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1. 发明申请

WO2007027661A3 HUMAN G PROTEIN-COUPLED RECEPTOR AND MODULATORS THEREOF FOR THE TREATMENT OF ATHEROSCLEROSIS AND ATHEROSCLEROTIC DISEASE AND FOR THE TREATMENT OF CONDITIONS RELATED TO MCP-1 EXPRESSION 审中-公开
公开(公告)号：WO2007027661A3
公开(公告)日：2007-03-08
申请号：PCT/US2006/033651
申请日：2006-08-29
申请人： ARENA PHARMACEUTICALS, INC. , HAKAK, Yaron , UNETT, David J. , GATLIN, Joel , LIAW, Chen W.
发明人： HAKAK, Yaron , UNETT, David J. , GATLIN, Joel , LIAW, Chen W.
IPC分类号： G01N33/74 , C07K14/72
摘要： The present invention relates to methods of using a G protein-coupled receptor (GPCR), for example GPR84, 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-I expression, including but not limited to rheumatoid arthritis, Crohn's disease, and multiple sclerosis.

2. 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。

3. 发明申请

WO2006055734A2 3-PHENYL-PYRAZOLE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
标题翻译：作为用于治疗相关疾病的5-HT2A丝氨酸受体的调节剂的3-苯基 - 吡唑衍生物
公开(公告)号：WO2006055734A2
公开(公告)日：2006-05-26
申请号：PCT/US2005/041726
申请日：2005-11-17
申请人： ARENA PHARMACEUTICALS, INC. , TEEGARDEN, Bradley , XIONG, Yifeng , STRAH-PLEYNET, Sonja , JAYAKUMAR, Honnappa , DOSA, Peter I. , FEICHTINGER, Konrad , CASPER, Martin , LEHMANN, Juerg , JONES, Robert M. , UNETT, David J.
发明人： TEEGARDEN, Bradley , XIONG, Yifeng , STRAH-PLEYNET, Sonja , JAYAKUMAR, Honnappa , DOSA, Peter I. , FEICHTINGER, Konrad , CASPER, Martin , LEHMANN, Juerg , JONES, Robert M. , UNETT, David J.
CPC分类号： C07D231/12 , A61K31/5377 , C07D231/16 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/10 , C07D413/12 , C07D417/12 , C07D487/08
摘要： The present invention relates to certain 3-phenyl-pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT 2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT 2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together.
摘要翻译：本发明涉及式（Ia）的某些3-苯基 - 吡唑衍生物及其药物组合物，其调节5-HT 2A / 5-羟色胺受体的活性。化合物及其药物组合物涉及可用于治疗血小板凝集，冠状动脉疾病，心肌梗死，短暂性脑缺血发作，心绞痛，中风，心房颤动，降低血块形成风险，哮喘或其症状，激动或症状，行为障碍，药物诱导的精神病，兴奋性精神病，吉列斯图雷特综合征，躁狂症，有机或非精神病精神病，精神病，精神病，急性精神分裂症，慢性精神分裂症，精神分裂症精神分裂症和相关疾病，以及睡眠障碍，睡眠障碍，糖尿病相关病症，进行性多灶性脑白质病等。本发明还涉及与单独或一起施用的其它药剂组合治疗5-HT 2A 5-羟色胺受体介导的病症的方法。

4. 发明申请

WO2005116653A3 MODULATORS OF HUMAN G PROTEIN-COUPLED RECEPTORS FOR THE TREATMENT OF HYPERGLYCEMIA AND RELATED DISORDERS 审中-公开
标题翻译：人G蛋白相关受体调节剂治疗高血压和相关疾病
公开(公告)号：WO2005116653A3
公开(公告)日：2006-05-18
申请号：PCT/US2005012447
申请日：2005-04-12
申请人： ARENA PHARM INC , QIU JUN , WEBB ROBERT R , UNETT DAVID J , GATLIN JOEL E , CONNOLLY DANIEL T
发明人： QIU JUN , WEBB ROBERT R , UNETT DAVID J , GATLIN JOEL E , CONNOLLY DANIEL T
IPC分类号： G01N33/566 , A61K31/427 , A61K31/4439 , A61K45/06 , C07D417/04 , G01N33/68 , G01N33/76
CPC分类号： C07D417/04 , A61K31/427 , A61K31/4439 , G01N33/76 , G01N2333/726
摘要： The present invention relates to methods of identifying whether one or more candidate compounds is a modulator of a G protein-coupled receptor (GPCR) or a modulator of blood glucose concentration. In certain embodiments, the GPCR is human. The present invention also relates to methods of using a modulator of the GPCR. A preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for lowering blood glucose concentration, for preventing or treating certain metabolic disorders, such as insulin resistance, impaired glucose tolerance, and diabetes, and for preventing or treating a complication of an elevated blood glucose concentration, such as atherosclerosis, heart disease, stroke, hypertension and peripheral vascular disease.
摘要翻译：本发明涉及鉴定一种或多种候选化合物是G蛋白偶联受体（GPCR）或血糖浓度调节剂的调节剂的方法。在某些实施方案中，GPCR是人。本发明还涉及使用GPCR的调制器的方法。优选的调节剂是激动剂。本发明的激动剂可用作降低血糖浓度的治疗剂，用于预防或治疗某些代谢紊乱，例如胰岛素抵抗，葡萄糖耐量异常和糖尿病，以及用于预防或治疗血糖浓度升高的并发症，作为动脉粥样硬化，心脏病，中风，高血压和外周血管疾病。

