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公开(公告)号：US20140120087A1
公开(公告)日：2014-05-01
申请号：US14113017
申请日：2012-04-16
申请人： Volker Schulze , Dirk Kosemund , Antje Margret Wengner , Gerhard Siemeister , Detlef Stöckigt , Philip Lienau , Hartmut Schirok , Hans Briem
发明人： Volker Schulze , Dirk Kosemund , Antje Margret Wengner , Gerhard Siemeister , Detlef Stöckigt , Philip Lienau , Hartmut Schirok , Hans Briem
IPC分类号： C07D471/04 , A61K45/06 , A61K31/437
CPC分类号： C07D471/04 , A61K31/437 , A61K45/06
摘要： The present invention relates to triazolopyridine compounds of general formula (I): in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.
摘要翻译： 本发明涉及通式（I）的三唑并吡啶化合物：其中R1，R2，R3，R4和R5如说明书和权利要求书中所述，涉及制备所述化合物的方法，药物组合物和组合，包括 所述化合物涉及所述化合物用于制备用于治疗或预防疾病的药物组合物的用途，以及可用于制备所述化合物的中间体化合物。
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公开(公告)号：US09555022B2
公开(公告)日：2017-01-31
申请号：US13704859
申请日：2011-06-14
申请人： Volker Schulze , Dirk Kosemund , Hartmut Schirok , Benjamin Bader , Philip Lienau , Antje Margret Wengner , Hans Briem , Simon Holton , Gerhard Siemeister , Stefan Prechtl , Marcus Koppitz , Detlef Stöckigt , Olaf Prien
发明人： Volker Schulze , Dirk Kosemund , Hartmut Schirok , Benjamin Bader , Philip Lienau , Antje Margret Wengner , Hans Briem , Simon Holton , Gerhard Siemeister , Stefan Prechtl , Marcus Koppitz , Detlef Stöckigt , Olaf Prien
IPC分类号： C07D513/02 , C07D515/02 , C07D249/08 , A61K31/44 , A61K31/437 , A61K45/06 , C07D471/04 , C07D519/00 , A61K31/167 , A61K31/277 , A61K31/282 , A61K31/337 , A61K31/427 , A61K31/428 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/513 , A61K31/5377 , A61K31/541 , A61K31/565 , A61K31/675 , A61K31/69 , A61K31/704 , A61K31/7048 , A61K33/24 , A61K38/14 , A61K39/395 , C07D491/08 , C07D491/107
CPC分类号： A61K31/437 , A61K31/167 , A61K31/277 , A61K31/282 , A61K31/337 , A61K31/427 , A61K31/428 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/513 , A61K31/5377 , A61K31/541 , A61K31/565 , A61K31/675 , A61K31/69 , A61K31/704 , A61K31/7048 , A61K33/24 , A61K38/14 , A61K39/395 , A61K45/06 , C07D471/04 , C07D491/08 , C07D491/107 , C07D519/00 , A61K2300/00
摘要： The present invention relates to substituted triazolopyridine compounds of general formula (I): in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease of uncontrolled cell growth, proliferation and/or survival as well as to the use of intermediate compounds for the preparation of said compounds.
摘要翻译： 本发明涉及通式（I）的取代三唑并吡啶化合物：其中R1，R2，R3，R4和R5如说明书和权利要求书中所述，涉及制备所述化合物的方法，药物组合物和组合 包括所述化合物，用于制备用于治疗或预防不受控制的细胞生长，增殖和/或存活的疾病的药物组合物以及使用中间体化合物来制备所述化合物的用途。
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公开(公告)号：US20140255392A1
公开(公告)日：2014-09-11
申请号：US14110105
申请日：2012-03-28
IPC分类号： C07D471/04 , A61K31/444 , A61K45/06 , A61K31/437
CPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K45/06 , A61K2300/00
摘要： The present invention relates to substituted imidazopyridine 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）的取代的咪唑并吡啶化合物，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的用途 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：US20130210846A1
公开(公告)日：2013-08-15
申请号：US13638833
申请日：2011-03-28
IPC分类号： C07D239/47 , C07D239/48
CPC分类号： C07D239/47 , A61K31/505 , C07D239/48
摘要： The invention relates to the use of selected sulfoximine-substituted anilinopyrimidine derivatives of the formula (I) for treating tumors.
