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1. 发明申请

WO2010011305A1 5-HT6 RECEPTOR AND MODULATORS THEREOF FOR THE TREATMENT OF INSULIN-RELATED DISORDERS 审中-公开
标题翻译：用于治疗胰岛素相关疾病的5-HT6受体及其调节剂
公开(公告)号：WO2010011305A1
公开(公告)日：2010-01-28
申请号：PCT/US2009/004247
申请日：2009-07-22
申请人： ARENA PHARMACEUTICALS, INC. , LEONARD, James, N. , CHU, Zhi-Liang , SMITH, Brian, M.
发明人： LEONARD, James, N. , CHU, Zhi-Liang , SMITH, Brian, M.
IPC分类号： G01N33/48 , G01N33/50
CPC分类号： G01N33/942 , G01N2333/62 , G01N2500/04 , G01N2800/042
摘要： The present invention relates to a method for identifying a glycemic stabilizing compound, by: a) contacting a candidate compound with a 5-HT 6 receptor, b) determining whether 5-HT 6 receptor functionality is increased, and c) determining whether a glycemic marker is directly modulated, where an increase in 5-HT 6 receptor functionality and direct modulation of a glycemic marker identifies the candidate compound as the glycemic stabilizing compound. In addition, the invention relates to a method for identifying a glycemic stabilizing compound, by: a) contacting a single dose of a candidate compound with a 5-HT 6 receptor, b) determining whether 5-HT 6 receptor functionality is increased, and c) determining whether a glycemic marker is directly modulated, where an increase in 5-HT 6 receptor functionality and direct modulation of a glycemic marker identifies the candidate compound as the glycemic stabilizing compound. Further, the invention relates to a method for identifying a glycemic stabilizing compound, by: a) contacting a candidate compound with a 5-HT 6 receptor in an isolated cell, b) determining whether 5-HT 6 receptor functionality is increased, and c) determining whether a glycemic marker is directly modulated, where an increase in 5-HT 6 receptor functionality and direct modulation of a glycemic marker identifies the candidate compound as the glycemic stabilizing compound.
摘要翻译：本发明涉及通过以下方式来鉴定血糖稳定化合物的方法：a）使候选化合物与5-HT 6受体接触，b）确定5-HT 6受体功能是否增加，以及c）确定血糖标志物是否为直接调节，其中5-HT 6受体功能的增加和血糖标志物的直接调节将候选化合物鉴定为血糖稳定化合物。此外，本发明涉及通过以下方式鉴定血糖稳定化合物的方法：a）使单剂量的候选化合物与5-HT 6受体接触，b）确定5-HT 6受体功能是否增加，以及c）确定血糖标志物是否被直接调节，其中5-HT 6受体功能的增加和血糖标志物的直接调节将候选化合物识别为血糖稳定化合物。此外，本发明涉及通过以下方式鉴定血糖稳定化合物的方法：a）在分离的细胞中使候选化合物与5-HT 6受体接触，b）确定5-HT 6受体功能是否增加，以及c）确定是否直接调节血糖标志物，其中5-HT 6受体功能的增加和血糖标志物的直接调节将候选化合物鉴定为血糖稳定化合物。

2. 发明申请

WO2009126245A1 METHODS OF USING A G PROTEIN-COUPLED RECEPTOR TO IDENTIFY PEPTIDE YY (PYY) SECRETAGOGUES AND COMPOUNDS USEFUL IN THE TREATMENT OF CONDITIONS MODULATED BY PYY 审中-公开
标题翻译：使用G蛋白偶联受体鉴定PYY（PYY）秘密肽和化合物的方法可用于治疗由PYY调节的病症
公开(公告)号：WO2009126245A1
公开(公告)日：2009-10-15
申请号：PCT/US2009/002154
申请日：2009-04-06
申请人： ARENA PHARMACEUTICALS, INC. , CHU, Zhi-liang , LEONARD, James, N. , JONES, Robert, M.
发明人： CHU, Zhi-liang , LEONARD, James, N. , JONES, Robert, M.
IPC分类号： G01N33/74
CPC分类号： G01N33/68 , G01N33/5044 , G01N2333/726 , G01N2800/042 , G01N2800/044 , G01N2800/065 , G01N2800/108 , G01N2800/323
摘要： The present invention relates to methods of using GPR119 receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY, such as conditions modulated by stimulation of NPY Y2 receptor (Y2R). Agonists of GPR119 receptor are useful as therapeutic agents for treating or preventing a condition modulated by PYY, such as a condition modulated by stimulation of Y2R. Conditions modulated by PYY such as may be a condition modulated by stimulation of Y2R include bone-related conditions, metabolic disorders, angiogenesis-related conditions, ischemia-related conditions, convulsive disorders, malabsorptive disorders, cancers, and inflammatory disorders.
摘要翻译：本发明涉及使用GPR119受体鉴定肽YY（PYY）促分泌素和可用于治疗由PYY调节的病症的化合物的方法，例如通过刺激NPY Y2受体（Y2R）调节的病症。 GPR119受体的激动剂可用作治疗或预防由PYY调节的病症的治疗剂，例如通过刺激Y2R调节的病症。由PYY调节的病症例如可以通过Y2R刺激调节的病症包括骨相关病症，代谢紊乱，血管发生相关病症，缺血相关病症，惊厥性疾病，吸收不良障碍，癌症和炎症性疾病。

