公开(公告)号：WO2011127051A1

公开(公告)日：2011-10-13

申请号：PCT/US2011/031243

申请日：2011-04-05

Applicant: ARENA PHARMACEUTICALS, INC. ,  JONES, Robert M. ,  HAN, Sangdon ,  BUZARD, Daniel J. ,  LEHMANN, Juerg ,  NARAYANAN, Sanju ,  YUE, Dawei

Inventor： JONES, Robert M. ,  HAN, Sangdon ,  BUZARD, Daniel J. ,  LEHMANN, Juerg ,  NARAYANAN, Sanju ,  YUE, Dawei

IPC: C07D211/46 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D413/06 ,  C07D413/14 ,  C07D417/14 ,  A61K31/445 ,  A61K31/454 ,  A61K31/495 ,  A61P3/10

CPC classification number: C07D211/46 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D413/06 ,  C07D413/14 ,  C07D417/14

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 additional pharmacetical agents, such as, an inhibitor of DPP-IV, a biguanide, an SGLT2 inhibitor, 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另外的药物制剂如DPP-IV抑制剂组合使用， 双胍类，SGLT2抑制剂或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：WO2011005929A1

公开(公告)日：2011-01-13

申请号：PCT/US2010/041325

申请日：2010-07-08

Applicant: ARENA PHARMACEUTICALS, INC. ,  JONES, Robert M. ,  LEHMANN, Juerg

Inventor： JONES, Robert M. ,  LEHMANN, Juerg

IPC: C07D403/14 ,  A61K31/506 ,  A61P3/04 ,  A61P3/10

CPC classification number: C07D403/14

Abstract: The present invention relates to the GPR119 agonist, N-(2-fluoro-4-(methylsulfonyl)phenyl)-5-methyl-6-(1-(5-methylpyrazin-2-yl)piperidin-4-yloxy)pyrimidin-4-amine (Compound 1, Formula (I)), and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful in the treatment of GPR119-related disorders, such as, metabolic-related disorders and complications thereof, such as, diabetes and obesity.

Abstract translation: 本发明涉及GPR119激动剂N-（2-氟-4-（甲基磺酰基）苯基）-5-甲基-6-（1-（5-甲基吡嗪-2-基）哌啶-4-基氧基） （化合物1，式（I））及其药学上可接受的盐，溶剂合物和水合物，其可用于治疗GPR119相关疾病，例如代谢相关障碍及其并发症， 糖尿病和肥胖。

公开(公告)号：WO2010114631A8

公开(公告)日：2010-12-23

申请号：PCT/US2010001026

申请日：2010-04-05

Applicant: JONES ROBERT M ,  LISIECKI JOSEPH M

Inventor： JONES ROBERT M ,  LISIECKI JOSEPH M

IPC: H02K23/00 ,  H02K7/00

CPC classification number: H02K16/00 ,  H02K1/185 ,  H02K3/32 ,  H02K5/225 ,  H02K9/22 ,  H02K11/33 ,  H02K29/08 ,  H02P5/747 ,  Y10T29/49009

Abstract: A brushless, liquid or air cooled, direct current motor formed from a three stack stator and three section rotor assembly using an integrated water cooled or air cooled housing and over-molding techniques.

Abstract translation: 由三层定子和三段式转子组件形成的无刷，液体或空气冷却的直流电动机，其使用集成的水冷或空气冷却的外壳和过度成型技术。

公开(公告)号：WO2010129539A2

公开(公告)日：2010-11-11

申请号：PCT/US2010/033534

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：WO2009078983A1

公开(公告)日：2009-06-25

申请号：PCT/US2008/013753

申请日：2008-12-15

Applicant: ARENA PHARMACEUTICALS, INC. ,  JONES, Robert, M. ,  BUZARD, Daniel, J. ,  KAWASAKI, Andrew, M. ,  LOPEZ, Luis, A. ,  MOODY, Jeanne, V. ,  THORESEN, Lars ,  ULLMAN, Brett

Inventor： JONES, Robert, M. ,  BUZARD, Daniel, J. ,  KAWASAKI, Andrew, M. ,  LOPEZ, Luis, A. ,  MOODY, Jeanne, V. ,  THORESEN, Lars ,  ULLMAN, Brett

IPC: C07D413/04 ,  C07D413/14 ,  A61K31/4245 ,  A61P37/00

CPC classification number: C07D413/14 ,  C07D413/04

Abstract: The present invention relates to certain (1,2,4-oxadiazol-3-yl)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl carboxylic acid derivatives of Formula (Ia) and pharmaceutically acceptable salts 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, microbial infections or diseases and viral infections or diseases.

Abstract translation: 本发明涉及式（Ia）的某些（1,2,4-恶二唑-3-基）-1,2,3,4-四氢环 - 五[b]吲哚-3-基甲酸衍生物和药学上可接受的 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 ，系统性红斑狼疮，溃疡性结肠炎，I型糖尿病，痤疮，微生物感染或疾病以及病毒感染或疾病。

公开(公告)号：WO2009009044A1

公开(公告)日：2009-01-15

申请号：PCT/US2008/008366

申请日：2008-07-08

Applicant: JONES, Robert, M.

Inventor： JONES, Robert, M. ,  VANHOOZEN, Bruce, L. ,  SIMS, Jesse, H.

IPC: B60K17/00

CPC classification number: B60K17/16 ,  B60L11/12 ,  B60L2200/22 ,  Y02T10/7077

Abstract: A differential for a vehicle having a suspension includes a first axle shaft, and a second axle shaft. The first axle shaft and the second axle shaft are disposed along a first axis of rotation. A first electric motor is disposed along a second axis of rotation. The second axis of rotation is spaced from the first axis of rotation. A housing is configured to support the first and second axle shafts. The shafts are disposed in a transverse manner through the housing. The first electric motor is also disposed in a transverse manner through the housing. The housing is configured to support the first electric motor as sprung weight, and in a location below the vehicle.

