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1. 发明申请

US20110104066A1 PROPHYLACTIC/THERAPEUTIC AGENTS FOR LIFESTYLE-RELATED DISEASES 有权
标题翻译：生物相容性疾病的预防/治疗药物
公开(公告)号：US20110104066A1
公开(公告)日：2011-05-05
申请号：US12991155
申请日：2009-05-08
申请人： Hajime Nawata , Toshihiko Yanase , Takayoshi Nakagawa
发明人： Hajime Nawata , Toshihiko Yanase , Takayoshi Nakagawa
IPC分类号： A61K49/00 , C12Q1/68 , C07D311/78 , C07C49/563 , A61K31/573 , A61K31/585 , A61K31/352 , A61P3/04 , A61P3/10 , A61P3/06 , A61P9/12
CPC分类号： A61K31/57 , A61K31/56 , G01N33/5044 , G01N33/689 , G01N33/6893 , G01N33/74 , G01N2800/02 , G01N2800/042 , G01N2800/044 , G01N2800/321
摘要： Disclosed is a method for the screening of a compound having an activity to selectively modulate an androgen receptor. The method comprises the steps of: contacting a substance to be tested with a prostate cancer cell and measuring the level of expression of mRNA for a prostate-specific antigen or the level of production of the prostate-specific antigen in the prostate cancer cell; and contacting the substance with an adipocyte and measuring the level of expression of mRNA for uncoupling protein-1 or the level of production of uncoupling protein-1 in the adipocyte. Also disclosed is a selective androgen receptor modulator comprising a compound represented by any one formula selected from the structural formulae (I) to (III) as an active ingredient. Further disclosed is a composition for preventing or treating lifestyle-related diseases, which comprises the selective androgen receptor modulator.
摘要翻译：披露了筛选具有选择性调节雄激素受体活性的化合物的方法。该方法包括以下步骤：使待测物质与前列腺癌细胞接触，并测量前列腺特异性抗原mRNA表达水平或前列腺癌细胞中前列腺特异性抗原产生水平; 并将该物质与脂肪细胞接触并测量mRNA的表达水平以解偶联蛋白-1或脂肪细胞中解偶联蛋白-1的产生水平。还公开了包含由选自结构式（I）至（III）的任何一种式表示的化合物作为活性成分的选择性雄激素受体调节剂。进一步公开的是用于预防或治疗生活方式相关疾病的组合物，其包含选择性雄激素受体调节剂。

2. 发明授权

US08623909B2 Prophylactic/therapeutic agents for lifestyle-related diseases 有权
标题翻译：生活方式相关疾病的预防/治疗药物
公开(公告)号：US08623909B2
公开(公告)日：2014-01-07
申请号：US12991155
申请日：2009-05-08
申请人： Hajime Nawata , Toshihiko Yanase , Takayoshi Nakagawa
发明人： Hajime Nawata , Toshihiko Yanase , Takayoshi Nakagawa
IPC分类号： C07D311/78 , A61K31/35
CPC分类号： A61K31/57 , A61K31/56 , G01N33/5044 , G01N33/689 , G01N33/6893 , G01N33/74 , G01N2800/02 , G01N2800/042 , G01N2800/044 , G01N2800/321
摘要： Disclosed is a method for screening a compound having an activity that selectively modulates an androgen receptor, comprising a step of measuring the mRNA expression level of prostate-specific antigen or the production level of prostate-specific antigen in prostate cancer cells by contacting a test substance with the prostate cancer cells, and a step of measuring the mRNA expression level of uncoupling protein 1 or the production level of uncoupling protein 1 in adipocytes by contacting a test substance with the adipocytes. Additionally disclosed is a selective androgen receptor modulator, comprising as an active ingredient thereof a compound represented by any of structural formulas (I) to (III), and a composition for preventing or treating a lifestyle-related disease, comprising as an active ingredient thereof said selective androgen receptor modulator.
摘要翻译：公开了一种筛选具有选择性调节雄激素受体活性的化合物的方法，包括通过使测试物质接触测量前列腺癌细胞中前列腺特异性抗原的mRNA表达水平或前列腺特异性抗原的产生水平的步骤与前列腺癌细胞，以及通过使测试物质与脂肪细胞接触来测量解偶联蛋白1的mRNA表达水平或脂肪细胞中解偶联蛋白1的产生水平的步骤。另外公开了一种选择性雄激素受体调节剂，其包含作为其活性成分的由结构式（I）至（III）中任一项表示的化合物和用于预防或治疗与生活方式有关的疾病的组合物，其包含作为其活性成分所述选择性雄激素受体调节剂。

