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1.发明授权公开(公告)号：US08754079B2
公开(公告)日：2014-06-17
申请号：US13034855
申请日：2011-02-25
申请人： Thorsten Lehmann-Lintz , Armin Heckel , Joerg Kley , Elke Langkopf , Norbert Redemann , Achim Sauer , Leo Thomas , Dieter Wiedenmayer , Matthias Austen , John Danilewicz , Martin Schneider , Kay Schreiter , Phillip Black , Wesley Blackaby , Ian Linney
发明人： Thorsten Lehmann-Lintz , Armin Heckel , Joerg Kley , Elke Langkopf , Norbert Redemann , Achim Sauer , Leo Thomas , Dieter Wiedenmayer , Matthias Austen , John Danilewicz , Martin Schneider , Kay Schreiter , Phillip Black , Wesley Blackaby , Ian Linney
IPC分类号： C07D495/04 , A61K31/519 , A61K31/496 , A61K31/5355 , C07D413/12 , A61P25/28 , A61P29/00 , A61P35/00
CPC分类号： C07D495/04
摘要： The present invention relates to novel thienopyrimidine compounds of general formula pharmaceutical compositions comprising these compounds and their therapeutic use for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.
摘要翻译： 本发明涉及包含这些化合物的通式药物组合物的新型噻吩并嘧啶化合物及其用于预防和/或治疗可受到抑制Mnk1和/或Mnk2（Mnk2a或Mnk2b的激酶活性）的疾病的治疗用途 ）和/或其变体。
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2.发明授权Thienopyrimidines containing a substituted alkyl group for pharmaceutical compositions 有权含有用于药物组合物的取代烷基的噻吩并嘧啶公开(公告)号：US08853193B2
公开(公告)日：2014-10-07
申请号：US13035023
申请日：2011-02-25
申请人： Armin Heckel , Frank Himmelsbach , Joerg Kley , Thorsten Lehmann-Lintz , Norbert Redemann , Achim Sauer , Leo Thomas , Dieter Wiedenmayer , Phillip Black , Wesley Blackaby , Ian Linney , Matthias Austen , John Danilewicz , Martin Schneider , Kay Schreiter
发明人： Armin Heckel , Frank Himmelsbach , Joerg Kley , Thorsten Lehmann-Lintz , Norbert Redemann , Achim Sauer , Leo Thomas , Dieter Wiedenmayer , Phillip Black , Wesley Blackaby , Ian Linney , Matthias Austen , John Danilewicz , Martin Schneider , Kay Schreiter
IPC分类号： C07D495/04 , A61K31/519 , A61K31/5377 , A61K31/56 , A61P29/00 , A61P35/00 , A61P25/28 , A61P13/12 , A61K31/395
CPC分类号： C07D495/04
摘要： The present invention relates to novel thienopyrimidine compounds of general formula pharmaceutical compositions comprising these compounds and their therapeutic use for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.
摘要翻译： 本发明涉及包含这些化合物的通式药物组合物的新型噻吩并嘧啶化合物及其用于预防和/或治疗可受到抑制Mnk1和/或Mnk2（Mnk2a或Mnk2b的激酶活性）的疾病的治疗用途 ）和/或其变体。
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3.发明授权Heterocycloalkyl-containing thienopyrimidines for pharmaceutical compositions 有权用于药物组合物的含杂环烷基的噻吩并嘧啶公开(公告)号：US08648068B2
公开(公告)日：2014-02-11
申请号：US13034913
申请日：2011-02-25
申请人： Thorsten Lehmann-Lintz , Joerg Kley , Norbert Redemann , Achim Sauer , Leo Thomas , Dieter Wiedenmayer , Matthias Austen , John Danilewicz , Martin Schneider , Kay Schreiter , Phillip Black , Wesley Blackaby , Ian Linney
发明人： Thorsten Lehmann-Lintz , Joerg Kley , Norbert Redemann , Achim Sauer , Leo Thomas , Dieter Wiedenmayer , Matthias Austen , John Danilewicz , Martin Schneider , Kay Schreiter , Phillip Black , Wesley Blackaby , Ian Linney
IPC分类号： C07D495/04 , A61K31/519 , A61K31/5355 , A61P35/00 , A61P25/28 , A61P3/10
CPC分类号： C07D495/04 , C07D519/00
摘要： The present invention relates to novel pharmaceutical compositions comprising thienopyrimidine compounds. Moreover, the present invention relates to the use of the thienopyrimidine compounds of the invention for the production of pharmaceutical compositions for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.
