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1. 发明授权

US07846928B2 Substituted pyrazolopyridines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same 有权
标题翻译：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。

2. 发明申请

US20080058326A1 SUBSTITUTED PYRAZOLOPYRIDINES AND SALTS THEREOF, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, METHODS OF PREPARING SAME AND USES OF SAME 有权
标题翻译：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。

3. 发明申请

US20090018129A1 SUBSTITUTED AMINOPYRAZOLOPYRIDINES AND SALTS THEREOF, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, METHODS OF PREPARING SAME AND USES OF SAME 有权
标题翻译：取代的氨基亚氨基吡啶及其盐，其包含其的药物组合物，其制备方法及其用途
公开(公告)号：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。

4. 发明申请

US20090005373A1 SUBSTITUTED SULFONAMIDO-MACROCYCLES AS TIE2 INHIBITORS AND SALTS THEREOF, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, METHODS OF PREPARING SAME AND USES OF SAME 审中-公开
标题翻译：作为TIE2抑制剂及其盐的取代的磺酰胺 - 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：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。

5. 发明授权

US07825114B2 Substituted aminopyrazolopyridines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same 有权
标题翻译：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。

6. 发明申请

US20060252754A1 Pyrazolopyridines and salts thereof, a pharmaceutical composition comprising said compounds, a method of preparing same and use of same 有权
标题翻译：吡唑并吡啶及其盐，包含所述化合物的药物组合物，其制备方法和用途
公开(公告)号：US20060252754A1
公开(公告)日：2006-11-09
申请号：US11337114
申请日：2006-01-23
申请人： Wolfgang Schwede , Hans Briem , Hermann Kuenzer , Manfred Husemann , Georg Kettschau , Martina Schaefer , Antonius Ter Laak , Karl-Heinz Thierauch , Stuart Ince
发明人： Wolfgang Schwede , Hans Briem , Hermann Kuenzer , Manfred Husemann , Georg Kettschau , Martina Schaefer , Antonius Ter Laak , Karl-Heinz Thierauch , Stuart Ince
IPC分类号： A61K31/53 , A61K31/506 , A61K31/497 , A61K31/4745 , C07D471/02
CPC分类号： C07D471/04
摘要： The invention relates to pyrazolopyridines according to the general formula (I): and salts thereof, to pharmaceutical compositions comprising said pyrazolopyridines and to a method of preparing said pyrazolopyridines 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：本发明涉及根据通式（I）的吡唑并吡啶及其盐，其包含所述吡唑并吡啶的药物组合物和制备所述吡唑并吡啶的方法及其用于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。

7. 发明申请

US20060116380A1 Novel anthranilamide pyridinureas as vascular endothelial growth factor (VEGF) receptor kinase inhibitors 失效
公开(公告)号：US20060116380A1
公开(公告)日：2006-06-01
申请号：US11265517
申请日：2005-11-03
申请人： Rolf Bohlmann , Martin Haberey , Andreas Huth , Stuart Ince , Martin Krueger , Karl-Heinz Thierauch , Holger Hess-Stumpp , Andreas Reichel
发明人： Rolf Bohlmann , Martin Haberey , Andreas Huth , Stuart Ince , Martin Krueger , Karl-Heinz Thierauch , Holger Hess-Stumpp , Andreas Reichel
IPC分类号： A61K31/506 , A61K31/501 , A61K31/4709 , A61K31/497 , A61K31/444 , C07D403/14 , C07D401/14
CPC分类号： C07D401/12
摘要： The invention relates to novel anthranilamide pyridinureas as VEGF receptor kinase inhibitors, their production and use as pharmaceutical agents for preventing or treating diseases that are triggered by persistent angiogenesis.

8. 发明授权

US07202260B2 VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridones 失效
标题翻译： VEGFR-2和VEGFR-3抑制性邻氨基苯甲酰胺吡啶酮
公开(公告)号：US07202260B2
公开(公告)日：2007-04-10
申请号：US10866078
申请日：2004-06-14
申请人： Andreas Huth , Martin Krueger , Ludwig Zorn , Stuart Ince , Rolf Bohlmann , Karl Heinz Thierauch , Andreas Menrad , Martin Haberey , Holger Hess-Stumpp
发明人： Andreas Huth , Martin Krueger , Ludwig Zorn , Stuart Ince , Rolf Bohlmann , Karl Heinz Thierauch , Andreas Menrad , Martin Haberey , Holger Hess-Stumpp
IPC分类号： C07D401/01 , C07D213/02 , A61K31/44
CPC分类号： C07D213/64
摘要： Novel VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridones and their use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis are selected.
摘要翻译：选择新型VEGFR-2和VEGFR-3抑制性邻氨基苯甲酰胺吡啶酮及其作为用于治疗由持续性血管生成引发的疾病的药物的用途。

