公开(公告)号：US07750152B2

公开(公告)日：2010-07-06

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 Jurgen Quant ,  Flavio Solca ,  Florian Colbatzky

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

IPC: C07D475/00

CPC classification number: C07D295/073 ,  C07D475/00

Abstract: Disclosed are dihydropteridinones of general formula (I) wherein the groups L and R1-R5 have the meanings given in the claims and specification, the pharmaceutical compositions, isomers, intermediates thereof and processes for preparing these dihydropteridinones. The compounds are useful the treatment and/or prevention of cancer, infections, inflammatory and autoimmune diseases.

Abstract translation: 公开了通式（I）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，药物组合物，异构体，中间体和制备这些二氢蝶啶酮的方法。 该化合物可用于治疗和/或预防癌症，感染，炎症和自身免疫性疾病。

公开(公告)号：US07691888B2

公开(公告)日：2010-04-06

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 ,  A61K31/4162 ,  C07D513/02 ,  C07D417/14

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如权利要求1中所定义，其适用于治疗特征为过度或异常细胞增殖的疾病，以及其用于制备具有上述 属性。

公开(公告)号：US20080319192A1

公开(公告)日：2008-12-25

申请号：US12192478

申请日：2008-08-15

Applicant: Matthias GRAUERT ,  Matthias HOFFMANN ,  Martin STEEGMAIER ,  Flavio SOLCA ,  Jens Juergen QUANT

Inventor： Matthias GRAUERT ,  Matthias HOFFMANN ,  Martin STEEGMAIER ,  Flavio SOLCA ,  Jens Juergen QUANT

IPC: C07D487/04

CPC classification number: C07D295/155 ,  C07D487/04 ,  Y02P20/55

Abstract: Disclosed are new dihydropteridinones of the formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings provided herein, the isomers thereof, processes for preparing these dihydropteridinones and their use as pharmaceutical compositions.

Abstract translation: 公开了式（I）的新的二氢蝶啶酮，其中基团L，R 1，R 2，R 3，R 4和R 5具有本文提供的含义，其异构体，制备这些二氢蝶啶烷的方法及其作为药物组合物的用途。

公开(公告)号：US20080293944A1

公开(公告)日：2008-11-27

申请号：US12129728

申请日：2008-05-30

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

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

IPC: C07D241/04

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：US20080182837A1

公开(公告)日：2008-07-31

申请号：US11773508

申请日：2007-07-05

Applicant: Steffen STEURER ,  Peter Ettmayer ,  Andreas Mantoulidis ,  loannis Sapountzis ,  Martin Steegmaier

Inventor： Steffen STEURER ,  Peter Ettmayer ,  Andreas Mantoulidis ,  loannis Sapountzis ,  Martin Steegmaier

IPC: A61K31/397 ,  C07D213/02 ,  A61K31/44 ,  C07D249/04 ,  A61K31/4192 ,  C07D261/06 ,  A61K31/42 ,  C07D277/20 ,  A61P31/00 ,  A61P37/00 ,  A61P29/00 ,  A61P35/00 ,  A61K31/426 ,  A61K31/4164 ,  C07D295/00 ,  A61K31/4523 ,  C07D239/24 ,  A61K31/506

CPC classification number: C07D417/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  C07D413/12 ,  C07D413/14

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 the use thereof for preparing a medicament having the above-mentioned properties.

Abstract translation: 本发明包括通式（1）的化合物，其中基团R 2至R 4，L，Q和n如权利要求1中所定义，其适用于 以细胞增殖过度或异常为特征的疾病的治疗及其制备具有上述特性的药物的用途。

公开(公告)号：US07332491B2

公开(公告)日：2008-02-19

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 Juergen Quant

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

IPC: A61K31/541 ,  A61K31/5025 ,  A61K31/4985 ,  C07D273/01 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D475/12 ,  A61P19/02

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，其中基团L，R 1，R 2，R 3，R 4， ＆lt; 5＆gt;和＆lt; 5＆gt;具有权利要求书和说明书中给出的含义，其异构体，制备这些二氢蝶啶的方法及其作为药物组合物的用途。

公开(公告)号：US20070207999A1

公开(公告)日：2007-09-06

申请号：US11675936

申请日：2007-02-16

Applicant: Heinz Stadtmueller ,  Anke Baum ,  Guido Boehmelt ,  Harald Engelhardt ,  Jens Quant ,  Flavio Solca ,  Martin Steegmaier ,  Stephan Zahn

Inventor： Heinz Stadtmueller ,  Anke Baum ,  Guido Boehmelt ,  Harald Engelhardt ,  Jens Quant ,  Flavio Solca ,  Martin Steegmaier ,  Stephan Zahn

IPC: A61K31/55 ,  A61K31/553 ,  C07D403/02 ,  C07D413/02

CPC classification number: C07D498/04 ,  C07D403/12 ,  C07D413/12 ,  C07D487/04

Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R6, X and Y are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or anomalous cell proliferation, as well as the use thereof for preparing a pharmaceutical composition with the above-mentioned properties.

Abstract translation: 本发明包括其中R 1至R 6的通式（1）的化合物，X和Y如权利要求1中所定义，其适用于治疗疾病 其特征在于过度或异常的细胞增殖，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：US07241889B2

公开(公告)日：2007-07-10

申请号：US11179234

申请日：2005-07-12

Applicant: Matthias Hoffmann ,  Matthias Grauert ,  Martin Steegmaier ,  Flavio Solca

Inventor： Matthias Hoffmann ,  Matthias Grauert ,  Martin Steegmaier ,  Flavio Solca

IPC: C07D237/00 ,  C07D239/00 ,  C07D241/00 ,  C07D475/00 ,  A01N43/58 ,  A01N43/60 ,  A61K31/50 ,  A61K31/495

CPC classification number: C07D475/00

Abstract: Disclosed are 6-formyl-tetrahydropteridines of the formula (I) wherein the groups R1 to R6 have the meanings given in the claims and specification, the isomers thereof, methods of preparing these 6-formyl-tetrahydropteridines and their use as medicaments.

Abstract translation: 公开了式（I）的6-甲酰基 - 四氢喋啶，其中基团R 1至R 6具有权利要求书和说明书中给出的含义，其异构体，方法 制备这些6-甲酰基 - 四氢喋啶及其作为药物的用途。

公开(公告)号：US20060047118A1

公开(公告)日：2006-03-02

申请号：US11211048

申请日：2005-08-24

Applicant: Heinz Stadtmueller ,  Harald Engelhardt ,  Andreas Schoop ,  Martin Steegmaier

Inventor： Heinz Stadtmueller ,  Harald Engelhardt ,  Andreas Schoop ,  Martin Steegmaier

IPC: C07D487/02 ,  C07D475/02

CPC classification number: C07D471/04 ,  C07D487/04

Abstract: Disclosed compounds of general formula (1) wherein L, Q1, Q2, X, Y, Ra, Rb, Rc, R1, R2, R3 and R4 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 with the above-mentioned properties.

Abstract translation: 公开的通式（1）的化合物，其中L，Q 1，Q 2，X，Y，R a，R b， R 1，R 2，R 2，R 3，R 4和R 4， 如权利要求1中所定义的，其适用于治疗以细胞增殖过度或异常为特征的疾病，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：US20060025411A1

公开(公告)日：2006-02-02

申请号：US11219945

申请日：2005-09-06

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

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

IPC: A61K31/5377 ,  C07D475/02 ,  A61K31/525

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。