5. 发明申请

WO2005119252A3 MODULATORS OF GPR35 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：WO2005119252A3
公开(公告)日：2006-01-12
申请号：PCT/US2005018082
申请日：2005-05-23
申请人： ARENA PHARM 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： A61K31/425 , G01N33/50 , A61P3/06 , A61P3/10
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，其包括使GPR35与有效量的式（I）化合物或其药学上可接受的盐接触，其中X为O或S; 并且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烷氧基任选被碳-C 1-4 - 烷氧基或羧基取代。

6. 发明申请

WO2006055734A3 3-PHENYL-PYRAZOLE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
标题翻译： 3-苯基 - 吡唑衍生物作为用于治疗与其有关的疾病的5-HT2A血清素受体的调节剂
公开(公告)号：WO2006055734A3
公开(公告)日：2006-08-17
申请号：PCT/US2005041726
申请日：2005-11-17
申请人： ARENA PHARM INC , TEEGARDEN BRADLEY , XIONG YIFENG , STRAH-PLEYNET SONJA , JAYAKUMAR HONNAPPA , DOSA PETER I , FEICHTINGER KONRAD , CASPER MARTIN , LEHMANN JUERG , JONES ROBERT M , UNETT DAVID J
发明人： TEEGARDEN BRADLEY , XIONG YIFENG , STRAH-PLEYNET SONJA , JAYAKUMAR HONNAPPA , DOSA PETER I , FEICHTINGER KONRAD , CASPER MARTIN , LEHMANN JUERG , JONES ROBERT M , UNETT DAVID J
IPC分类号： C07D231/16 , A61K31/4155 , A61P29/00 , C07D231/12 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D487/08
CPC分类号： C07D231/12 , A61K31/5377 , C07D231/16 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/10 , C07D413/12 , C07D417/12 , C07D487/08
摘要： The present invention relates to certain 3-phenyl-pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT 2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT 2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together.
摘要翻译：本发明涉及调节5-HT 2A受体5-羟色胺受体活性的式（Ia）的某些3-苯基 - 吡唑衍生物及其药物组合物。其化合物和药物组合物涉及用于治疗血小板聚集，冠状动脉疾病，心肌梗塞，短暂性脑缺血发作，心绞痛，中风，心房纤颤，降低血块形成风险，哮喘或其症状，激动或精神病，精神病，急性精神分裂症，慢性精神分裂症，NOS精神分裂症和相关障碍，以及睡眠障碍，睡眠障碍，睡眠障碍，睡眠障碍，精神病症状，行为障碍，药物诱导的精神病，兴奋性精神病，吉勒斯德拉图雷特综合征，，糖尿病相关病症，进行性多灶性白质脑病等。本发明还涉及与单独或一起施用的其他药剂联合治疗5-HT 2A受体5-羟色胺受体介导的病症的方法。

7. 发明申请

WO2006060762A3 PYRAZOLE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
公开(公告)号：WO2006060762A3
公开(公告)日：2006-06-08
申请号：PCT/US2005/043893
申请日：2005-12-01
申请人： ARENA PHARMACEUTICALS, INC. , STRAH-PLEYNET, Sonja , TEEGARDEN, Bradley , UNETT, David J.
发明人： STRAH-PLEYNET, Sonja , TEEGARDEN, Bradley , UNETT, David J.
IPC分类号： C07D231/38 , C07D401/12 , A61K31/415 , A61P25/00
摘要： The present invention relates to certain pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together.