3. 发明申请

WO2007027225A3 COMBINATION THERAPY FOR THE TREATMENT OF OBESITY AND DIABETES AND CONDITIONS RELATED THERETO AND FOR THE TREATMENT OF CONDITIONS AMELIORATED BY INCREASING A BLOOD GLP-1 LEVEL 审中-公开
标题翻译：联合治疗肥胖和糖尿病的相关治疗以及相关的治疗条件和增加血液GLP-1水平
公开(公告)号：WO2007027225A3
公开(公告)日：2007-11-22
申请号：PCT/US2006016024
申请日：2006-04-26
申请人： ARENA PHARM INC , CHU ZHI-LIANG , LEONARD JAMES N
发明人： CHU ZHI-LIANG , LEONARD JAMES N
IPC分类号： A61K31/40 , A61K31/403 , A61K31/405 , A61K31/4172 , A61K31/426 , A61K31/4439 , A61K31/445 , A61K31/497 , A61K31/4985 , A61K31/513 , A61K38/08 , A61P3/04 , A61P3/10 , A61P9/10 , A61P25/28
CPC分类号： G01N33/6893 , A61K31/40 , A61K31/403 , A61K31/405 , A61K31/4172 , A61K31/426 , A61K31/4439 , A61K31/445 , A61K31/497 , A61K31/4985 , A61K31/513 , A61K38/177 , A61K38/26 , A61K45/06 , C07K14/605 , C07K14/715 , G01N33/567 , G01N2333/726 , G01N2500/04 , G01N2800/042 , A61K2300/00
摘要： The present invention concerns combination of an amount of a BRS-3 agonist with an amount of a dipeptidyl peptidase IV (DPP-IV) inhibitor such that the combination provides an effect in lowering a blood glucose level or in increasing a blood GLP-1 level in a subject over that provided by the amount of the BRS-3 agonist alone and by the amount of the DPP-IV inhibitor alone and the use of such a combination for treating or preventing obesity and diabetes and conditions related thereto and conditions ameliorated by increasing a blood GLP-1 level. The present invention also relates to the use of a G protein-coupled receptor to screen for GLP-1 secretagogues.
摘要翻译：本发明涉及一定量的BRS-3激动剂与一定量的二肽基肽酶IV（DPP-IV）抑制剂的组合，使得该组合提供降低血糖水平或增加血液GLP-1水平的作用在超过由单独BRS-3激动剂的量和仅由DPP-IV抑制剂的量提供的受试者中，以及这种组合用于治疗或预防肥胖症和糖尿病及其相关病症和通过增加血液GLP-1水平。本发明还涉及G蛋白偶联受体用于筛选GLP-1促分泌素的用途。

4. 发明申请

WO2007120689A3 METHODS OF USING GPR119 RECEPTOR TO IDENTIFY COMPOUNDS USEFUL FOR INCREASING BONE MASS IN AN INDIVIDUAL 审中-公开
公开(公告)号：WO2007120689A3
公开(公告)日：2007-10-25
申请号：PCT/US2007/008902
申请日：2007-04-10
申请人： ARENA PHARMACEUTICALS, INC. , CHU, Zhi-Liang , LEONARD, James, N.
发明人： CHU, Zhi-Liang , LEONARD, James, N.
IPC分类号： G01N33/50
摘要： The present invention relates to methods of using GPR119 receptor to identify compounds useful for increasing bone mass in an individual. Agonists of GPR119 receptor are useful as therapeutic agents for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. Agonists of GPR119 receptor promote bone formation in an individual.

