公开(公告)号：US08193188B2

公开(公告)日：2012-06-05

申请号：US12578737

申请日：2009-10-14

Applicant: Matthias Hoffmann ,  Matthias Grauert ,  Trixi Brandl ,  Martin Steegmaier ,  Rudolf Hauptmann

Inventor： Matthias Hoffmann ,  Matthias Grauert ,  Trixi Brandl ,  Martin Steegmaier ,  Rudolf Hauptmann

IPC: A01N43/58 ,  A01N43/60 ,  A61K31/50 ,  A61K31/495

CPC classification number: C07D471/04

Abstract: Disclosed are pyridodihydropyrazinone compounds, processes for preparing them and their use as pharmaceutical compositions. The compounds according to the invention correspond to general formula (I), while the groups L, R1, R2, R3, R4 and R5 may have the meanings given in the claims and specification.

Abstract translation: 公开了吡啶二氢吡嗪酮化合物，其制备方法及其作为药物组合物的用途。 根据本发明的化合物对应于通式（I），而基团L，R 1，R 2，R 3，R 4和R 5可以具有权利要求和说明书中给出的含义。

公开(公告)号：US08058270B2

公开(公告)日：2011-11-15

申请号：US12120740

申请日：2008-05-15

Applicant: Gerd Munzert ,  Martin Steegmaier

Inventor： Gerd Munzert ,  Martin Steegmaier

IPC: A61K31/54 ,  A61K31/535 ,  A01N43/58 ,  C07D417/00

CPC classification number: A61K31/525 ,  A61K31/5377

Abstract: Disclosed is the use of a compound of general Formula (1), optionally in form of its tautomers, racemates, enantiomers, diastereomers and the mixtures thereof and optionally in form of the pharmacologically acceptable acid addition salts, solvates, hydrates, polymorphs, physiologically functional derivatives or prodrugs thereof, for the preparation of a pharmaceutical composition for the treatment of diseases characterized by abnormal cell proliferation in a human or non-human mammalian body by inhibition of polo like kinases as mitotic regulators.

Abstract translation: 公开了通式（1）的化合物，任选以其互变异构体，外消旋体，对映异构体，非对映体及其混合物的形式的用途，并且任选呈药理学上可接受的酸加成盐，溶剂化物，水合物，多晶型物，生理功能 衍生物或前体药物，用于通过抑制作为有丝分裂调节剂的马球状激酶来制备用于治疗特征在于人或非人哺乳动物体内异常细胞增殖的疾病的药物组合物。

公开(公告)号：US20100324288A1

公开(公告)日：2010-12-23

申请号：US12873687

申请日：2010-09-01

Applicant: Matthias HOFFMANN ,  Matthias GRAUERT ,  Martin STEEGMAIER ,  Gisela SCHNAPP ,  Anke BAUM ,  Jens Juergen QUANT ,  Flavio SOLCA ,  Florian COLBATZKY

Inventor： Matthias HOFFMANN ,  Matthias GRAUERT ,  Martin STEEGMAIER ,  Gisela SCHNAPP ,  Anke BAUM ,  Jens Juergen QUANT ,  Flavio SOLCA ,  Florian COLBATZKY

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：US20100152167A1

公开(公告)日：2010-06-17

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: A61K31/505 ,  C07D239/50 ,  C07D413/12 ,  A61K31/5377 ,  A61K31/506 ,  C07D403/04 ,  A61K31/55 ,  C07D403/12 ,  A61K31/551 ,  A61P31/00 ,  A61P35/00 ,  A61P9/00 ,  A61P19/08

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) wherein0Ra 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：US07521457B2

公开(公告)日：2009-04-21

申请号：US11206703

申请日：2005-08-17

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

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

IPC: C07D239/42 ,  C07D239/46 ,  A61K31/505 ,  A61K31/506 ,  A61P35/00

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.

