公开(公告)号：WO2012135570A1

公开(公告)日：2012-10-04

申请号：PCT/US2012/031355

申请日：2012-03-30

Applicant: ARENA PHARMACEUTICALS, INC. ,  JONES, Robert M. ,  HAN, Sangdon ,  LEHMANN, Juerg ,  THORESEN, Lars

Inventor： JONES, Robert M. ,  HAN, Sangdon ,  LEHMANN, Juerg ,  THORESEN, Lars

IPC: C07D211/22 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D413/04 ,  C07D413/06 ,  A61K31/4545 ,  A61K31/445 ,  A61P3/06

CPC classification number: A61K31/506 ,  A61K31/445 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/497 ,  A61K45/06 ,  C07D211/22 ,  C07D211/24 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D413/04 ,  C07D413/06

Abstract: The present invention relates to compounds of Formula (Ia) and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as a single agent or in combination with one or more pharmaceutical agents, such as, an inhibitor of DPP-IV, a biguanide, or an alpha-glucosidase inhibitor, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing a blood incretin level; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.

Abstract translation: 本发明涉及式（Ia）化合物及其药学上可接受的盐，溶剂合物和水合物，其可用作单一试剂或与一种或多种药剂组合使用，例如DPP-IV抑制剂， 双胍或α-葡糖苷酶抑制剂，用于治疗例如选自以下的病症：GPR119-受体相关病症; 通过增加血液肠降血糖水平来改善病情; 代谢相关疾病; 2型糖尿病; 肥胖; 和相关的并发症。

公开(公告)号：WO2012116279A1

公开(公告)日：2012-08-30

申请号：PCT/US2012/026517

申请日：2012-02-24

Applicant: ARENA PHARMACEUTICALS, INC. ,  THATTE, Jayant ,  BLACKBURN, Anthony C. ,  HAN, Sangdon ,  JONES, Robert M. ,  JUNG, Jae-Kyu ,  MONTALBAN, Anthony Garrido ,  PAL, Biman B. ,  RUETER, Jaimie Karyn ,  STRAH-PLEYNET, Sonja ,  THORESEN, Lars ,  XIONG, Yifeng ,  YUE, Dawei ,  ZHU, Xiuwen

Inventor： THATTE, Jayant ,  BLACKBURN, Anthony C. ,  HAN, Sangdon ,  JONES, Robert M. ,  JUNG, Jae-Kyu ,  MONTALBAN, Anthony Garrido ,  PAL, Biman B. ,  RUETER, Jaimie Karyn ,  STRAH-PLEYNET, Sonja ,  THORESEN, Lars ,  XIONG, Yifeng ,  YUE, Dawei ,  ZHU, Xiuwen

IPC: C07D231/54 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07F9/09 ,  A61K31/416 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/661 ,  A61P29/00

CPC classification number: A61K31/497 ,  A61K31/13 ,  A61K31/416 ,  A61K31/4439 ,  A61K31/485 ,  A61K31/675 ,  A61K45/06 ,  C07D231/54 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07F9/65583

Abstract: Provided are certain methods useful in the treatment of pain comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB 2 receptor.

Abstract translation: 提供某些方法可用于治疗疼痛，包括施用式Ia化合物及其调节大麻素CB 2受体活性的药物组合物。

公开(公告)号：WO2012116278A1

公开(公告)日：2012-08-30

申请号：PCT/US2012/026510

申请日：2012-02-24

Applicant: ARENA PHARMACEUTICALS, INC. ,  THATTE, Jayant ,  BLACKBURN, Anthony C. ,  HAN, Sangdon ,  JONES, Robert M. ,  JUNG, Jae-Kyu ,  MONTALBAN, Anthony Garrido ,  PAL, Biman B. ,  RUETER, Jaimie Karyn ,  STRAH-PLEYNET, Sonja ,  THORESEN, Lars ,  XIONG, Yifeng ,  YUE, Dawei ,  ZHU, Xiuwen

