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公开(公告)号：US6107324A
公开(公告)日：2000-08-22
申请号：US292071
申请日：1999-04-14
申请人： Dominic P. Behan , Derek T. Chalmers , Richard J. Foster , Robert C. Glen , Michael S. Lawless , Chen W. Liaw , Qian Liu , Joseph F. Russo , Julian R. Smith , William J. Thomsen
发明人： Dominic P. Behan , Derek T. Chalmers , Richard J. Foster , Robert C. Glen , Michael S. Lawless , Chen W. Liaw , Qian Liu , Joseph F. Russo , Julian R. Smith , William J. Thomsen
IPC分类号： C12N15/09 , A61K31/415 , A61K31/4155 , A61K31/4427 , A61K31/4433 , A61K31/4439 , A61P1/00 , A61P9/00 , A61P25/00 , A61P29/00 , A61P43/00 , C07D231/12 , C07D231/16 , C07D401/12 , C07D409/12 , C07H21/04 , C07K14/705 , C12Q1/02
CPC分类号： C07D231/12 , C07D231/16 , C07D409/12 , C07K14/70571
摘要： Disclosed herein is a new class of pyrazole compounds which act at the 5HT.sub.2A receptors.
摘要翻译： 本文公开的是一类新的在5HT2A受体上起作用的吡唑化合物。
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2.发明授权Small molecule modulators of non-endogenous, constitutively activated human serotonin receptors 有权非内源性，组成型激活的人类5-羟色胺受体的小分子调节剂
公开(公告)号：US6150393A
公开(公告)日：2000-11-21
申请号：US418721
申请日：1999-10-15
申请人： Dominic P. Behan , Derek T. Chalmers , Nigel R. A. Beeley , Richard J. Foster , Robert C. Glen , Michael S. Lawless , Chen W. Liaw , Qian Liu , Frederique Menzaghi , Joseph F. Russo , Julian R. Smith , William J. Thomsen
发明人： Dominic P. Behan , Derek T. Chalmers , Nigel R. A. Beeley , Richard J. Foster , Robert C. Glen , Michael S. Lawless , Chen W. Liaw , Qian Liu , Frederique Menzaghi , Joseph F. Russo , Julian R. Smith , William J. Thomsen
IPC分类号： A61P25/00 , C07D20060101 , C07D231/12 , C07D231/16 , C07D409/12 , C07K14/705 , A61K31/415
CPC分类号： C07D231/12 , C07D231/16 , C07D409/12 , C07K14/70571
摘要： Disclosed herein are non-endogenous, constitutively activated forms of the human 5-HT.sub.2A and human 5-HT.sub.2C receptors and uses of such receptors to screen candidate compounds. Further disclosed herein are candidate compounds identified by the screening method which act at the 5HT.sub.2A receptors. Yet further disclosed is a new class of compounds which act at the 5HT.sub.2A receptors.
摘要翻译： 本文公开了人5-HT2A和人5-HT 2C受体的非内源性，组成型活化形式以及这些受体用于筛选候选化合物的用途。 本文进一步公开的是通过在5HT2A受体上起作用的筛选方法鉴定的候选化合物。 还进一步公开了作为5HT2A受体的新类化合物。
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3.发明授权Non-endogenous, constitutively activated human serotonin receptors and small molecule modulators thereof 有权非内源性，组成型激活的人血清素受体及其小分子调节剂
公开(公告)号：US6140509A
公开(公告)日：2000-10-31
申请号：US292069
申请日：1999-04-14
申请人： Dominic P. Behan , Derek T. Chalmers , Richard J. Foster , Robert C. Glen , Michael S. Lawless , Chen W. Liaw , Qian Liu , Joseph F. Russo , Julian R. Smith , William J. Thomsen
发明人： Dominic P. Behan , Derek T. Chalmers , Richard J. Foster , Robert C. Glen , Michael S. Lawless , Chen W. Liaw , Qian Liu , Joseph F. Russo , Julian R. Smith , William J. Thomsen
IPC分类号： C07D231/12 , C07D231/16 , C07D409/12 , C07K14/705
CPC分类号： C07D231/12 , C07D231/16 , C07D409/12 , C07K14/70571
摘要： A compound of formula (C) useful as a serotonin receptor modulator
摘要翻译： 用作5-羟色胺受体调节剂的式（C）化合物
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4.发明申请NON-ENDOGENOUS, CONSTITUTIVELY ACTIVATED HUMAN SEROTONIN RECEPTORS AND SMALL MOLECULE MODULATORS THEREOF 失效非内源性，一般激活的人类丝氨酸受体及其小分子调节剂公开(公告)号：US20090076254A1
公开(公告)日：2009-03-19
申请号：US12051754
申请日：2008-03-19
IPC分类号： C07H21/04
CPC分类号： C07D231/12 , C07D231/16 , C07D409/12 , C07K14/70571 , C07K14/723 , G01N33/566 , G01N2333/70571 , G01N2333/726
摘要： Disclosed herein are non-endogenous, constitutively activated forms of the human 5-HT2A and human 5-HT2C receptors and uses of such receptors to screen candidate compounds. Further disclosed herein are candidate compounds identified by the screening method which act at the 5HT2A receptors. Yet further disclosed is a new class of compounds which act at the 5HT2A receptors.
