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公开(公告)号：US08198049B2
公开(公告)日：2012-06-12
申请号：US12958954
申请日：2010-12-02
申请人： Ruoping Chen , Huong T. Dang , Chen W. Liaw , I-Lin Lin
发明人： Ruoping Chen , Huong T. Dang , Chen W. Liaw , I-Lin Lin
IPC分类号： C12P21/06 , G01N33/53 , G01N33/567 , C12N1/20 , C12N15/00 , C12N5/00 , C12N5/02 , C12N15/74 , C07H21/02 , C07H21/04 , C07K1/00 , C07K14/00 , C07K17/00
CPC分类号： C07K14/723 , C07K14/705 , G01N33/74 , G01N2333/726 , G01N2500/02
摘要： The invention disclosed in this patent document relates to transmembrane receptors, more particularly to endogenous, human orphan G protein-coupled receptors.
摘要翻译： 本专利文献中公开的发明涉及跨膜受体，更具体地涉及内源性，孤儿G蛋白偶联受体。
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公开(公告)号：US20110195431A1
公开(公告)日：2011-08-11
申请号：US12958954
申请日：2010-12-02
申请人： Ruoping Chen , Huong T. Dang , Chen W. Liaw , I-Lin LIn
发明人： Ruoping Chen , Huong T. Dang , Chen W. Liaw , I-Lin LIn
CPC分类号： C07K14/723 , C07K14/705 , G01N33/74 , G01N2333/726 , G01N2500/02
摘要： The invention disclosed in this patent document relates to transmembrane receptors, more particularly to endogenous, human orphan G protein-coupled receptors.
摘要翻译： 本专利文献中公开的发明涉及跨膜受体，更具体地涉及内源性，孤儿G蛋白偶联受体。
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公开(公告)号：US07893235B2
公开(公告)日：2011-02-22
申请号：US11894692
申请日：2007-08-20
申请人： Ruoping Chen , Huong T. Dang , Chen W. Liaw , I-Lin Lin
发明人： Ruoping Chen , Huong T. Dang , Chen W. Liaw , I-Lin Lin
IPC分类号： C07H21/04 , G01N33/53 , G01N33/567 , C12P21/06 , C12N1/20 , C12N15/00 , C12N5/00 , C12N5/02 , C12N15/74
CPC分类号： C07K14/723 , C07K14/705 , G01N33/74 , G01N2333/726 , G01N2500/02
摘要： The invention disclosed in this patent document relates to transmembrane receptors, more particularly to endogenous, human orphan G protein-coupled receptors.
摘要翻译： 本专利文献中公开的发明涉及跨膜受体，更具体地涉及内源性，孤儿G蛋白偶联受体。
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公开(公告)号：US20080199889A1
公开(公告)日：2008-08-21
申请号：US11894692
申请日：2007-08-20
申请人： Ruoping Chen , Huong T. Dang , Chen W. Liaw , I-Lin Lin
发明人： Ruoping Chen , Huong T. Dang , Chen W. Liaw , I-Lin Lin
CPC分类号： C07K14/723 , C07K14/705 , G01N33/74 , G01N2333/726 , G01N2500/02
摘要： The invention disclosed in this patent document relates to transmembrane receptors, more particularly to endogenous, human orphan G protein-coupled receptors.
摘要翻译： 本专利文献中公开的发明涉及跨膜受体，更具体地涉及内源性，孤儿G蛋白偶联受体。
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公开(公告)号：US07829298B2
公开(公告)日：2010-11-09
申请号：US10930662
申请日：2004-08-31
申请人： David J. Unett , Ruoping Chen , Jeremy G. Richman , Daniel T. Connolly , Huong T. Dang , Bryan J. Choi , James N. Leonard , Yaron Hakak , Chen W. Liaw , Dominic P. Behan , Derek T. Chalmers , Michael R. Lerner , Kevin P. Lowitz
发明人： David J. Unett , Ruoping Chen , Jeremy G. Richman , Daniel T. Connolly , Huong T. Dang , Bryan J. Choi , James N. Leonard , Yaron Hakak , Chen W. Liaw , Dominic P. Behan , Derek T. Chalmers , Michael R. Lerner , Kevin P. Lowitz
IPC分类号： 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.
