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    Piperdine-amino-benzimidazole derivatives as inhibitors of respiratory syncytial virus replication
    1.
    发明申请
    Piperdine-amino-benzimidazole derivatives as inhibitors of respiratory syncytial virus replication 有权

    公开(公告)号：US20070093659A1

    公开(公告)日：2007-04-26

    申请号：US10596519

    申请日：2004-12-20

    申请人： Jean-Francois Bonfanti ,  Koenraad Andries ,  Frans Janssens ,  Francois Sommen ,  Jerome Guillemont ,  Jean Lacrampe

    发明人： Jean-Francois Bonfanti ,  Koenraad Andries ,  Frans Janssens ,  Francois Sommen ,  Jerome Guillemont ,  Jean Lacrampe

    IPC分类号： C07D473/00

    CPC分类号： C07D401/14 ,  C07D417/14

    摘要： The present invention concerns piperidine-amino-benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula their prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms wherein Q is C1-6alkyl optionally substituted with trifluoromethyl, C3-7cycloalkyl, Ar2, hydroxy, C1-4alkoxy, C1-4alkylthio, Ar2-oxy-, Ar2-thio-, Ar2(CH2)noxy, Ar2(CH2)nthio, hydroxycarbonyl, aminocarbonyl, C1-4alkylcarbonyl, Ar2carbonyl, C1-4alkoxycarbonyl, Ar2(CH2)ncarbonyl, aminocarbonyloxy, C1-4alkylcarbonyloxy, Ar2carbonyloxy, Ar2(CH2)ncarbonyloxy, C1-4alkoxy-carbonyl(CH2)noxy, mono- or di(C1-4alkyl)aminocarbonyl, mono- or di(C1-4alkyl)-aminocarbonyloxy, aminosulfonyl, mono- or di(C1-4alkyl)aminosulfonyl or a heterocycles selected from the group consisting of pyrrolidinyl, pyrrolyl, dihydropyrrolyl, imidazolyl, triazolyl, piperidinyl, homopiperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, 1-oxo-thiomorpholinyl, 1,1-dioxothiomorpholinyl, pyridyl and tetrahydropyridyl, wherein each of said heterocycle may optionally be substituted with oxo or C1-6alkyl; G is a direct bond or optionally substituted C1-10alkanediyl; R1 is Ar1 or a monocyclic or bicyclic heterocycle; one of R2a and R3a is C1-6alkyl and the other one of R2a and R3a is hydrogen; in case R2a is different from hydrogen then R2b is hydrogen or C1-6alkyl, and R3b is hydrogen; in case R3a is different from hydrogen then R3b is hydrogen or C1-6alkyl, and R2b is hydrogen; t is 1, 2 or 3; Ar1 is phenyl or substituted phenyl; and Ar2 is phenyl or substituted phenyl. It further concerns their preparation and compositions comprising them, as well as their use as a medicine.

    Substituted 4-(4-piperidin-4-yl-piperazin-1-yl)-azepane derivatives and their use as neurokinin antagonists
    4.
    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

    Substitituted 1-piperidin-3-yl-piperidin 4-yl-piperazine derivatives and their use as neurokinin auantagonists
    5.
    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.

    Novel formulations of opioid-based treatments of pain comprising substituted 1,4-di-piperidin-4-yl-piperazine derivatives
    6.
    发明申请
    Novel formulations of opioid-based treatments of pain comprising substituted 1,4-di-piperidin-4-yl-piperazine derivatives 审中-公开
    基于阿片样物质治疗疼痛的新型制剂包括取代的1,4-二哌啶-4-基 - 哌嗪衍生物

    公开(公告)号：US20060128721A1

    公开(公告)日：2006-06-15

    申请号：US10560476

    申请日：2004-06-07

    申请人： Frans Janssens ,  Francois Sommen ,  Benoit Christian Albert Ghislain De Boeck ,  Joseph Elisabeth Leenaerts ,  Yves Emiel, Maria Van Roosbroeck ,  Theo Frans Meert

    发明人： Frans Janssens ,  Francois Sommen ,  Benoit Christian Albert Ghislain De Boeck ,  Joseph Elisabeth Leenaerts ,  Yves Emiel, Maria Van Roosbroeck ,  Theo Frans Meert

    IPC分类号： A61K31/496

    CPC分类号： A61K45/06 ,  A61K31/496 ,  A61K31/551 ,  A61K2300/00

    摘要： This invention concerns novel formulations for opioid-based treatments of pain and/or nociception comprising opioid analgesics and 1,4-di-piperidin-4-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, the use of said formulation for the manufacture of a medicament for the prevention and/or treatment of emesis, pain and/or nociception, in particular in opioid-based acute and chronic pain treatments, more in particular in inflammatory, post-operative, emergency room (ER), breakthrough, neuropathic and cancer pain treatments and the use of an NK1-receptor antagonist for the manufacture of a medicament for the prevention and/or treatment of respiratory depression in opioid-based treatments of pain. The pharmaceutical formulations according to the invention comprise a pharmaceutically acceptable carrier and, as active ingredients, a therapeutically effective amount of an opioid analgesic and NK1-antagonists according to the general Formula (I) 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. The pharmaceutical composition according to the invention reduces to a large extent a number of unwanted side-effects associated with opioid analgesics, in particular emesis, respiratory depression and tolerance, thereby increasing the total tolerability of said opioids in pain treatment.

    摘要翻译： 本发明涉及用于基于阿片样物质治疗疼痛和/或伤害感受的新制剂，其包含具有神经激肽拮抗活性的阿片类镇痛药和1,4-二哌啶-4-基 - 哌嗪衍生物，特别是NK1 拮抗活性，所述制剂用于制备用于预防和/或治疗呕吐，疼痛和/或伤害感受，特别是基于阿片样物质的急性和慢性疼痛治疗的药物的用途，特别是在炎性， 手术，急诊室（ER），突破性，神经病理性和癌症疼痛治疗，以及使用NK 1受体拮抗剂制备用于预防和/或治疗阿片样物质中呼吸抑制的药物 的治疗疼痛。 根据本发明的药物制剂包含药学上可接受的载体，并且作为活性成分，具有治疗有效量的根据通式（I）的药学上可接受的酸的阿片样物质止痛剂和NK 1拮抗剂 或其碱加成盐，其立体化学异构形式，其N-氧化物形式和其前药，其中所有取代基如权利要求1中所定义。根据本发明的药物组合物在很大程度上降低了多个不需要的副产物， 与阿片类止痛药相关的作用，特别是呕吐，呼吸抑制和耐受性，从而增加所述阿片类药物在疼痛治疗中的总耐受性。

    Substituted 1-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives and their use as neurokinin antagonists
    7.
    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.

    Substituted 4-Alkyl-And 4-Alkanoyl-Piperidine Derivatives And Their Use As Neurokinin Antagonists
    9.
    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
    10.
    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。