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1. 发明授权

US08999982B2 Pharmaceutically active compounds as Axl inhibitors 有权
标题翻译：作为Axl抑制剂的药物活性化合物
公开(公告)号：US08999982B2
公开(公告)日：2015-04-07
申请号：US13819560
申请日：2011-08-26
申请人： Carsten Schultz-Fademrecht , Bert Klebl , Axel Choidas , Uwe Koch , Jan Eickhoff , Alexander Wolf , Axel Ullrich
发明人： Carsten Schultz-Fademrecht , Bert Klebl , Axel Choidas , Uwe Koch , Jan Eickhoff , Alexander Wolf , Axel Ullrich
IPC分类号： A61K31/495 , A61K31/47 , C07D401/12 , C07D401/14 , C07D417/12 , C07D417/14 , C07D413/12 , C07D413/14 , C07D215/233
CPC分类号： C07D401/12 , A61K31/47 , A61K31/495 , C07D215/233 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention relates to 1-nitrogen-heterocyclic-2-carboxamides and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the treatment and/or prevention of Axl receptor tyrosine kinase subfamily induced disorders, including cancer and primary tumor metastases, and pharmaceutical compositions containing at least one of said 1-nitrogen-heterocyclic-2-carboxamide derivatives and/or pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及1-氮杂环-2-甲酰胺和/或其药学上可接受的盐，这些衍生物用作药物活性剂，特别是用于治疗和/或预防Axl受体酪氨酸激酶亚家族诱导的病症，包括癌症和原发性肿瘤转移，以及含有至少一种所述1-氮杂环-2-甲酰胺衍生物和/或其药学上可接受的盐的药物组合物。

2. 发明申请

US20140018365A1 PHARMACEUTICALLY ACTIVE COMPOUNDS AS AXL INHIBITORS 有权
标题翻译：药物活性化合物作为AXL抑制剂
公开(公告)号：US20140018365A1
公开(公告)日：2014-01-16
申请号：US13819560
申请日：2011-08-26
申请人： Carsten Schultz-Fademrecht , Bert Klebl , Axel Choidas , Uwe Koch , Jan Eickhoff , Alexander Wolf , Axel Ullrich
发明人： Carsten Schultz-Fademrecht , Bert Klebl , Axel Choidas , Uwe Koch , Jan Eickhoff , Alexander Wolf , Axel Ullrich
IPC分类号： C07D401/12 , C07D215/233 , C07D417/12 , C07D413/14 , C07D417/14 , C07D401/14
CPC分类号： C07D401/12 , A61K31/47 , A61K31/495 , C07D215/233 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention relates to 1-nitrogen-heterocyclic-2-carboxamides and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the treatment and/or prevention of Axl receptor tyrosine kinase subfamily induced disorders, including cancer and primary tumor metastases, and pharmaceutical compositions containing at least one of said 1-nitrogen-heterocyclic-2-carboxamide derivatives and/or pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及1-氮杂环-2-甲酰胺和/或其药学上可接受的盐，这些衍生物用作药物活性剂，特别是用于治疗和/或预防Axl受体酪氨酸激酶亚家族诱导的病症，包括癌症和原发性肿瘤转移，以及含有至少一种所述1-氮杂环-2-甲酰胺衍生物和/或其药学上可接受的盐的药物组合物。

3. 发明授权

US08591903B2 Inhibition of TACE or amphiregulin for the modulation of EGF receptor signal transactivation 失效
公开(公告)号：US08591903B2
公开(公告)日：2013-11-26
申请号：US12400122
申请日：2009-03-09
申请人： Axel Ullrich , Andreas Gschwind , Stefan Hart
发明人： Axel Ullrich , Andreas Gschwind , Stefan Hart
IPC分类号： A61K39/00 , A61K39/395 , A61K49/00
CPC分类号： C12N9/6489 , A61K38/005 , C07K14/485
摘要： The present invention relates to the modulation of transactivation of receptor tyrosine kinases by G protein or G protein-coupled receptor (GPCR) mediated signal transduction in a cell or an organism comprising inhibiting the activity of the metalloprotease TACE/ADAM17 and/or the activity of the receptor tyrosine kinase ligand amphiregulin.

