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1. 发明授权

US07829298B2 Human G protein-coupled receptors for metabolic-related disorders 有权
标题翻译：人G蛋白偶联受体代谢相关疾病
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。

2. 发明申请

US20080139628A1 Compositions For Treating Flushing And Lipid-Associated Disorders Comprising Niacin Receptor Partial Agonists 审中-公开
标题翻译：用于治疗包含烟酸受体部分激动剂的潮红和脂质相关疾病的组合物
公开(公告)号：US20080139628A1
公开(公告)日：2008-06-12
申请号：US11718539
申请日：2005-11-01
申请人： Dominic P. Behan , Daniel T. Connolly , Jeremy G. Richman
发明人： Dominic P. Behan , Daniel T. Connolly , Jeremy G. Richman
IPC分类号： A61K31/4406 , C07D403/04 , A61K31/41 , A61P3/00 , C07D231/14 , A61K31/415
CPC分类号： A61K45/06 , A61K31/00 , A61K31/415 , A61K31/416 , A61K31/4162 , A61K31/455 , A61K2300/00
摘要： The invention provides a method of reducing flushing induced by niacin or a niacin analog in a subject, comprising administering to said subject an effective flush reducing amount of a niacin receptor partial agonist. In addition, the invention provides a method of reducing flushing induced by niacin or a niacin analog in a subject, comprising administering to said subject an effective flush reducing amount of a niacin receptor partial agonist and an effective lipid altering amount of niacin or a niacin analog. The invention further provides a method of reducing flushing induced by niacin or a niacin analog in a subject, comprising administering to said subject an effective flush reducing amount of a niacin receptor partial agonist and subsequently administering to said subject an effective lipid altering amount of niacin or a niacin analog.
摘要翻译：本发明提供了一种减少受试者中烟酸或烟酸类似物引起的潮红的方法，包括向所述受试者施用有效冲洗减少量的烟酸受体部分激动剂。此外，本发明提供了一种减少受试者中烟酸或烟酸类似物引起的潮红的方法，包括向所述受试者施用有效冲洗减少量的烟酸受体部分激动剂和有效的脂质改变量的烟酸或烟酸类似物。本发明进一步提供了一种减少受试者中烟酸或烟酸类似物引起的潮红的方法，包括向所述受试者施用有效冲洗减少量的烟酸受体部分激动剂，随后向所述受试者施用有效的脂质改变量的烟酸或烟酸类似物。

3. 发明授权

US06902902B2 Human G protein-coupled receptors and modulators thereof for the treatment of metabolic-related disorders 失效
公开(公告)号：US06902902B2
公开(公告)日：2005-06-07
申请号：US10314048
申请日：2002-12-06
申请人： David J. Unett , Ruoping Chen , Jeremy G. Richman , Daniel T. Connolly , Yaron Hakak , Dominic P. Behan , Derek T. Chalmers
发明人： David J. Unett , Ruoping Chen , Jeremy G. Richman , Daniel T. Connolly , Yaron Hakak , Dominic P. Behan , Derek T. Chalmers
IPC分类号： A61K31/4439 , G01N33/566 , G01N33/53 , C07H21/04 , C07K14/00
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. 发明授权

US07368539B2 Non-endogenous, constitutively activated human serotonin receptors and small molecule modulators thereof 有权
标题翻译：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
申请人： Dominic P. Behan , Derek T. Chalmers , Chen W. Liaw , Joseph F. Russo , William J. Thomsen
发明人： Dominic P. Behan , Derek T. Chalmers , Chen W. Liaw , Joseph F. Russo , William J. Thomsen
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。

5. 发明授权

US07119190B2 Endogenous and non-endogenous versions of human G protein-coupled receptors 失效
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
IPC分类号： C07H21/04 , C12N15/63 , C12N15/09
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.

6. 发明授权

US06653086B1 Endogenous constitutively activated G protein-coupled orphan receptors 有权
标题翻译：内源性组成型激活的G蛋白偶联受体
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

7. 发明授权

US5910428A Brain-derived membrane-associated CRF binding proteins 失效
标题翻译：脑衍生的膜相关CRF结合蛋白
公开(公告)号：US5910428A
公开(公告)日：1999-06-08
申请号：US637761
申请日：1996-07-02
申请人： Dominic P. Behan , Wylie W. Vale, Jr. , Wolfgang H. Fischer , Philip J. Lowry
发明人： Dominic P. Behan , Wylie W. Vale, Jr. , Wolfgang H. Fischer , Philip J. Lowry
IPC分类号： G01N33/53 , C07K7/08 , C07K14/72 , C12N5/10 , C12N15/09 , C12N15/12 , C12P21/02 , C12R1/91 , G01N33/566 , C07H21/04
CPC分类号： C07K14/72
摘要： Isolated, substantially pure mammalian brain-derived membrane-associated CRF-binding proteins and biologically active fragments thereof are provided as well as isolated and purified DNA fragments which encode the CRF binding proteins or biologically active fragments thereof or homologs of other mammalian species. By administering an amount of such CRF binding protein or a fragment thereof effective to modulate receptor activation, it is possible to modulate the action of CRF upon (a) the brain and nervous system, (b) the pituitary particularly for production of ACTH, beta endorphin and cortisol, (c) sites of inflammation, (d) the placenta, (e) the adrenal glands, (f) the gonads or (g) the gastrointestinal tract. Administration of an N-terminal fragment of the protein increases the binding site density for CRF and thus modulates its biological effect in vivo.
摘要翻译： PCT No.PCT / US94 / 12672 Sec。 371日期：1996年7月2日 102（e）日期1996年7月2日PCT 1994年11月7日PCT PCT。公开号WO95 / 13372 日期1995年5月18日提供了分离的，基本上纯的哺乳动物脑衍生的膜相关CRF结合蛋白及其生物活性片段，以及分离和纯化的DNA片段，其编码CRF结合蛋白或其生物活性片段或其他哺乳动物的同源物种类。通过施用一定量的有效调节受体激活的CRF结合蛋白或其片段，有可能在（a）脑和神经系统调节CRF的作用，（b）垂体特别是用于产生ACTH，β 内啡肽和皮质醇，（c）炎症部位，（d）胎盘，（e）肾上腺，（f）性腺或（g）胃肠道。施用蛋白质的N-末端片段增加CRF的结合位点密度，从而调节其在体内的生物学效应。

