公开(公告)号：EP1464335A3

公开(公告)日：2007-05-09

申请号：EP04007651.5

申请日：2004-03-30

申请人： Taisho Pharmaceutical Co. Ltd. ,  Arena Pharmaceuticals, Inc.

发明人： Sekiguchi, Yoshinori Taisho Pharmaceutical Co. Ltd ,  Kanuma, Kosuke Taisho Pharmaceutical Co. Ltd ,  Omodera, Katsunori Taisho Pharmaceutical Co. Ltd ,  Busujima, Tsuyoshi Taisho Pharmaceutical Co. Ltd ,  Tran, Thuy-Anh ,  Han, Sangdon ,  Casper, Martin ,  Kramer, Bryan A. ,  Semple, Graeme ,  Zou, Ning

IPC分类号： A61K31/4709 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D215/38 ,  A61K31/506 ,  A61P3/04

CPC分类号： C07D239/48 ,  C07D215/42 ,  C07D239/94 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

摘要： The present invention relates to compounds of the Formula (I)

wherein Q is:

which act as MCH receptor antagonists. These compositions are useful in pharmaceutical compositions whose use includes prophylaxis or treatment of improving memory function, sleeping and arousal, anxiety, depression, mood disorders, seizure, obesity, diabetes, appetite and eating disorders, cardiovascular disease, hypertension, dyslipidemia, myocardial infarction, binge eating disorders including bulimia, anorexia, mental disorders including manic depression, schizophrenia, delirium, dementia, stress, cognitive disorders, attention deficit disorder, substance abuse disorders and dyskinesias including Parkinson's disease, epilepsy, and addiction.

公开(公告)号：EP2857015A1

公开(公告)日：2015-04-08

申请号：EP14182803.8

申请日：2009-03-17

申请人： Arena Pharmaceuticals, Inc.

发明人： Tran, Thuy-Anh ,  Chen, Weichao ,  Kramer, Bryan A. ,  Sadeque, Abu J. M. ,  Shifrina, Hanna L. ,  Shin, Young-Jun ,  Vallar, Pureza ,  Zou, Ning

IPC分类号： A61K31/17 ,  A61K31/27 ,  C07C271/08 ,  C07C275/18 ,  A61P43/00

CPC分类号： A61K31/195 ,  A61K31/27 ,  A61K31/325 ,  A61K31/381 ,  A61K31/426 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4965 ,  C07B2200/07 ,  C07B2200/13 ,  C07C271/12 ,  C07C271/28 ,  C07C275/24 ,  C07C275/28 ,  C07C275/30 ,  C07C275/34 ,  C07C309/15 ,  C07C2601/14 ,  C07D213/75 ,  C07D241/20 ,  C07D277/48 ,  C07D333/36

摘要： The present invention relates to amide derivatives of Formula (XIIIa) and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.

Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pulmonary arterial hypertension (PAH); idiopathic PAH; familial PAH; PAH associated with a collagen vascular disease, a congenital heart disease, portal hypertension, HIV infection, ingestion of a drug or toxin, hereditary hemorrhagic telangiectasia, splenectomy, pulmonary veno-occlusive disease (PVOD) or pulmonary capillary hemangiomatosis (PCH); PAH with significant venous or capillary involvement; platelet aggregation; coronary artery disease; myocardial infarction; transient ischemic attack; angina; stroke; ischemia-reperfusion injury; restenosis; atrial fibrillation; blood clot formation in an angioplasty or coronary bypass surgery individual or in an individual suffering from atrial fibrillation; atherosclerosis; atherothrombosis; asthma or a symptom thereof; a diabetic-related disorder such as diabetic peripheral neuropathy, diabetic nephropathy or diabetic retinopathy; glaucoma or other disease of the eye with abnormal intraocular pressure; hypertension; inflammation; psoriasis; psoriatic arthritis; rheumatoid arthritis; Crohn's disease; transplant rejection; multiple sclerosis; systemic lupus erythematosus (SLE); ulcerative colitis; ischemia-reperfusion injury; restenosis; atherosclerosis; acne; type 1 diabetes; type 2 diabetes; sepsis; and chronic obstructive pulmonary disorder (COPD).

