公开(公告)号：AU2003282679A1

公开(公告)日：2004-05-04

申请号：AU2003282679

申请日：2003-10-02

Applicant: SEMPLE GRAEME ,  SHIN YOUNG JUN ,  ARENA PHARM INC

Inventor： SEMPLE GRAEME ,  SHIN YOUNG JUN

IPC: A61P3/00 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D231/00

公开(公告)号：AU2003282679A8

公开(公告)日：2004-05-04

申请号：AU2003282679

申请日：2003-10-02

Applicant: SHIN YOUNG JUN ,  SEMPLE GRAEME ,  ARENA PHARM INC

Inventor： SHIN YOUNG JUN ,  SEMPLE GRAEME

IPC: A61P3/00 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  A61K31/4152 ,  A61K31/44 ,  A61K31/495

公开(公告)号：WO2005051937A3

公开(公告)日：2005-09-15

申请号：PCT/US2004038920

申请日：2004-11-18

Applicant: ARENA PHARM INC ,  JUNG JAE-KYU ,  SEMPLE GRAEME ,  JOHNSON BENJAMIN R

Inventor： JUNG JAE-KYU ,  SEMPLE GRAEME ,  JOHNSON BENJAMIN R

IPC: C07D307/68 ,  C07D409/04 ,  C07D409/10 ,  A61K31/381 ,  A61P3/06

CPC classification number: C07D307/68 ,  C07D405/04 ,  C07D409/04 ,  C07D409/10

Abstract: System for selecting a colour shade comprising a very small number of colour dis­play cards with mixed shades of two or more colours. The system comprises means for selecting one shade among mixed shades, means for presenting the selected mixed shade as well as means for specifying the selected mixed shade for making paint in the desired colour tone.

Abstract translation: 用于选择颜色阴影的系统，其包括具有两种或更多种颜色的混合阴影的非常少量的彩色显示卡。 该系统包括用于在混合色调中选择一种色调的装置，用于呈现所选择的混合色调的装置以及用于指定所选择的混合色调以使油漆以期望色调的装置。

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：WO1995006040A1

公开(公告)日：1995-03-02

申请号：PCT/GB1994001859

申请日：1994-08-25

Applicant: YAMANOUCHI PHARMACEUTICAL CO. LTD. ,  FERRING RESEARCH LTD. ,  SEMPLE, Graeme ,  RYDER, Hamish ,  SZELKE, Michael ,  SATOH, Masato ,  OHTA, Mitsuaki ,  MIYATA, Keiji ,  NISHIDA, Akito ,  ISHII, Masato

Inventor： YAMANOUCHI PHARMACEUTICAL CO. LTD. ,  FERRING RESEARCH LTD.

IPC: C07D243/14

CPC classification number: C07D401/04 ,  C07D403/04 ,  C07D417/04

Abstract: A benzodiazepine derivative of formula (I), or a pharmaceutically acceptable salt thereof, wherein: (a) R is an alkyl, cycloalkyl or aryl group; (b) R is chosen from halo, OH, CH3, OCH3, NR R , NO2, NHCHO, CO2H and CN, and R and R are independently selected from H and alkyl (C1-C5) or together NR R form a cyclic structure (II), wherein a is 1-6; and (c) R is an aromatic 5- or 6-membered, substituted or unsubstituted heterocycle containing at least two heteroatoms of which at least one is nitrogen. These compounds are gastrin and/or CCK-B receptor antagonists.

Abstract translation: 式（I）的苯并二氮杂衍生物或其药学上可接受的盐，其中：（a）R 4是烷基，环烷基或芳基; （b）R 10选自卤素，OH，CH 3，OCH 3，NR 11 R 12，NO 2，NHCHO，CO 2 H和CN，R 11和R 12独立地选自H 和（C 1 -C 5）烷基或NR 11 R 12一起形成环状结构（II），其中a为1-6; 和（c）R 2是含有至少两个其中至少一个是氮的杂原子的芳族5-或6-元，取代或未取代的杂环。 这些化合物是胃泌素和/或CCK-B受体拮抗剂。

公开(公告)号：WO1994000438A1

公开(公告)日：1994-01-06

申请号：PCT/JP1993000844

申请日：1993-06-22

Applicant: YAMANOUCHI PHARMACEUTICAL CO., LTD. ,  FERRING B.V. ,  SATOH, Masato ,  OKAMOTO, Yoshinori ,  KOSHIO, Hiroyuki ,  NISHIDA, Akito ,  MIYATA, Keiji ,  OHTA, Mitsuaki ,  RYDER, Hamish ,  KENDRICK, David, A. ,  SEMPLE, Graeme ,  SZELKE, Michael

Inventor： YAMANOUCHI PHARMACEUTICAL CO., LTD. ,  FERRING B.V.

