公开(公告)号：US20080200491A1

公开(公告)日：2008-08-21

申请号：US11917731

申请日：2006-06-21

申请人： Thuy-Anh Tran ,  Sangdon Han ,  P. Douglas Boatman

发明人： Thuy-Anh Tran ,  Sangdon Han ,  P. Douglas Boatman

IPC分类号： A61K31/438 ,  C07D471/10 ,  A61P9/10 ,  A61P25/02 ,  A61P25/16

CPC分类号： C07D471/10

摘要： The present invention relates to certain 1,2-dihydro-spiro[3H-indole-3,4′-piperidine]compounds of Formula (Ia): and pharmaceutically acceptable salts, solvates and hydrates thereof, wherein G, R1, R2, R3, R4, R5, and Ar are as disclosed herein (“Compound(s) of the Invention”), which are useful, for example, as cardio-protective and/or neuro-protective agents. The invention also provides pharmaceutical compositions comprising a Compound of the Invention and methods for treating, preventing and/or managing a vascular, cardiovascular or neurological disease or disorder, comprising administering to a patient in need thereof a Compound of the Invention.

摘要翻译： 本发明涉及式（Ia）的某些1,2-二氢螺[3H-吲哚-3,4'-哌啶]化合物及其药学上可接受的盐，溶剂化物和水合物，其中G，R1，R2，R3 ，R4，R5和Ar如本文所公开的（“本发明的化合物”），其可用作例如心保护和/或神经保护剂。 本发明还提供了包含本发明化合物和治疗，预防和/或控制血管，心血管或神经疾病或病症的方法的药物组合物，其包括向有需要的患者施用本发明的化合物。

公开(公告)号：US20050197350A1

公开(公告)日：2005-09-08

申请号：US10812075

申请日：2004-03-30

申请人： Yoshinori Sekiguchi ,  Kosuke Kanuma ,  Katsunori Omodera ,  Tsuyoshi Busujima ,  Thuy-Anh Tran ,  Sangdon Han ,  Martin Casper ,  Bryan Kramer ,  Graeme Semple ,  Ning Zou

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

IPC分类号： A61K31/47 ,  A61K31/4706 ,  A61K31/4709 ,  A61K31/498 ,  A61K31/505 ,  A61K31/506 ,  A61K31/513 ,  A61K31/517 ,  A61P1/14 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P25/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  C07D215/42 ,  C07D239/48 ,  C07D239/94 ,  C07D239/95 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

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 novel compounds of the Formula (I): 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： 本发明涉及作为MCH受体拮抗剂的式（I）的新化合物。 这些组合物可用于药物组合物，其用途包括改善记忆功能，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，心肌梗塞， 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，药物滥用障碍和包括帕金森氏病，癫痫和成瘾在内的运动障碍的暴饮暴食症。

公开(公告)号：US20070010671A1

公开(公告)日：2007-01-11

申请号：US10551431

申请日：2004-03-30

申请人： Yoshinori Sekiguchi ,  Kosuke Kanuma ,  Katsunori Omodera ,  Tsuyoshi Busujima ,  Thuy-Anh Tran ,  Sangdon Han ,  Martin Casper ,  Bryan Kramer

发明人： Yoshinori Sekiguchi ,  Kosuke Kanuma ,  Katsunori Omodera ,  Tsuyoshi Busujima ,  Thuy-Anh Tran ,  Sangdon Han ,  Martin Casper ,  Bryan Kramer

IPC分类号： C07D403/02 ,  C07D239/94

CPC分类号： C07D239/95 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12

摘要： The present invention relates to novel compounds of Formula (1): 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： 本发明涉及新的式（1）化合物：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，心肌梗塞， 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，药物滥用障碍和包括帕金森氏病，癫痫和成瘾在内的运动障碍的暴饮暴食症。