摘要翻译： 本发明涉及式的酰胺衍生物（XIIIa的）及其药物组合物做了调节PGI2受体的活性。 本发明与药物组合物的化合物及其被引导到在治疗有用的方法：肺动脉高血压（PAH）; 特发性肺动脉高压; 家族性PAH; PAH与胶原血管病，先天性心脏疾病，门静脉高压，HIV感染，摄入药物或者毒素，遗传性出血性毛细血管扩张，脾切除术，肺静脉闭塞性疾病（PVOD）或者肺毛细血管多发性血管瘤（PCH）相关联; PAH与显著静脉或毛细血管参与; 血小板聚集; 冠状动脉疾病; 心肌梗死; 短暂性脑缺血发作; 心绞痛; 中风; 缺血再灌注损伤; 再狭窄; 房颤; 在一个冠状血管成形术或旁路手术个体或在患有心房纤维性颤动的个体患有血块形成; 动脉粥样硬化; 动脉粥样硬化; 哮喘或其症状; 糖尿病相关病症：诸如糖尿病性周围神经病，糖尿病性肾病或糖尿病性视网膜病; 青光眼或者伴有异常眼内压的其它眼部疾病; 高血压; 炎症; 牛皮癣; 银屑病性关节炎; 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（SLE）; 溃疡性结肠炎; 缺血再灌注损伤; 再狭窄; 动脉粥样硬化; 痤疮; 1型糖尿病; 2型糖尿病; 败血症; 和慢性阻塞性肺病（COPD）。

公开(公告)号：EP1464335A2

公开(公告)日：2004-10-06

申请号：EP04007651.5

申请日：2004-03-30

申请人： Taisho Pharmaceutical Co. Ltd. ,  Arena Pharmaceuticals, Inc.

发明人： Sekiguchi, Yoshinori Taisho Pharmaceutical Co. Ltd ,  Kanuma, Kosuke Taisho Pharmaceutical Co. Ltd ,  Omodera, Katsunori Taisho Pharmaceutical Co. Ltd ,  Busujima, Tsuyoshi Taisho Pharmaceutical Co. Ltd ,  Tran, Thuy-Anh ,  Han, Sangdon ,  Casper, Martin ,  Kramer, Bryan A. ,  Semple, Graeme ,  Zou, Ning

IPC分类号： A61K31/4709 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D215/38 ,  A61K31/506 ,  A61P3/04

CPC分类号： C07D239/48 ,  C07D215/42 ,  C07D239/94 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

摘要： The present invention relates to compounds of the Formula (I)
wherein Q is:
which act as MCH receptor antagonists. These compositions are useful in pharmaceutical compositions whose use includes prophylaxis or treatment of improving memory function, sleeping and arousal, anxiety, depression, mood disorders, seizure, obesity, diabetes, appetite and eating disorders, cardiovascular disease, hypertension, dyslipidemia, myocardial infarction, binge eating disorders including bulimia, anorexia, mental disorders including manic depression, schizophrenia, delirium, dementia, stress, cognitive disorders, attention deficit disorder, substance abuse disorders and dyskinesias including Parkinson's disease, epilepsy, and addiction.

摘要翻译： 本发明涉及式（I）的化合物，其中Q为：其作为MCH受体拮抗剂。 这些组合物可用于药物组合物，其用途包括预防或治疗改善记忆功能，睡眠和觉醒，焦虑，抑郁，情绪障碍，癫痫发作，肥胖症，糖尿病，食欲和进食障碍，心血管疾病，高血压，血脂异常，心肌梗死， 包括贪食症，厌食症，包括躁狂抑郁症，精神分裂症，del妄，痴呆，压力，认知障碍，注意力缺陷障碍，药物滥用障碍和运动障碍，包括帕金森氏病，癫痫症和成瘾症的暴饮暴食症。