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公开(公告)号：US08912189B2
公开(公告)日：2014-12-16
申请号：US13439107
申请日：2012-04-04
Applicant: Matthias Gerlach , Irene Seipelt , Lars Blumenstein , Gilbert Mueller , Eckhard Guenther , Tilmann Schuster , Michael Teifel
Inventor： Matthias Gerlach , Irene Seipelt , Lars Blumenstein , Gilbert Mueller , Eckhard Guenther , Tilmann Schuster , Michael Teifel
IPC: A61K31/4985 , C07D471/04 , A61K31/501 , A61K31/5377
CPC classification number: A61K31/4985 , A61K31/501 , A61K31/5377 , C07D471/04
Abstract: The present invention provides new pyridopyrazine compounds of Formula (I) which are suitable for the treatment or prevention of physiological and/or pathophysiological states mediated and/or modulated by signal transduction pathways and/or enzymes in mammals and in particular in humans.
Abstract translation: 本发明提供了新的式（I）吡啶并吡嗪化合物，其适用于治疗或预防由哺乳动物，特别是人类中的信号转导途径和/或酶介导和/或调节的生理和/或病理生理状态。
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![Substituted pyrido[2,3-b]pyrazine compounds as modulators of tyrosine kinases](/abs-image/US/2012/06/19/US08202883B2/abs.jpg.150x150.jpg)
2.发明授权Substituted pyrido[2,3-b]pyrazine compounds as modulators of tyrosine kinases 失效取代的吡啶并[2,3-b]吡嗪化合物作为酪氨酸激酶的调节剂公开(公告)号：US08202883B2
公开(公告)日：2012-06-19
申请号：US12117942
申请日：2008-05-09
Applicant: Matthias Gerlach , Irene Seipelt , Eckhard Guenther , Emmanuel Polymeropoulos , Tilmann Schuster , Eckhard Claus
Inventor： Matthias Gerlach , Irene Seipelt , Eckhard Guenther , Emmanuel Polymeropoulos , Tilmann Schuster , Eckhard Claus
IPC: A61K31/44
CPC classification number: C07D471/04
Abstract: The invention relates to pyrido[2,3-b]pyrazine compounds of formulae (Ia) and (Ib) which have activity to the modulation of misdirected cellular signal transduction processes such as tyrosine kinases, serine/threonine kinases and/or lipid kinases, their preparation and use as medicaments, especially for the treatment of malignant disorders and other disorders based on pathological cell proliferations:
Abstract translation: 本发明涉及式（Ia）和（Ib）的吡啶并[2,3-b]吡嗪化合物，其具有调节错误定向的细胞信号转导过程如酪氨酸激酶，丝氨酸/苏氨酸激酶和/或脂质激酶的活性， 它们作为药物的制备和用途，特别是用于治疗基于病理性细胞增殖的恶性疾病和其它病症：
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3.发明授权公开(公告)号：US08148546B2
公开(公告)日：2012-04-03
申请号：US12109479
申请日：2008-04-25
Applicant: Tilmann Schuster , Klaus Paulini , Peter Schmidt , Silke Baasner , Emmanuel Polymeropoulos , Eckhard Guenther , Michael Teifel
Inventor： Tilmann Schuster , Klaus Paulini , Peter Schmidt , Silke Baasner , Emmanuel Polymeropoulos , Eckhard Guenther , Michael Teifel
IPC: C07D209/82 , A61K31/403
CPC classification number: C07K5/06191 , A61K38/00 , C07K5/0827
Abstract: The present invention provides novel tetrahydrocarbazole compounds according to formula (I) as ligands of G-protein coupled receptors (GPCR) which are useful in the treatment and/or prophylaxis of physiological and/or pathological conditions in mammals mediated by GPCR or of physiological and/or pathological conditions which can be treated by modulation of these receptors.
Abstract translation: 本发明提供了根据式（I）的新型四氢咔唑化合物作为G蛋白偶联受体（GPCR）的配体，其可用于治疗和/或预防由GPCR介导的哺乳动物的生理和/或病理状况或生理和/ /或可以通过调节这些受体来治疗的病理状况。
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4.发明授权Pyridopyrazines as highly selective ras-Raf-Mek-Erk signal transduction pathway inhibitors 有权吡吡嗪作为高选择性ras-Raf-Mek-Erk信号转导途径抑制剂公开(公告)号：US08791118B2
公开(公告)日：2014-07-29
申请号：US13439150
申请日：2012-04-04
Applicant: Matthias Gerlach , Irene Seipelt , Lars Blumenstein , Gilbert Mueller , Eckhard Guenther , Tilmann Schuster , Michael Teifel
Inventor： Matthias Gerlach , Irene Seipelt , Lars Blumenstein , Gilbert Mueller , Eckhard Guenther , Tilmann Schuster , Michael Teifel
IPC: A61K31/4985 , C07D487/04
CPC classification number: A61K31/4985 , A61K31/501 , A61K31/5377 , C07D471/04
Abstract: The invention provides new pyridopyrazine compounds according to formula (I) which are highly selective as Ras-Raf-Mek-Erk signal transduction pathway inhibitors and in particular are highly selective Erk inhibitors.
