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1. 发明授权

US06579972B1 Extracellular signal-regulated kinase, sequences, and methods of production and use 失效
标题翻译：细胞外信号调节激酶，序列和生产和使用方法
公开(公告)号：US06579972B1
公开(公告)日：2003-06-17
申请号：US09393212
申请日：1999-09-09
申请人： Cornelia Lechner , Niels Peter Møller , Axel Ullrich
发明人： Cornelia Lechner , Niels Peter Møller , Axel Ullrich
IPC分类号： C07K1640
CPC分类号： C07K16/40 , A61K38/00 , A61K48/00 , C07K2319/00 , C12N9/12 , C12N2799/021 , Y10S530/809
摘要： The present invention relates, in general, to an extracellular signal regulated kinase, ERK-5. In particular, the present invention relates to nucleic acid molecules coding for ERK-5; ERK-5 polypeptides; recombinant nucleic acid molecules; cells containing the recombinant nucleic acid molecules; antisense ERK-5 nucleic acid constructs; antibodies having binding affinity to an ERK-5 polypeptide; hybridomes containing the antibodies; nucleic acid probes for the detecting of ERK-5 nucleic acid; a method of detecting ERK-5 nucleic acid or polypeptide in a sample; kits containing nucleic acid probes or antibodies; a method of detecting a compound capable of binding to ERK-5 or a fragment thereof; a method of detecting an agonist or antagonist of ERK-5 activity; a method of agonizing or antagonizing ERK-5 associated activity in a mammal; a method of treating diabetes mellitus, skeletal muscle diseases, Alzheimer's disease, or peripheral neuropathies in a mammal with an agonist or antagonist of ERK-5 activity; and a pharmaceutical composition comprising an ERK-5 agonist or antagonist.
摘要翻译：本发明一般涉及细胞外信号调节激酶ERK-5。特别地，本发明涉及编码ERK-5的核酸分子; ERK-5多肽; 重组核酸分子; 含有重组核酸分子的细胞; 反义ERK-5核酸构建体; 对ERK-5多肽具有结合亲和力的抗体; 含有抗体的杂交瘤; 用于检测ERK-5核酸的核酸探针; 在样品中检测ERK-5核酸或多肽的方法; 含有核酸探针或抗体的试剂盒; 检测能够结合ERK-5或其片段的化合物的方法; 检测ERK-5活性的激动剂或拮抗剂的方法; 在哺乳动物中激动或拮抗ERK-5相关活性的方法; 在具有ERK-5活性的激动剂或拮抗剂的哺乳动物中治疗糖尿病，骨骼肌疾病，阿尔茨海默氏病或周围神经病变的方法; 和包含ERK-5激动剂或拮抗剂的药物组合物。

2. 发明授权

US5459036A Extracellular signal-regulated kinase, sequences, and methods of production and use 失效
标题翻译：细胞外信号调节激酶，序列和生产和使用方法
公开(公告)号：US5459036A
公开(公告)日：1995-10-17
申请号：US29404
申请日：1993-03-19
申请人： Cornelia Lechner , Niels P. H. Moller , Axel Ullrich
发明人： Cornelia Lechner , Niels P. H. Moller , Axel Ullrich
IPC分类号： C12N15/02 , A61K38/00 , A61K38/45 , A61K39/395 , A61K48/00 , A61P3/08 , A61P3/10 , A61P25/28 , A61P43/00 , C07H21/04 , C07K5/103 , C07K14/47 , C07K16/40 , C12N5/06 , C12N5/10 , C12N5/12 , C12N9/12 , C12N15/09 , C12N15/54 , C12P21/02 , C12P21/08 , C12Q1/68 , C12R1/91
CPC分类号： C07K16/40 , C12N9/12 , A61K38/00 , A61K48/00 , C07K2319/00 , C12N2799/021 , Y10S530/809
摘要： The present invention relates, in general, to an extracellular signal regulated kinase, ERK-5. In particular, the present invention relates to nucleic acid molecules coding for ERK-5; ERK-5 polypeptides; recombinant nucleic acid molecules; cells containing the recombinant nucleic acid molecules; antisense ERK-5 nucleic acid constructs; antibodies having binding affinity to an ERK-5 polypeptide; hybridomas containing the antibodies; nucleic acid probes for the detection of ERK-5 nucleic acid; a method of detecting ERK-5 nucleic acid or polypeptide in a sample; kits containing nucleic acid probes or antibodies; a method of detecting a compound capable of binding to ERK-5 or a fragment thereof; a method of detecting an agonist or antagonist of ERK-5 activity; a method of agonizing or antagonizing ERK-5 associated activity in a mammal; and a pharmaceutical composition comprising an ERK-5 agonist or antagonist.
摘要翻译：本发明一般涉及细胞外信号调节激酶ERK-5。特别地，本发明涉及编码ERK-5的核酸分子; ERK-5多肽; 重组核酸分子; 含有重组核酸分子的细胞; 反义ERK-5核酸构建体; 对ERK-5多肽具有结合亲和力的抗体; 含有抗体的杂交瘤; 用于检测ERK-5核酸的核酸探针; 在样品中检测ERK-5核酸或多肽的方法; 含有核酸探针或抗体的试剂盒; 检测能够结合ERK-5或其片段的化合物的方法; 检测ERK-5活性的激动剂或拮抗剂的方法; 在哺乳动物中激动或拮抗ERK-5相关活性的方法; 和包含ERK-5激动剂或拮抗剂的药物组合物。