摘要翻译： 本发明涉及包含噻吩并嘧啶化合物的新型药物组合物。 此外，本发明涉及本发明的噻吩并嘧啶化合物用于生产药物组合物用于预防和/或治疗可受到抑制Mnk1和/或Mnk2（Mnk2a）激酶活性的疾病的用途 或Mnk2b）和/或其变体。
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![HALOGEN OR CYANO SUBSTITUTED THIENO [2,3-D]PYRIMIDINES HAVING MNK1/MNK2 INHIBITING ACTIVITY FOR PHARMACEUTICAL COMPOSITIONS](/abs-image/US/2013/03/14/US20130065914A1/abs.jpg.150x150.jpg)
4.发明申请HALOGEN OR CYANO SUBSTITUTED THIENO [2,3-D]PYRIMIDINES HAVING MNK1/MNK2 INHIBITING ACTIVITY FOR PHARMACEUTICAL COMPOSITIONS 审中-公开取代三氮唑[2,3-D]具有MNK1 / MNK2抑制活性的药物组合物的吡嗪公开(公告)号：US20130065914A1
公开(公告)日：2013-03-14
申请号：US13580184
申请日：2011-02-25
申请人： Armin Heckel , Frank Himmelsbach , Thorsten Lehmann-Lintz , Norbert Redemann , Achim Sauer , Leo Thomas , Phillip Black , Wesley Blackaby , John Danilewicz , Ian Linney , Matthias Austen , Martin Schneider , Kay Schreiter
发明人： Armin Heckel , Frank Himmelsbach , Thorsten Lehmann-Lintz , Norbert Redemann , Achim Sauer , Leo Thomas , Phillip Black , Wesley Blackaby , John Danilewicz , Ian Linney , Matthias Austen , Martin Schneider , Kay Schreiter
IPC分类号： C07D495/04 , A61P3/10 , A61P3/06 , A61P35/00 , A61P7/00 , A61P25/28 , A61P13/12 , A61P29/00 , A61K31/519 , A61P3/00
CPC分类号： C07D495/04 , A61K31/519 , Y02A50/411
摘要： The present invention relates to novel thienopyhmidine compounds of general formula (I), pharmaceutical compositions comprising these compounds and their therapeutic use for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.
摘要翻译： 本发明涉及通式（I）的新型噻吩并嘧啶化合物，包含这些化合物的药物组合物及其用于预防和/或治疗可受到抑制Mnk1和/或Mnk2的激酶活性的疾病的治疗用途 （Mnk2a或Mnk2b）和/或其变体。
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5.发明授权2-benzylaminodihydropteridinones, process for their manufacture and use thereof as medicaments 有权2-苄基氨基二氢蝶啶酮，其制备方法和用途作为药物公开(公告)号：US07759347B2
公开(公告)日：2010-07-20
申请号：US12357731
申请日：2009-01-22
申请人： Matthias Hoffmann , Matthias Grauert , Thorsten Lehmann-Lintz , Martin Steegmaier , Flavio Solca , Norbert Redemann
发明人： Matthias Hoffmann , Matthias Grauert , Thorsten Lehmann-Lintz , Martin Steegmaier , Flavio Solca , Norbert Redemann
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495 , C07D475/00
CPC分类号： C07D475/00
摘要： The present invention relates to new 2-benzylaminodihydropteridinones of general formula (I) wherein the groups R1 to R7, R10 and R11 have the meanings given in the claims and specification, the isomers thereof, methods of preparing these dihydropteridinones and their use as medicaments.