摘要翻译： 本文公开了人5-HT2A和人5-HT 2C受体的非内源性，组成型活化形式以及这些受体用于筛选候选化合物的用途。 本文进一步公开的是通过在5HT2A受体上起作用的筛选方法鉴定的候选化合物。 还进一步公开了作为5HT2A受体的新类化合物。
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5.发明授权Non-endogenous, constitutively activated human serotonin receptors and small molecule modulators thereof 有权非内源性，组成型激活的人血清素受体及其小分子调节剂公开(公告)号：US07368539B2
公开(公告)日：2008-05-06
申请号：US10980560
申请日：2004-11-02
IPC分类号： C07K14/435 , C07K14/705
CPC分类号： C07D231/12 , C07D231/16 , C07D409/12 , C07K14/70571 , C07K14/723 , G01N33/566 , G01N2333/70571 , G01N2333/726
摘要： Disclosed herein are non-endogenous, constitutively activated forms of the human 5-HT2A and human 5-HT2C receptors and uses of such receptors to screen candidate compounds. Further disclosed herein are candidate compounds identified by the screening method which act at the 5HT2A receptors. Yet further disclosed is a new class of compounds which act at the 5HT2A receptors.
摘要翻译： 本文公开了非内源性，组成型活化形式的人5-HT 2A和人5-HT 2C受体以及这些受体用于筛选候选化合物的用途。 本文进一步公开的是通过在5HT 2A受体上起作用的筛选方法鉴定的候选化合物。 还进一步公开的是一类新的化合物，其作用于5HT 2A受体。
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6.发明授权Non-endogenous, constitutively activated human serotonin receptors and small molecule modulators thereof 失效非内源性，组成型激活的人血清素受体及其小分子调节剂公开(公告)号：US07754866B2
公开(公告)日：2010-07-13
申请号：US12051754
申请日：2008-03-19
IPC分类号： C07H21/04
CPC分类号： C07D231/12 , C07D231/16 , C07D409/12 , C07K14/70571 , C07K14/723 , G01N33/566 , G01N2333/70571 , G01N2333/726
摘要： Disclosed herein are non-endogenous, constitutively activated forms of the human 5-HT2A and human 5-HT2C receptors and uses of such receptors to screen candidate compounds. Further disclosed herein are candidate compounds identified by the screening method which act at the 5HT2A receptors. Yet further disclosed is a new class of compounds which act at the 5HT2A receptors.
摘要翻译： 本文公开了人5-HT2A和人5-HT 2C受体的非内源性，组成型活化形式以及这些受体用于筛选候选化合物的用途。 本文进一步公开的是通过在5HT2A受体上起作用的筛选方法鉴定的候选化合物。 还进一步公开了作为5HT2A受体的新类化合物。
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公开(公告)号：US06541209B1
公开(公告)日：2003-04-01
申请号：US09292072
申请日：1999-04-14
IPC分类号： G01N3350
CPC分类号： C07D231/12 , C07D231/16 , C07D409/12 , C07K14/70571 , C07K14/723 , G01N33/566 , G01N2333/70571 , G01N2333/726
摘要： Disclosed herein are non-endogenous, constitutively activated forms of the human 5-HT2A and human 5-HT2C receptors and uses of such receptors to screen candidate compounds. Further disclosed herein are candidate compounds identified by the screening method which act at the 5HT2A receptors. Yet further disclosed is a new class of compounds which act at the 5HT2A receptors.
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8.发明授权Non-endogenous, constitutively activated human serotonin receptors and small molecule modulators thereof 有权非内源性，组成型激活的人血清素受体及其小分子调节剂公开(公告)号：US06420541B1
公开(公告)日：2002-07-16
申请号：US09767013
申请日：2000-12-22
IPC分类号： C07K2104
CPC分类号： C07D231/12 , C07D231/16 , C07D409/12 , C07K14/70571 , C07K14/723 , G01N33/566 , G01N2333/70571 , G01N2333/726
摘要： Disclosed herein are non-endogenous, constitutively activated forms of the human 5-HT2A and human 5-HT2C receptors and uses of such receptors to screen candidate compounds. Further disclosed herein are candidate compounds identified by the screening method which act at the 5HT2A receptors. Yet further disclosed is a new class of compounds which act at the 5HT2A receptors.
摘要翻译： 本文公开了人5-HT2A和人5-HT 2C受体的非内源性，组成型活化形式以及这些受体用于筛选候选化合物的用途。 本文进一步公开的是通过在5HT2A受体上起作用的筛选方法鉴定的候选化合物。 还进一步公开了作为5HT2A受体的新类化合物。
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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：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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