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    Substituted 4-(4-piperidin-4-yl-piperazin-1-yl)-azepane derivatives and their use as neurokinin antagonists
    1.
    发明申请
    Substituted 4-(4-piperidin-4-yl-piperazin-1-yl)-azepane derivatives and their use as neurokinin antagonists 失效
    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：US20060058285A1

    公开(公告)日：2006-03-16

    申请号：US10540456

    申请日：2003-12-17

    申请人： Frans Janssens ,  Francois Sommen ,  Benoit Christian De Boeck ,  Joseph Leenaerts

    发明人： Frans Janssens ,  Francois Sommen ,  Benoit Christian De Boeck ,  Joseph Leenaerts

    IPC分类号： A61K31/55 ,  C07D403/14

    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 NK1 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. 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 1拮抗活性，其制备方法，包含它们的组合物和 它们用作药物，特别是用于治疗疼痛，呕吐，焦虑，抑郁和我

    Substituted 4-Alkyl-And 4-Alkanoyl-Piperidine Derivatives And Their Use As Neurokinin Antagonists
    2.
    发明申请
    Substituted 4-Alkyl-And 4-Alkanoyl-Piperidine Derivatives And Their Use As Neurokinin Antagonists 审中-公开
    取代的4-烷基和4-烷酰基 - 哌啶衍生物及其作为神经激肽拮抗剂的用途

    公开(公告)号：US20070213346A1

    公开(公告)日：2007-09-13

    申请号：US11547868

    申请日：2005-04-04

    申请人： Frans Janssens ,  Francois Sommen ,  Benoit Christian De Boeck ,  Joseph Leenaerts

    发明人： Frans Janssens ,  Francois Sommen ,  Benoit Christian De Boeck ,  Joseph Leenaerts

    IPC分类号： A61K31/496 ,  C07D401/14

    CPC分类号： C07D409/14 ,  C07D401/02 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

    摘要： The invention concerns substituted 4-alkyl- and 4-alkanoyl-piperidine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity and a combined NK1/NK3 antagonistic activity, compositions comprising them and their use as a medicine, in particular for the treatment and/or prophylaxis of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pre-eclampsia, nociception, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, chronic obstructive pulmonary disease (COPD) and micturition disorders such as urinary incontinence. 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.

    摘要翻译： 本发明涉及具有神经激肽拮抗活性，特别是NK 1拮抗活性的取代的4-烷基 - 和4-烷酰基 - 哌啶衍生物，以及组合的NK1 / 包括它们的组合物及其作为药物的用途，特别是用于治疗和/或预防精神分裂症，呕吐，焦虑和抑郁，肠易激综合征（IBS），昼夜节律紊乱，先兆子痫 疼痛，特别是内脏和神经性疼痛，胰腺炎，神经源性炎症，哮喘，慢性阻塞性肺病（COPD）和排尿障碍如尿失禁。 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 在权利要求1中。

    Substituted 1,4,-di-piperidin-4-yl-piperazine derivatives and their use as neurokinin antagonists
    3.
    发明申请
    Substituted 1,4,-di-piperidin-4-yl-piperazine derivatives and their use as neurokinin antagonists 失效
    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：US20060167008A1

    公开(公告)日：2006-07-27

    申请号：US10527821

    申请日：2003-10-07

    申请人： Frans Janssens ,  Francois Sommen ,  Benoit Christian De Boeck ,  Joseph Leenaerts ,  Yves Van Roosbroeck ,  Gaston Stanislas Diels

    发明人： Frans Janssens ,  Francois Sommen ,  Benoit Christian De Boeck ,  Joseph Leenaerts ,  Yves Van Roosbroeck ,  Gaston Stanislas Diels

    IPC分类号： A61K31/496 ,  C07D403/14

    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. 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 neurokinins by blocking the neurokinin receptors, and in particular antagonizing the actions of substance P by blocking the NK1 receptor, the compounds according to the invention are useful as a medicine, in particular in the prophylactic and therapeutic treatment of neurokinin-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.

