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1. 发明授权

US08940891B2 Modulators of the prostacyclin (PGI2) receptor useful for the treatment of disorders related thereto 有权
标题翻译：前列环素（PGI2）受体的调节剂可用于治疗与之相关的疾病
公开(公告)号：US08940891B2
公开(公告)日：2015-01-27
申请号：US13133036
申请日：2009-12-07
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： C07D253/07 , C07D401/04 , C07D403/04 , A61K31/53 , A61K31/4427 , A61P9/12 , A61P11/08 , C07D409/04 , C07D237/14 , A61K31/50 , A61K31/501
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）。

2. 发明申请

US20130217700A1 PYRAZOLE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
标题翻译：作为用于治疗与相关疾病相关的疾病的5-HT2A丝氨酸受体的调节剂的吡唑衍生物
公开(公告)号：US20130217700A1
公开(公告)日：2013-08-22
申请号：US13614537
申请日：2012-09-13
申请人： Yifeng Xiong , Martin C. Cherrier , Jin Sun Karoline Choi , Peter I. Dosa , Brian M. Smith , Sonja Strah-Pleynet , Brett Ullman , Bradley Teegarden
发明人： Yifeng Xiong , Martin C. Cherrier , Jin Sun Karoline Choi , Peter I. Dosa , Brian M. Smith , Sonja Strah-Pleynet , Brett Ullman , Bradley Teegarden
IPC分类号： C07D231/14 , C07D403/06 , C07D405/04 , C07D403/12
CPC分类号： C07D231/16 , C07D231/14 , C07D231/54 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/04
摘要： Pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the serotonin 5HT2A receptor. Formula (Ia). Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of insomnia and related sleep disorders, platelet aggregation, 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 symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-IIT2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together.
摘要翻译：式（Ia）的吡唑衍生物及其药物组合物，其调节5-羟色胺5HT2A受体的活性。式（Ia）。化合物及其药物组合物涉及可用于治疗失眠和相关睡眠障碍，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，降低血块形成风险，哮喘的方法精神病，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，精神分裂症及相关疾病，以及其他症状，症状或症状，激动或其症状，行为障碍，药物诱发的精神病，兴奋性精神病，糖尿病相关疾病，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-IIT2A 5-羟色胺受体介导的病症的方法。

3. 发明申请

US20110245251A1 MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 有权
标题翻译：用于治疗相关疾病的前列腺素（PGI2）受体的调节剂
公开(公告)号：US20110245251A1
公开(公告)日：2011-10-06
申请号：US13133036
申请日：2009-12-07
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： A61K31/53 , C07D237/14 , C07D401/04 , C07D409/04 , C07D403/04 , C07D253/07 , A61K31/50 , A61K31/501 , C12N5/071 , A61P9/12 , A61P7/02 , A61P9/00 , A61P9/10 , A61P11/06 , A61P3/10 , A61P13/12 , A61P27/02 , A61P25/02 , A61P27/06 , A61P29/00 , A61P17/06 , A61P19/02 , A61P37/06 , A61P25/28 , A61P17/10 , A61P11/00
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）。

4. 发明申请

US20110130409A1 SUBSTITUTED 1,2,3,4-TETRAHYDROCYCLOPENTA[B]INDOL-3-YL)ACETIC ACID DERIVATIVES USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS 有权
标题翻译：取代的1,2,3,4-四氢环戊二烯并[B]吲哚-3-基）乙酸衍生物用于治疗自身免疫和炎症性疾病
公开(公告)号：US20110130409A1
公开(公告)日：2011-06-02
申请号：US13055333
申请日：2009-07-22
申请人： Robert M. Jones , Daniel J. Buzard , Sangdon Han , Sun Hee Kim , Juerg Lehmann , Brett Ullman , Jeanne V. Moody , Xiuwen Zhu , Scott Stirn
发明人： Robert M. Jones , Daniel J. Buzard , Sangdon Han , Sun Hee Kim , Juerg Lehmann , Brett Ullman , Jeanne V. Moody , Xiuwen Zhu , Scott Stirn
IPC分类号： A61K31/497 , C07D209/94 , C07D403/12 , C07D401/12 , C07D417/12 , A61K31/403 , A61K31/4439 , A61K31/433 , A61P37/06 , A61P29/00 , A61P35/00 , A61P17/06 , A61P25/28 , A61P3/10 , A61P1/00 , A61P17/10 , A61P31/00 , A61P31/12
CPC分类号： C07D209/94 , A61K31/137 , A61K31/198 , A61K31/404 , A61K31/433 , A61K31/4439 , A61K31/497 , C07C211/27 , C07C229/26 , C07C255/03 , C07C279/14 , C07D209/70 , C07D209/88 , C07D401/12 , C07D401/14 , C07D403/12 , C07D417/12 , Y02A50/475
摘要： The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic 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 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.
摘要翻译：本发明涉及式（Ia）的某些取代的1,2,3,4-四氢环戊并[b]吲哚-3-基）乙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，微生物感染或疾病以及病毒感染或疾病。

