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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 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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7.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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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：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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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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10.发明授权公开(公告)号：US06555339B1
公开(公告)日：2003-04-29
申请号：US09170496
申请日：1998-10-13
IPC分类号： C12N1500
CPC分类号： C07D231/12 , A61K38/00 , C07D231/16 , C07D409/12 , C07K14/705 , C07K14/70571 , C07K14/723 , G01N33/566 , G01N2333/726 , G01N2500/00
摘要： Disclosed are constitutively activated, non-endogenous versions of endogenous human GPCRs comprising the following amino acid sequence region (C-terminus to N-terminus orientation) and/or the following nucleic acid sequence region (3′ to 5′ orientation) transversing the transmembrane-6 (TM6) and intracellular loop-3 (IC3) regions of the GPCR: P1AA15X (a) and/or Pcodon(AA-codon)15Xcodon, (b) respectively. In a preferred embodiment, P1 and Pcodon are endogenous proline and an endogenous nucleic acid encoding region encoding proline, respectively, located within TM6 of the non-endogenous GPCR; AA15 and (AA-codon)15 are 15 endogenous amino acid residues and 15 codons encoding endogenous amino acid residues, respectively; and X and Xcodon are non-endogenous lysine and non-endogenous nucleic acid region encoding lysine, respectively, located within IC3 of the non-endogenous GPCR. The purified and isolated non-endogenous human GPCRs having these mutations, and the receptors incorporated into mammalian cells, are well within the present disclosure.
摘要翻译： 公开了包含以下氨基酸序列区（C末端至N末端取向）和/或跨越跨膜的以下核酸序列区（3'至5'取向）的内源性人GPCR的组成型激活非内源型 -6（TM6）和细胞内环3（IC3）区域：和/或分别。 在优选的实施方案中，P1和Pcodon是分别位于非内源性GPCR TM6内的内源性脯氨酸和编码脯氨酸的内源核酸编码区; AA15和（AA-密码子）15分别是15个内源氨基酸残基和15个编码内源氨基酸残基的密码子; X和Xcodon是分别位于非内源性GPCR的IC3内的非内源赖氨酸和编码赖氨酸的非内源核酸区域。 具有这些突变的纯化和分离的非内源性人GPCR以及并入哺乳动物细胞中的受体完全在本公开内。
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