公开(公告)号：US07488731B2

公开(公告)日：2009-02-10

申请号：US11782415

申请日：2007-07-24

申请人： Dale S. Dhanoa ,  Dongli Chen ,  Oren Becker ,  Silvia Noiman ,  Srinivasa R. Cheruku ,  Yael Marantz ,  Anurag Sharadendu ,  Sharon Shacham ,  Alexander Heifetz ,  Pradyumna Mohanty ,  Boaz Inbal ,  Merav Fichman ,  Raphael Nudelman ,  Shay Bar-Haim

发明人： Dale S. Dhanoa ,  Dongli Chen ,  Oren Becker ,  Silvia Noiman ,  Srinivasa R. Cheruku ,  Yael Marantz ,  Anurag Sharadendu ,  Sharon Shacham ,  Alexander Heifetz ,  Pradyumna Mohanty ,  Boaz Inbal ,  Merav Fichman ,  Raphael Nudelman ,  Shay Bar-Haim

IPC分类号： A61K31/495 ,  C07D295/13

CPC分类号： C07D213/74 ,  C07D211/96 ,  C07D239/42 ,  C07D295/13 ,  C07D401/12

摘要： The invention relates to 5-HT receptor agonists or antagonists. Novel arylpiperazinyl sulfonamide compounds represented by Formula I, and synthesis and uses thereof for treating diseases including those mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include central nervous system disorders such as generalized anxiety disorder, ADD/ADHD, neural injury, stroke, and migraine. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.

公开(公告)号：US07491727B2

公开(公告)日：2009-02-17

申请号：US11516345

申请日：2006-09-05

申请人： Dale S. Dhanoa ,  Dongli Chen ,  Oren Becker ,  Silvia Noiman ,  Srinivasa R. Cheruku ,  Yael Marantz ,  Anurag Sharadendu ,  Sharon Shacham ,  Alexander Heifetz ,  Pradyumna Mohanty ,  Boaz Inbal ,  Merav Fichman ,  Raphael Nudelman ,  Shay Bar-Haim

发明人： Dale S. Dhanoa ,  Dongli Chen ,  Oren Becker ,  Silvia Noiman ,  Srinivasa R. Cheruku ,  Yael Marantz ,  Anurag Sharadendu ,  Sharon Shacham ,  Alexander Heifetz ,  Pradyumna Mohanty ,  Boaz Inbal ,  Merav Fichman ,  Raphael Nudelman ,  Shay Bar-Haim

IPC分类号： A61K31/495 ,  A61K31/496

CPC分类号： C07D213/74 ,  C07D211/96 ,  C07D239/42 ,  C07D295/13 ,  C07D401/12

摘要： The invention relates to 5-HT receptor agonists or antagonists. Novel arylpiperazinyl sulfonamide compounds represented by Formula I, and synthesis and uses thereof for treating diseases including those mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include central nervous system disorders such as generalized anxiety disorder, ADD/ADHD, neural injury, stroke, and migraine. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.

摘要翻译： 本发明涉及5-HT受体激动剂或拮抗剂。 公开了由式I表示的新型芳基哌嗪基磺酰胺化合物及其用于治疗包括由5-HT受体直接或间接介导的疾病的疾病的合成和用途。 这些病症包括中枢神经系统疾病，如广泛性焦虑症，ADD / ADHD，神经损伤，中风和偏头痛。 还包括制备方法和新型中间体及其药物盐。

公开(公告)号：US07153858B2

公开(公告)日：2006-12-26

申请号：US10768579

申请日：2004-01-30

申请人： Dale S. Dhanoa ,  Dongli Chen ,  Oren Becker ,  Silvia Noiman ,  Srinivasa Rao Cheruku ,  Yael Marantz ,  Anurag Sharadendu ,  Sharon Shachem ,  Alexander Heifetz ,  Pradyumna Mohanty ,  Boaz Inbal ,  Merav Fichman ,  Raphael Nudelman ,  Shay Bar-Haim

发明人： Dale S. Dhanoa ,  Dongli Chen ,  Oren Becker ,  Silvia Noiman ,  Srinivasa Rao Cheruku ,  Yael Marantz ,  Anurag Sharadendu ,  Sharon Shachem ,  Alexander Heifetz ,  Pradyumna Mohanty ,  Boaz Inbal ,  Merav Fichman ,  Raphael Nudelman ,  Shay Bar-Haim

IPC分类号： A61K31/495 ,  A61K31/496 ,  C07D295/13 ,  C07D401/06 ,  A61K31/506 ,  C07D403/04

CPC分类号： C07D213/74 ,  C07D211/96 ,  C07D239/42 ,  C07D295/13 ,  C07D401/12

摘要： The invention relates to 5-HT receptor agonists or antagonists. Novel arylpiperazinyl sulfonamide compounds represented by Formulae I: and II, and synthesis and uses of those compounds for treating diseases including those mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include central nervous system disorders such as generalized anxiety disorder, ADD/ADHD, neural injury, stroke, and migraine. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.

