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1. 发明授权

US08394801B2 Quinoxaline derivatives and their use for treating benign and malignant tumour disorders 失效
标题翻译：喹喔啉衍生物及其用于治疗良性和恶性肿瘤疾病的用途
公开(公告)号：US08394801B2
公开(公告)日：2013-03-12
申请号：US12731243
申请日：2010-03-25
申请人： Matthias Gerlach , Irene Seipelt , Eckhard Guenther , Tilmann Schuster , Emmanuel Polymeropoulos , Michael Czech , Eckhard Claus
发明人： Matthias Gerlach , Irene Seipelt , Eckhard Guenther , Tilmann Schuster , Emmanuel Polymeropoulos , Michael Czech , Eckhard Claus
IPC分类号： A61K31/495
CPC分类号： C07D241/44 , C07D401/12 , C07D403/04 , C07D409/12 , C07D413/12
摘要： The invention provides quinoxalines of the general formula I which are used as medicaments preferably for treating tumour disorders, in particular in cases of drug resistance to other active compounds and in cases of metastasic carcinoma. The possible applications are not limited to tumour disorders.
摘要翻译：本发明提供了通式I的喹喔啉，其用作优选用于治疗肿瘤病症的药物，特别是在对其它活性化合物的耐药性和转移性癌症的情况下。可能的应用不限于肿瘤病症。

2. 发明申请

US20070123494A1 PYRIDOPYRAZINE DERIVATIVES AND THEIR USE 有权
标题翻译：吡咯并吡啶衍生物及其用途
公开(公告)号：US20070123494A1
公开(公告)日：2007-05-31
申请号：US11558493
申请日：2006-11-10
申请人： Irene SEIPELT , Eckhard Claus , Eckhard Guenther , Tilmann Schuster , Michael Czech , Emmanuel Polymeropoulos
发明人： Irene SEIPELT , Eckhard Claus , Eckhard Guenther , Tilmann Schuster , Michael Czech , Emmanuel Polymeropoulos
IPC分类号： A61K31/5415 , A61K31/5377 , A61K31/506 , A61K31/501 , A61K31/498 , C07D487/02
CPC分类号： A61K45/06 , A61K31/4985 , C07D471/04
摘要： The present invention provides new pyridopyrazine compounds which are suitable for the treatment or prevention of physiological and/or pathophysiological states mediated and/or modulated by signal transduction pathways and/or enzymes in mammals and in particular in humans.
摘要翻译：本发明提供了适用于治疗或预防由哺乳动物，特别是人类中的信号转导途径和/或酶介导和/或调节的生理和/或病理生理状态的新的吡啶并吡嗪化合物。

3. 发明申请

US20070026436A1 GLUCOSE TRANSPORT-RELATED GENES, POLYPEPTIDES, AND METHODS OF USE THEREOF 审中-公开
标题翻译：葡萄糖运输相关基因，多肽及其使用方法
公开(公告)号：US20070026436A1
公开(公告)日：2007-02-01
申请号：US11460102
申请日：2006-07-26
申请人： Michael Czech , Abhijit Chakladar , Adilson Guilherme , Xiaoqing Tang
发明人： Michael Czech , Abhijit Chakladar , Adilson Guilherme , Xiaoqing Tang
IPC分类号： C12Q1/68 , C12Q1/54 , A61K48/00
CPC分类号： G01N33/6872 , A61K48/00 , C12N15/111 , C12N15/1137 , C12N2310/11 , C12N2310/12 , C12N2310/14 , C12N2320/12 , C12Q1/485 , G01N33/66 , G01N2500/00 , G01N2800/044
摘要： Methods and compositions for modulating glucose transport are provided herein.
摘要翻译：本文提供了调节葡萄糖转运的方法和组合物。