4. 发明申请

US20120277231A1 QUINOLINYLOXYPHENYLSULFONAMIDES 有权
标题翻译：喹啉啉氧基硅烷
公开(公告)号：US20120277231A1
公开(公告)日：2012-11-01
申请号：US13500761
申请日：2010-10-16
申请人： Axel Ullrich , Robert Torku , Yixiang Zhang , György Kéri , László Örfi , István Szabadkai
发明人： Axel Ullrich , Robert Torku , Yixiang Zhang , György Kéri , László Örfi , István Szabadkai
IPC分类号： A61K31/47 , A61K31/4709 , A61P35/00 , A61K31/496 , C07D405/12 , C07D401/14 , C07D413/12 , A61K31/5375 , C07D215/233 , C07D401/12 , C07D409/14
CPC分类号： C07D417/12 , C07D215/20 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12
摘要： The present invention relates to quinolinyloxyphenylsulfonamides and stereoisomeric forms, solvates, hydrates and/or pharmaceutically acceptable salts of these quinolinyloxyphenylsulfonamide compounds as well as pharmaceutical compositions containing at least one of these compounds together with at least one pharmaceutically acceptable carrier, excipient and/or diluent. Said quinolinyloxyphenylsulfonamides are useful for prophylaxsis, treatment and/or after-treatment of hyperproliferative disorders, such as cancer, tumors and particularly cancer metastases.
摘要翻译：本发明涉及这些喹啉氧基苯基磺酰胺化合物的喹啉氧基苯磺酰胺和立体异构形式，溶剂合物，水合物和/或药学上可接受的盐，以及含有至少一种这些化合物以及至少一种药学上可接受的载体，赋形剂和/或稀释剂的药物组合物。所述喹啉氧基苯基磺酰胺可用于预防，治疗和/或治疗过度增殖性疾病，如癌症，肿瘤，特别是癌症转移。

5. 发明授权

US08277802B2 Diagnosis and prevention of cancer cell invasion 有权
标题翻译：诊断和预防癌细胞侵袭
公开(公告)号：US08277802B2
公开(公告)日：2012-10-02
申请号：US10521410
申请日：2003-07-17
申请人： Axel Ullrich , Pjotr Knyazev , Tatjana Knyazeva , Yuri Cheburkin , Peter Vajkoczy
发明人： Axel Ullrich , Pjotr Knyazev , Tatjana Knyazeva , Yuri Cheburkin , Peter Vajkoczy
IPC分类号： A61K39/395 , A61K39/00
CPC分类号： A61K39/3955 , A61K2039/505 , C07K16/2863 , C12Q1/6886 , C12Q2600/136
摘要： The present invention relates to diagnostic and therapeutic methods in the field of malignant disorders. Most particularly, the invention provides methods of determining the invasivity of malignant disorders and methods for reducing the invasivity of malignant disorders including the prevention or treatment of cancer cell invasion.
摘要翻译：本发明涉及恶性疾病领域的诊断和治疗方法。最特别地，本发明提供了确定恶性疾病的侵袭性的方法和降低恶性疾病的侵袭性的方法，包括预防或治疗癌细胞侵袭。

6. 发明申请

US20110179505A1 RODENT CANCER MODEL FOR HUMAN FGFR4 ARG388 POLYMORPHISM 审中-公开
标题翻译：人类FGFR4 ARG388多态性模型
公开(公告)号：US20110179505A1
公开(公告)日：2011-07-21
申请号：US13121202
申请日：2009-09-29
申请人： Axel Ullrich , Thomas Mayer , Sylvia Streit , Nina Seitzer
发明人： Axel Ullrich , Thomas Mayer , Sylvia Streit , Nina Seitzer
IPC分类号： A01K67/00 , A01K67/027 , C12N5/10 , A61K38/22 , C07H21/00 , C12N15/85 , G01N33/574 , C07H21/02 , C07K16/18
CPC分类号： C12N15/8509 , A01K67/0275 , A01K2217/072 , A01K2227/105 , A01K2267/0331 , C07K14/71
摘要： The present invention provides a rodent animal for studying the molecular mechanisms and physiological processes associated with uncontrolled cell growth, e.g. cancer, and with a modified FGFR4.
摘要翻译：本发明提供了一种啮齿动物，用于研究与不受控制的细胞生长相关的分子机制和生理过程，例如，癌症和改良的FGFR4。

