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1.发明授权Furopyridinyl-substituted 1,4-dihydropyridine derivatives and methods of use thereof 有权呋喃啶基取代的1,4-二氢吡啶衍生物及其使用方法公开(公告)号：US08604028B2
公开(公告)日：2013-12-10
申请号：US13510483
申请日：2010-11-15
IPC分类号： A61K31/5383 , A61K45/06 , C07D498/04 , A61K31/437
CPC分类号： A61K31/5383 , A61K31/4355 , A61K31/437 , A61K45/06 , C07D491/048 , C07D498/04 , C07D519/00 , A61K2300/00
摘要： This invention relates to novel 4-(furo[3,2-c]pyridin-2-yl)-1,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders.
摘要翻译： 本发明涉及具有蛋白酪氨酸激酶抑制活性的新型4-（呋喃并[3,2-c]吡啶-2-基）-1,4-二氢吡啶衍生物及其制备方法及其用途 治疗c-Met介导的疾病或c-Met介导的病症，特别是癌症和其他增殖性疾病。
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2.发明申请FUROPYRIDINYL-SUBSTITUTED 1,4-DIHYDROPYRIDINE DERIVATIVES AND METHODS OF USE THEREOF 有权呋喃并吡啶基取代的1,4-二氢吡啶衍生物及其使用方法公开(公告)号：US20130131055A1
公开(公告)日：2013-05-23
申请号：US13510483
申请日：2010-11-15
IPC分类号： A61K31/5383 , A61K45/06 , C07D498/04 , A61K31/437 , C07D491/048 , A61K31/4355
CPC分类号： A61K31/5383 , A61K31/4355 , A61K31/437 , A61K45/06 , C07D491/048 , C07D498/04 , C07D519/00 , A61K2300/00
摘要： This invention relates to novel 4-(furo[3,2-c]pyridin-2-yl)-1,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders.
摘要翻译： 本发明涉及具有蛋白酪氨酸激酶抑制活性的新型4-（呋喃并[3,2-c]吡啶-2-基）-1,4-二氢吡啶衍生物及其制备方法及其用途 治疗c-Met介导的疾病或c-Met介导的病症，特别是癌症和其他增殖性疾病。
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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：US09206185B2
公开(公告)日：2015-12-08
申请号：US14007427
申请日：2012-04-05
申请人： Lars Bärfacker , William Scott , Andrea Hägebarth , Stuart Ince , Hartmut Rehwinkel , Oliver Politz , Roland Neuhaus , Hans Briem , Ulf Bömer
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 application relates to imidazopyridazines of formula (I) which are useful as Akt inhibitors suitable for the treatment of cancer, and processes for their production and the use thereof.
摘要翻译： 本申请涉及可用作适于治疗癌症的Akt抑制剂及其制备方法及其用途的式（I）咪唑并哒嗪。
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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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6.发明授权Substituted sulphoximines as TIE2 inhibitors and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same 有权作为TIE2抑制剂及其盐的取代的亚磺酰亚胺，包含其的药物组合物，其制备方法及其用途公开(公告)号：US08003655B2
公开(公告)日：2011-08-23
申请号：US11776231
申请日：2007-07-11
申请人： Ingo Hartung , Georg Kettschau , Hans Briem , Karl-Heinz Thierauch , Ulrich Luecking , Ulf Boemer , Martin Krueger
发明人： Ingo Hartung , Georg Kettschau , Hans Briem , Karl-Heinz Thierauch , Ulrich Luecking , Ulf Boemer , Martin Krueger
IPC分类号： C07D439/02 , C07D239/42 , A01N43/54
CPC分类号： C07D239/48 , C07D239/47 , C07D401/12 , C07D407/12 , C07D413/12
摘要： The invention relates to substituted sulphoximines according to the general formula (I): in which A, E, G, X, R1, R2, R3, R4, R5, R6, R7, R8, m, p, q, are given in the claims, and salts thereof, to pharmaceutical compositions comprising said substituted sulphoximines, to methods of preparing said substituted sulphoximines as well as the use thereof for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth, wherein the compounds effectively interfere with Tie2 signalling.
摘要翻译： 本发明涉及根据通式（I）的取代的亚磺酰亚胺：其中A，E，G，X，R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，m，p，q， 权利要求书及其盐，涉及包含所述取代的亚硫酰亚胺的药物组合物，制备所述取代的亚硫酰亚胺的方法及其用于制备用于治疗失调的血管生长疾病或伴随失调的疾病的药物组合物的用途 血管生长，其中所述化合物有效地干扰Tie2信号传导。
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7.发明授权Substituted aminopyrazolopyridines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same 有权取代的氨基吡唑并吡啶及其盐，包含其的药物组合物，其制备方法及其用途公开(公告)号：US07825114B2
公开(公告)日：2010-11-02
申请号：US11761621
申请日：2007-06-12
申请人： Ingo Hartung , Stuart Ince , Georg Kettschau , Karl-Heinz Thierauch , Hans Briem , Wolfgang Schwede , Antonius M. Laak Ter
发明人： Ingo Hartung , Stuart Ince , Georg Kettschau , Karl-Heinz Thierauch , Hans Briem , Wolfgang Schwede , Antonius M. Laak Ter
IPC分类号： A61K31/5377 , C07D471/04 , A61P35/00 , A61P27/02 , A61K31/437
CPC分类号： C07D471/04
摘要： The invention relates to substituted aminopyrazolopyridines according to the general formula (I): in which A, B, D, E, Ra, R1, R2, R3, R4, R5 and q are as defined in the claims, and salts thereof, to pharmaceutical compositions comprising said substituted aminopyrazolopyridines, to methods of preparing said substituted aminopyrazolopyridines as well as the use thereof for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth, wherein the compounds effectively interfere with Tie2 signalling.