摘要翻译： 本发明涉及通式（I）的新的2-苄基氨基二氢蝶啶酮，其中基团R 1至R 7，R 10和R 11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方法及其作为药物的用途。
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6.发明授权Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions 有权二氢蝶啶酮，其制备方法及其作为药物组合物的用途公开(公告)号：US06806272B2
公开(公告)日：2004-10-19
申请号：US10226710
申请日：2002-08-23
申请人： Eckhart Bauer , Steffen Breitfelder , Christian Eickmeier , Matthias Grauert , Matthias Hoffmann , Thorsten Lehmann-Lintz , Gerald Pohl , Jens Quant , Norbert Redemann , Gisela Schnapp , Martin Steegmaier
发明人： Eckhart Bauer , Steffen Breitfelder , Christian Eickmeier , Matthias Grauert , Matthias Hoffmann , Thorsten Lehmann-Lintz , Gerald Pohl , Jens Quant , Norbert Redemann , Gisela Schnapp , Martin Steegmaier
IPC分类号： C07D48704
CPC分类号： C07D487/04 , C07D475/00
摘要： The present invention relates to new dihydropteridinones of the formula (I) wherein the groups X, R1, R2, R3, R4, R5 and R7 have the meanings given in the claims and the specification, the isomers thereof, processes and intermediates for preparing these dihydropteridinones as well as the use thereof as pharmaceutical compositions.
摘要翻译： 本发明涉及式（I）的新的二氢蝶啶酮，其中基团X，R 1，R 2，R 3，R 4，R 5和R 7具有如下含义： 权利要求书和说明书中给出的其异构体，用于制备这些二氢蝶啶烷酮的方法和中间体以及其作为药物组合物的用途。
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7.发明申请2-Benzylaminodihydropteridinones, process for their manufacture and use thereof as medicaments 审中-公开2-苄基氨基二氢蝶啶酮，其制备方法和用作药物公开(公告)号：US20060004014A1
公开(公告)日：2006-01-05
申请号：US11157883
申请日：2005-06-21
申请人： Matthias Hoffmann , Matthias Grauert , Thorsten Lehmann-Lintz , Martin Steegmaier , Flavio Solca , Norbert Redemann
发明人： Matthias Hoffmann , Matthias Grauert , Thorsten Lehmann-Lintz , Martin Steegmaier , Flavio Solca , Norbert Redemann
IPC分类号： A61K31/525 , C07D475/06
CPC分类号： C07D475/00
摘要： The present invention relates to new 2-benzylaminodihydropteridinones of general formula (I) wherein the groups R1 to R7, R10 and R11 have the meanings given in the claims and specification, the isomers thereof, methods of preparing these dihydropteridinones and their use as medicaments.
摘要翻译： 本发明涉及通式（I）的新的2-苄基氨基二氢蝶啶酮，其中基团R 1至R 7，R 10和R 10， SUP> 11 具有权利要求书和说明书中给出的含义，其异构体，制备这些二氢蝶啶酮的方法及其作为药物的用途。
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公开(公告)号：US06545035B1
公开(公告)日：2003-04-08
申请号：US09969912
申请日：2001-10-03
IPC分类号： A61K314035
CPC分类号： C07D209/30 , C07D209/34
摘要： Substituted indolinones of general formula having effect on various kinases and cycline/CDK complexes and on the proliferation of various tumour cells. Exemplary compounds are: 3-Z-[1-(4-(N-Benzyl-N-methyl-aminomethyl)-phenylamino)-1-methyl-methylene]-5-amido-2-indolinone and 3-Z-[1-(4-(2,3,4,5-Tetrahydro-benzo(d)azepin-3-yl-methyl)-phenylamino)-1-methyl-methylene]-5-amido-2-indolinone.