Abstract translation: 本发明提供了根据式（I）的新的吡啶并吡嗪化合物，其作为Ras-Raf-Mek-Erk信号转导途径抑制剂具有高选择性，特别是高度选择性的Erk抑制剂。
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![Modulating signal transduction pathways with 1-ethyl-3-[3-(1-methyl-1H-pyrazol-4-yl)-pyrido[2.3-B]pyrazine-6-yl]thiourea](/abs-image/US/2013/12/10/US08604196B2/abs.jpg.150x150.jpg)
5.发明授权Modulating signal transduction pathways with 1-ethyl-3-[3-(1-methyl-1H-pyrazol-4-yl)-pyrido[2.3-B]pyrazine-6-yl]thiourea 失效用1-乙基-3- [3-（1-甲基-1H-吡唑-4-基） - 吡啶并[2,3-B]吡嗪-6-基]硫脲调制信号转导途径公开(公告)号：US08604196B2
公开(公告)日：2013-12-10
申请号：US13542101
申请日：2012-07-05
Applicant: Matthias Gerlach , Irene Seipelt , Eckhard Guenther , Emmanuel Polymeropoulos , Tilmann Schuster , Eckhard Claus
Inventor： Matthias Gerlach , Irene Seipelt , Eckhard Guenther , Emmanuel Polymeropoulos , Tilmann Schuster , Eckhard Claus
IPC: C07D495/00
CPC classification number: C07D471/04
Abstract: A method of modulating one or more of ras-Raf-Mek-Erk signal transduction pathway, PI3K-Akt signal transduction pathway and SAPK signal transduction pathway with 1-ethyl-3-[3-(1-methyl-1H-pyrazol-4-yl)-pyrido[2,3-b]pyrazine-6-yl]thiourea, its geometric isomer, or its tautomer.
Abstract translation: 一种调节ras-Raf-Mek-Erk信号转导途径，PI3K-Akt信号转导途径和SAPK信号转导途径中的一种或多种与1-乙基-3- [3-（1-甲基-1H-吡唑-4-基） - 基） - 吡啶并[2,3-b]吡嗪-6-基]硫脲，其几何异构体或其互变异构体。
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Patent Agency Ranking
公开(公告)号：US20120258080A1
公开(公告)日：2012-10-11
申请号：US13439150
申请日：2012-04-04
Applicant: Matthias GERLACH , Irene SEIPELT , Lars BLUMENSTEIN , Gilbert MUELLER , Eckhard GUENTHER , Tilmann SCHUSTER , Michael TEIFEL
Inventor： Matthias GERLACH , Irene SEIPELT , Lars BLUMENSTEIN , Gilbert MUELLER , Eckhard GUENTHER , Tilmann SCHUSTER , Michael TEIFEL
IPC: A61K31/4985 , A61K31/5377 , C07F9/6561 , A61K31/675 , A61P29/00 , A61P35/00 , A61P19/02 , A61P37/00 , A61P31/18 , A61P25/00 , A61P25/28 , A61P17/06 , A61P17/02 , A61P3/10 , A61P35/02 , A61P7/02 , A61P37/06 , A61P3/00 , A61P27/02 , A61P11/06 , A61P37/08 , A61P11/00 , A61P9/00 , A61P1/00 , A61P9/10 , A61P13/12 , A61P5/14 , A61P9/04 , A61P9/08 , A61P3/04 , A61P3/08 , A61P9/12 , A61K38/50 , A61K38/14 , A61K33/24 , A61K31/7048 , A61K39/395 , A61K38/21 , A61K31/704 , A61N5/00 , C07D471/04
CPC classification number: A61K31/4985 , A61K31/501 , A61K31/5377 , C07D471/04
Abstract: The present invention provides new pyridopyrazine compounds which are suitable for the treatment or prevention of physiological and/or pathophysiological states mediated and/or modulated by signal transduction pathways and/or enzymes in mammals and in particular in humans.
