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1. 发明授权

US07514424B2 Substituted 4-(4-piperidin-4-yl-piperazin-1-yl)-azepane derivatives and their use as neurokinin antagonists 失效
标题翻译：取代的4-（4-哌啶-4-基 - 哌嗪-1-基） - 氮杂环庚烷衍生物及其作为神经激肽拮抗剂的用途
公开(公告)号：US07514424B2
公开(公告)日：2009-04-07
申请号：US10540456
申请日：2003-12-17
申请人： Frans Eduard Janssens , François Maria Sommen , Benoît Christian Albert Ghislain De Boeck , Joseph Elisabeth Leenaerts
发明人： Frans Eduard Janssens , François Maria Sommen , Benoît Christian Albert Ghislain De Boeck , Joseph Elisabeth Leenaerts
IPC分类号： A61P25/00 , A61K31/55 , C07D401/14 , C07D405/14 , C07D413/14
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14
摘要： The invention concerns substituted 4-(4-piperidin-4-yl-piperazin-1-yl)-azepane derivatives having neurokinin antagonistic activity, in particular NK˜antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of pain, emesis, anxiety, depression and IBS.
摘要翻译：本发明涉及具有神经激肽拮抗活性的取代的4-（4-哌啶-4-基 - 哌嗪-1-基） - 氮杂环庚烷衍生物，特别是NK拮抗活性，其制备方法，包含它们的组合物及其作为药物的用途特别用于治疗疼痛，呕吐，焦虑，抑郁和IBS。

2. 发明授权

US07410970B2 Substituted 1,4,-di-piperidin-4-yl-piperazine derivatives and their use as neurokinin antagonists 失效
标题翻译：取代的1,4-二 - 哌啶-4-基 - 哌嗪衍生物及其作为神经激肽拮抗剂的用途
公开(公告)号：US07410970B2
公开(公告)日：2008-08-12
申请号：US10527821
申请日：2003-10-07
申请人： Frans Eduard Janssens , François Maria Sommen , Benoît Christian Albert Ghislain De Boeck , Joseph Elisabeth Leenaerts , Yves Emiel Maria Van Roosbroeck , Gaston Stanislas Marcella Diels
发明人： Frans Eduard Janssens , François Maria Sommen , Benoît Christian Albert Ghislain De Boeck , Joseph Elisabeth Leenaerts , Yves Emiel Maria Van Roosbroeck , Gaston Stanislas Marcella Diels
IPC分类号： A61K31/496 , A61K31/497 , C07D401/00 , C07D403/00 , C07D403/14 , C07D405/00 , C07D409/00
CPC分类号： C07D401/14 , C07D211/58 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： The invention concerns substituted 1,4-di-piperidin-4-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of emesis, anxiety, depression, pain, pancreatitis and IBS.
摘要翻译：本发明涉及具有神经激肽拮抗活性的取代的1,4-二哌啶-4-基 - 哌嗪衍生物，特别是NK 1拮抗活性，其制备方法，包含它们的组合物及其作为药物的用途，特别是用于治疗呕吐，焦虑，抑郁，疼痛，胰腺炎和IBS。