8. 发明授权

US5464757A DNA encoding CRF binding protein 失效
标题翻译：编码CRF结合蛋白的DNA
公开(公告)号：US5464757A
公开(公告)日：1995-11-07
申请号：US97828
申请日：1993-07-23
申请人： Ellen Potter , Dominic P. Behan , Wolfgang H. Fischer , Elizabeth A. Linton , Philip J. Lowry , Wylie W. Vale, Jr.
发明人： Ellen Potter , Dominic P. Behan , Wolfgang H. Fischer , Elizabeth A. Linton , Philip J. Lowry , Wylie W. Vale, Jr.
IPC分类号： A61K38/00 , C07K14/47 , C07K16/18 , C12N15/12 , C12P21/08 , G01N33/566 , G01N33/68 , G01N33/74 , C07K14/435 , C12N15/16 , C12N15/63
CPC分类号： G01N33/566 , C07K14/47 , C07K16/18 , G01N33/6872 , G01N33/689 , G01N33/74 , A61K38/00 , G01N2800/368
摘要： A Corticotropin Releasing Factor-binding protein (CRF-BP) is isolated and purified sufficient to provide AA sequence data from which the DNA is obtained, which is then used to produce the protein recombinantly. The CRF-BP is useful for modulating the biological activity of CRF, such as reducing the high ACTH levels in mammals caused by excess CRF. The CRF-BP or fragments thereof and/or antibodies to the proteins may be employed in diagnostic assays to determine the levels of CRF, CRF-BP and the ratio of CRF/CRF-BP in a vascular fluid sample. The DNA or subsequence thereof can be used as probes for genetic material in certain assays. The anti-CRF-BP antibodies are also useful to purify the CRF-BP protein and to modulate the biological effect of CRF-BPs proteins.
摘要翻译：分离和纯化促肾上腺皮质激素释放因子结合蛋白（CRF-BP），以提供获得DNA的AA序列数据，然后将其用于重组产生蛋白质。 CRF-BP可用于调节CRF的生物活性，例如降低由过量CRF引起的哺乳动物中的高ACTH水平。 CRF-BP或其片段和/或抗体可用于诊断测定中以确定血管流体样品中CRF，CRF-BP的水平和CRF / CRF-BP的比例。在某些测定中，DNA或其子序列可用作遗传物质的探针。抗CRF-BP抗体也可用于纯化CRF-BP蛋白并调节CRF-BPs蛋白的生物学作用。

9. 发明授权

US08546378B2 5HT2C receptor modulator compositions and methods of use 失效
标题翻译： 5HT2C受体调节剂组合物和使用方法
公开(公告)号：US08546378B2
公开(公告)日：2013-10-01
申请号：US13418151
申请日：2012-03-12
申请人： Dominic P. Behan , Brian M. Smith , Christina Bjenning
发明人： Dominic P. Behan , Brian M. Smith , Christina Bjenning
IPC分类号： A61K31/55 , A61K31/50
CPC分类号： A61K31/55 , A61K31/135 , A61K31/137
摘要： The present invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist. In addition, the invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist having Formula (I): or a pharmaceutically acceptable salt, solvate or hydrate thereof. These compositions are useful in pharmaceutical compositions whose use includes the treatment of obesity.
摘要翻译：本发明涉及包含苯丁胺和选择性5HT-2C受体激动剂的组合物。此外，本发明涉及包含苯丁胺和具有式（I）的选择性5HT-2C受体激动剂或其药学上可接受的盐，溶剂合物或水合物的组合物。这些组合物可用于其用途包括治疗肥胖症的药物组合物中。

10. 发明申请

US20120252786A1 5HT2C RECEPTOR MODULATOR COMPOSITIONS AND METHODS OF USE 失效
标题翻译： 5HT2C受体调节剂组合物及其使用方法
公开(公告)号：US20120252786A1
公开(公告)日：2012-10-04
申请号：US13418151
申请日：2012-03-12
申请人： Dominic P. Behan , Brian M. Smith , Christina Bienning
发明人： Dominic P. Behan , Brian M. Smith , Christina Bienning
IPC分类号： A61K31/55 , A61P3/10
CPC分类号： A61K31/55 , A61K31/135 , A61K31/137
摘要： The present invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist. In addition, the invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist having Formula (I): or a pharmaceutically acceptable salt, solvate or hydrate thereof. These compositions are useful in pharmaceutical compositions whose use includes the treatment of obesity.
摘要翻译：本发明涉及包含苯丁胺和选择性5HT-2C受体激动剂的组合物。此外，本发明涉及包含苯丁胺和具有式（I）的选择性5HT-2C受体激动剂或其药学上可接受的盐，溶剂合物或水合物的组合物。这些组合物可用于其用途包括治疗肥胖症的药物组合物中。

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