公开(公告)号：US20110105456A1

公开(公告)日：2011-05-05

申请号：US12976887

申请日：2010-12-22

申请人： Bradley Teegarden ,  Yifeng Xiong ,  Sonja Strah-Pleynet ,  Honnappa Jayakumar ,  Peter I. Dosa ,  Konrad Feichtinger ,  Matin Casper ,  Juerg Lehmann ,  Robert M. Jones ,  David J. Unett ,  Jin Sun Karoline Choi

发明人： Bradley Teegarden ,  Yifeng Xiong ,  Sonja Strah-Pleynet ,  Honnappa Jayakumar ,  Peter I. Dosa ,  Konrad Feichtinger ,  Matin Casper ,  Juerg Lehmann ,  Robert M. Jones ,  David J. Unett ,  Jin Sun Karoline Choi

IPC分类号： A61K31/4155 ,  C07D403/12 ,  C07D401/12 ,  A61K31/454 ,  A61K31/496 ,  C07D413/12 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/553 ,  C07D417/12 ,  A61K31/54 ,  A61P9/00 ,  A61P9/10 ,  A61P7/02 ,  A61P25/20 ,  A61P9/12

CPC分类号： C07D231/12 ,  A61K31/5377 ,  C07D231/16 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/10 ,  C07D413/12 ,  C07D417/12 ,  C07D487/08

摘要： The present invention relates to certain 3-phenyl-pyrazole 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 platelet aggreagation, 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 a symptom, 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 mediated disorders in combination with other pharmaceutical agents administered separately or together.

摘要翻译： 本发明涉及式（Ia）的某些3-苯基 - 吡唑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，降低血块形成风险，哮喘或其症状，激动或 症状，行为障碍，药物诱导的精神病，兴奋性精神病，吉列斯图雷特综合征，躁狂症，有机或非精神病精神病，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，以及睡眠障碍，睡眠障碍 ，糖尿病相关病症，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。

公开(公告)号：US07884101B2

公开(公告)日：2011-02-08

申请号：US11602164

申请日：2006-11-20

申请人： Bradley Teegarden ,  Yifeng Xiong ,  Sonja Strah-Pleynet ,  Honnappa Jayakumar ,  Peter I. Dosa ,  Konrad Feichtinger ,  Martin Casper ,  Juerg Lehmann ,  Robert M. Jones ,  David J. Unett ,  Jin Sun Karoline Choi

发明人： Bradley Teegarden ,  Yifeng Xiong ,  Sonja Strah-Pleynet ,  Honnappa Jayakumar ,  Peter I. Dosa ,  Konrad Feichtinger ,  Martin Casper ,  Juerg Lehmann ,  Robert M. Jones ,  David J. Unett ,  Jin Sun Karoline Choi

IPC分类号： A61K31/5355 ,  C07D413/10

CPC分类号： C07D231/12 ,  A61K31/5377 ,  C07D231/16 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/10 ,  C07D413/12 ,  C07D417/12 ,  C07D487/08

摘要： The present invention relates to certain 3-phenyl-pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor and are useful, optionally in combination with other pharmaceutical agents administered separately or together, in the treatment of 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 a symptom, 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.

摘要翻译： 本发明涉及式（Ia）的某些3-苯基 - 吡唑衍生物及其药物组合物，其调节5-HT2A 5-羟色胺受体的活性，并且可任选地与分开或一起施用的其它药物组合使用 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，降低血块形成风险，哮喘或其症状，激动或症状，行为障碍，药物诱导的精神病，精神病性精神病 ，Gilles de la Tourette综合征，躁狂症，有机或NOS精神病，精神病，精神病，急性精神分裂症，慢性精神分裂症，NOS精神分裂症和相关疾病，以及睡眠障碍，睡眠障碍，糖尿病相关疾病，进行性多灶性脑白质病等 。

公开(公告)号：US08785441B2

公开(公告)日：2014-07-22

申请号：US13616842

申请日：2012-09-14

申请人： Bradley Teegarden ,  Yifeng Xiong ,  Sonja Strah-Pleynet ,  Honnappa Jayakumar ,  Peter I. Dosa ,  Konrad Feichtinger ,  Martin Casper ,  Juerg Lehmann ,  Robert M. Jones ,  David J. Unett ,  Jin Sun Karoline Choi

发明人： Bradley Teegarden ,  Yifeng Xiong ,  Sonja Strah-Pleynet ,  Honnappa Jayakumar ,  Peter I. Dosa ,  Konrad Feichtinger ,  Martin Casper ,  Juerg Lehmann ,  Robert M. Jones ,  David J. Unett ,  Jin Sun Karoline Choi

IPC分类号： A61K31/4155 ,  C07D413/10

CPC分类号： C07D231/12 ,  A61K31/5377 ,  C07D231/16 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/10 ,  C07D413/12 ,  C07D417/12 ,  C07D487/08

摘要： The present invention relates to certain 3-phenyl-pyrazole 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 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 a symptom, 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 mediated disorders in combination with other pharmaceutical agents administered separately or together.