公开(公告)号：US20140235622A1

公开(公告)日：2014-08-21

申请号：US14166511

申请日：2014-01-28

申请人： Bradley Teegarden ,  Dennis Chapman ,  Juyi Choi ,  Konrad Feichtinger ,  Sangdon Han ,  Honnappa Jayakumar ,  Thuy-Anh Tran ,  Jay Xu ,  Ning Zou

发明人： Bradley Teegarden ,  Dennis Chapman ,  Juyi Choi ,  Konrad Feichtinger ,  Sangdon Han ,  Honnappa Jayakumar ,  Thuy-Anh Tran ,  Jay Xu ,  Ning Zou

IPC分类号： C07D417/12 ,  C07D401/12 ,  C07D231/16 ,  C07D413/12 ,  C07D403/12 ,  C07D409/12 ,  C07D405/12 ,  C07D231/12

CPC分类号： A61K31/415 ,  C07D231/12 ,  C07D231/16 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

摘要： The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A 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, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, 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-HT2A serotonin receptor associated disorders in combination with other pharmaceutical agents administered separately or together.

摘要翻译： 本发明涉及某些调节5-HT2A 5-羟色胺受体活性的式（Ia）化合物及其药物组合物。 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，心肌梗塞，短暂性脑缺血发作，心绞痛，中风，心房颤动，血块形成，哮喘或其症状，躁动或其症状的方法， 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，睡眠障碍，睡眠障碍，糖尿病性精神病，精神病，精神病， 相关疾病，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-HT2A 5-羟色胺受体相关疾病的方法。

公开(公告)号：US20090197935A1

公开(公告)日：2009-08-06

申请号：US12301172

申请日：2007-05-17

申请人： Bradley Teegarden ,  Dennis Chapman ,  Juyi Choi ,  Konrad Feichtinger ,  Sangdon Han ,  Honnappa Jayakumar ,  Thuy-Anh Tran ,  Jingdong Xu ,  Ning Zou

发明人： Bradley Teegarden ,  Dennis Chapman ,  Juyi Choi ,  Konrad Feichtinger ,  Sangdon Han ,  Honnappa Jayakumar ,  Thuy-Anh Tran ,  Jingdong Xu ,  Ning Zou

IPC分类号： A61K31/415 ,  C07D231/12 ,  A61P25/24

CPC分类号： A61K31/415 ,  C07D231/12 ,  C07D231/16 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

摘要： The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, 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-HT2A serotonin receptor associated disorders in combination with other pharmaceutical agents administered separately or together.

摘要翻译： 本发明涉及某些调节5-HT2A 5-羟色胺受体活性的式（Ia）化合物及其药物组合物。 化合物及其药物组合物涉及可用于治疗血小板聚集，冠状动脉疾病，心肌梗死，短暂性脑缺血发作，心绞痛，中风，心房颤动，血块形成，哮喘或其症状，躁动或其症状的方法， 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，睡眠障碍，睡眠障碍，糖尿病性精神病，精神病，精神病， 相关疾病，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-HT2A 5-羟色胺受体相关疾病的方法。

公开(公告)号：US08664258B2

公开(公告)日：2014-03-04

申请号：US13417028

申请日：2012-03-09

申请人： Bradley Teegarden ,  Dennis Chapman ,  Juyi Choi ,  Konrad Feichtinger ,  Sangdon Han ,  Honnappa Jayakumar ,  Thuy-Anh Tran ,  Jay Xu ,  Ning Zou

发明人： Bradley Teegarden ,  Dennis Chapman ,  Juyi Choi ,  Konrad Feichtinger ,  Sangdon Han ,  Honnappa Jayakumar ,  Thuy-Anh Tran ,  Jay Xu ,  Ning Zou

IPC分类号： A61K31/415 ,  C07D231/00

CPC分类号： A61K31/415 ,  C07D231/12 ,  C07D231/16 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

摘要： The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A 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, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, 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-HT2A serotonin receptor associated disorders in combination with other pharmaceutical agents administered separately or together.