摘要翻译： 本发明涉及式（I）的选择的亚磺酰亚胺取代的苯胺基嘧啶衍生物用于治疗肿瘤的用途。
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公开(公告)号：US09676766B2
公开(公告)日：2017-06-13
申请号：US13512701
申请日：2010-11-17
申请人： Volker Schulze , Marcus Koppitz , Dirk Kosemund , Hartmut Schirok , Benjamin Bader , Philip Lienau , Antje Margret Wengner , Hans Briem , Simon Holton , Gerhard Siemeister , Stefan Prechtl , Ulf Bömer
发明人： Volker Schulze , Marcus Koppitz , Dirk Kosemund , Hartmut Schirok , Benjamin Bader , Philip Lienau , Antje Margret Wengner , Hans Briem , Simon Holton , Gerhard Siemeister , Stefan Prechtl , Ulf Bömer
IPC分类号： A61K31/437 , A61K31/5377 , C07D491/08 , C07D471/04
CPC分类号： C07D471/04 , A61K31/437 , A61K31/5377 , A61K2300/00
摘要： The present invention relates to triazolopyridine compounds of general formula (I) which are Monopolar Spindle 1 kinase (Mps-1 or TTK) inhibitors: Formula (I), in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis proliferative of diseases, as well as to intermediate compounds useful in the preparation of said compounds.
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公开(公告)号：US09255100B2
公开(公告)日：2016-02-09
申请号：US13822175
申请日：2011-09-06
申请人： Ulrich Klar , Marcus Koppitz , Rolf Jautelat , Dirk Kosemund , Rolf Bohlmann , Philip Lienau , Gerhard Siemeister , Antje Margret Wengner
发明人： Ulrich Klar , Marcus Koppitz , Rolf Jautelat , Dirk Kosemund , Rolf Bohlmann , Philip Lienau , Gerhard Siemeister , Antje Margret Wengner
IPC分类号： C07D487/04 , A61K31/5025 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D471/04
CPC分类号： C07D487/04 , A61K31/5025 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D471/04
摘要： The present invention relates to substituted imidazopyridazine compounds of general formula (I), which are Mps-1 (Monopolar Spindle 1) Kinase inhibitors (also known as Tyrosine Threonine Kinase, TTK) 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，其是Mps-1（单极主轴1）激酶抑制剂（也称为酪氨酸苏氨酸激酶，TTK），其中R3，R5和A如 对于制备所述化合物的方法，涉及包含所述化合物的药物组合物和组合，以及所述化合物用于制备用于治疗或预防疾病，特别是高增殖和/或血管生成障碍的药物组合物的用途 ，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：US20130338133A1
公开(公告)日：2013-12-19
申请号：US13822175
申请日：2011-09-06
申请人： Ulrich Klar , Marcus Koppitz , Rolf Jautelat , Dirk Kosemund , Rolf Bohlmann , Philip Lienau , Gerhard Siemeister , Antje Margret Wengner
发明人： Ulrich Klar , Marcus Koppitz , Rolf Jautelat , Dirk Kosemund , Rolf Bohlmann , Philip Lienau , Gerhard Siemeister , Antje Margret Wengner
IPC分类号： C07D487/04 , A61K45/06 , A61K31/5377 , A61K31/506 , C07D471/04 , A61K31/5025
CPC分类号： C07D487/04 , A61K31/5025 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D471/04
摘要： The present invention relates to substituted imidazopyridazine compounds of general formula (I), which are Mps-1 (Monopolar Spindle 1) Kinase inhibitors (also known as Tyrosine Threonine Kinase, TTK) 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，其是Mps-1（单极主轴1）激酶抑制剂（也称为酪氨酸苏氨酸激酶，TTK），其中R3，R5和A如 对于制备所述化合物的方法，涉及包含所述化合物的药物组合物和组合，以及所述化合物用于制备用于治疗或预防疾病，特别是高增殖和/或血管生成障碍的药物组合物的用途 ，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：US20130156756A1
公开(公告)日：2013-06-20
申请号：US13704859
申请日：2011-06-14
申请人： Volker Schulze , Dirk Kosemund , Hartmut Schirok , Benjamin Bader , Philip Lienau , Antje Margret Wengner , Hans Briem , Simon Holton , Gerhard Siemeister , Stefan Prechtl , Marcus Koppitz , Detlef Stöckigt , Olaf Prien
发明人： Volker Schulze , Dirk Kosemund , Hartmut Schirok , Benjamin Bader , Philip Lienau , Antje Margret Wengner , Hans Briem , Simon Holton , Gerhard Siemeister , Stefan Prechtl , Marcus Koppitz , Detlef Stöckigt , Olaf Prien
IPC分类号： A61K31/437 , A61K31/5377 , A61K31/496 , A61K31/444 , C07D491/08 , C07D491/107 , A61K31/541 , A61K31/4545 , A61K31/337 , A61K31/427 , A61K31/428 , A61K31/167 , A61K31/565 , A61K31/277 , A61K33/24 , A61K31/282 , A61K39/395 , A61K38/14 , A61K31/704 , A61K31/513 , A61K31/675 , A61K31/7048 , A61K31/69 , C07D471/04
CPC分类号： A61K31/437 , A61K31/167 , A61K31/277 , A61K31/282 , A61K31/337 , A61K31/427 , A61K31/428 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/513 , A61K31/5377 , A61K31/541 , A61K31/565 , A61K31/675 , A61K31/69 , A61K31/704 , A61K31/7048 , A61K33/24 , A61K38/14 , A61K39/395 , A61K45/06 , C07D471/04 , C07D491/08 , C07D491/107 , C07D519/00 , A61K2300/00
摘要： The present invention relates to substituted triazolopyridine compounds of general formula (I): in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease of uncontrolled cell growth, proliferation and/or survival as well as to the use of intermediate compounds for the preparation of said compounds.
