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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：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：US09370517B2
公开(公告)日：2016-06-21
申请号：US14371567
申请日：2013-01-08
发明人： Lars Bärfacker , William Scott , Andrea Hägebarth , Hartmut Rehwinkel , Oliver Politz , Roland Neuhaus , Ulf Bömer
IPC分类号： A61K31/519 , C07D487/04 , A61K45/06
CPC分类号： A61K31/519 , A61K45/06 , C07D487/04
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：US09512126B2
公开(公告)日：2016-12-06
申请号：US14384828
申请日：2013-03-11
IPC分类号： A01N43/00 , A61K31/33 , C07D487/00 , C07D487/04 , A61K31/5025 , A61K45/06
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.
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公开(公告)号：US09260435B2
公开(公告)日：2016-02-16
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 , A61K45/06 , A61K31/4985
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：US09604989B2
公开(公告)日：2017-03-28
申请号：US14792205
申请日：2015-07-06
发明人： Lars Bärfacker , William Scott , Andrea Hägebarth , Stuart Ince , Hartmut Rehwinkel , Oliver Politz , Roland Neuhaus , Hans Briem , Ulf Bömer
IPC分类号： C07D487/04 , A61K31/5025 , A61K45/06
CPC分类号： C07D487/04 , A61K31/5025 , A61K45/06
摘要： The present invention relates to a method for the treatment of a cancer that is sensitive to Pi3K/Akt pathway inhibition by administering a therapeutically effective amount of a compound of formula (I)
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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：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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