IPC: C07D243/24

CPC classification number: C07D401/04 ,  C07D243/24 ,  C07D401/12 ,  C07D403/12

Abstract: A novel benzodiazepine derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof. These compounds are useful as medicines, in particular, for treating and preventing diseases in which CCK-B receptor and gastrin receptor participate, because they have CCK-B receptor antagonism, gastrin receptor antagonism and the effect of inhibiting gastric juice secretion.

Abstract translation: 一种由通式（I）表示的新型苯二氮卓衍生物或其药学上可接受的盐。 这些化合物可用作药物，特别是用于治疗和预防CCK-B受体和胃泌素受体参与的疾病，因为它们具有CCK-B受体拮抗作用，胃泌素受体拮抗作用和抑制胃液分泌的作用。

公开(公告)号：WO2009058300A1

公开(公告)日：2009-05-07

申请号：PCT/US2008/012272

申请日：2008-10-29

Applicant: ARENA PHARMACEUTICALS, INC. ,  SANTORA, Vincent J. ,  COVEL, Jonathan A. ,  ESTRADA, Scott A. ,  IBARRA, Jason B. ,  REN, Albert S. ,  SCHULTZ, Jeffrey A. ,  SEMPLE, Graeme ,  SMITH, Brian M. ,  SMITH, Jeffrey ,  WEINHOUSE, Michael I.

Inventor： SANTORA, Vincent J. ,  COVEL, Jonathan A. ,  ESTRADA, Scott A. ,  IBARRA, Jason B. ,  REN, Albert S. ,  SCHULTZ, Jeffrey A. ,  SEMPLE, Graeme ,  SMITH, Brian M. ,  SMITH, Jeffrey ,  WEINHOUSE, Michael I.

IPC: C07D403/10 ,  C07D405/10 ,  C07D413/10 ,  A61K31/422 ,  A61K31/4025 ,  A61K31/5355 ,  A61P37/08

CPC classification number: C07D413/10 ,  C07D403/10 ,  C07D405/10

Abstract: Biphenyl derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the H3 histamine receptor. (Ia) Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of histamine H3-associated disorders, such as cognitive disorders, epilepsy, brain trauma, depression, obesity, disorders of sleep and wakefulness, such as narcolepsy, shift-work syndrome, drowsiness as a side effect from a medication, maintenance of vigilance to aid in completion of tasks and the like, cataplexy, hypersomnia, somnolence syndrome, jet lag, sleep apnea and the like, attention deficit hyperactivity disorder (ADHD), schizophrenia, allergies, allergic responses in the upper airway, allergic rhinitis, nasal congestion, dementia, Alzheimer's disease, pain and the like.

Abstract translation: 式（Ia）的联苯衍生物及其药物组合物，其调节H3组胺受体的活性。 （Ia）本发明化合物及其药物组合物涉及可用于治疗组胺H3相关疾病如认知障碍，癫痫，脑外伤，抑郁症，肥胖症，睡眠障碍和觉醒症如发作性睡病的方法 注意力缺陷多动障碍（ADHD），偏头痛综合征，转移综合征，嗜睡作为药物的副作用，维持警惕以帮助完成任务等，猝死，睡眠过多，嗜睡症，时差，睡眠呼吸暂停等 ），精神分裂症，过敏，上呼吸道过敏反应，过敏性鼻炎，鼻塞，痴呆，阿尔茨海默病，疼痛等。

公开(公告)号：WO2008005338A1

公开(公告)日：2008-01-10

申请号：PCT/US2007/015139

申请日：2007-06-28

Applicant: ARENA PHARMACEUTICALS, INC. ,  PARK, Douglas, M. ,  SANTORA, Vincent, J. ,  COVEL, Jonathan, A. ,  IBARRA, Jason, B. ,  SEMPLE, Graeme ,  SMITH, Brian ,  SMITH, Jeffrey ,  WEINHOUSE, Michael, I. ,  SCHULTZ, Jeffrey, A.

Inventor： SANTORA, Vincent, J. ,  COVEL, Jonathan, A. ,  IBARRA, Jason, B. ,  SEMPLE, Graeme ,  SMITH, Brian ,  SMITH, Jeffrey ,  WEINHOUSE, Michael, I. ,  SCHULTZ, Jeffrey, A.