3. 发明授权

US6030822A Extracellular signal-regulated kinase, sequences, and methods of production and use 失效
公开(公告)号：US6030822A
公开(公告)日：2000-02-29
申请号：US459953
申请日：1995-06-02
申请人： Cornelia Lechner , Niels Peter M.o slashed.ller , Axel Ullrich
发明人： Cornelia Lechner , Niels Peter M.o slashed.ller , Axel Ullrich
IPC分类号： C12N15/02 , A61K38/00 , A61K38/45 , A61K39/395 , A61K48/00 , A61P3/08 , A61P3/10 , A61P25/28 , A61P43/00 , C07H21/04 , C07K5/103 , C07K14/47 , C07K16/40 , C12N5/06 , C12N5/10 , C12N5/12 , C12N9/12 , C12N15/09 , C12N15/54 , C12P21/02 , C12P21/08 , C12Q1/68 , C12R1/91 , C07K14/46
CPC分类号： C07K16/40 , C12N9/12 , A61K38/00 , A61K48/00 , C07K2319/00 , C12N2799/021 , Y10S530/809
摘要： The present invention relates, in general, to an extracellular signal regulated kinase, ERK-5. In particular, the present invention relates to nucleic acid molecules coding for ERK-5; ERK-5 polypeptides; recombinant nucleic acid molecules; cells containing the recombinant nucleic acid molecules; antisense ERK-5 nucleic acid constructs; antibodies having binding affinity to an ERK-5 polypeptide; hybridomes containing the antibodies; nucleic acid probes for the detecting of ERK-5 nucleic acid; a method of detecting ERK-5 nucleic acid or polypeptide in a sample; kits containing nucleic acid probes or antibodies; a method of detecting a compound capable of binding to ERK-5 or a fragment thereof; a method of detecting an agonist or antagonist of ERK-5 activity; a method of agonizing or antagonizing ERK-5 associated activity in a mammal; a method of treating diabetes mellitus, skeletal muscle diseases, Alzheimer's disease, or peripheral neuropathies in a mammal with an agonist or antagonist of ERK-5 activity; and a pharmaceutical composition comprising an ERK-5 agonist or antagonist.

4. 发明授权

US07371828B2 Extracellular signal-regulated kinase sequences and methods of production and use 失效
标题翻译：细胞外信号调节激酶序列及其生产和使用方法
公开(公告)号：US07371828B2
公开(公告)日：2008-05-13
申请号：US10461402
申请日：2003-06-16
申请人： Cornelia Lechner , Niels P. Moller , Axel Ullrich
发明人： Cornelia Lechner , Niels P. Moller , Axel Ullrich
IPC分类号： C07K16/40
CPC分类号： C07K16/40 , A61K38/00 , A61K48/00 , C07K2319/00 , C12N9/12 , C12N2799/021 , Y10S530/809
摘要： The present invention relates, in general, to an extracellular signal regulated kinase, ERK-5. In particular, the present invention relates to nucleic acid molecules coding for ERK-5; ERK-5 polypeptides; recombinant nucleic acid molecules; cells containing the recombinant nucleic acid molecules; antisense ERK-5 nucleic acid constructs; antibodies having binding affinity to an ERK-5 polypeptide; hybridomes containing the antibodies; nucleic acid probes for the detecting of ERK-5 nucleic acid; a method of detecting ERK-5 nucleic acid or polypeptide in a sample; kits containing nucleic acid probes or antibodies; a method of detecting a compound capable of binding to ERK-5 or a fragment thereof; a method of detecting an agonist or antagonist of ERK-5 activity; a method of agonizing or antagonizing ERK-5 associated activity in a mammal; a method of treating diabetes mellitus, skeletal muscle diseases, Alzheimer's disease, or peripheral neuropathies in a mammal with an agonist or antagonist of ERK-5 activity; and a pharmaceutical composition comprising an ERK-5 agonist or antagonist.
摘要翻译：本发明一般涉及细胞外信号调节激酶ERK-5。特别地，本发明涉及编码ERK-5的核酸分子; ERK-5多肽; 重组核酸分子; 含有重组核酸分子的细胞; 反义ERK-5核酸构建体; 对ERK-5多肽具有结合亲和力的抗体; 含有抗体的杂交瘤; 用于检测ERK-5核酸的核酸探针; 在样品中检测ERK-5核酸或多肽的方法; 含有核酸探针或抗体的试剂盒; 检测能够结合ERK-5或其片段的化合物的方法; 检测ERK-5活性的激动剂或拮抗剂的方法; 在哺乳动物中激动或拮抗ERK-5相关活性的方法; 在具有ERK-5活性的激动剂或拮抗剂的哺乳动物中治疗糖尿病，骨骼肌疾病，阿尔茨海默氏病或周围神经病变的方法; 和包含ERK-5激动剂或拮抗剂的药物组合物。

5. 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.

6. 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。

7. 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。

8. 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。

9. 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。

10. 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。

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