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1. 发明申请

US20050154029A1 Human G protein-coupled receptors and modulators thereof for the treatment of metabolic-related disorders 有权
标题翻译：人G蛋白偶联受体及其调节剂用于治疗代谢相关疾病
公开(公告)号：US20050154029A1
公开(公告)日：2005-07-14
申请号：US10930662
申请日：2004-08-31
申请人： David Unett , Ruoping Chen , Jeremy Richman , Daniel Connolly , Huong Dang , Bryan Choi , James Leonard , Yaron Hakak , Chen Liaw , Dominic Behan , Derek Chalmers , Michael Lerner , Kevin Lowitz
发明人： David Unett , Ruoping Chen , Jeremy Richman , Daniel Connolly , Huong Dang , Bryan Choi , James Leonard , Yaron Hakak , Chen Liaw , Dominic Behan , Derek Chalmers , Michael Lerner , Kevin Lowitz
IPC分类号： A61K31/4439 , G01N33/566 , C07D43/02
CPC分类号： C07D403/02 , A01K2217/00 , A01K2227/105 , A01K2267/03 , A61K31/4439 , C07K14/705 , G01N33/566 , G01N2333/726 , G01N2500/00
摘要： The present invention relates to methods of identifying whether a candidate compound is a modulator of a G protein-coupled receptor (GPCR). In preferred embodiments, the GPCR is human. In other preferred embodiments, the GPCR is coupled to Gi and lowers the level of intracellular cAMP. In other preferred embodiments, the GPCR is expressed endogenously by adipocytes. In further preferred embodiments, the GPCR inhibits intracellular lipolysis. In other further preferred embodiments, the GPCR is a nicotinic acid receptor. The present invention also relates to methods of using a modulator of said GPCR. Preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for the prevention or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, stroke, insulin resistance, and type 2 diabetes.
摘要翻译：本发明涉及鉴定候选化合物是G蛋白偶联受体（GPCR）的调节剂的方法。在优选的实施方案中，GPCR是人。在其它优选实施方案中，GPCR与Gi偶联并降低细胞内cAMP的水平。在其它优选实施方案中，GPCR由脂肪细胞内源性表达。在进一步优选的实施方案中，GPCR抑制细胞内脂肪分解。在其它进一步优选的实施方案中，GPCR是烟酸受体。本发明还涉及使用所述GPCR的调节剂的方法。优选的调节剂是激动剂。本发明的激动剂可用作预防或治疗代谢相关疾病，包括血脂异常，动脉粥样硬化，冠心病，中风，胰岛素抵抗和2型糖尿病的治疗剂。

2. 发明申请

US20070079392A1 Human G protein-coupled receptors and modulators thereof for the treatment of metabolic-related disorders 审中-公开
标题翻译：人G蛋白偶联受体及其调节剂用于治疗代谢相关疾病
公开(公告)号：US20070079392A1
公开(公告)日：2007-04-05
申请号：US11603625
申请日：2006-11-22
申请人： Chen Liaw , Dominic Behan , Derek Chalmers , Michael Lerner , Huong Dang , Bryan Choi , James Leonard , Yaron Hakak , Kevin Lowitz , David Unett , Ruoping Chen , Jeremy Richman , Daniel Connolly
发明人： Chen Liaw , Dominic Behan , Derek Chalmers , Michael Lerner , Huong Dang , Bryan Choi , James Leonard , Yaron Hakak , Kevin Lowitz , David Unett , Ruoping Chen , Jeremy Richman , Daniel Connolly
IPC分类号： A01K67/027 , G01N33/53 , C12P21/06 , C07D403/02 , C07K14/705
CPC分类号： C07D403/02 , A01K2217/00 , A01K2227/105 , A01K2267/03 , A61K31/4439 , C07K14/705 , G01N33/566 , G01N2333/726 , G01N2500/00
摘要： The present invention relates to methods of identifying whether a candidate compound is a modulator of a G protein-coupled receptor (GPCR). In preferred embodiments, the GPCR is human. In other preferred embodiments, the GPCR is coupled to Gi and lowers the level of intracellular cAMP. In other preferred embodiments, the GPCR is expressed endogenously by adipocytes. In further preferred embodiments, the GPCR inhibits intracellular lipolysis. In other further preferred embodiments, the GPCR is a nicotinic acid receptor. The present invention also relates to methods of using a modulator of said GPCR. Preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for the prevention or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, stroke, insulin resistance, and type 2 diabetes.
摘要翻译：本发明涉及鉴定候选化合物是G蛋白偶联受体（GPCR）的调节剂的方法。在优选的实施方案中，GPCR是人。在其它优选实施方案中，GPCR与Gi偶联并降低细胞内cAMP的水平。在其它优选实施方案中，GPCR由脂肪细胞内源性表达。在进一步优选的实施方案中，GPCR抑制细胞内脂肪分解。在其它进一步优选的实施方案中，GPCR是烟酸受体。本发明还涉及使用所述GPCR的调节剂的方法。优选的调节剂是激动剂。本发明的激动剂可用作预防或治疗代谢相关疾病，包括血脂异常，动脉粥样硬化，冠心病，中风，胰岛素抵抗和2型糖尿病的治疗剂。

