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1.发明公开
公开(公告)号：EP1963282A1
公开(公告)日：2008-09-03
申请号：EP06829901.5
申请日：2006-12-19
发明人： LUECKING, Ulrich , NGUYEN, Duy , VON BONIN, Arne , VON AHSEN, Oliver , KRUEGER, Martin , BRIEM, Hans , KETTSCHAU, Georg , PRIEN, Olaf , MENGEL, Anne , KROLIKIEWICZ, Konrad , BOEMER, Ulf , BOTHE, Ulrich , HARTUNG, Ingo
IPC分类号： C07D239/47 , C07D239/48 , C07D401/04 , C07D403/04 , C07D403/14 , C07D405/04 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/04 , A61K31/506 , A61K31/505 , A61P29/00 , A61P35/00 , A61P37/00
CPC分类号： C07D239/28 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/04
摘要： The invention relates to sulfoximine-substituted pyrimidines of the general Formula (I) processes for the preparation thereof and their use as kinase inhibitors for treating for example cancer or inflammation.
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2.发明授权SUBSTITUTED SULPHOXIMINES AS TIE2 INHIBITORS AND SALTS THEREOF, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, METHODS OF PREPARING SAME AND USES OF SAME 有权取代亚磺酰亚胺AS TIE2抑制剂及其盐，药物组合物含有用于生产及其应用
公开(公告)号：EP2046758B1
公开(公告)日：2011-03-16
申请号：EP07765166.9
申请日：2007-07-06
发明人： KETTSCHAU, Georg , HARTUNG, Ingo , LÜCKING, Ulrich , THIERAUCH, Karl-Heinz , BRIEM, Hans , BÖMER, Ulf , KRUEGER, Martin
IPC分类号： C07D239/48 , C07D239/46 , C07D401/12 , C07D413/12 , C07D407/12 , A61K31/506 , A61K31/505 , A61P35/00
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.
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3.发明公开ALKYNYLARYL COMPOUNDS AND SALTS THEREOF, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, METHODS OF PREPARING SAME AND USES OF SAME 有权ALKINYLARYLVERBINDUNGEN及其盐，含药物组合物，方法及其及其用途
公开(公告)号：EP2229389A1
公开(公告)日：2010-09-22
申请号：EP08860474.9
申请日：2008-12-04
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The invention relates to alkynylaryl compounds according to the general formula (I) in which A, B, D, E, Ra, R1, R3, R4, R5 and q are as defined in the claims, and salts, N-oxides, solvates and prodrugs thereof, to pharmaceutical compositions comprising said alkynylaryl compounds, to methods of preparing said alkynylaryl compounds, to intermediate compounds useful in said methods, to uses of said intermediate compounds in the preparation of said alkynylaryl compounds, as well as to uses of said alkynylaryl compounds for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth.
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4.发明公开SULFOXIMINE-PYRIMIDINE MACROCYCLES AND THE SALTS THEREOF, A PROCESS FOR MAKING THEM, AND THEIR PHARMACEUTICAL USE AGAINST CANCER 审中-公开。亚嘧啶MACRO旋回及其盐，用于生产和它们的药物来对付癌症
公开(公告)号：EP1879900A2
公开(公告)日：2008-01-23
申请号：EP06742601.5
申请日：2006-04-10
发明人： LÜCKING, Ulrich , KETTSCHAU, Georg , BRIEM, Hans , SCHWEDE, Wolfgang , SCHÄFER, Martina , THIERAUCH, Karl-Heinz , HUSEMANN, Manfred
IPC分类号： C07D513/08 , C07D239/04 , A61K31/529 , C07C317/12
CPC分类号： C07D209/48 , C07D239/42 , C07D513/08
摘要： The invention relates to macrocyclic sulfoximines of the general Formula I : (I), wherein A, X, Y, R1, R2 and R3 have the meaning as given in the specification and the claims, and to salts thereof; to pharmaceutical compositions comprising the macrocyclic sulfoximines, and to a method of preparing the macrocyclic sulfoximines, 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 angiopoietin and therefore influence Tie2 signalling.
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公开(公告)号：EP1844056A2
公开(公告)日：2007-10-17
申请号：EP05820679.8
申请日：2005-12-19
发明人： KETTSCHAU, Georg , BRIEM, Hans , LUECKING, Ulrich , SCHAEFER, Martina , THIERAUCH, Karl-heinz , SCHWEDE, Wolfgang , HUSEMANN, Manfred , HUTH, Andreas
IPC分类号： C07D513/08
CPC分类号： C07D513/08
摘要： The invention relates to sulfonamido-macrocycles according to the general Formula I and the salts thereof, to pharmaceutical compositions comprising the sulfonamido-macrocycles and to a method of preparing the sulfonamido-macrocycles 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 angiopoietin and therefore influence Tie2 signalling. (I), wherein R1, R2 and R3 have the meaning as given in the specification and the claims.
