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

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 ,  A61K31/4196 ,  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 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。

公开(公告)号：WO2005007658A2

公开(公告)日：2005-01-27

申请号：PCT/US2004/022417

申请日：2004-07-13

Applicant: ARENA PHARMACEUTICALS, 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: C07D487/04

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：WO2004076413A2

公开(公告)日：2004-09-10

申请号：PCT/US2004/005555

申请日：2004-02-23

Applicant: ARENA PHARMACEUTICALS, 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: C07D

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：WO2012170702A1

公开(公告)日：2012-12-13

申请号：PCT/US2012/041375

申请日：2012-06-07

Applicant: ARENA PHARMACEUTICALS, INC. ,  JONES, Robert, M. ,  BUZARD, Daniel, J. ,  HAN, Sangdon ,  KIM, Sun, Hee ,  LEHMANN, Juerg

Inventor： JONES, Robert, M. ,  BUZARD, Daniel, J. ,  HAN, Sangdon ,  KIM, Sun, Hee ,  LEHMANN, Juerg

IPC: C07D401/14 ,  C07D413/12 ,  C07D413/14 ,  A61K31/4439 ,  A61P19/00 ,  A61P3/10

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

Abstract: The present invention relates to compounds of Formula (Ia) and pharmaceutically acceptable salts, solvates, hydrates, and N -oxides thereof, that are useful as single pharmaceutical agents or in combination with one or more additional pharmaceutical agents, such as, an inhibitor of DPP-IV, a biguanide, an alpha-glucosidase inhibitor, an insulin analogue, a sulfonylurea, an SGLT2 inhibitor, a meglitinide, a thiazolidinedione, or an anti-diabetic peptide analogue, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing secretion of an incretin; a condition ameliorated by increasing a blood incretin level; a condition characterized by low bone mass; a neurological disorder; 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，水合物和N-氧化物，其可用作单一药剂或与一种或多种另外的药剂组合使用，例如 DPP-IV，双胍类，α-葡糖苷酶抑制剂，胰岛素类似物，磺酰脲类，SGLT2抑制剂，氯噻嗪，噻唑烷二酮或抗糖尿病肽类似物，用于治疗例如选自 ：GPR119受体相关疾病; 通过增加肠降血糖素的分泌而改善的状况; 通过增加血液肠降血糖水平来改善病情; 以低骨量为特征的病症; 神经障碍 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：WO2012145361A1

公开(公告)日：2012-10-26

申请号：PCT/US2012/034022

申请日：2012-04-18

Applicant: ARENA PHARMACEUTICALS, INC. ,  JONES, Robert M. ,  BUZARD, Daniel J. ,  HAN, Sangdon ,  KIM, Sun Hee ,  LEHMANN, Juerg ,  YUE, Dawei ,  ZHU, Xiuwen

Inventor： JONES, Robert M. ,  BUZARD, Daniel J. ,  HAN, Sangdon ,  KIM, Sun Hee ,  LEHMANN, Juerg ,  YUE, Dawei ,  ZHU, Xiuwen

IPC: C07D213/68 ,  C07D213/71 ,  C07D213/85 ,  C07D231/12 ,  C07D233/60 ,  C07D239/34 ,  C07D239/42 ,  C07D241/04 ,  C07D241/08 ,  C07D241/38 ,  C07D249/06 ,  C07D249/10 ,  C07D257/04 ,  C07D271/06 ,  C07D305/08

CPC classification number: C07D295/205 ,  A61K31/495 ,  A61K31/496 ,  A61K31/499 ,  A61K31/4995 ,  A61K31/506 ,  A61K45/06 ,  C07D207/325 ,  C07D213/68 ,  C07D213/71 ,  C07D213/85 ,  C07D231/12 ,  C07D233/60 ,  C07D239/34 ,  C07D239/42 ,  C07D241/04 ,  C07D241/08 ,  C07D241/38 ,  C07D249/06 ,  C07D249/08 ,  C07D249/10 ,  C07D257/04 ,  C07D271/06 ,  C07D271/07 ,  C07D295/21 ,  C07D295/26 ,  C07D305/08 ,  C07D401/12 ,  C07D403/12 ,  C07D471/08 ,  C07D487/08

Abstract: The present invention relates to compounds of Formula I and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as single pharmaceutical agents or in combination with one or more additional pharmaceutical agents, such as, a DPP-IV inhibitor, a biguanide, an alpha-glucosidase inhibitor, an insulin analogue, a sulfonylurea, an SGLT2 inhibitor, a meglitinide, a thiazolidinedione, or an anti-diabetic peptide analogue, 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 condition characterized by low bone mass; a neurological disorder; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.

Abstract translation: 本发明涉及式I化合物及其药学上可接受的盐，溶剂合物和水合物，其可用作单一药剂或与一种或多种另外的药剂组合使用，例如DPP-IV抑制剂，双胍类， α-葡萄糖苷酶抑制剂，胰岛素类似物，磺酰脲类，SGLT2抑制剂，氯噻嗪，噻唑烷二酮或抗糖尿病肽类似物，用于治疗例如选自以下的病症：GPR119-受体相关 紊乱; 通过增加血液肠降血糖水平来改善病情; 以低骨量为特征的病症; 神经障碍 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：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：WO2010114631A1

公开(公告)日：2010-10-07

申请号：PCT/US2010/001026

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: 无刷，液体或空气冷却的直流电机，由三层定子和三段转子组件构成，采用集成水冷或空气冷却外壳和包覆成型技术。

公开(公告)号：WO2009151621A1

公开(公告)日：2009-12-17

申请号：PCT/US2009/003524

申请日：2009-06-12

Applicant: ARENA PHARMACEUTICALS, INC. ,  JONES, Robert, M. ,  HAN, Sangdon ,  BUZARD, Daniel, J. ,  THORESEN, Lars ,  MOODY, Jeanne, V.

Inventor： JONES, Robert, M. ,  HAN, Sangdon ,  BUZARD, Daniel, J. ,  THORESEN, Lars ,  MOODY, Jeanne, V.

IPC: C07D413/04 ,  C07D413/14 ,  A61K31/4196 ,  A61P1/00 ,  A61P31/10 ,  A61P17/06 ,  A61P19/00 ,  A61P29/00 ,  A61P37/06

CPC classification number: C07D413/04 ,  C07D413/14

Abstract: The present invention relates to certain substituted (1,2,4-oxadiazol-3-yl)indolin-1-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 disorders associated with the S1P1, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, and acne.

Abstract translation: 本发明涉及具有有用的药理学性质的式（Ia）的某些取代的（1,2,4-恶二唑-3-基）二氢吲哚-1-基羧酸衍生物及其药学上可接受的盐，例如作为激动剂 的S1P1受体。 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与S1P1相关疾病的方法，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型糖尿病和痤疮。

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

Applicant: ARENA PHARMACEUTICALS, INC. ,  CHU, Zhi-liang ,  LEONARD, James, N. ,  JONES, Robert, M.

Inventor： CHU, Zhi-liang ,  LEONARD, James, N. ,  JONES, Robert, M.

IPC: G01N33/74

CPC classification number: G01N33/68 ,  G01N33/5044 ,  G01N2333/726 ,  G01N2800/042 ,  G01N2800/044 ,  G01N2800/065 ,  G01N2800/108 ,  G01N2800/323

Abstract: 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.

Abstract translation: 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。

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）