5. 发明申请

WO2007120689A2 METHODS OF USING GPR119 RECEPTOR TO IDENTIFY COMPOUNDS USEFUL FOR INCREASING BONE MASS IN AN INDIVIDUAL 审中-公开
标题翻译：使用GPR119受体鉴定化合物有助于增加个体骨质量的方法
公开(公告)号：WO2007120689A2
公开(公告)日：2007-10-25
申请号：PCT/US2007008902
申请日：2007-04-10
申请人： ARENA PHARM INC , CHU ZHI-LIANG , LEONARD JAMES N
发明人： CHU ZHI-LIANG , LEONARD JAMES N
IPC分类号： C12Q1/68
CPC分类号： G01N33/74 , G01N33/5005 , G01N2333/726 , G01N2800/108
摘要： The present invention relates to methods of using GPR119 receptor to identify compounds useful for increasing bone mass in an individual. Agonists of GPR119 receptor are useful as therapeutic agents for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. Agonists of GPR119 receptor promote bone formation in an individual.
摘要翻译：本发明涉及使用GPR119受体鉴定可用于增加个体骨量的化合物的方法。 GPR119受体的激动剂可用作治疗或预防以低骨量为特征的疾病如骨质疏松症和用于增加个体骨量的治疗剂。 GPR119受体的激动剂促进个体的骨形成。

6. 发明申请

WO2005119252A2 GPR35 AND MODULATORS THEREOF FOR THE TREATMENT OF METABOLIC-RELATED DISORDERS 审中-公开
标题翻译： GPR35的调节剂用于治疗与代谢相关的疾病
公开(公告)号：WO2005119252A2
公开(公告)日：2005-12-15
申请号：PCT/US2005/018082
申请日：2005-05-23
申请人： ARENA PHARMACEUTICALS, INC. , LEONARD, James N. , CHU, Zhi Liang , UNETT, David J. , GATLIN, Joel E. , GAIDAROV, Ibragim , QIU, Jun , SKINNER, Philip J. , BOATMAN, P. Douglas
发明人： LEONARD, James N. , CHU, Zhi Liang , UNETT, David J. , GATLIN, Joel E. , GAIDAROV, Ibragim , QIU, Jun , SKINNER, Philip J. , BOATMAN, P. Douglas
IPC分类号： G01N33/50
CPC分类号： G01N33/6893 , A61K31/425 , G01N2333/726 , G01N2500/00
摘要： The present invention relates to a method for identifying a metabolic stabilizing compound, comprising: a) contacting a candidate compound with GPR35, and b) determining whether GPR35 functionality is increased, wherein an increase in GPR35 functionality is indicative of the candidate compound being a metabolic stabilizing compound. The invention further relates to use of a GPR35 modulator for the manufacture of a medicament for use as a metabolic stabilizing agent. In addition, the invention relates to a method for increasing GPR35 function, comprising contacting GPR35 with an effective amount of a compound of Formula (I): or a pharmaceutically acceptable salt thereof, wherein X is O or S; and R1, R2, R3, R4, and R5 are each independently selected from the group consisting of H, C1-4 alkoxy, C1-4 alkyl, halogen, hydroxyl, and nitro; wherein said C1-4 alkoxy is optionally substituted with carbo-C1-4-alkoxy or carboxy.
摘要翻译：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GPR35接触，和b）确定GPR35的功能是否增加，其中GPR35功能的增加指示候选化合物是代谢稳定化合物。本发明还涉及GPR35调节剂在制备用作代谢稳定剂的药物中的用途。另外，本发明涉及增加GPR35功能的方法，包括使GPR35与有效量的式（I）化合物或其可药用盐接触，其中X为O或S; R 1，R 2，R 3，R 4和R 5各自独立地选自H，C 1-4烷氧基，C 1-4烷基，卤素，羟基和硝基; 其中所述C 1-4烷氧基任选被C 1-4 - 烷氧基或羧基取代。

7. 发明申请

WO2007120702A3 USE OF GPR119 RECEPTOR AGONISTS FOR INCREASING BONE MASS AND FOR TREATING OSTEOPOROSIS, AND COMBINATION THERAPY RELATING THERETO 审中-公开
标题翻译：使用GPR119受体激素增加骨质量和治疗骨质疏松症，以及与之相关的组合治疗
公开(公告)号：WO2007120702A3
公开(公告)日：2008-05-22
申请号：PCT/US2007008926
申请日：2007-04-10
申请人： ARENA PHARM INC , CHU ZHI-LIANG , LEONARD JAMES N , LEHMANN JUERG , JONES ROBERT M
发明人： CHU ZHI-LIANG , LEONARD JAMES N , LEHMANN JUERG , JONES ROBERT M
IPC分类号： A61K31/00 , A61K31/4375 , A61K31/4439 , A61K31/4545 , A61K31/505 , A61K31/506 , A61K31/519 , A61K31/522 , A61K45/06 , A61P19/02 , A61P19/08 , A61P19/10
CPC分类号： A61K31/00 , A61K31/4375 , A61K31/4439 , A61K31/4545 , A61K31/505 , A61K31/506 , A61K31/519 , A61K31/522 , A61K45/06 , A61K2300/00
摘要： The present invention relates to the use of GPR119 receptor agonists for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. The present invention further relates to the use of a GPR119 receptor agonist in combination with a dipeptidyl peptidase IV (DPP-IV) inhibitor for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. A GPR119 receptor agonist and the combination of a GPR119 receptor agonist and a DPP-IV inhibitor promote bone formation in an individual.
摘要翻译：本发明涉及GPR119受体激动剂用于治疗或预防以低骨量为特征的疾病，例如骨质疏松症，以及增加个体骨量。本发明还涉及GPR119受体激动剂与二肽基肽酶IV（DPP-IV）抑制剂组合用于治疗或预防以低骨量为特征的疾病如骨质疏松症以及增加个体中的骨量的用途。 GPR119受体激动剂和GPR119受体激动剂和DPP-IV抑制剂的组合促进个体中的骨形成。