Abstract translation: 本发明提供了适用于治疗或预防由哺乳动物，特别是人类中的信号转导途径和/或酶介导和/或调节的生理和/或病理生理状态的新的吡啶并吡嗪化合物。
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公开(公告)号：US20120252760A1
公开(公告)日：2012-10-04
申请号：US13523968
申请日：2012-06-15
Applicant: Eckhard Claus , Irene Seipelt , Eckhard Guenther , Emmanuel Polymeropoulos , Michael Czech , Tilmann Schuster
Inventor： Eckhard Claus , Irene Seipelt , Eckhard Guenther , Emmanuel Polymeropoulos , Michael Czech , Tilmann Schuster
IPC: A61K31/4985 , C07F7/18 , C07F9/6561 , A61P1/16 , A61K31/695 , A61K31/675 , A61P17/06 , A61P9/10 , C07D471/04 , A61K31/5377
CPC classification number: A61K31/4985 , A61K31/5377 , A61K31/675 , A61K31/695 , C07D487/04
Abstract: The invention relates to novel pyrido[2,3-b]pyrazine derivatives of the general formulae (I) and (II), and to their preparation and use as medicaments, especially for the treatment of malignant disorders and other disorders based on pathological cell proliferations.
Abstract translation: 本发明涉及通式（I）和（II）的新型吡啶并[2,3-b]吡嗪衍生物及其作为药物的制备和用途，特别是用于治疗基于病理细胞的恶性疾病和其它病症 激增。
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8.发明申请公开(公告)号：US20090275534A1
公开(公告)日：2009-11-05
申请号：US12117942
申请日：2008-05-09
Applicant: Matthias Gerlach , Irene Seipelt , Eckhard Guenther , Emmanuel Polymeropoulos , Tilmann Schuster , Eckhard Claus
Inventor： Matthias Gerlach , Irene Seipelt , Eckhard Guenther , Emmanuel Polymeropoulos , Tilmann Schuster , Eckhard Claus
IPC: A61K31/675 , C07D471/04 , A61K31/4985 , A61K31/536 , A61K31/54 , A61K31/5513 , C12N5/02
CPC classification number: C07D471/04
Abstract: The invention relates to pyrido[2,3-b]pyrazine compounds of general formulae (Ia) and (Ib), to their preparation and use, for example, for the treatment of malignant disorders and other disorders based on pathological cell proliferations.
Abstract translation: 本发明涉及通式（Ia）和（Ib）的吡啶并[2,3-b]吡嗪化合物及其制备和用途，例如用于治疗基于病理细胞增殖的恶性病症和其它病症。
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9.发明申请NOVEL TETRAHYDROCARBAZOLE DERIVATIVES AS LIGANDS OF G-PROTEIN COUPLED RECEPTORS 有权新型四氮唑衍生物作为G蛋白偶联受体的配体公开(公告)号：US20090170783A1
公开(公告)日：2009-07-02
申请号：US12109479
申请日：2008-04-25
Applicant: Tilmann Schuster , Klaus Paulini , Peter Schmidt , Silke Baasner , Emmanuel Polymeropoulos , Eckhard Guenther , Michael Teifel
Inventor： Tilmann Schuster , Klaus Paulini , Peter Schmidt , Silke Baasner , Emmanuel Polymeropoulos , Eckhard Guenther , Michael Teifel
CPC classification number: C07K5/06191 , A61K38/00 , C07K5/0827
Abstract: The present invention provides novel tetrahydrocarbazole compounds according to formula (I) as ligands of G-protein coupled receptors (GPCR) which are useful in the treatment and/or prophylaxis of physiological and/or pathological conditions in mammals mediated by GPCR or of physiological and/or pathological conditions which can be treated by modulation of these receptors.
Abstract translation: 本发明提供了根据式（I）的新型四氢咔唑化合物作为G蛋白偶联受体（GPCR）的配体，其可用于治疗和/或预防由GPCR介导的哺乳动物的生理和/或病理状况或生理和/ /或可以通过调节这些受体来治疗的病理状况。
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10.发明授权公开(公告)号：US08507486B2
公开(公告)日：2013-08-13
申请号：US13455435
申请日：2012-04-25
Applicant: Matthias Gerlach , Irene Seipelt , Eckhard Guenther , Emmanuel Polymeropoulos , Tilmann Schuster , Eckhard Claus
Inventor： Matthias Gerlach , Irene Seipelt , Eckhard Guenther , Emmanuel Polymeropoulos , Tilmann Schuster , Eckhard Claus
IPC: A61K31/495
CPC classification number: C07D471/04
Abstract: 1-ethyl-3-[3-(1-methyl-1H-pyrazol-4-yl)-pyrido[2.3-b]pyrazine-6-yl]thiourea which HAS activity to the modulation of misdirected cellular signal transduction processes such as tyrosine kinases, serine/threonine kinases and/or lipid kinases.
Abstract translation: 1-乙基-3- [3-（1-甲基-1H-吡唑-4-基） - 吡啶并[2,3-b]吡嗪-6-基]硫脲，其对调制错误定向的细胞信号转导过程具有活性 酪氨酸激酶，丝氨酸/苏氨酸激酶和/或脂质激酶。
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