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公开(公告)号：US20050256153A1
公开(公告)日：2005-11-17
申请号：US10955434
申请日：2004-09-30
申请人： Dale Dhanoa , Oren Becker , Silvia Noiman , Pradyumna Mohanty , Dongli Chen , Mercedes Lobera , Laurence Wu , Yael Marantz , Boaz Inbal , Alexander Heifetz , Shay Bar-Haim , Sharon Shacham
发明人： Dale Dhanoa , Oren Becker , Silvia Noiman , Pradyumna Mohanty , Dongli Chen , Mercedes Lobera , Laurence Wu , Yael Marantz , Boaz Inbal , Alexander Heifetz , Shay Bar-Haim , Sharon Shacham
IPC分类号： A61K31/4743 , C07D495/04 , C07D498/02
CPC分类号： C07D495/04
摘要： The invention relates to 5-HT receptor agonists and partial agonists. Novel thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, nonulcer dyspepsia, depression, anxiety, urinary incontinence, migraine, arrhythmia, atrial fibrillation, ischemic stroke, gastritis, gastric emptying disorders, feeding disorders, gastrointestinal disorders, constipation, erectile dysfunction, and respiratory depression. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.
摘要翻译： 本发明涉及5-HT受体激动剂和部分激动剂。 公开了由式I表示的新型噻吩并吡啶酮化合物及其用于治疗由5-HT受体直接或间接介导的疾病的合成和用途。 这些病症包括阿尔茨海默病，认知障碍，肠易激综合征，恶心，呕吐，呕吐，运动失调，胃食管反流病，非溃疡性消化不良，抑郁症，焦虑症，尿失禁，偏头痛，心律失常，心房颤动，缺血性卒中，胃炎，胃排空障碍 ，喂食障碍，胃肠道疾病，便秘，勃起功能障碍和呼吸抑制。 还包括制备方法和新型中间体及其药物盐。
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公开(公告)号：US07407966B2
公开(公告)日：2008-08-05
申请号：US10960769
申请日：2004-10-07
申请人： Dale S. Dhanoa , Oren Becker , Silvia Noiman , Laurence Wu , Mercedes Lobera , Pradyumna Mohanty , Yael Marantz , Boaz Inbal , Sharon Shacham , Dongli Chen
发明人： Dale S. Dhanoa , Oren Becker , Silvia Noiman , Laurence Wu , Mercedes Lobera , Pradyumna Mohanty , Yael Marantz , Boaz Inbal , Sharon Shacham , Dongli Chen
IPC分类号： A01N43/42 , C07D471/02
CPC分类号： C07D495/04
摘要： The invention relates to 5-HT4 receptor agonists and partial agonists. Thienopyridinone compounds and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT4 receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, Parkinson's disease, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, and nonulcer dyspepsia. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.
摘要翻译： 本发明涉及5-HT 4受体激动剂和部分激动剂。 公开了噻吩并吡啶酮化合物及其用于治疗由5-HT 4受体直接或间接介导的疾病的合成及其用途。 这些病症包括阿尔茨海默氏病，认知障碍，肠易激综合征，帕金森病，恶心，呕吐，呕吐，运动失调，胃食管反流病和非溃疡性消化不良。 还包括制备方法和新型中间体及其药物盐。
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公开(公告)号：US07576211B2
公开(公告)日：2009-08-18
申请号：US11269042
申请日：2005-11-08
申请人： Dale S. Dhanoa , Oren Becker , Silvia Noiman , Dongli Chen , Yael Marantz , Sharon Shacham , Alexander Heifetz , Boaz Inbal , Shay Bar-Haim , Pradyumna Mohanty , Mercedes Lobera , Laurence Wu
发明人： Dale S. Dhanoa , Oren Becker , Silvia Noiman , Dongli Chen , Yael Marantz , Sharon Shacham , Alexander Heifetz , Boaz Inbal , Shay Bar-Haim , Pradyumna Mohanty , Mercedes Lobera , Laurence Wu
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： The invention relates to 5-HT receptor agonists and partial agonists. Novel thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, nonulcer dyspepsia, depression, anxiety, urinary incontinence, migraine, arrhythmia, atrial fibrillation, ischemic stroke, gastritis, gastric emptying disorders, feeding disorders, gastrointestinal disorders, constipation, erectile dysfunction, and respiratory depression. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.