Inventor： THATTE, Jayant ,  BLACKBURN, Anthony C. ,  HAN, Sangdon ,  JONES, Robert M. ,  JUNG, Jae-Kyu ,  MONTALBAN, Anthony Garrido ,  PAL, Biman B. ,  RUETER, Jaimie Karyn ,  STRAH-PLEYNET, Sonja ,  THORESEN, Lars ,  XIONG, Yifeng ,  YUE, Dawei ,  ZHU, Xiuwen

IPC: A61K31/416 ,  A61K45/06 ,  A61P19/02

CPC classification number: A61K31/416 ,  A61K31/4439 ,  A61K31/497 ,  A61K45/06 ,  A61K2300/00

Abstract: Provided are certain methods useful in the treatment of osteoarthritis comprising administering a compound of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB 2 receptor.

Abstract translation: 提供的某些方法可用于治疗骨关节炎，包括施用调节大麻素CB 2受体活性的式（Ia）化合物及其药物组合物。

公开(公告)号：WO2011005290A1

公开(公告)日：2011-01-13

申请号：PCT/US2010/001787

申请日：2010-06-22

Applicant: ARENA PHARMACEUTICALS, INC. ,  JONES, Robert M. ,  BUZARD, Daniel J. ,  HAN, Sangdon ,  LEHMANN, Juerg ,  LOPEZ, Luis A. ,  ULLMAN, Brett ,  KAWASAKI, Andrew M. ,  THORESEN, Lars ,  ZHU, Xiuwen

Inventor： JONES, Robert M. ,  BUZARD, Daniel J. ,  HAN, Sangdon ,  LEHMANN, Juerg ,  LOPEZ, Luis A. ,  ULLMAN, Brett ,  KAWASAKI, Andrew M. ,  THORESEN, Lars ,  ZHU, Xiuwen

IPC: C07D487/04 ,  A61K31/4245 ,  A61P17/06 ,  A61P17/10 ,  A61P19/02 ,  A61P29/00 ,  A61P31/12 ,  A61P43/00

CPC classification number: C07D487/04

Abstract: The present invention relates to certain disubstituted oxadiazole derivatives of Formula (Ia) and pharmaceutically acceptable salts, solvates, and hydrates thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, myocardial ischemia-reperfusion injury, hypertensive nephropathy, glomerulosclerosis, gastritis, polymyositis, thyroiditis, vitiligo, hepatitis, biliary cirrhosis, microbial infections and associated diseases, viral infections and associated diseases, diseases and disorders mediated by lymphocytes, auto immune diseases, inflammatory diseases, and cancer.

Abstract translation: 本发明涉及式（Ia）的某些二取代恶二唑衍生物及其药学上可接受的盐，溶剂合物和水合物，其表现出有用的药理学性质，例如作为S1P1受体的激动剂。 本发明还提供了含有本发明化合物的药物组合物，以及使用本发明化合物和组合物治疗S1P1相关病症的方法，例如牛皮癣，类风湿性关节炎，克罗恩病，移植排斥反应，多发性 硬化症，系统性红斑狼疮，溃疡性结肠炎，I型糖尿病，痤疮，心肌缺血再灌注损伤，高血压性肾病，肾小球硬化，胃炎，多发性肌炎，甲状腺炎，白癜风，肝炎，胆汁性肝硬化，微生物感染和相关疾病，病毒感染和相关疾病 ，由淋巴细胞介导的疾病和病症，自身免疫疾病，炎性疾病和癌症。

公开(公告)号：WO2008011015A2

公开(公告)日：2008-01-24

申请号：PCT/US2007/016182

申请日：2007-07-17

Applicant: JONES, Robert, M. ,  LISIECKI, Joseph, M.

Inventor： JONES, Robert, M. ,  LISIECKI, Joseph, M.

