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1. 发明申请

WO2004041256A3 SAFE CHEMICAL UNCOUPLERS FOR THE TREATMENT OF OBESITY 审中-公开
标题翻译：治疗肥胖的安全化学联合疗法
公开(公告)号：WO2004041256A3
公开(公告)日：2004-09-02
申请号：PCT/DK0300742
申请日：2003-10-31
申请人： NOVO NORDISK AS
发明人： HANSEN BIRGIT SEHESTED , TULLIN SOEREN , HANSEN THOMAS KRUSE , COLDING-JOERGENSEN MORTEN
IPC分类号： A61K31/166 , A61K31/17 , A61K31/19 , A61K31/216 , A61K31/40 , A61K31/404 , C07D213/70 , C07D277/32 , C07D295/192 , C07D295/26 , C07D307/28 , C07D307/38 , C07D311/16 , C07D333/34 , A61K31/04 , A61K31/06 , C07C205/12 , C12N5/00 , C12Q1/00 , G01N33/50
CPC分类号： C07D213/70 , A61K31/166 , A61K31/17 , A61K31/19 , A61K31/216 , A61K31/40 , A61K31/404 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/42 , C07D277/32 , C07D295/192 , C07D295/26 , C07D307/28 , C07D307/38 , C07D311/16 , C07D333/34
摘要： This invention relates to chemical uncouplers with a broader safety window making the use of them in treating obesity and, consequently, in the treatment of obesity related dis-eases and conditions such as atherosclerosis, hypertension, diabetes, especially type 2 dia-betes (NIDDM (non-insulin dependent diabetes mellitus)), impaired glucose tolerance, dyslip-idemia, coronary heart disease, gallbladder disease, osteoarthritis and various types of can-cer such as endometrial, breast, prostate and colon cancers and the risk for premature death as well as other conditions, such as diseases and disorders, which conditions are improved by an increase in mitochondrial respiration, more attractive.
摘要翻译：本发明涉及具有更宽安全窗口的化学解偶联剂，使其用于治疗肥胖症，并因此用于治疗与肥胖有关的疾病和病症，如动脉粥样硬化，高血压，糖尿病，特别是2型糖尿病（NIDDM （非胰岛素依赖型糖尿病）），葡萄糖耐量降低，血脂异常，冠心病，胆囊疾病，骨关节炎和各种类型的癌症，如子宫内膜癌，乳腺癌，前列腺癌和结肠癌以及过早死亡的风险以及其他条件，如疾病和病症，这些条件通过增加线粒体呼吸而得到改善，更具吸引力。

2. 发明申请

WO9845704A2 A METHOD FOR EXTRACTING QUANTITATIVE INFORMATION RELATING TO AN INFLUENCE ON A CELLULAR RESPONSE 审中-公开
标题翻译：提取与细胞响应影响相关的量化信息的方法
公开(公告)号：WO9845704A2
公开(公告)日：1998-10-15
申请号：PCT/DK9800145
申请日：1998-04-07
申请人： NOVO NORDISK AS , THASTRUP OLE , PETERSEN BJOERN SARA , TULLIN SOEREN , KASPER ALMHOLT , SCUDDER KURT
发明人： THASTRUP OLE , PETERSEN BJOERN SARA , TULLIN SOEREN , KASPER ALMHOLT , SCUDDER KURT
IPC分类号： C12Q1/25 , C12Q1/48 , G01N33/50 , G01N33/533 , G01N33/58 , G01N33/53
CPC分类号： G01N33/5041 , G01N33/5005 , G01N33/5008 , G01N33/5014 , G01N33/5035 , G01N33/533 , G01N33/582 , G01N2333/43595 , G01N2333/9121
摘要： Cells are genetically modified to expresss a luminophore, e.g., a modified (F64L, S65T, Y66H) Green Fluorescent Protein (GFP, EGFP) coupled to a component of an intracellular signalling pathway such as a transcription factor, a cGMP- or cAMP-dependent protein kinase, a cyclin-, calmodulin- or phospholipid-dependent or mitogen-activated serine/threonin protein kinase, a tyrosine protein kinase, or a protein phosphatase (e.g. PKA, PKC, Erk, Smad, VASP, actin, p38, Jnk1, PKG, IkappaB, CDK2, Grk5, Zap70, p85, protein-tyrosine phosphatase 1C, Stat5, NFAT, NFkappaB, RhoA, PKB). An influence modulates the intracellular signalling pathway in such a way that the luminophore is being redistributed or translocated with the component in living cells in a manner experimentally determined to be correlated to the degree of the influence. Measurement of redistribution is performed by recording of light intensity, fluorescence lifetime, polarization, wavelength shift, resonance energy transfer, or other properties by an apparatus consisting of e.g. a fluorescence microscope and a CCD camera. Data stored as digital images are processed to numbers representing the degree of redistribution. The method can be used as a screening program for identifying a compound that modulates a component and is capable of treating a disease related to the function of the component.
摘要翻译：细胞被遗传修饰以表达发光体，例如与细胞内信号传导途径的组分偶联的经修饰的（F64L，S65T，Y66H）绿色荧光蛋白（GFP，EGFP），例如转录因子，cGMP-或cAMP依赖性蛋白激酶，细胞周期蛋白，钙调蛋白或磷脂依赖性或丝裂原活化丝氨酸/苏氨酸蛋白激酶，酪氨酸蛋白激酶或蛋白磷酸酶（例如PKA，PKC，Erk，Smad，VASP，肌动蛋白，p38，Jnk1， PKG，IkappaB，CDK2，Grk5，Zap70，p85，蛋白质 - 酪氨酸磷酸酶1C，Stat5，NFAT，NFkappaB，RhoA，PKB）。影响调节细胞内信号传导途径，使得发光体在活细胞中以组分重新分配或移位，其方式经实验确定与影响程度相关。重新分布的测量是通过记录光强度，荧光寿命，极化，波长偏移，共振能量转移或其它性质通过由例如，荧光显微镜和CCD相机。作为数字图像存储的数据被处理成表示再分配程度的数字。该方法可以用作鉴定调节成分并能够治疗与该成分的功能有关的疾病的化合物的筛选程序。

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