摘要翻译： 本发明涉及某些调节5-HT2A 5-羟色胺受体活性的式（Ia）化合物及其药物组合物。 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，心肌梗塞，短暂性脑缺血发作，心绞痛，中风，心房颤动，血块形成，哮喘或其症状，躁动或其症状的方法， 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，睡眠障碍，睡眠障碍，糖尿病性精神病，精神病，精神病， 相关疾病，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-HT2A 5-羟色胺受体相关疾病的方法。

公开(公告)号：US08148417B2

公开(公告)日：2012-04-03

申请号：US12301172

申请日：2007-05-17

申请人： Bradley Teegarden ,  Dennis Chapman ,  Juyi Choi ,  Konrad Feichtinger ,  Sangdon Han ,  Honnappa Jayakumar ,  Thuy-Anh Tran ,  Jingdong Xu ,  Ning Zou

发明人： Bradley Teegarden ,  Dennis Chapman ,  Juyi Choi ,  Konrad Feichtinger ,  Sangdon Han ,  Honnappa Jayakumar ,  Thuy-Anh Tran ,  Jingdong Xu ,  Ning Zou

IPC分类号： A61K31/415 ,  C07D231/12 ,  A61P25/24

CPC分类号： A61K31/415 ,  C07D231/12 ,  C07D231/16 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

摘要： The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, 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-HT2A serotonin receptor associated disorders in combination with other pharmaceutical agents administered separately or together.

摘要翻译： 本发明涉及某些调节5-HT2A 5-羟色胺受体活性的式（Ia）化合物及其药物组合物。 化合物及其药物组合物涉及可用于治疗血小板聚集，冠状动脉疾病，心肌梗死，短暂性脑缺血发作，心绞痛，中风，心房颤动，血块形成，哮喘或其症状，躁动或其症状的方法， 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，睡眠障碍，睡眠障碍，糖尿病性精神病，精神病，精神病， 相关疾病，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-HT2A 5-羟色胺受体相关疾病的方法。

公开(公告)号：US08895776B2

公开(公告)日：2014-11-25

申请号：US12933196

申请日：2009-03-17

申请人： Thuy-Anh Tran ,  Weichao Chen ,  Bryan A. Kramer ,  Abu J. M. Sadeque ,  Anna Shifrina ,  Young-Jun Shin ,  Pureza Vallar ,  Ning Zou

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

IPC分类号： C07C241/00 ,  C07C271/12 ,  C07D213/75 ,  C07D241/20 ,  C07D277/48 ,  C07C275/24 ,  C07C275/34 ,  C07C271/28 ,  C07C309/15 ,  C07C275/28 ,  C07C275/30 ,  C07D333/36

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（XIIIa）的酰胺衍生物及其调节PGI 2受体活性的药物组合物。 本发明的化合物及其药物组合物涉及可用于治疗肺动脉高压（PAH）的方法; 特发性PAH; 家族性PAH; PAH与胶原血管疾病，先天性心脏病，门静脉高压，HIV感染，摄入药物或毒素，遗传性出血性毛细血管扩张症，脾切除术，肺静脉闭塞性疾病（PVOD）或肺毛细血管血管病变（PCH）有关）。 PAH具有明显的静脉或毛细血管介入; 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 行程; 缺血再灌注损伤; 再狭窄; 房颤; 在血管成形术或冠状动脉旁路手术个体或患有心房颤动的个体中血凝块形成; 动脉粥样硬化 动脉粥样硬化血栓形成 哮喘或其症状; 糖尿病性相关疾病如糖尿病性周围神经病变，糖尿病性肾病或糖尿病性视网膜病变; 青光眼或其他眼睛异常眼内疾病; 高血压; 炎; 银屑病; 牛皮癣关节炎 类风湿关节炎; 克罗恩病; 移植排斥反应 多发性硬化症 系统性红斑狼疮（SLE）; 溃疡性结肠炎 缺血再灌注损伤; 再狭窄; 动脉粥样硬化 粉刺; 1型糖尿病; 2型糖尿病; 败血症 和慢性阻塞性肺疾病（COPD）。