IPC: C07D207/06 ,  C07D207/12 ,  C07D207/48 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D419/10 ,  A61K31/4025 ,  A61K31/4439 ,  A61K31/40 ,  A61K31/541 ,  A61K31/4409 ,  A61K31/5377

CPC classification number: C07D405/12 ,  C07D207/06 ,  C07D207/12 ,  C07D207/48 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D419/10

Abstract: The present invention relates to certain biphenyl sulfonamide derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the histamine H3-receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of histamine H3-receptor associated disorders, such as, cognitive disorders, epilepsy, brain trauma, depression, obesity, disorders of sleep and wakefulness such as narcolepsy, hypersomnia, somnolence syndrome, jet lag, sleep apnea and the like, attention deficit hyperactivity disorder (ADHD), schizophrenia, allergies, allergic responses in the upper airway, allergic rhinitis, nasal congestion, dementia, Alzheimer's disease and the like.

Abstract translation: 本发明涉及式（Ia）的某些联苯磺酰胺衍生物及其药物组合物，其调节组胺H3受体的活性。 化合物及其药物组合物涉及可用于治疗组胺H3-受体相关疾病的方法，例如认知障碍，癫痫症，脑外伤，抑郁症，肥胖症，睡眠障碍和觉醒症，例如发作性睡病，睡眠不足，嗜睡症， 射精滞后，睡眠呼吸暂停等，注意缺陷多动障碍（ADHD），精神分裂症，过敏，上呼吸道过敏反应，过敏性鼻炎，鼻塞，痴呆，阿尔茨海默氏病等。

公开(公告)号：WO2007061741A2

公开(公告)日：2007-05-31

申请号：PCT/US2006044479

申请日：2006-11-16

Applicant: ARENA PHARM INC ,  SANTORA VINCENT J ,  COVEL JONATHAN A ,  HAYASHI RENA ,  WEBB ROBERT R ,  REN ALBERT S ,  CHEN WEICHAO G ,  DUFFIELD JONATHAN J ,  IBARRA JASON B ,  PULLEY MICHELLE ,  SEMPLE GRAEME ,  WEINHOUSE MICHAEL I

Inventor： SANTORA VINCENT J ,  COVEL JONATHAN A ,  HAYASHI RENA ,  WEBB ROBERT R ,  REN ALBERT S ,  CHEN WEICHAO G ,  DUFFIELD JONATHAN J ,  IBARRA JASON B ,  PULLEY MICHELLE ,  SEMPLE GRAEME ,  WEINHOUSE MICHAEL I

CPC classification number: C07D209/52 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D405/10 ,  C07D405/14 ,  C07D409/06 ,  C07D413/06 ,  C07D417/04

Abstract: The present invention relates to certain fused heterobicyclic derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the H3 receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of H3-associated disorders, such as, cognitive disorders, epilepsy, brain trauma, depression, obesity, motion sickness and vertigo, disorders of sleep and wakefulness such as narcolepsy, shift-work syndrome, drowsiness as a side effect from a medication, maintenance of vigilance to aid in completion of tasks and the like, cataplexy, hypersomnia, somnolence syndrome, jet lag, sleep apnea and the like, attention deficit hyperactivity disorder (ADHD), schizophrenia, allergies, allergic responses in the upper airway, allergic rhinitis, nasal congestion, dementia, Alzheimer's disease and the like.

Abstract translation: 本发明涉及调节H3受体活性的式（Ia）的某些稠合杂双环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H3相关病症例如认知障碍，癫痫症，脑创伤，抑郁症，肥胖症，晕动病和眩晕，睡眠和觉醒失调例如发作性睡病，偏头痛， 工作综合症，作为药物副作用的困倦，保持警惕以帮助完成任务等，猝倒，睡眠过度，嗜睡综合征，时差，睡眠呼吸暂停等，注意力缺陷多动障碍（ADHD），精神分裂症 ，过敏，上呼吸道过敏反应，过敏性鼻炎，鼻充血，痴呆，阿尔茨海默病等。

公开(公告)号：WO2006069242A3

公开(公告)日：2006-06-29

申请号：PCT/US2005/046599

申请日：2005-12-22

Applicant: ARENA PHARMACEUTICALS, INC. ,  BOATMAN, Douglas, P. ,  SCHRADER, Thomas, O. ,  SEMPLE, Graeme ,  SKINNER, Philip, J. ,  JUNG, Jae-Kyu

Inventor： BOATMAN, Douglas, P. ,  SCHRADER, Thomas, O. ,  SEMPLE, Graeme ,  SKINNER, Philip, J. ,  JUNG, Jae-Kyu

IPC: C07D231/54 ,  A61K31/416 ,  A61P9/10 ,  C07D403/04 ,  A61K31/4155

Abstract: The present invention relates to certain fused pyrazole derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 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 metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, DP receptor antagonists, and the like.