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    Modulators of the prostacyclin (PGI2) receptor useful for the treatment of disorders related thereto
    2.
    发明授权
    Modulators of the prostacyclin (PGI2) receptor useful for the treatment of disorders related thereto 有权
    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）。

    MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
    3.
    发明申请
    MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 有权
    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）。

    MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
    4.
    发明申请
    MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
    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：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）。

    PYRAZOLE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
    5.
    发明申请
    PYRAZOLE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
    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。

    PYRAZOLE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
    9.
    发明申请
    PYRAZOLE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 有权
    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。

    Imidazo[1,2-a]pyridine derivatives as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto
    10.
    发明授权
    Imidazo[1,2-a]pyridine derivatives as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto 有权
    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。