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1.发明申请SUBSTITUTED SULPHOXIMINES AS TIE2 INHIBITORS AND SALTS THEREOF, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, METHODS OF PREPARING SAME AND USES OF SAME 有权替代的硫霉素作为TIE2抑制剂及其制备方法，包含其的药物组合物，其制备方法及其用途公开(公告)号：US20080064696A1
公开(公告)日：2008-03-13
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： C07D239/28 , A61K31/496 , A61K31/505 , A61K31/5377 , C07D403/12 , C07D413/12 , A61P19/00 , A61P35/00 , A61P9/00
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.
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 5，R 6，R 7，R 8， 权利要求书中给出m，p，q及其盐，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制备用于治疗的药物组合物的用途 的血管生长失调的疾病或伴有血管生长紊乱的疾病，其中所述化合物有效地干扰Tie2信号传导。
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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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3.发明申请SULFONAMIDO-MACROCYCLES AS TIE2 INHIBITORS AND SALTS THEREOF, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, METHODS OF PREPARING SAME AND USES OF SAME 审中-公开作为TIE2抑制剂及其制备方法的磺酰胺 - 大环化合物，包含其的药物组合物，其制备方法及其用途公开(公告)号：US20080039482A1
公开(公告)日：2008-02-14
申请号：US11765674
申请日：2007-06-20
申请人： Ingo Hartung , Hans Briem , Georg Kettschau , Karl-Heinz Thierauch , Ulrich Luecking , Ulf Boemer , Martina Schaefer , Philip Lienau
发明人： Ingo Hartung , Hans Briem , Georg Kettschau , Karl-Heinz Thierauch , Ulrich Luecking , Ulf Boemer , Martina Schaefer , Philip Lienau
IPC分类号： A61K31/519 , A61P35/00 , A61P9/00 , C07D513/02
CPC分类号： C07D513/08
摘要： The invention relates to sulfonamido-macrocycles according to the general formula (I): in which R1, R2, R4, R5, R6, A, B, C, L, X, Y, Z, n, and m are as defined in the claims, and salts, N-oxides, or solvates thereof, to pharmaceutical compositions comprising said sulfonamido-macrocycles, to methods of preparing said 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 Tie2 signalling.
摘要翻译： 本发明涉及根据通式（I）的磺酰氨基 - 大环化合物：其中R 1，R 2，R 4，R 4， A，B，C，L，X，Y，Z，n和m如权利要求中所定义，盐，N-氧化物， 或其溶剂化物，涉及包含所述磺酰氨基 - 大环化合物的药物组合物，制备所述磺酰胺 - 大环化合物的方法及其用于制备用于治疗失调血管生长疾病的药物组合物或伴随调节血管的疾病 生长，其中化合物有效地干扰Tie2信号传导。
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4.发明授权Substituted pyrazolopyridines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same 有权取代的吡唑并吡啶及其盐，包含其的药物组合物，其制备方法及其用途公开(公告)号：US07846928B2
公开(公告)日：2010-12-07
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，Ra，R1，R2，R3，R4，R5和q如权利要求中所定义， 包含所述取代的吡唑并吡啶化合物的药物组合物，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有血管生长失调的疾病的用途，其中所述化合物 有效干扰Tie2信号。
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5.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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6.发明申请Sulfonamido-macrocycles as Tie2 inhibitors and the salts thereof, a pharmaceutical composition comprising these compounds, the method of preparing and the use thereof 审中-公开作为Tie2抑制剂的磺酰胺 - 大环化合物及其盐，包含这些化合物的药物组合物，其制备方法及其应用公开(公告)号：US20060194823A1
公开(公告)日：2006-08-31
申请号：US11312648
申请日：2005-12-21
申请人： Georg Kettschau , Hans Briem , Ingo Hartung , Ulrich Luecking , Martina Schaefer , Karl-Heinz Thierauch , Wolfgang Schwede , Manfred Husemann
发明人： Georg Kettschau , Hans Briem , Ingo Hartung , Ulrich Luecking , Martina Schaefer , Karl-Heinz Thierauch , Wolfgang Schwede , Manfred Husemann
IPC分类号： A61K31/519 , C07D498/14
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. 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的磺酰胺 - 大环化合物及其盐，涉及包含磺酰氨基 - 大环化合物的药物组合物以及制备磺酰氨基 - 大环化合物的方法及其用于制备用于治疗的药物组合物的用途 的血管生长失调的疾病或伴随血管生成紊乱的疾病，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。 其中R 1，R 2，R 4，A，X，Y，Z和m具有说明书中给出的含义，并且 声称。