IPC: H02K15/085

CPC classification number: H02K15/085 ,  Y10T29/49009 ,  Y10T29/49071 ,  Y10T29/53143

Abstract: An apparatus for manufacturing an internal wound stator includes a winding arbor configured to receive a conductive wire. The apparatus also has a stator loader, and receives a stator having a generally cylindrical shape with an interior opening and having a plurality of axial slots formed therein. The interior dimension of the stator is larger than the exterior dimension of the winding arbor such that the winding arbor and stator may traverse with respect to one another. The apparatus also has a first movable member configured for moving at least one of the winding arbor and the stator. The apparatus also has a second rotating member configured to rotate at least one of the stator and the winding arbor. The conductive wire is introduced through an interior of the winding arbor. The first movable member is configured to move at least one of the winding arbor and the stator relative to one another to wind the conductive wire in a first longitudinal manner and into a first of the plurality of axial slots. The second rotating member is configured to rotate at least one of the first winding arbor or the stator relative to one another to align the wire relative to a second axial slot of the plurality of axial slots. The first movable member is configured to move at least one of the winding arbor and the stator relative to one another to wind the conductive wire in a second opposite longitudinal manner and into the second axial slot.

Abstract translation: 一种用于制造内部缠绕定子的装置包括构造成接纳导线的绕线轴。 该装置还具有定子装载器，并且接收具有大致圆柱形形状的定子，其具有内部开口并且在其中形成有多个轴向槽。 定子的内部尺寸大于绕组心轴的外部尺寸，使得绕组心轴和定子可以相对于彼此横越。 该装置还具有构造成用于移动绕组轴和定子中的至少一个的第一可动构件。 该装置还具有构造成旋转定子和绕组心轴中的至少一个的第二旋转构件。 导线通过绕组心轴的内部引入。 第一可移动构件被构造成相对于彼此移动至少一个绕组心轴和定子，以使第一纵向方式缠绕导线并进入多个轴向槽中的第一个。 第二旋转构件被配置为相对于彼此旋转第一卷绕心轴或定子中的至少一个，以使线相对于多个轴向槽中的第二轴向槽对准。 第一可移动部件构造成相对于彼此移动绕组轴和定子中的至少一个，以使第二相对纵向方式缠绕导线并进入第二轴向槽。

公开(公告)号：WO2006083491A3

公开(公告)日：2007-01-18

申请号：PCT/US2006000567

申请日：2006-01-09

Applicant: ARENA PHARM INC ,  JONES ROBERT M ,  LEHMANN JUERG ,  WONG AMY SIU-TING ,  HURST DAVID ,  SHIN YOUNG-JUN

Inventor： JONES ROBERT M ,  LEHMANN JUERG ,  WONG AMY SIU-TING ,  HURST DAVID ,  SHIN YOUNG-JUN

IPC: C07D401/14 ,  A61K31/44 ,  A61K31/505

CPC classification number: C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14

Abstract: The present invention relates to certain substituted pyridinyl and pyrimidinyl derivatives of Fomula (Ia) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the treatment of metabolic- related disorders and complications thereof, such as, diabetes and obesity.

Abstract translation: 本发明涉及作为代谢调节剂的Fomula（Ia）的某些取代的吡啶基和嘧啶基衍生物。 因此，本发明的化合物可用于治疗代谢相关疾病及其并发症，例如糖尿病和肥胖症。

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

Applicant: 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

Inventor： 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: C07D231/16 ,  A61K31/4155 ,  A61P29/00 ,  C07D231/12 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D487/08

CPC classification number: C07D231/12 ,  A61K31/5377 ,  C07D231/16 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/10 ,  C07D413/12 ,  C07D417/12 ,  C07D487/08

Abstract: 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.

Abstract translation: 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。

公开(公告)号：WO2006076231A2

公开(公告)日：2006-07-20

申请号：PCT/US2006/000510

申请日：2006-01-09

Applicant: ARENA PHARMACEUTICALS, INC. ,  CHI, Zhi-liang ,  LEONARD, James N. ,  AL-SHAMMA, Hussien A. ,  JONES, Robert M.

Inventor： CHI, Zhi-liang ,  LEONARD, James N. ,  AL-SHAMMA, Hussien A. ,  JONES, Robert M.

IPC: A61K31/00 ,  A61K31/401 ,  A61K31/4196 ,  A61P3/10

CPC classification number: 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

Abstract: The present invention concerns combination of an amount of a GPRl 19 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-I level in a subject over that provided by the amount of the GPRl 19 agonist or the amount of the DPP-FV 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-I level. The present invention also relates to the use of a G protein-coupled receptor to screen for GLP-I secretagogues.