摘要翻译： 本发明涉及5-HT受体激动剂或拮抗剂。 公开了由式I和II表示的新型芳基哌嗪基磺酰胺化合物，以及用于治疗包括由5-HT受体直接或间接介导的那些疾病的那些化合物的合成和用途。 这些病症包括中枢神经系统疾病，如广泛性焦虑症，ADD / ADHD，神经损伤，中风和偏头痛。 还包括制备方法和新型中间体及其药物盐。

公开(公告)号：US07612078B2

公开(公告)日：2009-11-03

申请号：US11075565

申请日：2005-03-08

申请人： Dale S. Dhanoa ,  Oren Becker ,  Silvia Noiman ,  A. Sekar Reddy ,  Srinivasa R. Cheruku ,  Rosa E. Melendez ,  Anurag Sharadendu ,  Dongli Chen ,  Yael Marantz ,  Sharon Shacham ,  Alexander Heifetz ,  Boaz Inbal ,  Venkitasamy Kesavan ,  Shay Bar-Haim

发明人： Dale S. Dhanoa ,  Oren Becker ,  Silvia Noiman ,  A. Sekar Reddy ,  Srinivasa R. Cheruku ,  Rosa E. Melendez ,  Anurag Sharadendu ,  Dongli Chen ,  Yael Marantz ,  Sharon Shacham ,  Alexander Heifetz ,  Boaz Inbal ,  Venkitasamy Kesavan ,  Shay Bar-Haim

IPC分类号： C07D495/04 ,  A61K31/519 ,  A61P25/06 ,  A61P9/12

CPC分类号： C07D495/04

摘要： The invention relates to 5-HT receptor modulators, particularly 5-HT2B antagonists. Novel piperidinylamino-thieno[2,3-d]pyrimidine compounds represented by Formula I, II and III, and uses thereof for treating conditions including pulmonary arterial hypertension, congestive heart failure, and hypertension.

摘要翻译： 本发明涉及5-HT受体调节剂，特别是5-HT 2B拮抗剂。 由式I，II和III表示的新型哌啶基氨基 - 噻吩并[2,3-d]嘧啶化合物及其用于治疗包括肺动脉高压，充血性心力衰竭和高血压的病症的用途。

公开(公告)号：US20110082157A1

公开(公告)日：2011-04-07

申请号：US12795987

申请日：2010-06-08

申请人： Dale S. Dhanoa ,  Oren Becker ,  Silvia Noiman ,  Sekar A. Reddy ,  Srinivasa Rao Cheruku ,  Rosa E. Mele'ndez ,  Anurag Sharadendu ,  Dongli Chen ,  Yael Marantz ,  Sharon Shacham ,  Alexander Heifetz ,  Boaz Inbal ,  Venkitasamy Kesavan ,  Shay Bar-Haim

发明人： Dale S. Dhanoa ,  Oren Becker ,  Silvia Noiman ,  Sekar A. Reddy ,  Srinivasa Rao Cheruku ,  Rosa E. Mele'ndez ,  Anurag Sharadendu ,  Dongli Chen ,  Yael Marantz ,  Sharon Shacham ,  Alexander Heifetz ,  Boaz Inbal ,  Venkitasamy Kesavan ,  Shay Bar-Haim

IPC分类号： A61K31/519 ,  C07D495/04 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P25/06

CPC分类号： C07D495/04

摘要： The invention relates to 5-HT receptor antagonists. Novel piperidinylamino-thieno [2,3-d] pyrimidine 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 central nervous system disorders such as pulmonary arterial hypertension, migraine, hypertension, disorders of the gastrointestinal tract, restenosis, asthma, obstructive airway disease, prostatic hyperplasia and priapism, anxiety, depression, schizophrenia, neural injury and stroke. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also provided.

摘要翻译： 本发明涉及5-HT受体拮抗剂。 公开了由式I表示的新型哌啶基氨基 - 噻吩并[2,3-d]嘧啶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。 这些病症包括中枢神经系统疾病如肺动脉高压，偏头痛，高血压，胃肠道疾病，再狭窄，哮喘，阻塞性气道疾病，前列腺增生和阴茎异常勃起，焦虑，抑郁，精神分裂症，神经损伤和中风。 还提供了制备方法和新型中间体及其药用盐。

公开(公告)号：US20100113485A1

公开(公告)日：2010-05-06

申请号：US12609470

申请日：2009-10-30

申请人： Dale S. Dhanoa ,  Oren Becker ,  Silvia Noiman ,  Sekar Reddy Alla ,  Srinivasa Rao Cheruku ,  Rosa E. Mele'ndez ,  Anurag Sharadendu ,  Dongli Chen ,  Yael Marantz ,  Sharon Shacham ,  Alexander Heifetz ,  Boaz Inbal ,  Venkitasamy Kesavan ,  Shay Bar-Haim

发明人： Dale S. Dhanoa ,  Oren Becker ,  Silvia Noiman ,  Sekar Reddy Alla ,  Srinivasa Rao Cheruku ,  Rosa E. Mele'ndez ,  Anurag Sharadendu ,  Dongli Chen ,  Yael Marantz ,  Sharon Shacham ,  Alexander Heifetz ,  Boaz Inbal ,  Venkitasamy Kesavan ,  Shay Bar-Haim

IPC分类号： A61K31/519 ,  C07D495/04 ,  A61P35/00 ,  A61P9/12 ,  A61P15/10 ,  A61P9/00 ,  A61P25/06 ,  A61P1/00 ,  A61P11/06 ,  A61P11/00 ,  A61P29/00 ,  A61P25/00 ,  A61P25/28 ,  A61P25/24 ,  A61P25/22 ,  A61P15/00 ,  A61P19/00 ,  A61P5/00 ,  A61P5/08

CPC分类号： C07D495/04

摘要： The invention relates to 5-HT receptor modulators, particularly 5-HT2B antagonists. Novel piperidinylamino-thieno[2,3-d]pyrimidine compounds represented by Formula I, II and III, and uses thereof for treating conditions including pulmonary arterial hypertension, congestive heart failure, and hypertension.

摘要翻译： 本发明涉及5-HT受体调节剂，特别是5-HT 2B拮抗剂。 由式I，II和III表示的新型哌啶基氨基 - 噻吩并[2,3-d]嘧啶化合物及其用于治疗包括肺动脉高压，充血性心力衰竭和高血压的病症的用途。

公开(公告)号：US07982040B2

公开(公告)日：2011-07-19

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： C07D221/02 ,  C07D515/02

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。

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。

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。

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。