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7.发明申请Sulfonamido-macrocycles and the salts thereof, a pharmaceutical composition comprising these compounds, the method of preparing and the use thereof 审中-公开磺酰胺 - 大环化合物及其盐，包含这些化合物的药物组合物，其制备方法和用途公开(公告)号：US20060167030A1
公开(公告)日：2006-07-27
申请号：US11312646
申请日：2005-12-21
申请人： Georg Kettschau , Hans Briem , Andreas Huth , Ulrich Luecking , Martina Schaefer , Karl-Heinz Thierauch , Wolfgang Schwede , Manfred Husemann
发明人： Georg Kettschau , Hans Briem , Andreas Huth , Ulrich Luecking , Martina Schaefer , Karl-Heinz Thierauch , Wolfgang Schwede , Manfred Husemann
IPC分类号： A61K31/519 , C07D498/04
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. wherein R1, R2 and R3 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的磺酰胺 - 大环化合物及其盐，涉及包含磺酰氨基 - 大环化合物的药物组合物以及制备磺酰氨基 - 大环化合物的方法及其用于制备用于治疗的药物组合物的用途 的血管生长失调的疾病或伴随血管生成紊乱的疾病，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。 其中R 1，R 2，R 3和R 3具有说明书和权利要求书中给出的含义。
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8.发明申请Sulfoximine-macrocycle compounds and salts thereof, pharmaceutical compositions comprising said compounds, methods of preparing same and uses of same 审中-公开磺酰亚胺 - 大环化合物及其盐，包含所述化合物的药物组合物，其制备方法及其用途公开(公告)号：US20060252782A1
公开(公告)日：2006-11-09
申请号：US11399619
申请日：2006-04-07
申请人： Ulrich Luecking , Georg Kettschau , Hans Briem , Wolfgang Schwede , Martina Schaefer , Karl-Heinz Thierauch , Manfred Husemann
发明人： Ulrich Luecking , Georg Kettschau , Hans Briem , Wolfgang Schwede , Martina Schaefer , Karl-Heinz Thierauch , Manfred Husemann
IPC分类号： A61K31/519 , C07D487/14
CPC分类号： C07D209/48 , C07D239/42 , C07D513/08
摘要： The invention relates to macrocyctic sulfoximines of the general Formula 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.
摘要翻译： 本发明涉及通式I的大环氰基亚砜：其中A，X，Y，R 1，R 2和R 3具有 在说明书和权利要求书中给出的含义及其盐; 涉及包含大环亚磺酰亚胺的药物组合物，以及制备大环亚砜亚胺的方法及其制备用于治疗失调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 该化合物有效地干扰血管生成素，因此影响Tie2信号。
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9.发明授权Alkynylaryl compounds and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same 有权炔基芳基化合物及其盐，包含其的药物组合物，其制备方法及其用途公开(公告)号：US08481539B2
公开(公告)日：2013-07-09
申请号：US12747880
申请日：2008-12-04
申请人： Ingo Hartung , Hans Briem , Georg Kettschau , Karl-Heinz Thierauch , Ulf Bömer
发明人： Ingo Hartung , Hans Briem , Georg Kettschau , Karl-Heinz Thierauch , Ulf Bömer
IPC分类号： A01N43/58 , A01N43/60 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00 , C07D513/02 , C07D515/02 , A61K31/50 , A61K31/495
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.
摘要翻译： 本发明涉及根据通式（I）的炔基芳基化合物，其中A，B，D，E，Ra，R 1，R 3，R 4，R 5和q如权利要求中所定义，和盐，N-氧化物， 包括所述炔基芳基化合物的药物组合物，制备所述炔基芳基化合物的方法，可用于所述方法的中间体化合物，所述中间体化合物在制备所述炔基芳基化合物中的用途，以及所述炔基芳基 用于制备用于治疗失调的血管生长疾病或伴随血管生长失调的疾病的药物组合物的化合物。
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10.发明申请ALKYNYLARYL COMPOUNDS AND SALTS THEREOF, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, METHODS OF PREPARING SAME AND USES OF SAME 有权烷基化合物及其盐，其包含其的药物组合物，其制备方法及其用途公开(公告)号：US20100261730A1
公开(公告)日：2010-10-14
申请号：US12747880
申请日：2008-12-04
申请人： Ingo Hartung , Hans Briem , Georg Kettschau , Karl-Heinz Thierauch , Ulf Bömer
发明人： Ingo Hartung , Hans Briem , Georg Kettschau , Karl-Heinz Thierauch , Ulf Bömer
IPC分类号： A61K31/437 , C07D471/04 , A61K31/496
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.
摘要翻译： 本发明涉及根据通式（I）的炔基芳基化合物，其中A，B，D，E，Ra，R 1，R 3，R 4，R 5和q如权利要求中所定义，和盐，N-氧化物， 包括所述炔基芳基化合物的药物组合物，制备所述炔基芳基化合物的方法，可用于所述方法的中间体化合物，所述中间体化合物在制备所述炔基芳基化合物中的用途，以及所述炔基芳基 用于制备用于治疗失调的血管生长疾病或伴随血管生长失调的疾病的药物组合物的化合物。
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