    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。 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神经激肽的作用的能力，特别是通过阻断NK 1受体拮抗物质P的作用，本发明的化合物 可用作药物，特别是用于预防和治疗神经激肽介导的病症，例如中枢神经系统疾病，特别是抑郁症，焦虑障碍，应激相关疾病，睡眠障碍，认知障碍，人格障碍，分裂情感 疾病，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 相关条件; 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。

    Substitituted 1-piperidin-3-yl-piperidin 4-yl-piperazine derivatives and their use as neurokinin auantagonists
    4.
    发明申请
    Substitituted 1-piperidin-3-yl-piperidin 4-yl-piperazine derivatives and their use as neurokinin auantagonists 失效

    公开(公告)号：US20060252747A1

    公开(公告)日：2006-11-09

    申请号：US10540045

    申请日：2003-12-17

    申请人： Frans Janssens ,  Francois Sommen ,  Benoit Christian De Boeck ,  Joseph Leenaerts

    发明人： Frans Janssens ,  Francois Sommen ,  Benoit Christian De Boeck ,  Joseph Leenaerts

    IPC分类号： A61K31/551 ,  A61K31/496 ,  C07D403/14

    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.

    Substituted 1-piperidin-4-yl-4-azetidin-3-yl-piperazine derivatives and their use as neurokinin antagonists
    5.
    发明申请
    Substituted 1-piperidin-4-yl-4-azetidin-3-yl-piperazine derivatives and their use as neurokinin antagonists 失效

    公开(公告)号：US20060074069A1

    公开(公告)日：2006-04-06

    申请号：US10540304

    申请日：2003-12-17

    申请人： Frans Janssens ,  Francois Sommen ,  Benoit Christian Albert De Boeck ,  Joseph Leenaerts

    发明人： Frans Janssens ,  Francois Sommen ,  Benoit Christian Albert De Boeck ,  Joseph Leenaerts

    IPC分类号： A61K31/496 ,  A61K31/551 ,  C07D403/14

    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.

    Substituted 1-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives and their use as neurokinin antagonists
    6.
    发明申请
    Substituted 1-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives and their use as neurokinin antagonists 有权

    公开(公告)号：US20060040950A1

    公开(公告)日：2006-02-23

    申请号：US10540447

    申请日：2003-12-17

    申请人： Frans Janssens ,  Francois Sommen ,  Benoit Christian Albert De Boeck ,  Joseph Leenaerts

    发明人： Frans Janssens ,  Francois Sommen ,  Benoit Christian Albert De Boeck ,  Joseph Leenaerts

    IPC分类号： A61K31/496 ,  C07D403/14

    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.

    Novel Substituted 4-Phenyl-4[H-Imidazol-2-YL]-Piperidine Derivatived And Their Use As Selective Non-Peptide Delta Opioid Agonists
    7.
    发明申请
    Novel Substituted 4-Phenyl-4[H-Imidazol-2-YL]-Piperidine Derivatived And Their Use As Selective Non-Peptide Delta Opioid Agonists 审中-公开
    新型取代的4-苯基-4 [H-咪唑-2-YL] - 哌啶衍生物及其作为选择性非肽Δ阿片样物质激动剂

    公开(公告)号：US20080096925A1

    公开(公告)日：2008-04-24

    申请号：US11753830

    申请日：2007-05-25

    申请人： Frans Janssens ,  Joseph Leenaerts ,  Francisco Fernandez-Gadea ,  Antonio Gomez-sanchez ,  Theo Meert

    发明人： Frans Janssens ,  Joseph Leenaerts ,  Francisco Fernandez-Gadea ,  Antonio Gomez-sanchez ,  Theo Meert

    IPC分类号： A61K31/454 ,  C07D401/04

    CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

    摘要： The present invention relates to novel 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives according to Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof and the N-oxide forms thereof. In particular are claimed compounds according to Formula (I) in which A=B is C═O or SO2, X is a covalent bond, R1 is alkyloxy, alkyloxyalkyl, Ar or NR9R10, wherein R9 and R10 each independently are hydrogen or Ar; or A=B and R1 together form a benzoxazolyl radical; p is zero, R3 is benzyl optionally substituted with hydroxy, alkyl or alkyloxycarbonyl and R4 and R5 each are hydrogen. The invention also relates to processes for the preparation of the compounds according to the invention and their use in medicine, in particular as selective non-peptide δ-opioid agonists for use in the treatment of various pain conditions.