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6.发明公开SUBSTITUTED AMINOPYRAZOLOPYRIDINES AND SALTS THEREOF, THEIR PREPARATIONS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM 有权取代的氨基吡唑并吡啶及其盐，包含它们的制剂和药物组合物
公开(公告)号：EP2032572A1
公开(公告)日：2009-03-11
申请号：EP07764751.9
申请日：2007-06-12
发明人： HARTUNG, Ingo , INCE, Stuart , KETTSCHAU, Georg , THIERAUCH, Karl-Heinz , BRIEM, Hans , SCHWEDE, Wolfgang , TER LAAK, Antonius, M.
IPC分类号： C07D471/04 , A61K31/437 , A61P9/00 , A61P35/00
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，Ra，R1，R2，R3，R4，R5和q如权利要求中所定义，及其盐， 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，以及其用于制备用于治疗血管生长失调疾病或伴随血管生长失调的疾病的药物组合物的用途，其中所述化合物有效地干扰 与Tie2信号。
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公开(公告)号：EP1828209A2
公开(公告)日：2007-09-05
申请号：EP05826661.0
申请日：2005-12-19
发明人： KETTSCHAU, Georg , BRIEM, Hans , HARTUNG, Ingo , LUECKING, Ulrich , SCHAEFER, Martina , THIERAUCH, Karl-Heinz , SCHWEDE, Wolfgang , HUSEMANN, Manfred
IPC分类号： C07D513/08 , A61K31/529 , A61P35/00
CPC分类号： C07D513/08
摘要： The invention relates to sulfonamido-macrocycles according to the general Formula (I) and the salts thereof, to pharmaceutical compositions comprising the sulfonamido-macrocycles and to a method of preparing the sulfonamido-macrocycles 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 angiopoietin and therefore influence Tie2 signalling. (I), wherein R1, R2, R4, A, X, Y, Z and m have the meaning as given in the specification and the claims.
摘要翻译： 本发明涉及根据通式（I）的亚磺酰氨基大环及其盐，涉及包含磺酰氨基大环的药物组合物，以及制备磺酰氨基大环的方法以及其用于制备用于 治疗血管生长失调的疾病或伴随血管生长失调的疾病，其中所述化合物有效地干扰血管生成素并因此影响Tie2信号传导。 （I）的化合物，其中R1，R2，R4，A，X，Y，Z和m具有说明书和权利要求书中给出的含义。
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公开(公告)号：EP2170839A1
公开(公告)日：2010-04-07
申请号：EP08773692.2
申请日：2008-06-19
发明人： HARTUNG, Ingo , BOTHE, Ulrich , KETTSCHAU, Georg , LUECKING, Ulrich , MENGEL, Anne , KRUEGER, Martin , THIERAUCH, Karl-Heinz , LIENAU, Philip , BOEMER, Ulf
IPC分类号： C07D239/48 , C07D401/06 , C07D403/06 , A61K31/495 , A61P29/00 , A61P35/00
CPC分类号： C07D239/48 , C07D401/06 , C07D403/06
摘要： The invention relates to alkynylpyrimidines according to the general formula (I) in which A, R
1 , R
2 , R
3 , R
4 , R
5 , and R
6 are as defined in the claims, to pharmaceutical compositions comprising said alkynylpyrimidines, to methods of preparing said alkynylpyrimidines, 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 and VEGFR2 signalling.摘要翻译： 本发明涉及根据通式（I）的炔基嘧啶，其中A，R 1，R 2，R 3，R 4，R 5和R 6如权利要求中所定义，涉及包含所述炔基嘧啶， 制备所述炔基嘧啶的方法以及其用于制备用于治疗血管生长失调疾病或伴随血管生长失调的疾病的药物组合物的用途，其中所述化合物有效地干扰Tie2和VEGFR2信号传导。
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9.发明公开3-H-PYRAZOLOPYRIDINES AND SALTS THEREOF, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, METHODS OF PREPARING SAME AND USES OF SAME 审中-公开3H-的吡唑并及其盐，药物组合物含有用于生产及其用途
公开(公告)号：EP2125808A2
公开(公告)日：2009-12-02
申请号：EP07857005.8
申请日：2007-12-14
IPC分类号： C07D471/04 , A61K31/437
CPC分类号： C07D471/04
摘要： The invention relates to 3-H-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, N-oxides, solvates and prodrugs thereof, to pharmaceutical compositions comprising said 3-H-pyrazolopyridine compounds, to methods of preparing said 3-H-pyrazolopyridines, to intermediate compounds useful in said methods, to uses of said intermediate compounds in the preparation of said 3-H-pyrazolopyridines, as well as to uses of said 3-H-pyrazolopyridines 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.
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10.发明公开SUBSTITUTED AMINOPYRAZOLOPYRIDINES AND SALTS THEREOF, THEIR PREPARATIONS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM 有权取代Aminopyrazolopyridine和它们的盐，它们的制备和含有它们的药物组合物
公开(公告)号：EP2061790A1
公开(公告)日：2009-05-27
申请号：EP07764753.5
申请日：2007-06-12
发明人： HARTUNG, Ingo , INCE, Stuart , KETTSCHAU, Georg , THIERAUCH, Karl-Heinz , BRIEM, Hans , BÖMER, Ulf
IPC分类号： C07D471/04 , A61K31/437 , A61P9/00 , A61P35/00 , C07D213/85 , C07F5/00
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.
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