5. 发明申请

US20190142826A1 IMIDAZO[1,2-A]PYRIDINE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
公开(公告)号：US20190142826A1
公开(公告)日：2019-05-16
申请号：US16101896
申请日：2018-08-13
申请人： Yifeng XIONG , Konrad FEICHTINGER , Albert S, REN , Brett ULLMAN
发明人： Yifeng XIONG , Konrad FEICHTINGER , Albert S, REN , Brett ULLMAN
IPC分类号： A61K31/496 , A61K31/5377 , C07D471/04 , A61K9/00
摘要： rmidazo[1,2-α]pyridine derivatives 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 insomnia, dyssomnia, parasomnia and related sleep disorders, platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, thrombosis, asthma or symptoms thereof, agitation or symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de Ia Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to methods for the treatment of 5-HT2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together.

6. 发明授权

US09567327B2 Imidazo[1,2-a]pyridine derivatives as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto 有权
标题翻译：咪唑并[1,2-a]吡啶衍生物作为可用于治疗与之相关疾病的5-HT2A 5-羟色胺受体的调节剂
公开(公告)号：US09567327B2
公开(公告)日：2017-02-14
申请号：US12673463
申请日：2008-08-14
申请人： Yifeng Xiong , Konrad Feichtinger , Albert S. Ren , Brett Ullman
发明人： Yifeng Xiong , Konrad Feichtinger , Albert S. Ren , Brett Ullman
IPC分类号： A61K31/5377 , A61P7/02 , C07D471/04
CPC分类号： A61K31/496 , A61K9/0019 , A61K9/0053 , A61K31/5377 , C07D471/04
摘要： rmidazo[1,2-α]pyridine derivatives 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 insomnia, dyssomnia, parasomnia and related sleep disorders, platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, thrombosis, asthma or symptoms thereof, agitation or symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de Ia Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to methods for the treatment of 5-HT2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together.
摘要翻译：式（Ia）的咪唑并[1,2-α]吡啶衍生物及其药物组合物，其调节5-HT2A 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失眠，睡眠不良，失眠和相关睡眠障碍，血小板聚集，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，血栓形成，哮喘或症状的方法糖尿病，糖尿病，精神病，精神病，精神分裂症，慢性精神分裂症，精神分裂症，精神分裂症，糖尿病，糖尿病，糖尿病，糖尿病，糖尿病，糖尿病，糖尿病，糖尿病，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-羟色胺受体介导的病症的方法。

7. 发明授权

US08580841B2 Substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives useful in the treatment of autoimmune and inflammatory disorders 有权
标题翻译：取代的1,2,3,4-四氢环戊二烯并[b]吲哚-3-基）乙酸衍生物，用于治疗自身免疫性和炎性疾病
公开(公告)号：US08580841B2
公开(公告)日：2013-11-12
申请号：US13055333
申请日：2009-07-22
申请人： Robert M Jones , Daniel J Buzard , Sangdon Han , Sun Hee Kim , Juerg Lehmann , Brett Ullman , Jeanne V Moody , Xiuwen Zhu , Scott Stirn
发明人： Robert M Jones , Daniel J Buzard , Sangdon Han , Sun Hee Kim , Juerg Lehmann , Brett Ullman , Jeanne V Moody , Xiuwen Zhu , Scott Stirn
IPC分类号： A61K31/403
CPC分类号： C07D209/94 , A61K31/137 , A61K31/198 , A61K31/404 , A61K31/433 , A61K31/4439 , A61K31/497 , C07C211/27 , C07C229/26 , C07C255/03 , C07C279/14 , C07D209/70 , C07D209/88 , C07D401/12 , C07D401/14 , C07D403/12 , C07D417/12 , Y02A50/475
摘要： The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic 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 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.
摘要翻译：本发明涉及式（Ia）的某些取代的1,2,3,4-四氢环戊二烯并[b]吲哚-3-基）乙酸衍生物及其药学上可接受的盐，它们具有有用的药理学性质，例如： 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，微生物感染或疾病以及病毒感染或疾病。

