公开(公告)号：WO2006036688A2

公开(公告)日：2006-04-06

申请号：PCT/US2005033795

申请日：2005-09-21

Applicant: ARENA PHARM INC ,  LEONARD JAMES N ,  HAKAK YARON

Inventor： LEONARD JAMES N ,  HAKAK YARON

CPC classification number: G01N33/566 ,  G01N33/6845 ,  G01N2333/726 ,  G01N2500/00

Abstract: The present invention relates to a method for identifying a metabolic stabilizing compound by: a) contacting a candidate compound with GPR43, and b) determining whether GPR43 functionality is modulated, where a modulation in GPR43 functionality is indicative of the candidate compound being a metabolic stabilizing compound. In addition, the invention relates to a method for identifying a metabolic stabilizing compound, comprising: a) contacting a candidate compound with GPR43, and b) determining whether GPR43 functionality is increased, wherein an increase in GPR43 functionality is indicative of the candidate compound being a metabolic stabilizing compound. Further, the invention relates to a method for identifying a metabolic stabilizing compound, comprising: a) contacting a candidate compound with GPR43, and b) determining whether GPR43 functionality is decreased, wherein a decrease in GPR43 functionality is indicative of the candidate compound being a metabolic stabilizing compound.

Abstract translation: 本发明涉及通过以下步骤鉴定代谢稳定化合物的方法：a）使候选化合物与GPR43接触，和b）确定GPR43功能性是否被调节，其中GPR43功能性的调节指示候选化合物是代谢稳定化的 复合。 此外，本发明涉及用于鉴定代谢稳定化合物的方法，其包括：a）使候选化合物与GPR43接触，和b）确定GPR43功能性是否增加，其中GPR43功能性的增加指示候选化合物为 一种代谢稳定化合物。 此外，本发明涉及鉴定代谢稳定化合物的方法，其包括：a）使候选化合物与GPR43接触，和b）确定GPR43功能性是否降低，其中GPR43功能性的降低指示候选化合物为 代谢稳定化合物。

公开(公告)号：WO2006036688A9

公开(公告)日：2007-05-03

申请号：PCT/US2005033795

申请日：2005-09-21

Applicant: ARENA PHARM INC ,  LEONARD JAMES N ,  HAKAK YARON

Inventor： LEONARD JAMES N ,  HAKAK YARON

IPC: G01N33/68

CPC classification number: G01N33/566 ,  G01N33/6845 ,  G01N2333/726 ,  G01N2500/00

Abstract: The present invention relates to a method for identifying a metabolic stabilizing compound by: a) contacting a candidate compound with GPR43, and b) determining whether GPR43 functionality is modulated, where a modulation in GPR43 functionality is indicative of the candidate compound being a metabolic stabilizing compound. In addition, the invention relates to a method for identifying a metabolic stabilizing compound, comprising: a) contacting a candidate compound with GPR43, and b) determining whether GPR43 functionality is increased, wherein an increase in GPR43 functionality is indicative of the candidate compound being a metabolic stabilizing compound. Further, the invention relates to a method for identifying a metabolic stabilizing compound, comprising: a) contacting a candidate compound with GPR43, and b) determining whether GPR43 functionality is decreased, wherein a decrease in GPR43 functionality is indicative of the candidate compound being a metabolic stabilizing compound.

Abstract translation: 本发明涉及通过以下方式鉴定代谢稳定化合物的方法：a）使候选化合物与GPR43接触，和b）确定是否调节GPR43功能性，其中GPR43功能性的调节指示候选化合物是代谢稳定剂 复合。 此外，本发明涉及用于鉴定代谢稳定化合物的方法，其包括：a）使候选化合物与GPR43接触，和b）确定GPR43的功能是否增加，其中GPR43功能的增加指示候选化合物为 代谢稳定化合物。 此外，本发明涉及用于鉴定代谢稳定化合物的方法，包括：a）使候选化合物与GPR43接触，以及b）确定GPR43的功能性是否降低，其中GPR43功能的降低指示候选化合物为 代谢稳定化合物。

公开(公告)号：WO2007027661A2

公开(公告)日：2007-03-08

申请号：PCT/US2006033651

申请日：2006-08-29

Applicant: ARENA PHARM INC ,  HAKAK YARON ,  UNETT DAVID J ,  GATLIN JOEL ,  LIAW CHEN W

Inventor： HAKAK YARON ,  UNETT DAVID J ,  GATLIN JOEL ,  LIAW CHEN W

IPC: G01N33/74 ,  C07K14/72

CPC classification number: G01N33/5041 ,  A61K38/1709 ,  A61K49/0008 ,  C07K14/47 ,  C07K14/723 ,  G01N33/6893 ,  G01N33/74 ,  G01N2333/726 ,  G01N2500/00 ,  G01N2800/32 ,  G01N2800/323

Abstract: The present invention relates to methods of using a G protein-coupled receptor (GPCR) to identify whether a candidate compound is a modulator of atherogenesis. In certain embodiments, the GPCR couples to Gi. In certain embodiments, the GPCR is human. Agonists of the invention are useful as therapeutic agents for the prevention or treatment of atherosclerosis and atherosclerotic disease, including coronary artery disease, myocardial infarction, peripheral arterial disease, and ischemic stroke. Agonists of the invention are additionally useful as therapeutic agents for the prevention or treatment of conditions related to MCP-1 expression, including but not limited to rheumatoid arthritis, Crohn's disease, and multiple sclerosis.

Abstract translation: 本发明涉及使用G蛋白偶联受体（GPCR）鉴定候选化合物是否是动脉粥样硬化形成的调节剂的方法。 在某些实施方案中，GPCR与Gi连接。 在某些实施方案中，GPCR是人。 本发明的激动剂可用作预防或治疗动脉粥样硬化和动脉粥样硬化疾病（包括冠状动脉疾病，心肌梗死，外周动脉疾病和缺血性中风）的治疗剂。 本发明的激动剂另外可用作预防或治疗与MCP-1表达相关的病症的治疗剂，包括但不限于类风湿性关节炎，克罗恩氏病和多发性硬化症。