公开(公告)号：WO2004076413A3

公开(公告)日：2004-12-02

申请号：PCT/US2004005555

申请日：2004-02-23

Applicant: ARENA PHARM INC ,  JONES ROBERT M ,  SEMPLE GRAEME ,  CHOI JIN SUN KAROLINE ,  XIONG YIFENG ,  FIORAVANTI BEATRIZ

Inventor： JONES ROBERT M ,  SEMPLE GRAEME ,  CHOI JIN SUN KAROLINE ,  XIONG YIFENG ,  FIORAVANTI BEATRIZ

IPC: A61P3/00 ,  C07D211/14 ,  C07D211/62 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D413/04 ,  C07D413/12 ,  C07D417/14 ,  A61K31/435

CPC classification number: C07D401/04 ,  C07D211/14 ,  C07D211/62 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D413/04 ,  C07D413/12 ,  C07D417/14

Abstract: The present invention relates to certain certain substituted aryl and heteroaryl derivatives as shown in Formula (Ia) 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（Ia）所示的某些取代的芳基和杂芳基衍生物。 因此，本发明的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。

公开(公告)号：WO2010129539A3

公开(公告)日：2011-03-24

申请号：PCT/US2010033534

申请日：2010-05-04

Applicant: JONES ROBERT M

Inventor： JONES ROBERT M ,  LISIECKI JOSEPH M

IPC: F16D43/20 ,  F16D43/02

CPC classification number: F16D9/08

Abstract: A torque-limiling coupling may be used lo provide a torsion drive between an engine or motor and a driven accessory. If an accessory should experience a catastrophic failure a torsion limit is exceeded and a spline breaks away from the coupling. This guarantees that the internal engine gearing used to drive the accessory is not compromised and interfering with essential moving parts inside the engine. Further, a misalignment compensation limits the side load and wear that occurs when coupling two precision shafts with little clearance on the bearings. With a misalignment coupling, the mount can be slightly out of parallel with no negative effects.

Abstract translation: 可以使用扭矩 - 接头联接器来提供发动机或电动机和从动附件之间的扭转驱动。 如果配件遇到灾难性故障，则超出扭转极限，并且花键与联轴器脱离。 这确保用于驱动附件的内部发动机传动装置不会受到损害，并干扰发动机内部的主要运动部件。 此外，不对准补偿限制了在轴承上具有很小间隙的两个精密轴联接时发生的侧向载荷和磨损。 通过不对准耦合，安装座可以略微不平行，没有负面影响。

公开(公告)号：WO2008005569A3

公开(公告)日：2008-04-10

申请号：PCT/US2007015670

申请日：2007-07-05

Applicant: ARENA PHARM INC ,  JONES ROBERT M ,  LEHMANN JUERG ,  SIU-TING WONG AMY

Inventor： JONES ROBERT M ,  LEHMANN JUERG ,  SIU-TING WONG AMY

IPC: C07D401/14 ,  A61K31/506 ,  A61P3/00

CPC classification number: C07D401/14

Abstract: The present invention relates to 4-[5-Methoxy-6-(2-methyl-6-[l,2,4]triazol-l-yl-pyridin-3- ylamino)-pyrimidin-4-yloxy]-piperidine-l -carboxylic acid isopropyl ester, pharmaceutically acceptable salts, solvates and hydrates thereof that are modulators of glucose metabolism. Accordingly, compounds of the present invention are useful in the treatment of metabolic-related disorders and complications thereof, such as, diabetes and obesity. (Formula I)

Abstract translation: 本发明涉及4- [5-甲氧基-6-（2-甲基-6- [1,2,4]三唑-1-基 - 吡啶-3-基氨基） - 嘧啶-4-基氧基] 1-羧酸异丙酯，其药学上可接受的盐，溶剂合物和水合物，其是葡萄糖代谢的调节剂。 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。 （式I）

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：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。

公开(公告)号：US1065529A

公开(公告)日：1913-06-24

申请号：US1912671533

申请日：1912-01-16

Applicant: JONES ROBERT M

Inventor： JONES ROBERT M

CPC classification number: E04C3/34

公开(公告)号：WO2008011015A3

公开(公告)日：2008-03-06

申请号：PCT/US2007016182

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: 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。 该设备还具有定子装载器，并且容纳具有大致圆柱形形状的定子，该定子具有内部开口并且具有在其中形成的多个轴向槽。 定子的内部尺寸大于缠绕心轴的外部尺寸，使得缠绕心轴和定子可以相对于彼此横向运动。 该设备还具有第一可动构件，该第一可动构件被构造成用于移动绕线轴和定子中的至少一个。 该设备还具有第二旋转构件，该第二旋转构件构造成旋转定子和缠绕心轴中的至少一个。 导线通过缠绕心轴的内部引入。 第一可移动构件构造成使绕线轴和定子中的至少一个相对于彼此移动以将导线以第一纵向方式缠绕到多个轴向狭槽中的第一个中。 第二旋转构件构造成使第一缠绕心轴或定子中的至少一个相对于彼此旋转，以将线材相对于多个轴向狭槽中的第二轴向狭槽对准。 第一可移动构件被构造成使绕线轴和定子中的至少一个相对于彼此移动以将导线以第二相反纵向方式缠绕并且进入第二轴向狭槽中。

公开(公告)号：WO2006076231A3

公开(公告)日：2007-01-18

申请号：PCT/US2006000510

申请日：2006-01-09

Applicant: ARENA PHARM INC ,  CHU ZHI-LIANG ,  LEONARD JAMES N ,  AL-SHAMMA HUSSIEN A ,  JONES ROBERT M

Inventor： CHU ZHI-LIANG ,  LEONARD JAMES N ,  AL-SHAMMA HUSSIEN A ,  JONES ROBERT M

IPC: A61K31/00 ,  A61K31/401 ,  A61K31/415 ,  A61K31/4196 ,  A61P3/00 ,  A61P3/10 ,  C12N15/12 ,  G01N33/566 ,  G01N33/58

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 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.

Abstract translation: 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。