7. 发明申请

US20100184686A1 USE OF INHIBITORS FOR THE TREATMENT OF RTK-HYPERFUNCTION-INDUCED DISORDERS, PARTICULARLY CANCER 有权
标题翻译：使用抑制剂治疗RTK超敏感性疾病，特别是癌症
公开(公告)号：US20100184686A1
公开(公告)日：2010-07-22
申请号：US12689672
申请日：2010-01-19
申请人： Axel Ullrich , Johannes Bange , Pjotr Knyazev
发明人： Axel Ullrich , Johannes Bange , Pjotr Knyazev
IPC分类号： A61K38/17 , C07K14/71 , C07H21/04 , C07K16/28 , A61P35/04 , A61P35/00 , C12Q1/68 , C12Q1/48
CPC分类号： C07K14/71 , A61K38/00 , G01N33/574
摘要： The present invention concerns the use of inhibitors for the treatment and/or prophylaxis of diseases which are the consequence of increased receptor tyrosine kinase activity, particularly cancer. The use is particularly directed towards inhibition or lowering of the overexpression and/or altered activity of receptor tyrosine kinases (RTKs). In particular, this altered activity of receptor tyrosine kinase can be triggered by a mutation of FGFR-4, wherein this mutation is in particular a point mutation in the transmembrane domain of FGFR-4 and leads to an exchange of a hydrophobic amino acid for a hydrophilic amino acid. The invention further concerns the use of an inhibitor directed against FGFR-4, for the treatment and/or prophylaxis of cancer. Furthermore, the invention concerns a mutated FGFR-4, which leads to over-expression and/or altered activity in cells. Finally, the invention concerns a DNA and RNA sequence of a mutated FGFR-4 molecule. Finally, in addition the invention concerns a pharmaceutical composition, containing the inhibitor as described above and further a diagnostic and screening procedure.
摘要翻译：本发明涉及抑制剂用于治疗和/或预防由于受体酪氨酸激酶活性增加，特别是癌症引起的疾病的用途。该用途特别涉及抑制或降低受体酪氨酸激酶（RTK）的过表达和/或改变的活性。特别地，受体酪氨酸激酶的这种改变的活性可以由FGFR-4的突变引发，其中该突变特别是FGFR-4的跨膜结构域中的点突变，并导致疏水性氨基酸的交换亲水氨基酸。本发明还涉及使用针对FGFR-4的抑制剂来治疗和/或预防癌症。此外，本发明涉及突变的FGFR-4，其导致细胞中过度表达和/或改变的活性。最后，本发明涉及突变的FGFR-4分子的DNA和RNA序列。最后，本发明还涉及包含如上所述的抑制剂的药物组合物，并进一步进行诊断和筛选程序。

