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公开(公告)号：US09951027B2
公开(公告)日：2018-04-24
申请号：US15118157
申请日：2015-02-10
发明人： Hartmut Rehwinkel , Holger Siebeneicher , Sonja Anlauf , Duy Nguyen , Olaf Panknin , Sven Ring , Wolfgang Schwede , Marcus Bauser , Katja Zimmermann , Stefan Kaulfuss , Roland Neuhaus
IPC分类号： C07D235/30 , C07D409/12 , C07D401/12 , C07D405/12
CPC分类号： C07D235/30 , C07D401/12 , C07D405/12 , C07D409/12
摘要： The present invention relates to benzimidazol-2-amines of general formula (I): in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and R12 are as defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.
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公开(公告)号：US09512130B2
公开(公告)日：2016-12-06
申请号：US14771648
申请日：2014-02-25
发明人： Marcus Koppitz , Ulrich Klar , Antje Margret Wengner , Roland Neuhaus , Gerhard Siemeister , Michael Brüning
IPC分类号： A61K31/4188 , C07D237/00 , C07D487/04 , A61K31/282 , A61K31/5025 , A61K31/52 , A61K31/573 , A61K31/675 , A61K31/69 , A61K31/704 , A61K31/7068 , A61K33/24 , A61K38/14 , A61K39/395 , A61K39/00
CPC分类号： C07D487/04 , A61K31/282 , A61K31/4188 , A61K31/5025 , A61K31/52 , A61K31/573 , A61K31/675 , A61K31/69 , A61K31/704 , A61K31/7068 , A61K33/24 , A61K38/14 , A61K39/3955 , A61K2039/505 , C07D237/00
摘要： The present invention relates to substituted imidazopyridazine compounds, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
摘要翻译： 本发明涉及取代的咪唑并哒嗪化合物，制备所述化合物的方法，药物组合物和包含所述化合物的组合以及所述化合物用于制备药物组合物用于治疗或预防疾病，特别是超级 增殖和/或血管生成障碍，作为唯一的药剂或与其它活性成分组合。
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公开(公告)号：US20150104526A1
公开(公告)日：2015-04-16
申请号：US14384828
申请日：2013-03-11
IPC分类号： C07D487/04 , A61K45/06 , A61K31/5025
CPC分类号： C07D487/04 , A61K31/5025 , A61K45/06
摘要： The present invention relates to substituted imidazopyridazine compounds of general formula I in which R3, R5 and A are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
摘要翻译： 本发明涉及通式I的取代的咪唑并哒嗪化合物，其中R3，R5和A如权利要求中所定义，所述化合物的制备方法，药物组合物和包含所述化合物的组合以及所述化合物用于制造 用于治疗或预防疾病，特别是高增殖性和/或血管生成障碍的药物组合物，作为唯一试剂或与其它活性成分组合。
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公开(公告)号：US11427578B1
公开(公告)日：2022-08-30
申请号：US16632273
申请日：2018-07-12
发明人： Jeffrey Stuart Mowat , Bernd Buchmann , Nuria Aiguabella Font , Gabriele Leder , Rafael Carretero , Olaf Panknin , Roland Neuhaus , Robin Michael Meier , Sandra Berndt , Kirstin Petersen , Rienk Offringa
IPC分类号： C07D471/04 , A61K45/06
摘要： The present invention relates to protein-inhibitory substituted pyrrolopyridine derivatives of formula (I), in which A, X, R1, R2a, R2b, R3a, R3b, R4a and R4b are as defined herein, to pharmaceutical compositions and combinations comprising the compounds according to the invention, and to the prophylactic and therapeutic use of the inventive compounds, respectively to the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular for neoplastic disorders, respectively cancer or conditions with dysregulated immune responses or other disorders associated with aberrant MAP4K1 signaling, as a sole agent or in combination with other active ingredients. The present invention further relates to the use, respectively to the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of protein inhibitors in benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, in neurodegenerative disorders, in inflammatory disorders, in atherosclerotic disorders and in male fertility control.
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公开(公告)号：US10179123B2
公开(公告)日：2019-01-15
申请号：US15742363
申请日：2016-07-04
发明人： Olaf Panknin , Katja Zimmermann , Roland Neuhaus
IPC分类号： A61K31/4184 , A61K31/427 , C07D235/08 , C07D235/18 , C07D403/06 , C07D417/06 , A61K45/06
摘要： The present invention relates to 2-Aryl- and 2-Arylalkyl-benzimidazoles of general formula (I): in which A, R1, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.