摘要翻译： 本发明涉及式（Ia）的某些3-苯基 - 吡唑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，哮喘或其症状，激动或 症状，行为障碍，药物诱导的精神病，兴奋性精神病，吉列斯图雷特综合征，躁狂症，有机或非精神病精神病，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，以及睡眠障碍，睡眠障碍 ，糖尿病相关病症，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。

公开(公告)号：US20070244086A1

公开(公告)日：2007-10-18

申请号：US11597306

申请日：2005-11-17

申请人： Bradley Teegarden ,  Yifeng Xiong ,  Sonja Strah-Pleynet ,  Honnappa Jayakumar ,  Peter Dosa ,  Konrad Feichtinger ,  Martin Casper ,  Juerg Lehmann ,  Robert Jones ,  David Unett ,  Jin Karoline Choi

发明人： Bradley Teegarden ,  Yifeng Xiong ,  Sonja Strah-Pleynet ,  Honnappa Jayakumar ,  Peter Dosa ,  Konrad Feichtinger ,  Martin Casper ,  Juerg Lehmann ,  Robert Jones ,  David Unett ,  Jin Karoline Choi

IPC分类号： A61K31/4155 ,  A61K31/397 ,  A61K31/4178 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5355 ,  A61K31/541 ,  A61K31/553 ,  A61P29/00 ,  C07D231/12 ,  C07D231/16 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D487/08

CPC分类号： C07D231/12 ,  A61K31/5377 ,  C07D231/16 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/10 ,  C07D413/12 ,  C07D417/12 ,  C07D487/08

摘要： The present invention relates to certain 3-phenyl-pyrazole 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 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 a symptom, 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 mediated disorders in combination with other pharmaceutical agents administered separately or together.

摘要翻译： 本发明涉及式（Ia）的某些3-苯基 - 吡唑衍生物及其药物组合物，其调节5-HT 2A / 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，哮喘或其症状，激动或 症状，行为障碍，药物诱导的精神病，兴奋性精神病，吉列斯图雷特综合征，躁狂症，有机或非精神病精神病，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，以及睡眠障碍，睡眠障碍 ，糖尿病相关病症，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物组合治疗5-HT 2A 5-羟色胺受体介导的病症的方法。

公开(公告)号：US20070207994A1

公开(公告)日：2007-09-06

申请号：US11602164

申请日：2006-11-20

申请人： Bradley Teegarden ,  Yifeng Xiong ,  Sonja Strah-Pleynet ,  Honnappa Jayakumar ,  Peter Dosa ,  Konrad Feichtinger ,  Martin Casper ,  Juerg Lehmann ,  Robert Jones ,  David Unett ,  Jin Karoline Choi

发明人： Bradley Teegarden ,  Yifeng Xiong ,  Sonja Strah-Pleynet ,  Honnappa Jayakumar ,  Peter Dosa ,  Konrad Feichtinger ,  Martin Casper ,  Juerg Lehmann ,  Robert Jones ,  David Unett ,  Jin Karoline Choi

IPC分类号： A61K31/553 ,  A61K31/55 ,  A61K31/541 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/454 ,  A61K31/416 ,  A61K31/4152 ,  C07D417/02 ,  C07D413/02 ,  C07D403/02

CPC分类号： C07D231/12 ,  A61K31/5377 ,  C07D231/16 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/10 ,  C07D413/12 ,  C07D417/12 ,  C07D487/08

摘要： The present invention relates to certain 3-phenyl-pyrazole 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 platelet aggreagation, 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 a symptom, 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 mediated disorders in combination with other pharmaceutical agents administered separately or together.

摘要翻译： 本发明涉及式（Ia）的某些3-苯基 - 吡唑衍生物及其药物组合物，其调节5-HT 2A / 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，降低血块形成风险，哮喘或其症状，激动或 症状，行为障碍，药物诱导的精神病，兴奋性精神病，吉列斯图雷特综合征，躁狂症，有机或非精神病精神病，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，以及睡眠障碍，睡眠障碍 ，糖尿病相关病症，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物组合治疗5-HT 2A 5-羟色胺受体介导的病症的方法。

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。

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。

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.

公开(公告)号：US20080200530A1

公开(公告)日：2008-08-21

申请号：US11795489

申请日：2006-01-17

申请人： David J. Unett ,  Bradley Teegarden ,  Honnappa Jayakumar ,  Hongmei Li ,  Sonja Strah-Pleynet ,  Peter I. Dosa

发明人： David J. Unett ,  Bradley Teegarden ,  Honnappa Jayakumar ,  Hongmei Li ,  Sonja Strah-Pleynet ,  Peter I. Dosa

IPC分类号： A61K31/415 ,  A61P37/00 ,  A61P31/18 ,  A61P25/28

CPC分类号： A61K31/415

摘要： The present invention relates to certain pyrazole derivatives of Formula (I) 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 prophylaxis or treatment of progressive multifocal leukoencephalopathy.

摘要翻译： 本发明涉及式（I）的某些吡唑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预防或治疗进行性多灶性脑白质脑病的方法。

公开(公告)号：US20140163032A1

公开(公告)日：2014-06-12

申请号：US14182994

申请日：2014-02-18

申请人： BRADLEY TEEGARDEN ,  Dennis Chapman ,  Marc Decaire ,  Peter I. Dosa ,  Konrad Feichtinger ,  HONNAPPA JAYAKUMAR ,  THUY-ANH Tran ,  Sonja Strah-Pleynet ,  Jay Xu

发明人： BRADLEY TEEGARDEN ,  Dennis Chapman ,  Marc Decaire ,  Peter I. Dosa ,  Konrad Feichtinger ,  HONNAPPA JAYAKUMAR ,  THUY-ANH Tran ,  Sonja Strah-Pleynet ,  Jay Xu

IPC分类号： C07D207/335 ,  C07D207/34 ,  C07D417/12 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D405/12

CPC分类号： C07D231/12 ,  A61K31/415 ,  C07D207/335 ,  C07D207/34 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  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。