公开(公告)号：WO2007035355A2

公开(公告)日：2007-03-29

申请号：PCT/US2006/035651

申请日：2006-09-14

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

Inventor： JONES, Robert, M. ,  LEHMANN, Juerg

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-羧酸异丙酯， 其为糖代谢调节剂的药学上可接受的盐，溶剂化物和水合物。 因此，本发明化合物可用于治疗代谢相关病症及其并发症，例如糖尿病和肥胖症。

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

Applicant: 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.

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.

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。

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：WO2021127459A1

公开(公告)日：2021-06-24

申请号：PCT/US2020/066044

申请日：2020-12-18

Applicant: BLACKTHORN THERAPEUTICS, INC. ,  BRANDT, Gray Edward Lee ,  DAVENPORT, Adam James ,  JONES, Robert M. ,  LOKE, Pui Leng ,  PACE, Robert ,  MORAO, Inaki ,  ELLWOOD, Simon

Inventor： BRANDT, Gray Edward Lee ,  DAVENPORT, Adam James ,  JONES, Robert M. ,  LOKE, Pui Leng ,  PACE, Robert ,  MORAO, Inaki ,  ELLWOOD, Simon

IPC: A61K31/4196 ,  C07D249/02 ,  C07D249/08

Abstract: Compounds are provided that modulate the GPR139 receptor, compositions containing the same, and to methods of their preparation and use for treatment of a malcondition wherein modulation of the GPR139 receptor is medically indicated or beneficial. Such compounds have the structure of Formula (I): or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein R1, R4, R5, R9, R10, Q6, Q7, and Q12 are as defined herein.

公开(公告)号：WO2019050988A1

公开(公告)日：2019-03-14

申请号：PCT/US2018/049607

申请日：2018-09-05

Applicant: BLACKTHORN THERAPEUTICS, INC. ,  JONES, Robert, M. ,  URBANO, Mariangela ,  BRANDT, Gary

Inventor： JONES, Robert, M. ,  URBANO, Mariangela ,  BRANDT, Gary ,  CHAMBERS, Mark ,  HARDICK, David ,  TIERNEY, Jason ,  KNIGHT, Chris ,  LOCK, Chris

IPC: C07D487/10 ,  C07D519/00 ,  A61P25/00 ,  A61P9/00 ,  A61K31/538 ,  A61K31/4439 ,  A61K31/553 ,  A61K31/5513 ,  A61K31/5415

Abstract: Compounds are provided that antagonize vasopressin receptors, particularly the V1a receptor products containing such compounds, as well as to methods of their use and synthesis. Such compounds have the structure of Formula (I), or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof: (I) wherein Q 1 , Q 2 , Q 3 , R 2a , R 2b , R 3 and X are as defined herein.

公开(公告)号：WO2012116277A1

公开(公告)日：2012-08-30

申请号：PCT/US2012/026507

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 ,  A61P35/00

CPC classification number: A61K31/675 ,  A61K31/416 ,  A61K31/4439 ,  A61K31/497 ,  A61K45/06 ,  A61K2300/00

Abstract: Provided are certain methods useful in the treatment of cancer comprising administering a compound of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor.

Abstract translation: 提供一些可用于治疗癌症的方法，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：WO2011005295A1

公开(公告)日：2011-01-13

申请号：PCT/US2010/001803

申请日：2010-06-23

Applicant: ARENA PHARMACEUTICALS, INC. ,  JONES, Robert M. ,  BUZARD, Daniel J. ,  SCHRADER, Thomas O. ,  KASEM, Michelle ,  ZHU, Xiuwen ,  JOHNSON, Benjamin R. ,  LEHMANN, Juerg ,  HAN, Sangdon ,  KAWASAKI, Andrew M.

Inventor： JONES, Robert M. ,  BUZARD, Daniel J. ,  SCHRADER, Thomas O. ,  KASEM, Michelle ,  ZHU, Xiuwen ,  JOHNSON, Benjamin R. ,  LEHMANN, Juerg ,  HAN, Sangdon ,  KAWASAKI, Andrew M.

IPC: C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D498/04 ,  A61K31/407 ,  A61K31/437 ,  A61P29/00 ,  A61P31/12 ,  A61P37/00

CPC classification number: C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D498/04

Abstract: The present invention relates to certain compounds 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 receptor-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: 本发明涉及某些式（Ia）化合物及其药学上可接受的盐，溶剂化物和水合物，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受体相关疾病例如牛皮癣，类风湿性关节炎，克罗恩病，移植排斥反应的方法， 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， 由淋巴细胞介导的疾病，疾病和病症，自身免疫疾病，炎性疾病和癌症。

公开(公告)号：WO2010027431A1

公开(公告)日：2010-03-11

申请号：PCT/US2009/004851

申请日：2009-08-26

Applicant: ARENA PHARMACEUTICALS, INC. ,  JONES, Robert, M. ,  BUZARD, Daniel, J. ,  KAWASAKI, Andrew, M. ,  KIM, Sun, Hee ,  THORESEN, Lars ,  LEHMANN, Juerg ,  ZHU, Xiuwen

Inventor： JONES, Robert, M. ,  BUZARD, Daniel, J. ,  KAWASAKI, Andrew, M. ,  KIM, Sun, Hee ,  THORESEN, Lars ,  LEHMANN, Juerg ,  ZHU, Xiuwen

IPC: C07D487/04 ,  A61K31/407 ,  A61K31/437 ,  A61P29/00 ,  A61P31/12 ,  A61P37/00

CPC classification number: C07D487/04 ,  C07D471/04

Abstract: The present invention relates to certain substituted tricyclic acid derivatives of Formula (I) 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, myocardial ischemia-reperfusion injury 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: 本发明涉及某些取代的式（I）的三环酸衍生物及其药学上可接受的盐，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 由淋巴细胞介导的疾病，疾病和病症，自身免疫疾病，炎性疾病和癌症。

公开(公告)号：WO2009151626A1

公开(公告)日：2009-12-17

申请号：PCT/US2009/003530

申请日：2009-06-12

Applicant: ARENA PHARMACEUTICALS, INC. ,  JONES, Robert, M. ,  HAN, Sangdon ,  MOODY, Jeanne, V.

Inventor： JONES, Robert, M. ,  HAN, Sangdon ,  MOODY, Jeanne, V.

IPC: C07D413/04 ,  C07D413/14 ,  A61K31/4196 ,  A61P1/00 ,  A61P3/10 ,  A61P17/06 ,  A61P19/00 ,  A61P29/00 ,  A61P37/00 ,  A61P37/06

CPC classification number: C07D413/14 ,  C07D413/04

Abstract: The present invention relates to certain substituted (1,2,4-oxadiazol-3-yl)indolin-2-yl carboxylic acid derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the SlPl 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 SlPl receptor-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）的某些取代的（1,2,4-恶二唑-3-基）二氢吲哚-2-基甲酸衍生物及其药学上可接受的盐，其表现出有用的药理学性质，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S1P1受体相关疾病例如牛皮癣，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，微生物感染或疾病以及病毒感染或疾病。

公开(公告)号：WO2009094157A1

公开(公告)日：2009-07-30

申请号：PCT/US2009/000399

申请日：2009-01-22

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

CPC classification number: C07D487/04

Abstract: The present invention relates to certain (1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-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 S1P1 associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, sepsis, myocardial infarction, ischemic stroke, 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）-2,3-二氢-1H-吡咯并[1,2-a]吲哚-1-基羧酸衍生物和 其药学上可接受的盐，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，败血症，心肌梗塞，缺血性中风，痤疮，微生物感染或疾病以及病毒感染或疾病。