8. 发明申请

WO2007027661A2 HUMAN G PROTEIN-COUPLED RECEPTOR AND MODULATORS THEREOF FOR THE TREATMENT OF ATHEROSCLEROSIS AND ATHEROSCLEROTIC DISEASE AND FOR THE TREATMENT OF CONDITIONS RELATED TO MCP-1 EXPRESSION 审中-公开
标题翻译：人G蛋白偶联受体及其治疗ATHEROSCLOSOSIS和ATHEROSCLEROTIC DISEASE治疗与MCP-1表达相关的条件的调节剂
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
申请人： ARENA PHARM INC , HAKAK YARON , UNETT DAVID J , GATLIN JOEL , LIAW CHEN W
发明人： HAKAK YARON , UNETT DAVID J , GATLIN JOEL , LIAW CHEN W
IPC分类号： G01N33/74 , C07K14/72
CPC分类号： G01N33/5041 , A61K38/1709 , A61K49/0008 , C07K14/47 , C07K14/723 , G01N33/6893 , G01N33/74 , G01N2333/726 , G01N2500/00 , G01N2800/32 , G01N2800/323
摘要： 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.
摘要翻译：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。

9. 发明申请

WO2006078610A1 DIARYL AND ARYLHETEROARYL UREA DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE PROPHYLAXIS OR TREATMENT OF PROGRESSIVE MULTIFOCAL LEUKOENCEPHALOPATHY 审中-公开
标题翻译：作为有利于预防或治疗进展性多发性白血病的5-HT2A丝氨酸受体的调节剂的二元和尿苷尿素衍生物
公开(公告)号：WO2006078610A1
公开(公告)日：2006-07-27
申请号：PCT/US2006/001516
申请日：2006-01-17
申请人： ARENA PHARMACEUTICALS, INC. , UNETT, David J. , TEEGARDEN, Bradley , JAYAKUMAR, Honnappa , LI, Hongmei , STRAH-PLEYNET, Sonja , DOSA, Peter I.
发明人： UNETT, David J. , TEEGARDEN, Bradley , JAYAKUMAR, Honnappa , LI, Hongmei , STRAH-PLEYNET, Sonja , DOSA, Peter I.
IPC分类号： A61K31/415 , A61P25/28
CPC分类号： A61K31/415
摘要： The present invention relates to certain pyrazole derivatives of Formula (I) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the prophylaxis or treatment of progressive multifocal leukoencephalopathy.
摘要翻译：本发明涉及式（I）的某些吡唑衍生物及其药物组合物，其调节5-HT2A 5-羟色胺受体的活性。化合物及其药物组合物涉及可用于预防或治疗进行性多灶性脑白质脑病的方法。

10. 发明申请

WO2006060762A2 PYRAZOLE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
标题翻译：作为用于治疗与相关疾病相关的疾病的5-HT2A丝氨酸受体的调节剂的吡唑衍生物
公开(公告)号：WO2006060762A2
公开(公告)日：2006-06-08
申请号：PCT/US2005043893
申请日：2005-12-01
申请人： ARENA PHARM INC , STRAH-PLEYNET SONJA , TEEGARDEN BRADLEY , UNETT DAVID J
发明人： STRAH-PLEYNET SONJA , TEEGARDEN BRADLEY , UNETT DAVID J
IPC分类号： C07D231/38 , A61K31/415 , A61P25/00 , C07D401/12
CPC分类号： C07D231/38 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： The present invention relates to certain pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together.
摘要翻译：本发明涉及式（Ia）的某些吡唑衍生物及其调节5-HT2A 5-羟色胺受体活性的药物组合物。化合物及其药物组合物涉及可用于治疗血小板聚集，冠状动脉疾病，心肌梗死，短暂性脑缺血发作，心绞痛，中风，心房颤动，降低血块形成风险，哮喘或其症状，激动或症状，行为障碍，药物诱发的精神病，兴奋性精神病，吉列斯·杜列特综合征，躁狂症，有机或NOS精神病，精神病，精神病，急性精神分裂症，慢性精神分裂症，精神分裂症精神分裂症和相关疾病，睡眠障碍，糖尿病相关疾病，进行性多灶性脑白质病等。本发明还涉及与单独或一起施用的其它药剂组合治疗5-HT2A 5-羟色胺受体介导的病症的方法。

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