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公开(公告)号：US09663523B2
公开(公告)日：2017-05-30
申请号：US14432158
申请日：2013-09-25
申请人： BAYER PHARMA AKTIENGESELLSCHAFT , Helga Künzer , Klara Muno , Erich Künzer , Martin Künzer , Christel Bernsdorf
发明人： Norbert Schmees , Joachim Kuhnke , Bernard Haendler , Roland Neuhaus , Pascale Lejeune , Stephan Siegel , Martin Krüger , Amaury Ernesto Fernandez-Montalvan , Hermann Künzer , Daniel Gallenkamp
IPC分类号： A61K31/55 , C07D487/04 , C07D519/00
CPC分类号： C07D487/04 , A61K31/55 , C07D519/00
摘要： The present invention relates to BET-protein-inhibitory, in particular BRD4-inhibitory 5-aryltriazoloazepines of the general formula (I) in which R1, R2, R3 and R4 have the meanings given for the general formula (I), to pharmaceutical compositions comprising the compounds according to the invention, and to the prophylactic and therapeutic use thereof for hyperproliferative disorders, especially for neoplastic disorders. The present invention further relates to the use of BET protein inhibitors in viral infections, in neurodegenerative disorders, in inflammatory diseases, in atherosclerotic disorders and in male fertility control.
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公开(公告)号：US20160016959A1
公开(公告)日：2016-01-21
申请号：US14771648
申请日：2014-02-25
发明人： Marcus Koppitz , Ulrich Klar , Antje Margret Wengner , Roland Neuhaus , Gerhard Siemeister , Michael Bruning
IPC分类号： C07D487/04 , A61K39/395 , A61K33/24 , A61K31/282 , A61K31/675 , A61K31/7068 , A61K31/52 , A61K38/14 , A61K31/573 , A61K31/704 , A61K31/5025 , A61K31/69
CPC分类号： C07D487/04 , A61K31/282 , A61K31/4188 , A61K31/5025 , A61K31/52 , A61K31/573 , A61K31/675 , A61K31/69 , A61K31/704 , A61K31/7068 , A61K33/24 , A61K38/14 , A61K39/3955 , A61K2039/505 , C07D237/00
摘要： The present invention relates to substituted imidazopyridazine compounds, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
摘要翻译： 本发明涉及取代的咪唑并哒嗪化合物，制备所述化合物的方法，药物组合物和包含所述化合物的组合以及所述化合物用于制备药物组合物用于治疗或预防疾病，特别是超级 增殖和/或血管生成障碍，作为唯一的药剂或与其它活性成分组合。
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公开(公告)号：US20150005309A1
公开(公告)日：2015-01-01
申请号：US14370831
申请日：2013-01-08
发明人： Lars Bärfacker , William Scott , Andrea Hägebarth , Stuart Ince , Hartmut Rehwinkel , Oliver Politz , Roland Neuhaus , Ulf Bömer
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , A61K31/4985 , A61K45/06 , A61K2300/00
摘要： Compounds of formula (I) which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals.
摘要翻译： 作为Pi3K / Akt途径的有效抑制剂的式（I）化合物，其制备方法及其作为药物的用途。
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公开(公告)号：US11319324B2
公开(公告)日：2022-05-03
申请号：US16759262
申请日：2018-10-18
发明人： Marcus Koppitz , Holger Siebeneicher , Nico Bräuer , Elisabeth Pook , Andrea Rotgeri , Roland Neuhaus , Oliver Martin Fischer , Jens Nagel , Adam James Davenport , James Lindsay Carr , Robert James Townsend , Nina Connelly Ursinyova , Shelley Anne Parrott
IPC分类号： C07D487/14
摘要： The present invention covers substituted. Pyrazolo-pyrrolo-pyrimidine-dione (PPPD) compounds of general formula (I): in which R1, R2 and R3 are as defined herein, methods of preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of neurogenic diseases, as a sole agent or in combination with other active ingredients.
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公开(公告)号：US10919862B2
公开(公告)日：2021-02-16
申请号：US15746352
申请日：2016-07-14
发明人： Olaf Panknin , Ingo Hartung , Hartmut Rehwinkel , Duy Nguyen , Ludwig Zorn , Petra Helfrich , Katja Zimmermann , Roland Neuhaus
IPC分类号： C07D235/30 , C07D471/04 , A61P35/00 , A61K31/4184 , A61K31/437 , A61K45/06 , C12P17/10
摘要： The present invention relates to compounds of general formula (I): in which R1, R2, R3, R4, R6, R7, R8, R9, R10, R11, R12, R13 and X are as defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.
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