3. 发明授权

US07018806B2 Method for identifying endocrine disruptors and kit for carrying out the same 失效
公开(公告)号：US07018806B2
公开(公告)日：2006-03-28
申请号：US10929691
申请日：2004-08-31
申请人： Hajime Nawata , Toshihiko Yanase
发明人： Hajime Nawata , Toshihiko Yanase
IPC分类号： C12Q1/26
CPC分类号： G01N33/5011 , C12Q1/26 , G01N33/5008 , G01N33/502 , G01N33/5044
摘要： A method for identifying an endocrine disrupter using a cell line having aromatase activity, particularly, a human granulosa-like tumor cell line; and a kit for carrying out the method is disclosed.

4. 发明申请

US20050032136A1 Method for identifying endocrine disruptors and kit for carrying out the same 失效
标题翻译：确定内分泌干扰物的方法和用于实施内分泌干扰物的试剂盒
公开(公告)号：US20050032136A1
公开(公告)日：2005-02-10
申请号：US10929691
申请日：2004-08-31
申请人： Hajime Nawata , Toshihiko Yanase
发明人： Hajime Nawata , Toshihiko Yanase
IPC分类号： C12N5/08 , C12Q1/26 , G01N33/50 , G01N33/574
CPC分类号： G01N33/5011 , C12Q1/26 , G01N33/5008 , G01N33/502 , G01N33/5044
摘要： A method for identifying an endocrine disrupter using a cell line having aromatase activity, particularly, a human granulosa-like tumor cell line; and a kit for carrying out the method is disclosed.
摘要翻译：使用具有芳香酶活性的细胞系，特别是人粒细胞样肿瘤细胞系鉴定内分泌干扰物的方法; 并公开了用于实施该方法的套件。

5. 发明授权

US06803206B2 Method for identifying endocrine disruptors and kit for carrying out the same 失效
标题翻译：确定内分泌干扰物的方法和用于实施内分泌干扰物的试剂盒
公开(公告)号：US06803206B2
公开(公告)日：2004-10-12
申请号：US10029862
申请日：2001-12-31
申请人： Hajime Nawata , Toshihiko Yanase
发明人： Hajime Nawata , Toshihiko Yanase
IPC分类号： C12Q126
CPC分类号： G01N33/5011 , C12Q1/26 , G01N33/5008 , G01N33/502 , G01N33/5044
摘要： A method for identifying an endocrine disruptor using a cell line having aromatase activity, particularly, a human granulosa-like tumor cell line; and a kit for carrying out the method is disclosed.
摘要翻译：使用具有芳香酶活性的细胞系，特别是人粒细胞样肿瘤细胞系鉴定内分泌干扰物的方法; 并公开了用于实施该方法的套件。

6. 发明授权

US06794398B1 Preventive/remedies for liver diseases 有权
标题翻译：预防/治疗肝病
公开(公告)号：US06794398B1
公开(公告)日：2004-09-21
申请号：US09959441
申请日：2002-03-06
申请人： Makoto Nakamuta , Hajime Nawata , Masayoshi Uehata
发明人： Makoto Nakamuta , Hajime Nawata , Masayoshi Uehata
IPC分类号： A61K3153
CPC分类号： C07D471/04 , A61K31/16 , A61K31/437 , A61K31/44 , A61K31/4409 , C07D213/75
摘要： The invention provides an agent for the prophylaxis and treatment of liver disease and an activation inhibitor of hepatic stellate cells, which contains a compound having a Rho kinase inhibitory activity. The compound having a Rho kinase inhibitory activity, such as (+)-trans-4-(1-aminoethyl)-1-(4-pyridylcarbamoyl)cyclohexane, is useful for the prophylaxis and treatment of liver diseases, such as hepatitis, hepatic fibrosis, hepatic cirrhosis, hepatic cancer and the like, because it has various actions, such as a superior inhibitory action on the activation of hepatic stellate cell, suppressive action on hepatic fibrogenesis in liver tissues and the like.
摘要翻译：本发明提供了预防和治疗肝脏疾病的药剂和肝星状细胞的活化抑制剂，其含有具有Rho激酶抑制活性的化合物。具有Rho激酶抑制活性的化合物如（+） - 反式-4-（1-氨基乙基）-1-（4-吡啶基氨基甲酰基）环己烷可用于预防和治疗肝脏疾病如肝炎，肝脏纤维化，肝硬化，肝癌等，因为具有对肝星状细胞活化的优异抑制作用，对肝组织中肝纤维发生的抑制作用等各种作用。

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