摘要翻译： 本发明涉及5-HT受体激动剂和部分激动剂。 公开了由式I表示的新型噻吩并吡啶酮化合物及其用于治疗由5-HT受体直接或间接介导的疾病的合成和用途。 这些病症包括阿尔茨海默病，认知障碍，肠易激综合征，恶心，呕吐，呕吐，运动失调，胃食管反流病，非溃疡性消化不良，抑郁症，焦虑症，尿失禁，偏头痛，心律失常，心房颤动，缺血性卒中，胃炎，胃排空障碍 ，喂食障碍，胃肠道疾病，便秘，勃起功能障碍和呼吸抑制。 还包括制备方法和新型中间体及其药物盐。
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公开(公告)号：US07488736B2
公开(公告)日：2009-02-10
申请号：US10955434
申请日：2004-09-30
申请人： Dale S. Dhanoa , Oren Becker , Silvia Noiman , Pradyumna Mohanty , Dongli Chen , Mercedes Lobera , Laurence Wu , Yael Marantz , Boaz Inbal , Alexander Heifetz , Shay Bar-Haim , Sharon Shacham
发明人： Dale S. Dhanoa , Oren Becker , Silvia Noiman , Pradyumna Mohanty , Dongli Chen , Mercedes Lobera , Laurence Wu , Yael Marantz , Boaz Inbal , Alexander Heifetz , Shay Bar-Haim , Sharon Shacham
IPC分类号： A01N43/42 , C07D471/02
CPC分类号： C07D495/04
摘要： The invention relates to 5-HT receptor agonists and partial agonists. Thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, nonulcer dyspepsia, depression, anxiety, urinary incontinence, migraine, arrhythmia, atrial fibrillation, ischemic stroke, gastritis, gastric emptying disorders, feeding disorders, gastrointestinal disorders, constipation, erectile dysfunction, and respiratory depression. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.
摘要翻译： 本发明涉及5-HT受体激动剂和部分激动剂。 公开了由式I表示的噻吩并吡啶酮化合物及其用于治疗由5-HT受体直接或间接介导的疾病的合成及其用途。 这些病症包括阿尔茨海默病，认知障碍，肠易激综合征，恶心，呕吐，呕吐，运动失调，胃食管反流病，非溃疡性消化不良，抑郁症，焦虑症，尿失禁，偏头痛，心律失常，心房颤动，缺血性卒中，胃炎，胃排空障碍 ，喂食障碍，胃肠道疾病，便秘，勃起功能障碍和呼吸抑制。 还包括制备方法和新型中间体及其药物盐。
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公开(公告)号：US20110195953A1
公开(公告)日：2011-08-11
申请号：US12570510
申请日：2009-09-30
申请人： Dale S. Dhanoa , Oren Becker , Silvia Noiman , Pradyumna Mohanty , Dongli Chen , Mercedes Lobera , Laurence Wu , Yael Marantz , Boaz Inbal , Alexander Heifetz , Shay Bar-Haim , Sharon Shacham
发明人： Dale S. Dhanoa , Oren Becker , Silvia Noiman , Pradyumna Mohanty , Dongli Chen , Mercedes Lobera , Laurence Wu , Yael Marantz , Boaz Inbal , Alexander Heifetz , Shay Bar-Haim , Sharon Shacham
IPC分类号： A61K31/55 , A61K31/4365 , A61P25/28
CPC分类号： A61K45/06 , A61K31/4365 , A61K31/439 , A61K31/50 , A61K31/55 , A61K2300/00
摘要： The invention generally relates to thienopyridinone 5-HT4 receptor modulators, and in particular the use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with serotonin action, such as in treating Alzheimer's disease, cognition disorders, depression, and anxiety.
摘要翻译： 本发明一般涉及噻吩并吡啶酮5-HT4受体调节剂，特别是这些化合物及其药物组合物的用途，例如用于治疗，调节和/或预防与5-羟色胺作用有关的生理条件，例如治疗阿尔茨海默病 ，认知障碍，抑郁和焦虑。
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公开(公告)号：US07598265B2
公开(公告)日：2009-10-06
申请号：US11271019
申请日：2005-11-10
申请人： Dale S. Dhanoa , Oren Becker , Silvia Noiman , Pradyumna Mohanty , Dongli Chen , Mercedes Lobera , Laurence Wu , Yael Marantz , Boaz Inbal , Alexander Heifetz , Shay Bar-Haim , Sharon Shacham
发明人： Dale S. Dhanoa , Oren Becker , Silvia Noiman , Pradyumna Mohanty , Dongli Chen , Mercedes Lobera , Laurence Wu , Yael Marantz , Boaz Inbal , Alexander Heifetz , Shay Bar-Haim , Sharon Shacham
IPC分类号： A61K31/44 , C07D513/02
CPC分类号： A61K45/06 , A61K31/4365 , A61K31/439 , A61K31/50 , A61K31/55 , A61K2300/00
摘要： The invention generally relates to thienopyridinone 5-HT4 receptor modulators, and in particular the use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with serotonin action, such as in treating Alzheimer's disease, cognition disorders, depression, and anxiety.