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。
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公开(公告)号：US06653086B1
公开(公告)日：2003-11-25
申请号：US09364425
申请日：1999-07-30
申请人： Dominic P. Behan , Derek T. Chalmers , Chen W. Liaw , I Lin-Lin , Kevin P. Lowitz , Ruoping Chen
发明人： Dominic P. Behan , Derek T. Chalmers , Chen W. Liaw , I Lin-Lin , Kevin P. Lowitz , Ruoping Chen
IPC分类号： C12N1500
CPC分类号： C07D231/12 , C07D231/16 , C07D233/42 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D513/04 , C07K14/70571 , G01N33/68 , G01N2500/00
摘要： Disclosed herein are techniques for directly identifying candidate compounds as agonists, partial agonists and/or, most preferably, inverse agonists, to endogenous, constitutively activated orphan G protein-coupled receptors. Such directly identified compounds can be utilized, most preferably, in pharmaceutical compositions
摘要翻译： 本文公开了用于直接鉴定候选化合物作为内源性，组成型激活的孤儿G蛋白偶联受体的激动剂，部分激动剂和/或最优选的反向激动剂的技术。 这种直接鉴定的化合物可以最优选地用于药物组合物中
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公开(公告)号：US08440391B2
公开(公告)日：2013-05-14
申请号：US10723955
申请日：2003-11-26
IPC分类号： C12Q1/00 , C12Q1/68 , C07K14/435
CPC分类号： C07K14/705 , A61K38/00 , C07K14/723 , G01N33/566
摘要： The invention disclosed in this patent document relates to transmembrane receptors, more particularly to a human G protein-coupled receptor for which the endogenous ligand is unknown (“orphan GPCR receptors”), and most particularly to mutated (non-endogenous) versions of the human GPCRs for evidence of constitutive activity.
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8.发明授权公开(公告)号：US07381522B2
公开(公告)日：2008-06-03
申请号：US11404939
申请日：2006-04-14
申请人： Karin Lehmann-Bruinsma , Chen W. Liaw , I-Lin Lin
发明人： Karin Lehmann-Bruinsma , Chen W. Liaw , I-Lin Lin
IPC分类号： C12Q1/00 , G01N33/53 , G01N33/566
CPC分类号： G01N33/74 , A61K38/00 , C07K14/705 , C07K14/723 , C07K2319/00 , G01N2333/726 , G01N2500/10
摘要： The invention disclosed in this patent document relates to transmembrane receptors, more particularly to a human G protein-coupled receptor for which the endogenous ligand is known (“known GPCRs”), and most particularly to mutated (non-endogenous) versions of the known GPCRs for use, most preferably in screening assays for the direct identification of candidate compounds as inverse agonists, agonists and partial agonists.
摘要翻译： 本专利文献中公开的发明涉及跨膜受体，更具体地涉及内源性配体已知的人G蛋白偶联受体（“已知的GPCR”），最特别地涉及已知的突变的（非内源的）版本 GPCRs，最优选用于直接鉴定作为反向激动剂，激动剂和部分激动剂的候选化合物的筛选试验。
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9.发明授权公开(公告)号：US06806054B2
公开(公告)日：2004-10-19
申请号：US09826509
申请日：2001-04-05
申请人： Karin Lehmann-Bruinsma , Chen W. Liaw , I-Lin Lin
发明人： Karin Lehmann-Bruinsma , Chen W. Liaw , I-Lin Lin
IPC分类号： G01N3353
CPC分类号： G01N33/74 , A61K38/00 , C07K14/705 , C07K14/723 , C07K2319/00 , G01N2333/726 , G01N2500/10
摘要： The invention disclosed in this patent document relates to transmembrane receptors, more particularly to a human G protein-coupled receptor for which the endogenous ligand is known (“known GPCRs”), and most particularly to mutated (non-endogenous) versions of the known GPCRs for use, most preferably in screening assays for the direct identification of candidate compounds as inverse agonists, agonists and partial agonists.
摘要翻译： 本专利文献中公开的发明涉及跨膜受体，更具体地涉及内源性配体已知的人G蛋白偶联受体（“已知的GPCR”），最特别地涉及已知的突变的（非内源的）版本 GPCRs，最优选用于直接鉴定作为反向激动剂，激动剂和部分激动剂的候选化合物的筛选试验。
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公开(公告)号：US07119190B2
公开(公告)日：2006-10-10
申请号：US10083168
申请日：2002-02-26
申请人： Chen W. Liaw , Derek T. Chalmers , Dominic P. Behan , Dominique Maciejewski-Lenior , James N. Leonard , I-Lin Lin , Daniel Ortuño
发明人： Chen W. Liaw , Derek T. Chalmers , Dominic P. Behan , Dominique Maciejewski-Lenior , James N. Leonard , I-Lin Lin , Daniel Ortuño
CPC分类号： C07D231/12 , A61K38/00 , C07D231/16 , C07D409/12 , C07K14/705 , C07K14/70571 , C07K14/723 , G01N33/566 , G01N2333/70571 , G01N2333/726
摘要： The invention disclosed in this patent document relates to transmembrane receptors, more particularly to a human G protein-coupled receptor and to mutated (non-endogenous) versions of the human GPCRs for evidence of constitutive activity.
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