    摘要翻译： 本发明涉及式（I）的新颖的4-苯基-4- [1H-咪唑-2-基] - 哌啶衍生物，其药学上可接受的酸或碱加成盐，其立体化学异构形式，互变异构形式 及其N-氧化物形式。 特别是根据式（I）所述的化合物，其中A = B是CO或SO 2，X是共价键，R 1是烷氧基，烷氧基烷基，Ar 或其中R 9和R 10各自独立地是氢或Ar; R 9和R 10各自独立地是氢或Ar; 或A = B和R 1一起形成苯并恶唑基; p为0，R 3为任选被羟基，烷基或烷氧基羰基取代的苄基，R 4和R 5各自为氢。 本发明还涉及根据本发明的化合物的制备方法及其在医学中的用途，特别是用于治疗各种疼痛病症的选择性非肽δ-阿片样物质激动剂。

    Substituted 4-phenyl-4-[1h-imidazol-2-yl]-piperidine derivatives as selective non-peptide delta opiod agonists with antidepressant and anxiolytic activity
    9.
    发明申请
    Substituted 4-phenyl-4-[1h-imidazol-2-yl]-piperidine derivatives as selective non-peptide delta opiod agonists with antidepressant and anxiolytic activity 审中-公开
    取代的4-苯基-4- [1h-咪唑-2-基] - 哌啶衍生物作为具有抗抑郁和抗焦虑活性的选择性非肽δ阿片剂激动剂

    公开(公告)号：US20060287345A1

    公开(公告)日：2006-12-21

    申请号：US10552527

    申请日：2004-04-08

    申请人： Thomas Steckler ,  Frans Janssens ,  Joseph Leenaerts ,  Francisco Fernandez-Gadea ,  Antonio Gomez-Sanchez ,  Theo Meert

    发明人： Thomas Steckler ,  Frans Janssens ,  Joseph Leenaerts ,  Francisco Fernandez-Gadea ,  Antonio Gomez-Sanchez ,  Theo Meert

    IPC分类号： A61K31/513 ,  A61K31/454

    CPC分类号： A61K31/506 ,  A61K31/454

    摘要： The present invention relates to the use of 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives according to Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof and the N-oxide forms thereof as selective non-peptide δ-opioid agonists for use in the prevention and/or treatment of various central nervous system disorders, in particular as selective antidepressant and anxiolytic non-peptide δ-opioid agonists. In particular are claimed compounds according to Formula (I) in which A=B is C═O or SO2, X is a covalent bond, R1 is allyloxy, alkyloxyalkyl, Ar or NR9R10, wherein R9 and R10 each independently are hydrogen or Ar; or A=B and R1 together form a benzoxazolyl radical; p is zero, R3 is benzyl optionally substituted with hydroxy, alkyl or alkyloxycarbonyl and R4 and R5 each are hydrogen.

    摘要翻译： 本发明涉及式（I）的4-苯基-4- [1H-咪唑-2-基] - 哌啶衍生物，其药学上可接受的酸或碱加成盐，其立体化学异构形式，互变异构体 形式和其N-氧化物形式作为用于预防和/或治疗各种中枢神经系统疾病的选择性非肽δ-阿片样物质激动剂，特别是作为选择性抗抑郁药和抗焦虑性非肽δ-阿片样物质激动剂。 特别是根据式（I）所述的化合物，其中A = B是CO或SO 2，X是共价键，R 1是烯丙氧基，烷氧基烷基，Ar 或其中R 9和R 10各自独立地是氢或Ar; R 9和R 10各自独立地是氢或Ar; 或A = B和R 1一起形成苯并恶唑基; p为0，R 3为任选被羟基，烷基或烷氧基羰基取代的苄基，R 4和R 5各自为氢。