公开(公告)号：US20150191454A1

公开(公告)日：2015-07-09

申请号：US14566019

申请日：2014-12-10

申请人： Thuy-Anh Tran ,  Rena Hayashi ,  Jason B. Ibarra ,  Brett Ullman ,  Ning Zou

发明人： Thuy-Anh Tran ,  Rena Hayashi ,  Jason B. Ibarra ,  Brett Ullman ,  Ning Zou

IPC分类号： C07D409/04 ,  C07D403/04 ,  C07D253/07 ,  C07D237/14 ,  C07D401/04

CPC分类号： C07D237/14 ,  C07D253/07 ,  C07D401/04 ,  C07D403/04 ,  C07D409/04

摘要： Cyclohexane derivatives of Formula Ia 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) and related disorders; 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： 式Ia的环己烷衍生物及其药物组合物，其调节PGI 2受体的活性。 本发明的化合物及其药物组合物涉及可用于治疗肺动脉高压（PAH）和相关疾病的方法; 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 行程; 缺血再灌注损伤; 再狭窄; 房颤; 在血管成形术或冠状动脉旁路手术个体或患有心房颤动的个体中血凝块形成; 动脉粥样硬化 动脉粥样硬化血栓形成 哮喘或其症状; 糖尿病性相关疾病如糖尿病性周围神经病变，糖尿病性肾病或糖尿病性视网膜病变; 青光眼或其他眼睛异常眼内疾病; 高血压; 炎; 银屑病; 牛皮癣关节炎 类风湿关节炎; 克罗恩病; 移植排斥反应 多发性硬化症 系统性红斑狼疮（SLE）; 溃疡性结肠炎 缺血再灌注损伤; 再狭窄; 动脉粥样硬化 粉刺; 1型糖尿病; 2型糖尿病; 败血症 和慢性阻塞性肺疾病（COPD）。

公开(公告)号：US20150126527A1

公开(公告)日：2015-05-07

申请号：US14510669

申请日：2014-10-09

申请人： Thuy-Anh Tran ,  Weichao Chen ,  Bryan A. Kramer ,  Abu J.M. Sadeque ,  Anna Shifrina ,  Young-Jun Shin ,  Pureza Vallar ,  Ning Zou

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

IPC分类号： A61K31/195 ,  A61K31/4406 ,  A61K31/426 ,  A61K31/4402 ,  A61K31/44 ,  A61K31/4965 ,  A61K31/325 ,  A61K31/381

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（XIIIa）的酰胺衍生物及其调节PGI 2受体活性的药物组合物。 本发明化合物及其药物组合物涉及用于治疗肺动脉高压（PAH）的方法： 特发性PAH; 家族性PAH; PAH与胶原血管疾病，先天性心脏病，门静脉高压，HIV感染，摄入药物或毒素，遗传性出血性毛细血管扩张症，脾切除术，肺静脉闭塞性疾病（PVOD）或肺毛细血管血管病变（PCH）有关）。 PAH具有明显的静脉或毛细血管介入; 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; 行程; 缺血再灌注损伤; 再狭窄; 房颤; 在血管成形术或冠状动脉旁路手术个体或患有心房颤动的个体中血凝块形成; 动脉粥样硬化 动脉粥样硬化血栓形成 哮喘或其症状; 糖尿病性相关疾病如糖尿病性周围神经病变，糖尿病性肾病或糖尿病性视网膜病变; 青光眼或其他眼睛异常眼内疾病; 高血压; 炎; 银屑病; 牛皮癣关节炎 类风湿关节炎; 克罗恩病; 移植排斥反应 多发性硬化症 系统性红斑狼疮（SLE）; 溃疡性结肠炎 缺血再灌注损伤; 再狭窄; 动脉粥样硬化 粉刺; 1型糖尿病; 2型糖尿病; 败血症 和慢性阻塞性肺疾病（COPD）。