Abstract translation: 本发明涉及GPR119激动剂的量与二肽基肽酶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 GPR119激动剂的量或单独的DPP-FV抑制剂的量所提供的受试者以及用于治疗或预防糖尿病和与之有关的病症或通过增加血液GLP-1水平而改善的病症的用途 。 本发明还涉及G蛋白偶联受体筛选GLP-1促分泌素的用途。

公开(公告)号：WO2004046687A3

公开(公告)日：2005-07-21

申请号：PCT/US0336153

申请日：2003-11-14

Applicant: QTL BIOSYSTEMS LLC ,  WHITTEN DAVID G ,  JONES ROBERT M ,  KUSHON STUART A ,  LEY KEVIN D ,  XIA WENSHENG ,  KUMARASWAMY SRIRAM ,  MCBRANCH DUNCAN W

Inventor： WHITTEN DAVID G ,  JONES ROBERT M ,  KUSHON STUART A ,  LEY KEVIN D ,  XIA WENSHENG ,  KUMARASWAMY SRIRAM ,  MCBRANCH DUNCAN W

IPC: B05D3/00 ,  C12M1/34 ,  C12Q1/68 ,  G01N20060101 ,  G01N33/53 ,  G01N33/533 ,  G01N33/542 ,  G01N33/543 ,  G01N33/566 ,  G01N33/569 ,  G01N33/58

CPC classification number: G01N33/533

Abstract: Complexes of a biotinylated fluorescent polymer and a biotin binding protein and solid supports coated with the fluorescent polymer complexes are described. The complexes can be used as sensors for detecting biological recognition events (e.g., nucleic acid hybridization reactions or enzymatic induced polypeptide cleavage). Methods of making the complexes and methods of using the complexes for detecting the presence and/or amount of a target analyte in a sample are also described. The target analyte can be an enzyme (e.g., beta-secretase) or a nucleic acid (e.g., a single stranded or double stranded nucleic acid).

Abstract translation: 描述了生物素化荧光聚合物和生物素结合蛋白的复合物和涂覆有荧光聚合物复合物的固体载体。 复合物可以用作检测生物识别事件（例如，核酸杂交反应或酶诱导的多肽切割）的传感器。 还描述了制备复合物的方法和使用复合物检测样品中目标分析物的存在和/或量的方法。 靶分析物可以是酶（例如β-分泌酶）或核酸（例如，单链或双链核酸）。

公开(公告)号：WO2005007658A3

公开(公告)日：2005-06-16

申请号：PCT/US2004022417

申请日：2004-07-13

Applicant: ARENA PHARM INC ,  JONES ROBERT M ,  SEMPLE GRAEME ,  XIONG YIFENG ,  SHIN YOUNG-JUN ,  REN ALBERT S ,  CALDERON IMELDA ,  FIORAVANTI BEATRIZ ,  CHOI JIN SUN KAROLINE ,  SAGE CARLTON R

Inventor： JONES ROBERT M ,  SEMPLE GRAEME ,  XIONG YIFENG ,  SHIN YOUNG-JUN ,  REN ALBERT S ,  CALDERON IMELDA ,  FIORAVANTI BEATRIZ ,  CHOI JIN SUN KAROLINE ,  SAGE CARLTON R

IPC: A61P3/00 ,  A61P3/10 ,  C07D215/22 ,  C07D215/233 ,  C07D471/04 ,  C07D473/00 ,  C07D487/04 ,  C07D498/04 ,  A61K31/4375 ,  A61K31/47 ,  A61K31/519 ,  A61K31/52

CPC classification number: C07D215/233 ,  C07D471/04 ,  C07D473/00 ,  C07D487/04

Abstract: The present invention relates to certain fused aryl and heteroaryl derivatives of Formula (I) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of metabolic disorders and complications thereof, such as, diabetes and obesity.

Abstract translation: 本发明涉及作为代谢调节剂的式（I）的某些稠合芳基和杂芳基衍生物。 因此，本发明化合物可用于预防或治疗代谢紊乱及其并发症，例如糖尿病和肥胖症。