4. 发明申请

US20050208054A1 Methods of identifying insulin response modulators and uses therefor 审中-公开
标题翻译：识别胰岛素反应调节剂及其用途的方法
公开(公告)号：US20050208054A1
公开(公告)日：2005-09-22
申请号：US11009554
申请日：2004-12-09
申请人： Michael Czech , Zhen Jiang
发明人： Michael Czech , Zhen Jiang
IPC分类号： A61K39/395 , C07K16/40 , G01N33/50 , G01N33/53 , G01N33/567
CPC分类号： C07K16/40 , G01N33/5041 , G01N33/507 , G01N2333/62
摘要： Methods of identifying insulin response modulators are provided. In particular, methods that feature identifying modulators of Akt and its associated substrates (including R-type calcium channel alpha-1E subunit (R-CaC1E), WNK1, FMS interacting protein (FMIP), nGAP-like protein, nuclear matrix protein p84, HIRA interacting protein 3 (HIRIP3), HSP71, ribosomal protein L6, guanine nucleotide exchange factor Lbc (GEF Lbc), ATP citrate lyase, Mi-2b, peripheral benzodiazepine receptor-associated protein 1, heterogeneous nuclear ribonucleoprotein U (hnRNP U protein), pyruvate carboxylase precursor, Eps domain containing protein (RalBP1), nonmuscle myosin IIA (NMMIIA), and stress 70 protein (p66 mot1/GRP75), or activities associated therewith, are provided. Therapeutic methods utilizing compounds identified according to the methods of the invention are also provided.
摘要翻译：提供了确定胰岛素反应调节剂的方法。特别地，鉴定Akt及其相关底物（包括R型钙通道α-1E亚基（R-CaC1E），WNK1，FMS相互作用蛋白（FMIP），nGAP样蛋白，核基质蛋白p84， HIRA相互作用蛋白3（HIRIP3），HSP71，核糖体蛋白L6，鸟嘌呤核苷酸交换因子Lbc（GEF Lbc），ATP柠檬酸裂合酶，Mi-2b，外周苯并二氮杂受体相关蛋白1，异源核核糖核蛋白U（hnRNP U蛋白）丙酮酸羧化酶前体，含有Eps结构域的蛋白（RalBP1），非肌肉肌球蛋白IIA（NMMIIA）和应激70蛋白（p66 mot1 / GRP75）或与其相关的活性。使用根据本发明方法鉴定的化合物的治疗方法也提供。

5. 发明申请

US20050059007A1 Glucose transport-related genes and uses thereof 审中-公开
标题翻译：葡萄糖转运相关基因及其用途
公开(公告)号：US20050059007A1
公开(公告)日：2005-03-17
申请号：US10610018
申请日：2003-06-30
申请人： Michael Czech , Andrew Cherniack , Adilson Guilherme
发明人： Michael Czech , Andrew Cherniack , Adilson Guilherme
IPC分类号： C07K14/47 , C07K14/62 , C12Q1/68 , C12Q1/6883 , C12M1/34
CPC分类号： C07K14/47 , C07K14/62 , C12Q1/6883 , C12Q2600/158 , G01N2500/04
摘要： Nucleotide sequences and amino acid sequences from nucleic acids and proteins involved in glucose transport are disclosed. The sequences are useful for producing DNA arrays that can be used for the diagnosis of, predictive testing for, and development of treatments for disorders involving glucose transport such as type II diabetes.
摘要翻译：披露了参与葡萄糖转运的核酸和蛋白质的核苷酸序列和氨基酸序列。该序列可用于产生可用于诊断，预测测试和开发涉及葡萄糖转运的病症的治疗如II型糖尿病的DNA阵列。

6. 发明申请

US20120252760A1 NOVEL PYRIDOPYRAZINES AND THEIR USE AS MODULATORS OF KINASES 审中-公开
标题翻译：新颖的吡咯啉及其作为动物调节剂的使用
公开(公告)号：US20120252760A1
公开(公告)日：2012-10-04
申请号：US13523968
申请日：2012-06-15
申请人： Eckhard Claus , Irene Seipelt , Eckhard Guenther , Emmanuel Polymeropoulos , Michael Czech , Tilmann Schuster
发明人： Eckhard Claus , Irene Seipelt , Eckhard Guenther , Emmanuel Polymeropoulos , Michael Czech , Tilmann Schuster
IPC分类号： A61K31/4985 , C07F7/18 , C07F9/6561 , A61P1/16 , A61K31/695 , A61K31/675 , A61P17/06 , A61P9/10 , C07D471/04 , A61K31/5377
CPC分类号： A61K31/4985 , A61K31/5377 , A61K31/675 , A61K31/695 , C07D487/04
摘要： The invention relates to novel pyrido[2,3-b]pyrazine derivatives of the general formulae (I) and (II), and to their preparation and use as medicaments, especially for the treatment of malignant disorders and other disorders based on pathological cell proliferations.
摘要翻译：本发明涉及通式（I）和（II）的新型吡啶并[2,3-b]吡嗪衍生物及其作为药物的制备和用途，特别是用于治疗基于病理细胞的恶性疾病和其它病症激增。