摘要翻译： 本发明涉及通式（I）的取代三唑并吡啶化合物：其中R1，R2，R3，R4和R5如说明书和权利要求书中所述，涉及制备所述化合物的方法，药物组合物和组合 包括所述化合物，用于制备用于治疗或预防不受控制的细胞生长，增殖和/或存活的疾病的药物组合物以及使用中间体化合物来制备所述化合物的用途。
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公开(公告)号：US08551980B2
公开(公告)日：2013-10-08
申请号：US13512737
申请日：2010-11-17
申请人： Volker Schulze , Marcus Koppitz , Dirk Kosemund , Benjamin Bader , Philip Lienau , Hans Briem , Simon Holton , Gerhard Siemeister , Stefan Prechtl , Antje Margret Wengner
发明人： Volker Schulze , Marcus Koppitz , Dirk Kosemund , Benjamin Bader , Philip Lienau , Hans Briem , Simon Holton , Gerhard Siemeister , Stefan Prechtl , Antje Margret Wengner
IPC分类号： A01N43/00 , A01N43/40 , A01N43/64 , A61K31/33 , A61K31/445 , A61K31/41 , C07D221/02 , C07D471/02 , C07D249/08 , C07D249/00
CPC分类号： C07D471/04
摘要： The present invention relates to triazolopyridine compounds of general formula (I) which are Monopolar Spindle 1 kinase (Mps-1 or TTK) inhibitors: Formula (I), in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis proliferative of diseases, as well as to intermediate compounds useful in the preparation of said compounds.
摘要翻译： 本发明涉及通式（I）的三唑并吡啶化合物，它们是单极主轴1激酶（Mps-1或TTK）抑制剂：式（I），其中R 1，R 2，R 3，R 4和R 5如 描述和权利要求书中涉及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，用于制备用于治疗或预防疾病增殖的药物组合物的所述化合物的用途，以及可用于 所述化合物的制备。
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公开(公告)号：US20130121994A1
公开(公告)日：2013-05-16
申请号：US13512721
申请日：2010-11-26
申请人： Marcus Koppitz , Volker Schulze , Dirk Kosemund , Hartmut Schirok , Benjamin Bader , Philip Lienau , Tobias Marquardt , Christof Wegscheid-Gerlach , Gerhard Siemeister , Stefan Prechtl , Antje Margret Wengner , Ulf Bömer
发明人： Marcus Koppitz , Volker Schulze , Dirk Kosemund , Hartmut Schirok , Benjamin Bader , Philip Lienau , Tobias Marquardt , Christof Wegscheid-Gerlach , Gerhard Siemeister , Stefan Prechtl , Antje Margret Wengner , Ulf Bömer
IPC分类号： C07D471/04 , A61K31/506 , A61K31/444 , A61K31/337 , A61K39/395 , A61K33/24 , A61K31/282 , A61K31/513 , A61K31/664 , A61K31/427 , A61K31/573 , A61K31/565 , A61K31/704 , A61K31/7076 , A61K31/437
CPC分类号： C07D471/04 , A61K31/282 , A61K31/337 , A61K31/427 , A61K31/437 , A61K31/444 , A61K31/506 , A61K31/513 , A61K31/565 , A61K31/573 , A61K31/664 , A61K31/704 , A61K31/7076 , A61K33/24 , A61K39/3955
摘要： The present invention relates to triazolopyridine compounds of general formula (I) which are Monopolar Spindle 1 kinase (Mps-1 or TTK) inhibitors in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of proliferative diseases, as well as to intermediate compounds useful in the preparation of said compounds.
摘要翻译： 本发明涉及通式（I）的三唑并吡啶化合物，其是单极主轴1激酶（Mps-1或TTK）抑制剂，其中R1，R2，R3，R4和R5如说明书和权利要求书中所给出， 涉及制备所述化合物的方法，包含所述化合物的药物组合物和组合，以及所述化合物用于制备用于治疗或预防增殖性疾病的药物组合物的用途，以及可用于制备所述化合物的中间体化合物。
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