9. 发明申请

US20060264425A1 Novel anthranilamide pyridinureas as vascular endothelial growth factor (VEGF) receptor kinase inhibitors 失效
标题翻译：新型邻氨基苯甲酰胺吡啶脲作为血管内皮生长因子（VEGF）受体激酶抑制剂
公开(公告)号：US20060264425A1
公开(公告)日：2006-11-23
申请号：US11265516
申请日：2005-11-03
申请人： Rolf Bohlmann , Martin Haberey , Andreas Huth , Stuart Ince , Martin Krueger , Karl-Heinz Thierauch , Holger Hess-Stumpp
发明人： Rolf Bohlmann , Martin Haberey , Andreas Huth , Stuart Ince , Martin Krueger , Karl-Heinz Thierauch , Holger Hess-Stumpp
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/496 , C07D417/14 , C07D413/14 , C07D403/14
CPC分类号： C07D213/75 , C07D401/12 , C07D401/14 , C07D491/10
摘要： The invention relates to novel anthranilamide pyridinureas as VEGF receptor kinase inhibitors, their production and use as pharmaceutical agents for preventing or treating diseases that are triggered by persistent angiogenesis.
摘要翻译：本发明涉及作为VEGF受体激酶抑制剂的新型邻氨基苯甲酰胺吡啶脲，其作为用于预防或治疗由持续血管生成引发的疾病的药剂的生产和用途。

10. 发明授权

US07517894B2 VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridines 失效
标题翻译： VEGFR-2和VEGFR-3抑制性邻氨基苯甲酰胺吡啶
公开(公告)号：US07517894B2
公开(公告)日：2009-04-14
申请号：US10870491
申请日：2004-06-18
申请人： Andreas Huth , Ludwig Zorn , Martin Krueger , Stuart Ince , Karl Heinz Thierauch , Andreas Menrad , Martin Haberey , Holger Hess-Stumpp
发明人： Andreas Huth , Ludwig Zorn , Martin Krueger , Stuart Ince , Karl Heinz Thierauch , Andreas Menrad , Martin Haberey , Holger Hess-Stumpp
IPC分类号： A61K31/4439 , C07D401/04
CPC分类号： C07D213/61 , C07D213/73 , C07D213/74 , C07D213/75 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/12 , C07D413/04 , C07D413/14 , C07D417/04
摘要： VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridinamides, their production and use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis, as well as intermediate products for the production of the compounds are described. The compounds according to the invention can be used as or in the case of tumor or metastasis growth, psoriasis, Kaposi's sarcoma, restenosis, such as, e.g., stent-induced restenosis, endometriosis, Crohn's disease, Hodgkin's disease, leukemia; arthritis, such as rheumatoid arthritis, hemangioma, angiofibroma; eye diseases, such as diabetic retinopathy, neovascular glaucoma; renal diseases, such as glomerulonephritis, diabetic nephropathy, malignant nephrosclerosis, thrombic microangiopathic syndrome, transplant rejections and glomerulopathy; fibrotic diseases, such as cirrhosis of the liver; mesangial cell proliferative diseases, arteriosclerosis, injuries to nerve tissue, and inhibition of the reocclusion of vessels after balloon catheter treatment, in vascular prosthetics or after mechanical devices are used to keep vessels open, such as, e.g., stents, as immunosuppressive agents, as a support in scar-free healing, senile keratosis and contact dermatitis. The compounds according to the invention can also be used as VEGFR-3 inhibitors in the case of lymphangiogenesis.
摘要翻译：描述了VEGFR-2和VEGFR-3抑制性邻氨基苯酰胺吡啶酰胺，其作为用于治疗由持续血管发生引起的疾病的药物的制备和用途，以及用于制备化合物的中间产物。根据本发明的化合物可用于或在肿瘤或转移生长的情况下，牛皮癣，卡波西肉瘤，再狭窄，例如支架诱导的再狭窄，子宫内膜异位，克罗恩病，霍奇金病，白血病; 关节炎，如类风湿关节炎，血管瘤，血管纤维瘤; 眼睛疾病如糖尿病性视网膜病变，新生血管性青光眼; 肾脏疾病如肾小球性肾炎，糖尿病肾病，恶性肾硬化，血栓性微血管病综合征，移植排斥反应和肾小球病; 纤维化疾病，如肝硬化; 肾小球膜细胞增生性疾病，动脉硬化，神经组织损伤，以及球囊导管治疗后血管假体中或使用机械装置用于保持血管开放（例如，支架）作为免疫抑制剂的抑制，作为免疫抑制剂无疤痕愈合，老年角化病和接触性皮炎的支持。在淋巴管生成的情况下，根据本发明的化合物也可以用作VEGFR-3抑制剂。

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