7. 发明申请

US20050261223A1 RIP140 regulation of glucose transport 有权
标题翻译： RIP140调节葡萄糖转运
公开(公告)号：US20050261223A1
公开(公告)日：2005-11-24
申请号：US11075646
申请日：2005-03-07
申请人： Michael Czech , Aimee Powelka , Adilson Guilherme , Andrew Cherniack
发明人： Michael Czech , Aimee Powelka , Adilson Guilherme , Andrew Cherniack
IPC分类号： A61K38/17 , A61K39/395 , A61K48/00 , G01N33/50 , G01N33/68
CPC分类号： G01N33/6875 , G01N33/502 , G01N2500/00 , G01N2800/042 , G01N2800/044
摘要： Inhibition of RIP140 increases glucose transport. Compounds that inhibit RIP140 expression or activity are useful for treating disorders associated with aberrant glucose transport (e.g., diabetes), treating obesity, increasing metabolism (e.g., fatty acid metabolism), and increasing brown fat.
摘要翻译：抑制RIP140增加葡萄糖转运。抑制RIP140表达或活性的化合物可用于治疗与异常葡萄糖转运（例如糖尿病）相关的疾病，治疗肥胖症，增加代谢（例如脂肪酸代谢）和增加棕色脂肪。

8. 发明申请

US20050009809A1 Acridine derivatives and their use as medicaments 审中-公开
标题翻译：吖啶衍生物及其用作药物
公开(公告)号：US20050009809A1
公开(公告)日：2005-01-13
申请号：US10879280
申请日：2004-06-29
申请人： Matthias Gerlach , Peter Emig , Klaus Paulini , Michael Czech , Tilman Schuster , Eckhard Gunther
发明人： Matthias Gerlach , Peter Emig , Klaus Paulini , Michael Czech , Tilman Schuster , Eckhard Gunther
IPC分类号： A61K31/496 , A61K31/551 , C07D219/04 , C07D219/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D493/04 , C07
CPC分类号： C07D219/04 , C07D219/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D493/04
摘要： The invention relates to novel acridine derivatives of the formula 1, to their preparation and to their use as medicaments, in particular for the treatment of tumors.
摘要翻译：本发明涉及式1的新型吖啶衍生物，其制备及其用作药物，特别是用于治疗肿瘤。

9. 发明授权

US08937068B2 Pyridopyrazine derivatives and their use 有权
标题翻译：吡啶并吡嗪衍生物及其用途
公开(公告)号：US08937068B2
公开(公告)日：2015-01-20
申请号：US11558493
申请日：2006-11-10
申请人： Irene Seipelt , Eckhard Claus , Eckhard Guenther , Tilmann Schuster , Michael Czech , Emmanuel Polymeropoulos
发明人： Irene Seipelt , Eckhard Claus , Eckhard Guenther , Tilmann Schuster , Michael Czech , Emmanuel Polymeropoulos
IPC分类号： A61K31/4985 , C07D471/04 , C07D519/00 , A61K45/06
CPC分类号： A61K45/06 , A61K31/4985 , C07D471/04
摘要： Pyridopyrazine compounds which are suitable for the treatment or prevention of physiological and/or pathophysiological states mediated and/or modulated by signal transduction pathways and/or enzymes in mammals and in particular in humans. A compound according to the general formula (I)
摘要翻译：吡啶并吡嗪类化合物，其适用于治疗或预防由哺乳动物，特别是人类中的信号转导途径和/或酶介导和/或调节的生理和/或病理生理状态。根据通式（I）的化合物，

10. 发明申请

US20100266538A1 QUINOXALINE DERIVATIVES AND THEIR USE FOR TREATING BENIGN AND MALIGNANT TUMOUR DISORDERS 失效
标题翻译：喹啉衍生物及其用于治疗恶性肿瘤恶病质的用途
公开(公告)号：US20100266538A1
公开(公告)日：2010-10-21
申请号：US12731243
申请日：2010-03-25
申请人： Matthias Gerlach , Irene Seipelt , Eckhard Guenther , Tilmann Schuster , Emmanuel Polymeropoulos , Michael Czech , Eckhard Claus
发明人： Matthias Gerlach , Irene Seipelt , Eckhard Guenther , Tilmann Schuster , Emmanuel Polymeropoulos , Michael Czech , Eckhard Claus
IPC分类号： A61K38/21 , C07D241/44 , A61K31/498 , A61K38/46 , A61K38/14 , A61K33/24 , A61K31/573 , A61P35/00 , A61P35/04
CPC分类号： C07D241/44 , C07D401/12 , C07D403/04 , C07D409/12 , C07D413/12
摘要： The invention provides quinoxalines of the general formula I which are used as medicaments preferably for treating tumour disorders, in particular in cases of drug resistance to other active compounds and in cases of metastasic carcinoma. The possible applications are not limited to tumour disorders.
摘要翻译：本发明提供了通式I的喹喔啉，其用作优选用于治疗肿瘤病症的药物，特别是在对其它活性化合物的耐药性和转移性癌症的情况下。可能的应用不限于肿瘤病症。

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