8. 发明申请

US20100273806A1 TETRAHYDROCYCLOPENTA[B]INDOL-3-YL CARBOXYLIC ACID DERIVATIVES USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS 审中-公开
标题翻译：四氢叶酸[B]吲哚-3-基羧酸衍生物用于治疗自身免疫和炎症性疾病
公开(公告)号：US20100273806A1
公开(公告)日：2010-10-28
申请号：US12808872
申请日：2008-12-15
申请人： Robert M. Jones , Daniel J. Buzard , Andrew M. Kawasaki , Luis A. Lopez , Jeanne V. Moody , Lars Thoresen , Brett Ullman
发明人： Robert M. Jones , Daniel J. Buzard , Andrew M. Kawasaki , Luis A. Lopez , Jeanne V. Moody , Lars Thoresen , Brett Ullman
IPC分类号： A61K31/4245 , C07D413/14 , C07D413/10 , A61K31/501 , A61K31/496 , A61P37/00 , A61P29/00 , A61P35/00 , A61P17/10 , A61P37/06 , A61P1/00 , A61P3/10
CPC分类号： C07D413/14 , C07D413/04
摘要： The present invention relates to certain (1,2,4-oxadiazol-3-yl)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-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, acne, microbial infections or diseases and viral infections or diseases.
摘要翻译：本发明涉及式（Ia）的某些（1,2,4-恶二唑-3-基）-1,2,3,4-四氢环 - 五[b]吲哚-3-基甲酸衍生物和药学上可接受的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，痤疮，微生物感染或疾病以及病毒感染或疾病。

9. 发明申请

US20100004264A1 PYRAZOLE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 有权
标题翻译：作为用于治疗与相关疾病相关的疾病的5-HT2A丝氨酸受体的调节剂的吡唑衍生物
公开(公告)号：US20100004264A1
公开(公告)日：2010-01-07
申请号：US12444098
申请日：2007-10-02
申请人： Yifeng Xiong , Martin C. Cherrier , Jin Sun Karoline Choi , Peter I. Dosa , Brian M. Smith , Sonja Strah-Pleynet , Brett Ullman , Bradley Teegarden
发明人： Yifeng Xiong , Martin C. Cherrier , Jin Sun Karoline Choi , Peter I. Dosa , Brian M. Smith , Sonja Strah-Pleynet , Brett Ullman , Bradley Teegarden
IPC分类号： A61K31/497 , C07D403/06 , C07D403/14 , A61P25/20 , A61P7/02 , A61P7/12 , A61P9/12 , A61P29/00
CPC分类号： C07D231/16 , C07D231/14 , C07D231/54 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/04
摘要： Pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the serotonin 5HT2A receptor. Formula (Ia). Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of insomnia and related sleep disorders, platelet aggregation, 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 symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de Ia Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related 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 mediated disorders in combination with other pharmaceutical agents administered separately or together.
摘要翻译：式（Ia）的吡唑衍生物及其药物组合物，其调节5-羟色胺5HT2A受体的活性。式（Ia）。化合物及其药物组合物涉及可用于治疗失眠和相关睡眠障碍，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，降低血块形成风险，哮喘的方法精神病，精神病，精神分裂症，急性精神分裂症，慢性精神分裂症，精神分裂症，精神分裂症，精神分裂症及相关疾病，以及其它症状，症状或症状，激动或其症状，行为障碍，药物诱导的精神病，兴奋性精神病，Gilles de Ia Tourette综合征，糖尿病相关疾病，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-羟色胺受体介导的病症的方法。

10. 发明授权

US09434692B2 Pyrazole derivatives as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto 有权
标题翻译：吡唑衍生物作为可用于治疗与其相关的疾病的5-HT2A 5-羟色胺受体的调节剂
公开(公告)号：US09434692B2
公开(公告)日：2016-09-06
申请号：US12444098
申请日：2007-10-02
申请人： Yifeng Xiong , Martin C. Cherrier , Jin Sun Karoline Choi , Peter I. Dosa , Brian M. Smith , Sonja Strah-Pleynet , Brett Ullman , Bradley Teegarden
发明人： Yifeng Xiong , Martin C. Cherrier , Jin Sun Karoline Choi , Peter I. Dosa , Brian M. Smith , Sonja Strah-Pleynet , Brett Ullman , Bradley Teegarden
IPC分类号： C07D231/14 , C07D403/06 , C07D403/12 , C07D405/04 , C07D231/16 , C07D231/54 , C07D403/14
CPC分类号： C07D231/16 , C07D231/14 , C07D231/54 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/04
摘要： Pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the serotonin 5HT2A receptor. Formula (Ia). Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of insomnia and related sleep disorders, platelet aggregation, 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 symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de Ia Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related 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 mediated disorders in combination with other pharmaceutical agents administered separately or together.

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