3. 发明授权

US07795261B2 Substituted 1-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives and their use as neurokinin antagonists 有权
标题翻译：取代的1-哌啶-4-基-4-吡咯烷-3-基 - 哌嗪衍生物及其作为神经激肽拮抗剂的用途
公开(公告)号：US07795261B2
公开(公告)日：2010-09-14
申请号：US10540447
申请日：2003-12-17
申请人： Frans Eduard Janssens , François Maria Sommen , Benoît Christian Albert Ghislain De Boeck , Joseph Elisabeth Leenaerts
发明人： Frans Eduard Janssens , François Maria Sommen , Benoît Christian Albert Ghislain De Boeck , Joseph Elisabeth Leenaerts
IPC分类号： C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , A61K31/496 , A61K31/498
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： This invention concerns substituted I-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK3 antagonistic activity and a combined NK1/NK2/NK3 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of schizophrenia, anxiety, depression, emesis and IBS. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in claim 1. In view of their capability to antagonize the actions of tachykinins by blocking the neurokinin receptors, and in particular antagonizing the actions of substance P and Neurokinin B by blocking the NK1, NK2 and NK3 receptors, the compounds according to the invention are useful as a medicine, in particular in the prophylactic and therapeutic treatment of tachykinin-mediated conditions, such as, for instance CNS disorders, in particular schizoaffective disorders, depression, anxiety disorders, stress-related disorders, sleep disorders, cognitive disorders, personality disorders, eating disorders, neurodegenerative diseases, addiction disorders, mood disorders, sexual dysfunction, pain and other CNS-related conditions; inflammation; allergic disorders; emesis; gastrointestinal disorders, in particular irritable bowel syndrome (IBS); skin disorders; vasospastic diseases; fibrosing and collagen diseases; disorders related to immune enhancement or suppression and rheumatic diseases and body weight control.
摘要翻译：本发明涉及具有神经激肽拮抗活性的特异性N-哌啶-4-基-4-吡咯烷-3-基 - 哌嗪衍生物，特别是NK1拮抗活性，组合的NK1 / NK3拮抗活性和组合的NK1 / NK2 / NK3拮抗活性，它们的制备，包含它们的组合物及其作为药物的用途，特别是用于治疗精神分裂症，焦虑，抑郁，呕吐和IBS。根据本发明的化合物可以由通式（I）表示，并且还包括其药学上可接受的酸或碱加成盐，其立体化学异构形式，其N-氧化物形式及其前药，其中所有取代基定义为鉴于其通过阻断神经激肽受体拮抗速激肽的作用的能力，特别是通过阻断NK1，NK2和NK3受体拮抗物质P和神经激肽B的作用，本发明的化合物是可用作药物，特别是在速激肽介导的病症例如CNS疾病，特别是分裂情感障碍，抑郁症，焦虑障碍，应激相关疾病，睡眠障碍，认知障碍，人格障碍的预防和治疗中的治疗，进食障碍，神经变性疾病，成瘾症，情绪障碍，性功能障碍疼痛等CNS相关病情; 炎; 过敏性疾病; 呕吐胃肠道疾病，特别是肠易激综合征（IBS）; 皮肤病; 血管痉挛性疾病; 纤维化和胶原病; 与免疫增强或抑制相关的疾病和风湿性疾病和体重控制。

4. 发明授权

US07435736B2 Substituted 1-piperidin-4-yl-4-azetidin-3-yl-piperazine derivatives and their use as neurokinin antagonists 失效
公开(公告)号：US07435736B2
公开(公告)日：2008-10-14
申请号：US10540304
申请日：2003-12-17
申请人： Frans Eduard Janssens , François Maria Sommen , Benoît Christian Albert Ghislain De Boeck , Joseph Elisabeth Leenaerts
发明人： Frans Eduard Janssens , François Maria Sommen , Benoît Christian Albert Ghislain De Boeck , Joseph Elisabeth Leenaerts
IPC分类号： A61K31/496 , A61K31/497 , C07D401/12 , C07D401/14 , C07D409/14 , C07D417/14 , C07D405/14
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14
摘要： The invention concerns substituted 1-piperidin-4-yl-4-azetidin-3-yl-piperazine having neurokinin antagonistic activity, in particular NK1 and NK1/NK3-antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of schizophrenia, emesis, anxiety, depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pain, neurogenic inflammation, asthma, micturition disorders such as urinary incontinence and nociception. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1. In view of their capability to antagonize the actions of tachykinins by blocking the neurokinin receptors, and in particular antagonizing the actions of substance P by blocking the NK receptors, the compounds according to the invention are useful as a medicine, in particular in the prophylactic and therapeutic treatment of tachykinin-mediated conditions, such as, for instance CNS disorders, in particular depression, anxiety disorders, stress-related disorders, sleep disorders, cognitive disorders, personality disorders, schizoaffective disorders, eating disorders, neurodegenerative diseases, addiction disorders, mood disorders, sexual dysfunction, pain and other CNS-related conditions; inflammation; allergic disorders; emesis; gastrointestinal disorders, in particular irritable bowel syndrome (IBS); skin disorders; vasospastic diseases; fibrosing and collagen diseases; disorders related to immune enhancement or suppression and rheumatic diseases and body weight control.