3. 发明申请

US20050004178A1 Human G protein-coupled receptors and modulators thereof for the treatment of metabolic-related disorders 审中-公开
公开(公告)号：US20050004178A1
公开(公告)日：2005-01-06
申请号：US10897815
申请日：2004-07-23
申请人： David Unett , Ruoping Chen , Jeremy Richman , Daniel Connolly , Chen Liaw , Dominic Behan , Derek Chalmers , Michael Lerner , Huong Dang , Bryan Choi , James Leonard , Yaron Hakak , Kevin Lowitz
发明人： David Unett , Ruoping Chen , Jeremy Richman , Daniel Connolly , Chen Liaw , Dominic Behan , Derek Chalmers , Michael Lerner , Huong Dang , Bryan Choi , James Leonard , Yaron Hakak , Kevin Lowitz
IPC分类号： A61K31/4439 , G01N33/566 , G01N33/53
CPC分类号： C07D403/02 , A01K2217/00 , A01K2227/105 , A01K2267/03 , A61K31/4439 , C07K14/705 , G01N33/566 , G01N2333/726 , G01N2500/00
摘要： The present invention relates to methods of identifying whether a candidate compound is a modulator of a G protein-coupled receptor (GPCR). In preferred embodiments, the GPCR is human. In other preferred embodiments, the GPCR is coupled to Gi and lowers the level of intracellular cAMP. In other preferred embodiments, the GPCR is expressed endogenously by adipocytes. In further preferred embodiments, the GPCR inhibits intracellular lipolysis. In other further preferred embodiments, the GPCR is a nicotinic acid receptor. The present invention also relates to methods of using a modulator of said GPCR. Preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for the prevention or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, stroke, insulin resistance, and type 2 diabetes.

4. 发明申请

US20110177612A1 Human G Protein-Coupled Receptors and Modulators Thereof for the Treatment of Metabolic-Related Disorders 审中-公开
标题翻译：人类G蛋白偶联受体及其调节剂用于治疗代谢相关性疾病
公开(公告)号：US20110177612A1
公开(公告)日：2011-07-21
申请号：US12881014
申请日：2010-09-13
申请人： David J. Unett , Ruoping Chen , Jeremy G. Richman , Daniel Connolly , Huong T. Dang , Bryan Choi , James Leonard , Yaron Hakak , Chen Liaw , Dominic Behan , Derek Chalmers , Michael Lerner , Kevin P. Lowitz
发明人： David J. Unett , Ruoping Chen , Jeremy G. Richman , Daniel Connolly , Huong T. Dang , Bryan Choi , James Leonard , Yaron Hakak , Chen Liaw , Dominic Behan , Derek Chalmers , Michael Lerner , Kevin P. Lowitz
IPC分类号： G01N33/68
CPC分类号： C07D403/02 , A01K2217/00 , A01K2227/105 , A01K2267/03 , A61K31/4439 , C07K14/705 , G01N33/566 , G01N2333/726 , G01N2500/00
摘要： The present invention relates to methods of identifying whether a candidate compound is a modulator of a G protein-coupled receptor (GPCR). In preferred embodiments, the GPCR is human. In other preferred embodiments, the GPCR is coupled to Gi and lowers the level of intracellular cAMP. In other preferred embodiments, the GPCR is expressed endogenously by adipocytes. In further preferred embodiments, the GPCR inhibits intracellular lipolysis. In other further preferred embodiments, the GPCR is a nicotinic acid receptor. The present invention also relates to methods of using a modulator of said GPCR. Preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for the prevention or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, stroke, insulin resistance, and type 2 diabetes.
摘要翻译：本发明涉及鉴定候选化合物是G蛋白偶联受体（GPCR）的调节剂的方法。在优选的实施方案中，GPCR是人。在其它优选实施方案中，GPCR与Gi偶联并降低细胞内cAMP的水平。在其它优选实施方案中，GPCR由脂肪细胞内源性表达。在进一步优选的实施方案中，GPCR抑制细胞内脂肪分解。在其它进一步优选的实施方案中，GPCR是烟酸受体。本发明还涉及使用所述GPCR的调节剂的方法。优选的调节剂是激动剂。本发明的激动剂可用作预防或治疗代谢相关疾病，包括血脂异常，动脉粥样硬化，冠心病，中风，胰岛素抵抗和2型糖尿病的治疗剂。

