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。

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。

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。

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。

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。

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。

公开(公告)号：US20090018129A1

公开(公告)日：2009-01-15

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。

公开(公告)号：US20090005373A1

公开(公告)日：2009-01-01

申请号：US11765821

申请日：2007-06-20

申请人： Ingo Hartung ,  Hans Briem ,  Georg Kettschau ,  Karl-Heinz Thierauch ,  Ulrich Lucking ,  Ulf Bomer ,  Martina Schafer ,  Stuart Ince

发明人： Ingo Hartung ,  Hans Briem ,  Georg Kettschau ,  Karl-Heinz Thierauch ,  Ulrich Lucking ,  Ulf Bomer ,  Martina Schafer ,  Stuart Ince

IPC分类号： A61K31/5377 ,  C07D513/06 ,  A61P9/00 ,  A61P35/00 ,  A61K31/519

CPC分类号： C07D513/08

摘要： The invention relates to substituted sulfonamido-macrocycles according to the general formula (I): in which R1, R2, R4, R5, 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 substituted sulfonamido-macrocycles, to methods of preparing said substituted 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）的取代的亚磺酰氨基 - 大环化合物：其中R1，R2，R4，R5，A，B，C，L，X，Y，Z，n和m如 权利要求及其盐，N-氧化物或溶剂化物，包含所述取代的亚磺酰氨基 - 大环化合物的药物组合物，以及制备所述取代的亚磺酰氨基 - 大环化合物的方法及其制备用于治疗失调的疾病的药物组合物的用途 血管生长或伴随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。

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。

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。