摘要翻译： 本发明涉及根据通式（I）的取代的氨基吡唑并吡啶：其中A，B，D，E，R a，R 1，R 2，R 3，R 4，R 5和q如权利要求中所定义， 包含所述取代的氨基吡唑并吡啶的药物组合物，制备所述取代的氨基吡唑并吡啶的方法及其制备用于治疗失调的血管生长疾病的药物组合物或伴随血管生长失调的疾病的用途，其中所述化合物有效地干扰 与Tie2信令。
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8.发明申请SUBSTITUTED ARYLPYRAZOLOPYRIDINES AND SALTS THEREOF, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, METHODS OF PREPARING SAME AND USES OF SAME 有权取代的芳基吡唑并吡咯啉及其盐，其包含其的药物组合物，其制备方法及其用途公开(公告)号：US20080064707A1
公开(公告)日：2008-03-13
申请号：US11761605
申请日：2007-06-12
申请人： Ingo Hartung , Georg Kettschau , Karl-Heinz Thierauch , Hans Briem , Philip Lienau , Antonius Ter Laak
发明人： Ingo Hartung , Georg Kettschau , Karl-Heinz Thierauch , Hans Briem , Philip Lienau , Antonius Ter Laak
IPC分类号： A61K31/437 , A61K31/497 , A61P29/00 , A61P35/00 , A61P9/00 , C07D401/14 , C07D471/04
CPC分类号： C07D471/04 , C07D213/85
摘要： The invention relates to substituted arylpyrazolopyridines according to the general formula (I): in which A, B, D, E, Ra, R1, R2, R3, R4, R5 and q are as defined in the claims, and salts thereof, to pharmaceutical compositions comprising said substituted arylpyrazolopyridines, to methods of preparing said substituted arylpyrazolopyridines as well as the use thereof for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth, wherein the compounds effectively interfere with Tie2 signalling.
摘要翻译： 本发明涉及根据通式（I）的取代芳基吡唑并吡啶：其中A，B，D，E，R a，R 1，R 2， R 3，R 4，R 5和R 5如权利要求中所定义，及其盐如药物组合物 包括所述取代的芳基吡唑并吡啶的方法，涉及制备所述取代的芳基吡唑并吡啶的方法及其制备用于治疗失调的血管生长疾病的药物组合物或伴有血管生长失调的疾病的用途，其中所述化合物有效地干扰Tie2 信令。
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9.发明申请SUBSTITUTED PYRAZOLOPYRIDINES AND SALTS THEREOF, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, METHODS OF PREPARING SAME AND USES OF SAME 有权取代的吡唑啉酮及其盐，其包含其的药物组合物，其制备方法及其用途公开(公告)号：US20080058326A1
公开(公告)日：2008-03-06
申请号：US11761672
申请日：2007-06-12
申请人： Ingo Hartung , Stuart Ince , Georg Kettschau , Karl-Heinz Thierauch , Hans Briem , Ulf Boemer
发明人： Ingo Hartung , Stuart Ince , Georg Kettschau , Karl-Heinz Thierauch , Hans Briem , Ulf Boemer
IPC分类号： A61K31/44 , A61K31/501 , A61K31/535 , A61P43/00 , C07D401/00 , C07D413/00 , C07D471/02
CPC分类号： C07D213/85 , C07D471/04
摘要： The invention relates to substituted pyrazolopyridines according to the general formula (I): in which A, B, D, E, Ra, R1, R2, R3, R4, R5 and q are as defined in the claims, and salts thereof, to pharmaceutical compositions comprising said substituted pyrazolopyridine compounds, to methods of preparing said substituted pyrazolopyridines, as well as to uses thereof for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth, wherein the compounds effectively interfere with Tie2 signalling.
摘要翻译： 本发明涉及根据通式（I）的取代吡唑并吡啶：其中A，B，D，E，R a，R 1，R 2， R 3，R 4，R 5和R 5如权利要求中所定义，及其盐如药物组合物 包括所述取代的吡唑并吡啶化合物的方法，以及制备所述取代的吡唑并吡啶的方法，以及其用于制备用于治疗失调的血管生长的疾病的药物组合物或伴随血管生长失调的疾病的用途，其中所述化合物有效地干扰 与Tie2信令。
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10.发明授权公开(公告)号：US07312225B2
公开(公告)日：2007-12-25
申请号：US10644076
申请日：2003-08-20
IPC分类号： A61P35/00 , A61K31/505 , C07D245/00
CPC分类号： C07D239/42 , C07D239/48 , C07D409/12 , C07D487/08 , C07D513/08
摘要： Macrocyclic pyrimidine derivatives of general formula I in which R1 to R5, X, Y, A, B, m and n have the meanings that are contained in the description, as inhibitors of the cyclin-dependent kinase, their processes for production as well as their use as medications for treating various diseases are described.
摘要翻译： R 1至R 5，X，Y，A，B，m和n的通式I的大环嘧啶衍生物具有说明书中所含的含义， 作为细胞周期蛋白依赖性激酶的抑制剂，其生产方法以及它们作为用于治疗各种疾病的药物的用途。
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