,  Christian Klein ,  Andreas Mantoulidis ,  Martin Steegmaier ,  Steffen Steurer ,  Irene Waizenegger

Inventor： Ioannis Sapountzis ,  Peter Ettmayer ,  Christian Klein ,  Andreas Mantoulidis ,  Martin Steegmaier ,  Steffen Steurer ,  Irene Waizenegger

IPC: A61K31/5377 ,  C07C63/64 ,  A61K31/192 ,  C07D401/04 ,  A61K31/4439 ,  C07D277/22 ,  A61K31/427 ,  C07D263/32 ,  A61K31/422 ,  C07D249/06 ,  A61K31/4196 ,  C07D403/04 ,  A61K31/506 ,  C07D471/04 ,  A61K31/437 ,  C07C307/02 ,  A61K31/18 ,  C07D413/14 ,  A61K31/497 ,  C07C69/78 ,  A61K31/235 ,  A61P35/00 ,  A61P29/00 ,  A61P37/00

CPC classification number: C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D413/14 ,  C07D417/04

Abstract: The present invention encompasses compounds of general formula (1) wherein the groups R2 to R4, L, Q and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition with the above-mentioned properties.

Abstract translation: 本发明包括通式（1）的化合物，其中R 2至R 4，L，Q和n基团如权利要求1中所定义，其适用于治疗以细胞增殖过度或异常为特征的疾病， 制备具有上述性质的药物组合物。