8. 发明授权

US07297774B2 Use of inhibitors for the treatment of RTK-hyperfunction-induced disorders, particularly cancer 有权
标题翻译：使用抑制剂治疗RTK-超功能障碍，特别是癌症
公开(公告)号：US07297774B2
公开(公告)日：2007-11-20
申请号：US10863880
申请日：2004-06-08
申请人： Axel Ullrich , Johannes Bange , Pjotr Knyazev
发明人： Axel Ullrich , Johannes Bange , Pjotr Knyazev
IPC分类号： C07K14/00 , C12N15/11 , C12P21/06
CPC分类号： C07K14/71 , A61K38/00 , G01N33/574
摘要： The present invention concerns the use of inhibitors for the treatment and/or prophylaxis of diseases which are the consequence of increased receptor tyrosine kinase activity, particularly cancer. The use is particularly directed towards inhibition or lowering of the overexpression and/or altered activity of receptor tyrosine kinases (RTKs). In particular, this altered activity of receptor tyrosine kinase can be triggered by a mutation of FGFR-4, wherein this mutation is in particular a point mutation in the transmembrane domain of FGFR-4 and leads to an exchange of a hydrophobic amino acid for a hydrophilic amino acid. The invention further concerns the use of an inhibitor directed against FGFR-4, for the treatment and/or prophylaxis of cancer. Furthermore, the invention concerns a mutated FGFR-4, which leads to overexpression and/or altered activity in cells. Finally, the invention concerns a DNA and RNA sequence of a mutated FGFR-4 molecule. Finally, in addition the invention concerns a pharmaceutical composition, containing the inhibitor as described above and further a diagnostic and screening procedure.
摘要翻译：本发明涉及抑制剂用于治疗和/或预防由于受体酪氨酸激酶活性增加，特别是癌症引起的疾病的用途。该用途特别涉及抑制或降低受体酪氨酸激酶（RTK）的过表达和/或改变的活性。特别地，受体酪氨酸激酶的这种改变的活性可以由FGFR-4的突变引发，其中该突变特别是FGFR-4的跨膜结构域中的点突变，并导致疏水性氨基酸的交换亲水氨基酸。本发明还涉及使用针对FGFR-4的抑制剂来治疗和/或预防癌症。此外，本发明涉及突变的FGFR-4，其导致细胞中的过表达和/或改变的活性。最后，本发明涉及突变的FGFR-4分子的DNA和RNA序列。最后，本发明还涉及包含如上所述的抑制剂的药物组合物，并进一步进行诊断和筛选程序。

9. 发明申请

US20060148694A1 Inhibition of stress-induced ligand-dependent egfr activation 审中-公开
标题翻译：抑制应激诱导的配体依赖性egfr活化
公开(公告)号：US20060148694A1
公开(公告)日：2006-07-06
申请号：US10563211
申请日：2004-07-05
申请人： Axel Ullrich , Oliver Fischer
发明人： Axel Ullrich , Oliver Fischer
IPC分类号： A61K48/00 , A61K38/17
CPC分类号： C12N15/1137 , A61K39/3955 , A61K45/06 , C12N2310/14 , A61K2300/00
摘要： The present invention relates to the inhibition of stress-induced receptor tyrosine kinase activity by inhibiting a ligand of said receptor tyrosine kinase, particularly an extracellular ligand.
摘要翻译：本发明涉及通过抑制所述受体酪氨酸激酶，特别是细胞外配体的配体来抑制应激诱导的受体酪氨酸激酶活性。

10. 发明申请

US20060099708A1 Methods for diagnosis and treatment of MDK1 signal transduction disorders 审中-公开
标题翻译： MDK1信号转导障碍的诊断和治疗方法
公开(公告)号：US20060099708A1
公开(公告)日：2006-05-11
申请号：US11303935
申请日：2005-12-19
申请人： Thomas Ciossek , Axel Ullrich , Birgit Millauer
发明人： Thomas Ciossek , Axel Ullrich , Birgit Millauer
IPC分类号： C12N5/06 , C07K16/40
CPC分类号： C07K16/40 , A61K38/00 , C07K14/71
摘要： The present invention relates to MDK1 polypeptides, nucleic acids encoding such polypeptides, cells, tissues and animals containing such nucleic acids, antibodies to such polypeptides, assays utilizing such polypeptides, and methods relating to all of the foregoing. Methods for treatment, diagnosis, and screening are provided for diseases or conditions characterized by an abnormality in a signal transduction disorder. The signal transduction pathway involves an interaction between a MDK1 receptor tyrosine kinase and a receptor for the kinase. The MDK1 receptor tyrosine kinase may be truncated and lack a kinase domain and may be selected from the group consisting of MDK1.T1, MDK1.T2, MDK1.Δ1 and MDK1.Δ2.
摘要翻译：本发明涉及MDK1多肽，编码这种多肽的核酸，含有此类核酸的细胞，组织和动物，对这些多肽的抗体，利用这些多肽的测定法，以及与上述所有相关的方法。提供治疗，诊断和筛查的方法用于以信号转导障碍异常为特征的疾病或病症。信号转导途径涉及MDK1受体酪氨酸激酶与激酶受体之间的相互作用。 MDK1受体酪氨酸激酶可能被截短并缺少激酶结构域，并且可以选自MDK1.T1，MDK1T2，MDK1Delta1和MDK1Delta2。

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