5. 发明申请

US20070231263A1 Human G protein-coupled receptor and modulators thereof for the treatment of hyperglycemia and related disorders 审中-公开
标题翻译：人G蛋白偶联受体及其调节剂用于治疗高血糖症和相关疾病
公开(公告)号：US20070231263A1
公开(公告)日：2007-10-04
申请号：US11604178
申请日：2006-11-22
申请人： Jun Qiu , Robert Webb , David Unett , Joel Gatlin , Daniel Connolly
发明人： Jun Qiu , Robert Webb , David Unett , Joel Gatlin , Daniel Connolly
IPC分类号： A61K48/00 , A61K31/44 , A61K49/00 , C07D417/00 , C07K14/00 , C12N5/06
CPC分类号： C07D417/04 , G01N2333/726 , G01N2500/04 , G01N2800/042
摘要： The present invention relates to methods of identifying whether one or more candidate compounds is a modulator of a G protein-coupled receptor (GPCR) or a modulator of blood glucose concentration. In certain embodiments, the GPCR is human. The present invention also relates to methods of using a modulator of the GPCR. A preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for lowering blood glucose concentration, for preventing or treating certain metabolic disorders, such as insulin resistance, impaired glucose tolerance, and diabetes, and for preventing or treating a complication of an elevated blood glucose concentration, such as atherosclerosis, heart disease, stroke, hypertension and peripheral vascular disease.
摘要翻译：本发明涉及鉴定一种或多种候选化合物是G蛋白偶联受体（GPCR）或血糖浓度调节剂的调节剂的方法。在某些实施方案中，GPCR是人。本发明还涉及使用GPCR的调制器的方法。优选的调节剂是激动剂。本发明的激动剂可用作降低血糖浓度的治疗剂，用于预防或治疗某些代谢紊乱，例如胰岛素抵抗，葡萄糖耐量异常和糖尿病，以及用于预防或治疗血糖浓度升高的并发症，作为动脉粥样硬化，心脏病，中风，高血压和外周血管疾病。