Abstract translation: 具有悬架的车辆的差速器包括第一车轴和第二车轴。 第一车轴和第二车轴沿着第一旋转轴线设置。 第一电动机沿着第二旋转轴设置。 第二旋转轴线与第一旋转轴线间隔开。 壳体构造成支撑第一和第二车轴。 轴以横向方式设置穿过壳体。 第一电动机也以横向方式设置穿过壳体。 壳体构造成将第一电动机支撑为弹簧重量，并且在车辆下方的位置。

公开(公告)号：WO2007133499A3

公开(公告)日：2008-08-14

申请号：PCT/US2007011023

申请日：2007-05-07

Applicant: JONES ROBERT M ,  LISIECKI JOSEPH M

Inventor： JONES ROBERT M ,  LISIECKI JOSEPH M

IPC: H02K5/128 ,  H02K1/27 ,  H02K16/04

CPC classification number: H02K1/278 ,  H02K3/38 ,  H02K5/04 ,  H02K5/18 ,  H02K5/225 ,  H02K11/33 ,  H02K16/00 ,  H02K21/16 ,  H02K29/08

Abstract: A rotor having a substantially cylindrical configuration for use in a brushless direct current electric motor having a high torque to size ratio. The rotor has an outer peripheral surface. The rotor also has a central rotor shaft and a first and second retaining ends mounted on the central rotor shaft and spaced from one another. The rotor also has a plurality of magnets configured to provide a magnetic flux with a stator disposed around the central rotor shaft. The magnets are radially disposed on the shaft and the rotor also has a sheath. The sheath is crimped around the radially disposed permanent magnets, and holds the magnets around the shaft. The sheath is lightweight and minimizes a gap between the permanent magnets and the stator to provide for an electromagnetic flux between the magnets and the stator windings, and for rotation of the central rotor shaft.

Abstract translation: 具有大体圆柱形构造的转子，用于具有高扭矩与大尺寸比的无刷直流电动机。 转子具有外周面。 转子还具有中心转子轴和安装在中心转子轴上并彼此间隔开的第一和第二保持端。 转子还具有多个磁体，其被配置为提供磁通量，该定子设置在中心转子轴周围。 磁体径向设置在轴上，转子也具有护套。 鞘被卷绕在径向设置的永磁体周围，并将磁体保持在轴周围。 护套是轻质的，并且使永磁体和定子之间的间隙最小化，以提供磁体和定子绕组之间的电磁通量，并且用于中心转子轴的旋转。

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

Applicant: ARENA PHARM INC ,  CHU ZHI-LIANG ,  LEONARD JAMES N ,  LEHMANN JUERG ,  JONES ROBERT M

Inventor： CHU ZHI-LIANG ,  LEONARD JAMES N ,  LEHMANN JUERG ,  JONES ROBERT M

IPC: 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 classification number: A61K31/00 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/505 ,  A61K31/506 ,  A61K31/519 ,  A61K31/522 ,  A61K45/06 ,  A61K2300/00

Abstract: 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.

Abstract translation: 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。

公开(公告)号：WO2007133500A3

公开(公告)日：2008-04-03

申请号：PCT/US2007011024

申请日：2007-05-07

Applicant: JONES ROBERT M ,  LISIECKI JOSEPH M

Inventor： JONES ROBERT M ,  LISIECKI JOSEPH M

IPC: H02K16/04 ,  H02K3/04

CPC classification number: H02K1/278 ,  H02K3/38 ,  H02K5/04 ,  H02K5/18 ,  H02K5/225 ,  H02K11/33 ,  H02K16/00 ,  H02K21/16 ,  H02K29/08

Abstract: An electric machine, such as a brushless direct current motor, includes a number of stator formed as stator sections. The stator sections are longitudinally offset from each other along a common central axis of the electric machine. The stator sections are magnetically independent of one another, but are electrically driven with offset phases typically in a manner similar to a standard multi-phase motor. The stator sections may be further offset with one another in radial position. The structure of the stator sections provides advantages in terms of efficiency, powe consumption, torque, and thermal performance, and can be especially advantageous where a battery is used to power the motor, such as in portable hand tools or driving motors for vehicles.

Abstract translation: 诸如无刷直流电动机的电机包括定子部分形成的多个定子。 定子部分沿着电机的公共中心轴线彼此纵向偏移。 定子部分彼此磁性地独立，但是通常以类似于标准多相电动机的方式以偏移相电动驱动。 定子部分可以在径向位置上彼此进一步偏移。 定子部分的结构在效率，功率消耗，扭矩和热性能方面提供了优点，并且在电池用于为电动机供电（诸如便携式手动工具或用于车辆的驱动电动机）中是特别有利的。

公开(公告)号：WO2007035355A3

公开(公告)日：2007-06-21

申请号：PCT/US2006035651

申请日：2006-09-14

Applicant: ARENA PHARM INC ,  JONES ROBERT M ,  LEHMANN JUERG

Inventor： JONES ROBERT M ,  LEHMANN JUERG

IPC: C07D401/14 ,  A61K31/506 ,  A61P5/50

CPC classification number: C07D401/14

Abstract: The present invention relates to 4-[5-methyl-6-(2-methyl-pyridin-3-yloxy)-pyrimidin-4-yloxy]-piperidine-1-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.

Abstract translation: 本发明涉及4- [5-甲基-6-（2-甲基 - 吡啶-3-基氧基） - 嘧啶-4-基氧基] - 哌啶-1-甲酸异丙酯，其药学上可接受的盐，溶剂合物和水合物 这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。