Abstract translation: 本发明包括通式（1）的化合物，其中A，W，X，Y，Z，Ra，Rb，Rc，R 1和R 3如权利要求1中所定义，其适用于治疗以过量 或异常细胞增殖，以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：US07371753B2

公开(公告)日：2008-05-13

申请号：US11211783

申请日：2005-08-25

Applicant: Heinz Stadtmueller ,  Harald Engelhardt ,  Andreas Schoop ,  Martin Steegmaier ,  Matthias Hoffmann ,  Matthias Grauert

Inventor： Heinz Stadtmueller ,  Harald Engelhardt ,  Andreas Schoop ,  Martin Steegmaier ,  Matthias Hoffmann ,  Matthias Grauert

IPC: A61K31/5025 ,  A61K31/496 ,  A61K31/551 ,  A61K31/5355 ,  C07D237/20 ,  C07D237/22 ,  C07D239/10 ,  C07D241/18 ,  C07D243/08 ,  C07D413/12 ,  A61P35/00 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D211/74 ,  C07D211/72 ,  C07D211/84 ,  C07D211/86 ,  C07D213/73 ,  C07D213/76 ,  C07D213/22

CPC classification number: C07D475/04

Abstract: Disclosed are new dihydropteridinones of general formula (I) wherein the groups R1 to R5, Ra to Rc, W, Q1 and Q2 have the meanings given in the claims and specification, the isomers thereof and the use thereof for preparing a pharmaceutical composition for the treatment of diseases characterised by excessive or abnormal cell proliferation.

Abstract translation: 公开了通式（I）的新的二氢蝶啶酮，其中基团R 1至R 5，R a至R c， SUP，W，Q 1和Q 2具有权利要求书和说明书中给出的含义，其异构体及其用于制备治疗药物组合物的用途 以细胞增殖过度或异常为特征的疾病。

公开(公告)号：US07241769B2

公开(公告)日：2007-07-10

申请号：US11132091

申请日：2005-05-18

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

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

IPC: C07D239/42 ,  C07D239/46 ,  A61K31/505 ,  A61P35/00

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：US20060046990A1

公开(公告)日：2006-03-02

申请号：US11211783

申请日：2005-08-25

Applicant: Heinz Stadtmueller ,  Harald Engelhardt ,  Andreas Schoop ,  Martin Steegmaier ,  Matthias Hoffmann ,  Matthias Grauert

Inventor： Heinz Stadtmueller ,  Harald Engelhardt ,  Andreas Schoop ,  Martin Steegmaier ,  Matthias Hoffmann ,  Matthias Grauert

IPC: A61K31/525 ,  C07D475/04

CPC classification number: C07D475/04

Abstract: Disclosed are new dihydropteridinones of general formula (I) wherein the groups R1 to R5, Ra to Rc, W, Q1 and Q2 have the meanings given in the claims and specification, the isomers thereof and the use thereof for preparing a pharmaceutical composition for the treatment of diseases characterised by excessive or abnormal cell proliferation.

Abstract translation: 公开了通式（I）的新的二氢蝶啶酮，其中基团R 1至R 5，R a至R c， SUP，W，Q 1和Q 2具有权利要求书和说明书中给出的含义，其异构体及其用于制备治疗药物组合物的用途 以细胞增殖过度或异常为特征的疾病。

公开(公告)号：US20060009457A1

公开(公告)日：2006-01-12

申请号：US11176737

申请日：2005-07-07

Applicant: Matthias Hoffmann ,  Matthias Grauert ,  Trixi Brandl ,  Martin Steegmaier ,  Rudolf Hauptmann

Inventor： Matthias Hoffmann ,  Matthias Grauert ,  Trixi Brandl ,  Martin Steegmaier ,  Rudolf Hauptmann

IPC: A61K31/498 ,  C07D487/02

CPC classification number: C07D471/04

Abstract: Disclosed are pyridodihydropyrazinone compounds, processes for preparing them and their use as pharmaceutical compositions. The compounds according to the invention correspond to general formula (I), while the groups L, R1, R2, R3, R4 and R5 may have the meanings given in the claims and specification.

Abstract translation: 公开了吡啶二氢吡嗪酮化合物，其制备方法及其作为药物组合物的用途。 根据本发明的化合物对应于通式（I），而基团L，R 1，R 2，R 3，R “4”和“5”可以具有权利要求书和说明书中给出的含义。

公开(公告)号：US20050014761A1

公开(公告)日：2005-01-20

申请号：US10909008

申请日：2004-07-30

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

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

IPC: A61P35/00 ,  C07D475/00 ,  C07D519/00 ,  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具有权利要求书和说明书中给出的含义，其异构体，制备这些二氢蝶呤的中间体和方法及其用途 药物组合物。