6. 发明申请

US20070232519A1 Human G protein-coupled receptor and modulators thereof for the treatment of cardiovascualr disorders 审中-公开
标题翻译：人G蛋白偶联受体及其调节剂用于治疗心血管疾病
公开(公告)号：US20070232519A1
公开(公告)日：2007-10-04
申请号：US11604187
申请日：2006-11-22
申请人： John Adams , Daniel Connolly
发明人： John Adams , Daniel Connolly
IPC分类号： A61K48/00 , A01H5/00 , C12N5/06 , G01N33/53
CPC分类号： C07K14/705 , A01K2217/05 , A01K2217/075 , A01K2227/105 , A01K2227/108 , A01K2267/0375 , G01N2333/726 , G01N2500/10 , G01N2800/325
摘要： The present invention relates to methods of identifying whether a candidate compound is a modulator of a G protein-coupled receptor (GPCR). In some embodiments, the GPCR is mammalian, preferably human. In some embodiments, the GPCR is expressed endogenously by cardiomyocytes. In some embodiments, the GPCR is coupled to Gq. In some embodiments, the GPCR increases the intracellular level of inositol 1,4,5-triphosphate (IP3). In some embodiments, a modulator of the GPCR is a modulator of cardiomyocyte hypertrophy. The present invention further relates to methods of using a modulator of the GPCR. Preferred modulators are inverse agonists and antagonists. Inverse agonists and antagonists of the invention are useful as therapeutic agents for the prevention or treatment of heart disease, including hypertrophic cardiomyopathy and congestive heart failure, in particular hypertrophic cardiomyopathy resulting from post-myocardial infarction remodeling, cardiac valve disease, sustained cardiac afterload, myocarditis, and familial hypertrophic cardiomyopathy.
摘要翻译：本发明涉及鉴定候选化合物是G蛋白偶联受体（GPCR）的调节剂的方法。在一些实施方案中，GPCR是哺乳动物，优选人。在一些实施方案中，GPCR由心肌细胞内源性表达。在一些实施例中，GPCR耦合到Gq。在一些实施方案中，GPCR增加1,4,5-三磷酸肌醇（IP3）的细胞内水平。在一些实施方案中，GPCR的调节剂是心肌细胞肥大的调节剂。本发明还涉及使用GPCR调制器的方法。优选的调节剂是反向激动剂和拮抗剂。本发明的反向激动剂和拮抗剂可用作预防或治疗心脏病，包括肥厚性心肌病和充血性心力衰竭的治疗剂，特别是由心肌梗死后重建，心脏瓣膜疾病，持续的心脏后负荷，心肌炎引起的肥大性心肌病，和家族性肥厚型心肌病。

7. 发明申请

US20070224127A1 Human G protein-coupled receptor and modulators thereof for the treatment of ischemic heart disease and congestive heart failure 审中-公开
标题翻译：人G蛋白偶联受体及其调节剂用于治疗缺血性心脏病和充血性心力衰竭
公开(公告)号：US20070224127A1
公开(公告)日：2007-09-27
申请号：US11604179
申请日：2006-11-22
申请人： John Adams , Daniel Connolly
发明人： John Adams , Daniel Connolly
IPC分类号： A61K49/00 , A01K67/027 , C12N5/10 , G01N33/53 , G01N33/567 , G01N33/569
CPC分类号： G01N33/74 , A01K2217/05 , A01K2217/075 , A01K2267/03 , C07K14/705 , G01N2333/726 , G01N2500/04
摘要： The present invention relates to methods of identifying whether a candidate compound is a modulator of an orphan G protein-coupled receptor (GPCR). Preferably the GPCR is human. In some embodiments, the GPCR is expressed endogenously by cardiomyocytes. In some embodiments, the GPCR is coupled to Gi and lowers the level of intracellular cAMP. In some embodiments, overexpression of the GPCR promotes survival of cardiomyocytes. In some embodiments, overexpression of the GPCR rescues cardiomyoctes from hypoxia/reoxygenation induced apoptosis. In some embodiments, the GPCR is down-regulated in individuals with congestive heart failure. Agonists of the invention are envisioned to be useful as therapeutic agents for the treatment of ischemic heart disease, including myocardial infarction, post-myocardial infarction remodeling, and congestive heart failure.
摘要翻译：本发明涉及鉴定候选化合物是否为孤儿G蛋白偶联受体（GPCR）的调节剂的方法。优选GPCR是人。在一些实施方案中，GPCR由心肌细胞内源性表达。在一些实施方案中，GPCR与Gi偶联并降低细胞内cAMP的水平。在一些实施方案中，GPCR的过表达促进心肌细胞的存活。在一些实施方案中，GPCR的过表达从心肌缺血/再氧化诱导的细胞凋亡中拯救心肌细胞。在一些实施方案中，GPCR在具有充血性心力衰竭的个体中下调。预期本发明的激动剂可用作治疗缺血性心脏病，包括心肌梗死，心肌梗死后重建和充血性心力衰竭的治疗剂。

8. 发明授权

US06998828B2 Low audible noise power supply controller and method therefor 有权
标题翻译：低噪声电源控制器及其方法
公开(公告)号：US06998828B2
公开(公告)日：2006-02-14
申请号：US10810864
申请日：2004-03-29
申请人： Charles A. Casey , Daniel Connolly , Brant Johnson
发明人： Charles A. Casey , Daniel Connolly , Brant Johnson
IPC分类号： G05F1/44
CPC分类号： H02M3/156
摘要： In one embodiment, a power supply controller of a power supply system uses an algorithm to reduce the number of drive pulses to the output transistors under light load conditions. The algorithm groups the drive pulses to the output transistors into sets and removes some of the drive pulses for each set drive pulses issued by the controller. Each successive set removes additional drive pulses.
摘要翻译：在一个实施例中，供电系统的电源控制器使用一种算法来在轻负载条件下减少输出晶体管的驱动脉冲数。该算法将输出晶体管的驱动脉冲组合成组，并且去除由控制器发出的每组设置的驱动脉冲的一些驱动脉冲。每个连续的设置去除额外的驱动脉冲。