摘要翻译： 本发明一般涉及噻吩并吡啶酮5-HT4受体调节剂，特别是这些化合物及其药物组合物的用途，例如用于治疗，调节和/或预防与5-羟色胺作用有关的生理条件，例如治疗阿尔茨海默病 ，认知障碍，抑郁和焦虑。
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公开(公告)号：US20090163537A1
公开(公告)日：2009-06-25
申请号：US12343818
申请日：2008-12-24
申请人： Dale S. Dhanoa , Oren Becker , Silvia Noiman , Pradyumna Mohanty , Dongli Chen , Mercedes Lobera , Laurence Wu , Yael Marantz , Boaz Inbal , Alexander Heifetz , Shay Bar-Haim , Sharon Shacham
发明人： Dale S. Dhanoa , Oren Becker , Silvia Noiman , Pradyumna Mohanty , Dongli Chen , Mercedes Lobera , Laurence Wu , Yael Marantz , Boaz Inbal , Alexander Heifetz , Shay Bar-Haim , Sharon Shacham
IPC分类号： A61K31/4365 , C07D495/04
CPC分类号： C07D495/04
摘要： The invention relates to 5-HT receptor agonists and partial agonists. Novel thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, nonulcer dyspepsia, depression, anxiety, urinary incontinence, migraine, arrhythmia, atrial fibrillation, ischemic stroke, gastritis, gastric emptying disorders, feeding disorders, gastrointestinal disorders, constipation, erectile dysfunction, and respiratory depression. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.
摘要翻译： 本发明涉及5-HT受体激动剂和部分激动剂。 公开了由式I表示的新型噻吩并吡啶酮化合物及其用于治疗由5-HT受体直接或间接介导的疾病的合成和用途。 这些病症包括阿尔茨海默病，认知障碍，肠易激综合征，恶心，呕吐，呕吐，运动失调，胃食管反流病，非溃疡性消化不良，抑郁症，焦虑症，尿失禁，偏头痛，心律失常，心房颤动，缺血性卒中，胃炎，胃排空障碍 ，喂食障碍，胃肠道疾病，便秘，勃起功能障碍和呼吸抑制。 还包括制备方法和新型中间体及其药物盐。
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公开(公告)号：US20060234998A1
公开(公告)日：2006-10-19
申请号：US11271019
申请日：2005-11-10
申请人： Dale Dhanoa , Oren Becker , Silvia Noiman , Pradyumna Mohanty , Dongli Chen , Mercedes Lobera , Laurence Wu , Yael Marantz , Boaz Inbal , Alexander Heifetz , Shay Bar-Haim , Sharon Shacham
发明人： Dale Dhanoa , Oren Becker , Silvia Noiman , Pradyumna Mohanty , Dongli Chen , Mercedes Lobera , Laurence Wu , Yael Marantz , Boaz Inbal , Alexander Heifetz , Shay Bar-Haim , Sharon Shacham
IPC分类号： A61K31/4743 , A61K31/55 , A61K31/445 , A61K31/473 , A61K31/454 , A61K31/407
CPC分类号： A61K45/06 , A61K31/4365 , A61K31/439 , A61K31/50 , A61K31/55 , A61K2300/00
摘要： The invention generally relates to thienopyridinone 5-HT4 receptor modulators, and in particular the use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with serotonin action, such as in treating Alzheimer's disease, cognition disorders, depression, and anxiety.