5. 发明授权

US07572786B2 Substituted 1-piperidin-3-yl-4-piperidin-4-yl-piperazine derivatives and their use as neurokinin antagonists 失效
公开(公告)号：US07572786B2
公开(公告)日：2009-08-11
申请号：US10540045
申请日：2003-12-17
申请人： Frans Eduard Janssens , Francois Maria Sommen , Benoît Christian Albert Ghislain De Boeck , Joseph Elisabeth Leenaerts
发明人： Frans Eduard Janssens , Francois Maria Sommen , Benoît Christian Albert Ghislain De Boeck , Joseph Elisabeth Leenaerts
IPC分类号： A61K31/551 , A61K31/496 , C07D211/58 , C07D211/96 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D513/04
CPC分类号： C07D405/14 , C07D211/58 , C07D211/96 , C07D401/12 , C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D513/04
摘要： This invention concerns substituted 1-piperidin-3-yl-4-piperidin-4-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK3 antagonistic activity and a combined NK1/NK2/NK3 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of schizophrenia, emesis, anxiety and depression, irritable bowel syndrom (IBS), circadian rhythm disturbances, visceral pain, neurogenic inflammation, asthma, micturition disorders such as urinary incontinence and nociception. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in claim 1. In view of their capability to antagonize the actions of tachykinins by blocking the neurokinin receptors, and in particular antagonizing the actions of substance P, Neurokinin A and Neurokinin B by blocking the NK1, NK2 and NK3 receptors, the compounds according to the invention are useful as a medicine, in particular in the prophylactic and therapeutic treatment of tachykinin-mediated conditions, such as, for instance CNS disorders, in particular schizoaffective disorders, depression, anxiety disorders, stress-related disorders, sleep disorders, cognitive disorders, personality disorders, eating disorders, neurodegenerative diseases, addiction disorders, mood disorders, sexual dysfunction, pain and other CNS-related conditions; inflammation; allergic disorders; emesis; gastrointestinal disorders, in particular irritable bowel syndrome (IBS); skin disorders; vasospastic diseases; fibrosing and collagen diseases; disorders related to immune enhancement or suppression and rheumatic diseases and body weight control.

6. 发明申请

US20120238561A1 MORPHOLINOTHIAZOLES AS ALPHA 7 POSITIVE ALLOSTERIC MODULATORS 有权
标题翻译：作为ALPHA 7的阳离子调节剂的摩尔比洛兹
公开(公告)号：US20120238561A1
公开(公告)日：2012-09-20
申请号：US13512464
申请日：2010-11-25
申请人： Gregor James Macdonald , Benoît Christian Albert Ghislain De Boeck , Joseph Elisabeth Leenaerts
发明人： Gregor James Macdonald , Benoît Christian Albert Ghislain De Boeck , Joseph Elisabeth Leenaerts
IPC分类号： A61K31/5377 , A61P25/00 , A61P25/22 , A61P25/18 , A61P25/24 , A61P25/16 , A61P25/14 , A61P25/34 , A61P29/00 , A61P31/00 , A61P11/06 , A61P17/06 , A61P1/00 , A61P9/04 , A61P11/00 , A61P37/06 , C07D417/14 , C07D498/08 , A61K31/5386 , A61P25/28
CPC分类号： C07D417/14
摘要： The present invention relates to morpholinothiazole derivatives and pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulators having the capability to increase the efficacy of nicotinic receptor agonists.
摘要翻译：本发明涉及吗啉代噻唑衍生物及其药学上可接受的盐，其制备方法，含有它们的药物组合物及其在治疗中的用途。本发明特别涉及烟碱乙酰胆碱受体的正变构调节剂，这种正性变构调节剂具有增加烟碱受体激动剂功效的能力。

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