9. 发明申请

US20070072861A1 Method of using cyclooxygenase-2 inhibitors in the prevention of cardiovascular disorders 审中-公开
标题翻译：使用环氧合酶-2抑制剂预防心血管疾病的方法
公开(公告)号：US20070072861A1
公开(公告)日：2007-03-29
申请号：US11387554
申请日：2006-03-23
申请人： Barbara Roniker , Richard LaChapelle , Daniel Connolly , Karen Seibert , Philip Needleman
发明人： Barbara Roniker , Richard LaChapelle , Daniel Connolly , Karen Seibert , Philip Needleman
IPC分类号： A61K31/50 , A61K31/4439 , A61K31/415 , A61K31/421 , A61K31/42 , A61K31/401 , A61K31/366 , A61K31/365 , A61K31/22
CPC分类号： A61K45/06 , A61K31/22 , A61K31/365 , A61K31/366 , A61K31/401 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/4439 , A61K31/50 , A61K2300/00
摘要： This invention relates to the use of cyclooxygenase-2 inhibitors or derivatives thereof in preventing cardiovascular disorders.
摘要翻译：本发明涉及环氧合酶-2抑制剂或其衍生物在预防心血管疾病中的应用。

10. 发明申请

US20050238579A1 Human g protein-coupled receptor and modulators thereof for the treatment of ischemic heart disease and congestive heart failure 有权
标题翻译：人类g蛋白偶联受体及其调节剂用于治疗缺血性心脏病和充血性心力衰竭
公开(公告)号：US20050238579A1
公开(公告)日：2005-10-27
申请号：US10523100
申请日：2003-07-25
申请人： John Adams , Daniel Connolly
发明人： John Adams , Daniel Connolly
IPC分类号： A01K67/027 , A61K38/17 , A61K45/00 , A61K51/00 , A61K51/08 , A61P9/04 , A61P9/10 , A61P43/00 , C07K14/705 , C07K19/00 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/10 , C12N9/14 , C12N15/09 , C12Q1/02 , C12Q1/68 , G01N33/53 , G01N33/567 , G01N33/74
CPC分类号： G01N33/74 , A01K2217/05 , A01K2217/075 , A01K2267/03 , C07K14/705 , G01N2333/726 , G01N2500/04
摘要： The present invention relates to methods of identifying whether a candidate compound is a modulator of an orphan G protein-coupled receptor (GPCR). Preferably the GPCR is human. In some embodiments, the GPCR is expressed endogenously by cardiomyocytes. In some embodiments, the GPCR is coupled to Gi and lowers the level of intracellular cAMP. In some embodiments, overexpression of the GPCR promotes survival of cardiomyocytes. In some embodiments, overexpression of the GPCR rescues cardiomyoctes from hypoxia/reoxygenation induced apoptosis. In some embodiments, the GPCR is down-regulated in individuals with congestive heart failure. Agonists of the invention are envisioned to be useful as therapeutic agents for the treatment of ischemic heart disease, including myocardial infarction, post-myocardial infarction remodeling, and congestive heart failure.
摘要翻译：本发明涉及鉴定候选化合物是否为孤儿G蛋白偶联受体（GPCR）的调节剂的方法。优选GPCR是人。在一些实施方案中，GPCR由心肌细胞内源性表达。在一些实施方案中，GPCR与Gi偶联并降低细胞内cAMP的水平。在一些实施方案中，GPCR的过表达促进心肌细胞的存活。在一些实施方案中，GPCR的过表达从心肌缺血/再氧化诱导的细胞凋亡中拯救心肌细胞。在一些实施方案中，GPCR在具有充血性心力衰竭的个体中下调。预期本发明的激动剂可用作治疗缺血性心脏病，包括心肌梗死，心肌梗死后重建和充血性心力衰竭的治疗剂。

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