摘要翻译： 本发明一般涉及噻吩并吡啶酮5-HT 4受体调节剂，特别是这些化合物及其药物组合物的用途，例如用于治疗，调节和/或预防与5-羟色胺相关的生理条件 行为，例如治疗阿尔茨海默病，认知障碍，抑郁和焦虑。
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公开(公告)号：US20080027036A1
公开(公告)日：2008-01-31
申请号：US11726351
申请日：2007-03-21
申请人： Roland Burli , Victor Cee , Jennifer Golden , Brian Lanman , Susana Neira , Ashis Saha , Nili Schutz , Xiang Yu , Dilara McCauley , Mercedes Lobera , Yael Marantz , Jian Lin , Srinivasa Cheruku , Pini Orbach , Anurag Sharadendu , Robert Penland , Kimberley Gannon , Sharon Shacham , Silvia Noiman , Oren Becker , Zhaoda Zhang
发明人： Roland Burli , Victor Cee , Jennifer Golden , Brian Lanman , Susana Neira , Ashis Saha , Nili Schutz , Xiang Yu , Dilara McCauley , Mercedes Lobera , Yael Marantz , Jian Lin , Srinivasa Cheruku , Pini Orbach , Anurag Sharadendu , Robert Penland , Kimberley Gannon , Sharon Shacham , Silvia Noiman , Oren Becker , Zhaoda Zhang
IPC分类号： A61K31/397 , A61K31/343 , A61K31/4427 , A61K31/445 , A61K31/47 , A61K31/5377 , A61P1/00 , A61P19/02 , A61P29/00 , A61P3/10 , A61P35/00 , A61P37/00 , A61P43/00 , C07D205/12 , C07D213/00 , C07D217/00 , C07D221/00 , C07D235/02 , C07D239/70 , C07D257/04 , C07D263/52 , C07D277/00 , C07D295/00 , C07D307/77
CPC分类号： C07D307/79 , C07D307/80 , C07D307/81 , C07D403/10 , C07D405/04 , C07D405/10 , C07D405/14 , C07D409/14 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D471/04 , C07D491/048
摘要： The present invention relates to compounds of the general formula (I) that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.
摘要翻译： 本发明涉及具有作为S1P受体调节剂的活性的通式（I）的化合物，以及这些化合物用于治疗与不适当的S1P受体活性有关的疾病的用途。 这些化合物可用作免疫调节剂，例如用于治疗或预防诸如自身免疫性疾病和相关免疫疾病（包括系统性红斑狼疮），炎症性肠病如克罗恩病和溃疡性结肠炎，I型糖尿病，葡萄膜炎，牛皮癣，重症肌无力，类风湿 关节炎，非肾小球性肾病，肝炎，白塞病，肾小球性肾炎，慢性血小板减少性紫癜，溶血性贫血，肝炎和韦格纳肉芽肿; 并处理其他条件。
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公开(公告)号：US07855193B2
公开(公告)日：2010-12-21
申请号：US11491766
申请日：2006-07-24
申请人： Ashis K. Saha , Nili Schutz , Xiang Yu , Dilara McCauley , Mercedes Lobera , Yael Marantz , Jian Lin , Srinivasa R. Cheruku , Pini Orbach , Anurag Sharadendu , Robert Christian Penland , Kimberley Gannon , Sharon Shacham , Silvia Noiman , Oren Becker
发明人： Ashis K. Saha , Nili Schutz , Xiang Yu , Dilara McCauley , Mercedes Lobera , Yael Marantz , Jian Lin , Srinivasa R. Cheruku , Pini Orbach , Anurag Sharadendu , Robert Christian Penland , Kimberley Gannon , Sharon Shacham , Silvia Noiman , Oren Becker
IPC分类号： A61K31/397 , A61K31/5377 , A61K31/4525 , A61K31/4025 , A61K31/343 , C07D411/06 , C07D405/06 , C07D205/04 , C07D307/80
CPC分类号： C07D405/10 , C07D307/80 , C07D307/81 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/10 , C07D417/14
摘要： The present invention relates to compounds of the general formula (I) that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.
摘要翻译： 本发明涉及具有作为S1P受体调节剂的活性的通式（I）的化合物，以及这些化合物用于治疗与不适当的S1P受体活性有关的疾病的用途。 这些化合物可用作免疫调节剂，例如用于治疗或预防诸如自身免疫性疾病和相关免疫疾病（包括系统性红斑狼疮），炎症性肠病如克罗恩病和溃疡性结肠炎，I型糖尿病，葡萄膜炎，牛皮癣，重症肌无力，类风湿 关节炎，非肾小球性肾病，肝炎，白塞病，肾小球性肾炎，慢性血小板减少性紫癜，溶血性贫血，肝炎和韦格纳肉芽肿; 并处理其他条件。
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