摘要翻译： 通用结构式取代的吲哚酮对各种激酶和cyclin / CDK复合物的影响以及各种肿瘤细胞的增殖。 示例性化合物是：3-Z- [1-（4-（N-苄基-N-甲基 - 氨基甲基） - 苯基氨基）-1-甲基 - 亚甲基] -5-酰氨基-2-二氢吲哚酮和3-Z- [1- （4-（2,3,4,5-四氢 - 苯并（d）氮杂-3-基 - 甲基） - 苯基氨基）-1-甲基 - 亚甲基] -5-酰氨基-2-二氢吲哚酮。
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公开(公告)号：US06319918B1
公开(公告)日：2001-11-20
申请号：US09323499
申请日：1999-06-01
IPC分类号： A61K3155
CPC分类号： C07D209/30 , C07D209/34
摘要： Substituted indolinones of general formula having effect on various kinases and cycline/CDK complexes and on the proliferation of various tumour cells. Exemplary compounds are: 3-Z-[1-(4-(N-Benzyl-N-methyl-aminomethyl)-phenylamino)-1-methyl-methylene]-5-amido-2-indolinone and 3-Z-[1-(4-(2,3,4,5-Tetrahydro-benzo(d)azepin-3-yl-methyl)-phenylamino)-1-methyl-methylene]-5-amido-2-indolinone.
摘要翻译： 通用结构式取代的吲哚酮对各种激酶和cyclin / CDK复合物的影响以及各种肿瘤细胞的增殖。 示例性化合物是：3-Z- [1-（4-（N-苄基-N-甲基 - 氨基甲基） - 苯基氨基）-1-甲基 - 亚甲基] -5-酰氨基-2-二氢吲哚酮和3-Z- [1- （4-（2,3,4,5-四氢 - 苯并（d）氮杂-3-基 - 甲基） - 苯基氨基）-1-甲基 - 亚甲基] -5-酰氨基-2-二氢吲哚酮。
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10.发明授权Substituted indolines with an inhibitory effect on various kinases and complexes of CDKs 有权取代的吲哚啉对CDK的各种激酶和复合物具有抑制作用公开(公告)号：US06855710B2
公开(公告)日：2005-02-15
申请号：US10666643
申请日：2003-09-19
申请人： Rainer Walter , Wolfgang Grell , Armin Heckel , Frank Himmelsbach , Wolfgang Eberlein , Gerald Roth , Jacobus C.A. van Meel , Norbert Redemann , Walter Spevak , Ulrike Tontsch-Grunt , Thomas von Rueden
发明人： Rainer Walter , Wolfgang Grell , Armin Heckel , Frank Himmelsbach , Wolfgang Eberlein , Gerald Roth , Jacobus C.A. van Meel , Norbert Redemann , Walter Spevak , Ulrike Tontsch-Grunt , Thomas von Rueden
IPC分类号： C07D401/12 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/4427 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/541 , A61P35/00 , A61P43/00 , C07D20060101 , C07D209/34 , C07D209/36 , C07D209/48 , C07D401/14 , C07D403/12
CPC分类号： C07D401/12 , C07D209/34 , C07D403/12
摘要： The present invention relates to new substituted indolinones of general formula wherein X and R1 to R5 are defined as in claim 1, the isomers and the salts thereof which have valuable properties. The above compounds of general formula I wherein R1 denotes a hydrogen atom, a C1-3-alkyl group or a prodrug group have valuable pharmacological properties, particularly an inhibiting effect on various kinases, on viral cyclin and on receptor tyrosine kinases, and the other compounds of the above general formula I wherein R1 does not represent a hydrogen atom, a C1-3-alkyl group or a prodrug group are valuable intermediate products for the preparation of the abovementioned compounds.
摘要翻译： 本发明涉及新一代的取代的二氢吲哚酮，其通式为R，R 1至R 5如权利要求1所定义，其异构体及其盐具有有价值的性质。上述通式I的化合物，其中R 1表示氢原子， 3-烷基或前药基团具有有价值的药理学性质，特别是对各种激酶，对病毒细胞周期蛋白和受体酪氨酸激酶的抑制作用，以及上述通式I的其它化合物，其中R1不表示氢原子， C1-3烷基或前药基团是用于制备上述化合物的有价值的中间产物。
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