8. 发明申请

WO2006036688A9 GPR43 AND MODULATORS THEREOF FOR THE TREATMENT OF METABOLIC-RELATED DISORDERS 审中-公开
标题翻译： GPR43及其与代谢相关性疾病治疗的调节剂
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
申请人： ARENA PHARM INC , LEONARD JAMES N , HAKAK YARON
发明人： LEONARD JAMES N , HAKAK YARON
IPC分类号： G01N33/68
CPC分类号： G01N33/566 , G01N33/6845 , G01N2333/726 , G01N2500/00
摘要： 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.
摘要翻译：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。

9. 发明申请

WO2006076231A8 COMBINATION THERAPY FOR THE TREATMENT OF DIABETES AND CONDITIONS RELATED THERETO AND FOR THE TREATMENT OF CONDITIONS AMELIORATED BY INCREASING A BLOOD GLP-1 LEVEL 审中-公开
标题翻译：治疗与之相关的糖尿病和病症以及通过增加血液GLP-1水平来治疗条件的组合治疗
公开(公告)号：WO2006076231A8
公开(公告)日：2006-09-21
申请号：PCT/US2006000510
申请日：2006-01-09
申请人： ARENA PHARM INC , CHU ZHI-LIANG , LEONARD JAMES N , AL-SHAMMA HUSSIEN A , JONES ROBERT M
发明人： CHU ZHI-LIANG , LEONARD JAMES N , AL-SHAMMA HUSSIEN A , JONES ROBERT M
IPC分类号： A61K31/00 , A61K31/401 , A61K31/4196 , A61P3/10
CPC分类号： G01N33/76 , A61K31/00 , A61K31/401 , A61K31/415 , A61K31/4196 , A61K45/06 , G01N33/74 , G01N2333/726 , G01N2800/042 , G01N2800/2814 , G01N2800/2835 , G01N2800/2857 , G01N2800/2871 , A61K2300/00
摘要： The present invention concerns combination of an amount of a GPR119 agonist with an amount of a dipeptidyl peptidase IV (DPP-IV) inhibitor such that the combination provides an effect in lowering a blood glucose level or in increasing a blood GLP-1 level in a subject over that provided by the amount of the GPR119 agonist or the amount of the DPP-IV inhibitor alone and the use of such a combination for treating or preventing diabetes and conditions related thereto or conditions ameliorated by increasing a blood GLP-1 level. The present invention also relates to the use of a G protein-coupled receptor to screen for GLP-1 secretagogues.
摘要翻译：本发明涉及一定量的GPR119激动剂与二肽基肽酶IV（DPP-IV）抑制剂的量的组合，使得该组合提供降低血糖水平或增加血液GLP-1水平的效果受限于GPR119激动剂的量或单独的DPP-IV抑制剂的量以及这样的组合用于治疗或预防糖尿病和与之相关的病症或通过增加血液GLP-1水平而改善的病症。本发明还涉及G蛋白偶联受体筛选GLP-1促分泌素的用途。

10. 发明申请

WO2002068600A3 ENDOGENOUS AND NON-ENDOGENOUS VERSIONS OF HUMAN G PROTEIN-COUPLED RECEPTORS 审中-公开
公开(公告)号：WO2002068600A3
公开(公告)日：2002-09-06
申请号：PCT/US2002/005625
申请日：2002-02-26
申请人： ARENA PHARMACEUTICALS, INC. , LIAW, Chen, W. , CHALMERS, Derek, T. , BEHAN, Dominic, P. , MACIEJEWSKI-LENIOR, Dominique , LEONARD, James, N. , LIN, I-Lin , ORTUNO, Daniel
发明人： LIAW, Chen, W. , CHALMERS, Derek, T. , BEHAN, Dominic, P. , MACIEJEWSKI-LENIOR, Dominique , LEONARD, James, N. , LIN, I-Lin , ORTUNO, Daniel
IPC分类号： C07H21/04
摘要： The invention disclosed in this patent docuemnt 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 activity.

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