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    Substituted Diaza-Spiro-[4.5]-Decane Derivatives and Their Use as Neurokinin Antagonists
    1.
    发明申请
    Substituted Diaza-Spiro-[4.5]-Decane Derivatives and Their Use as Neurokinin Antagonists 失效
    取代的Diaza-Spiro- [4.5] - 癸烷衍生物及其用作神经激肽拮抗剂

    公开(公告)号：US20070254904A1

    公开(公告)日：2007-11-01

    申请号：US11547705

    申请日：2005-04-04

    申请人： Frans Janssens ,  Bruno Schoentjes ,  Sophie Coupa ,  Alain Poncelet ,  Yvan Simonnet

    发明人： Frans Janssens ,  Bruno Schoentjes ,  Sophie Coupa ,  Alain Poncelet ,  Yvan Simonnet

    IPC分类号： A61K31/438 ,  A61P1/12 ,  A61P13/00 ,  A61P25/18 ,  A61P25/24 ,  C07D401/02

    CPC分类号： C07D471/10

    摘要： This invention concerns substituted diaza-spiro-[4.5]-decane derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK2 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 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拮抗活性的组合NK 1 / NK 2的取代的二氮 - 螺 - [4.5] - 癸烷衍生物 组合的NK 1 / NK 3拮抗活性和组合的NK 1 / NK 2拮抗活性， 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，特别是用于治疗和/或预防精神分裂症，呕吐，焦虑和抑郁症，肠易激综合征（肠易激综合征 IBS），昼夜节律障碍，先兆子痫，伤害感受，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 Diaza-Spiro-[5.5]-Undecane Derivaties and Their Use as Neurokinin Antagonists
    2.
    发明申请
    Substituted Diaza-Spiro-[5.5]-Undecane Derivaties and Their Use as Neurokinin Antagonists 失效
    取代的Diaza-Spiro- [5.5] - 十二烷衍生物及其作为神经激肽拮抗剂的用途

    公开(公告)号：US20070232636A1

    公开(公告)日：2007-10-04

    申请号：US11547889

    申请日：2005-04-04

    申请人： Frans Janssens ,  Bruno Schoentjes ,  Sophie Coupa ,  Alain Poncelet ,  Yvan Simonnet

    发明人： Frans Janssens ,  Bruno Schoentjes ,  Sophie Coupa ,  Alain Poncelet ,  Yvan Simonnet

    IPC分类号： A61K31/438 ,  C07D215/00

    CPC分类号： C07D471/10 ,  C07D519/00

    摘要： This invention concerns substituted diaza-spiro-[5.5]-undecane derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK2 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 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, 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拮抗活性的组合NK 1 / NK 2的取代的二氮 - 螺 - [5.5] - 十一烷衍生物 组合的NK 1 / NK 3拮抗活性和组合的NK 1 / NK 2拮抗活性， 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，特别是用于治疗和/或预防精神分裂症，呕吐，焦虑和抑郁症，肠易激综合征（肠易激综合征 IBS），昼夜节律紊乱，先兆子痫，伤害感受，疼痛，特别是内脏和神经性疼痛，胰腺炎，神经源性炎症，哮喘，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-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.

    Respiratory syncytial virus replication inhibitors
    7.
    发明申请
    Respiratory syncytial virus replication inhibitors 失效

    公开(公告)号：US20060058309A1

    公开(公告)日：2006-03-16

    申请号：US11247392

    申请日：2005-10-11

    申请人： Frans Janssens ,  Jean Fernand Lacrampe ,  Jerome Guillemont ,  Marc Venet ,  Koenraad Jozef Andries

    发明人： Frans Janssens ,  Jean Fernand Lacrampe ,  Jerome Guillemont ,  Marc Venet ,  Koenraad Jozef Andries

    IPC分类号： A61K31/498 ,  A61K31/4709 ,  A61K31/454 ,  C07D403/02

    CPC分类号： C07D401/14 ,  C07D409/14 ,  C07D471/04 ,  Y02P20/55

    摘要： The present invention concerns compounds of formula (I), prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof wherein -a1=a2-a3=a4- represents a radical of formula —CH═CH—CH═CH—; —N═CH—CH═CH—; —CH═N—CH═CH—; —CH═CH—N═CH—; CH═CH—CH═N—; wherein each hydrogen atom may optionally be substituted; Q is a radical of formulae (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7) and (b-8), wherein Alk is C1-6alkanediyl; Y1 is a bivalent radical of formula —NR2— or —CH(NR2R4); X1 is NR4, S, S(═O), S(═O)2, O, CH2, C(═O), CH(═CH2), CH(OH), CH(CH3), CH(OCH3), CH(SCH3), CH(NR5aR5b), CH2—NR4 or NR4—CH2; X2 is a direct bond, CH2, C(═O), NR4, C1-4alkyl-NR4, NR4—C1-4alkyl, t is 2 to 5; u is 1 to 5; v is 2 or 3; and whereby each hydrogen in Alk and in (b-3), (b-4), (b-5), (b-6), (b-7) and (b-8), may optionally be replaced by R3; provided that when R3 is hydroxy or C1-6alkyloxy, then R3 cannot replace a hydrogen atom in the α position relative to a nitrogen atom; G is a direct bond or optionally substituted C1-10alkanediyl; R1 is an optionally substituted bicyclic heterocycle; R2 is hydrogen, formyl, C1-6alkylcarbonyl, Hetcarbonyl, pyrrolidinyl, piperidinyl, homopiperidinyl, C3-7cycloalkyl or C1-10alkyl substituted with N(R6)2 and optionally with another substituent; R3 is hydrogen, hydroxy, C1-6alkyl, C1-6alkyloxy, arylC1-6alkyl or arylC1-6alkyloxy, R4 is hydrogen, C1-6alkyl or arylC1-6alkyl; R5a, R5b, R5c and R5d are hydrogen or C1-6alkyl; or R5a and R5b, or R5c and R5d taken together from a bivalent radical of formula —(CH2)S— wherein S is 4 or 5; R6 is hydrogen, C1-4alkyl, formyl, hydroxyC1-6alkyl, C1-6alkylcarbonyl or C1-6alkyloxycarbonyl; aryl is optionally substituted phenyl; Het is pyridyl, pyrimidinyl, pyryzinyl, pyridazinyl; as respiratory syncytial virus replication inhibitors; their preparation, compositions containing them and their use as a medicine.

    Substituted 4-(4-piperidin-4-yl-piperazin-1-yl)-azepane derivatives and their use as neurokinin antagonists
    8.
    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

    N-phenyl-N-(4-piperidinyl)amides
    10.
    发明授权
    N-phenyl-N-(4-piperidinyl)amides 失效
    N-苯基-N-（4-哌啶基）酰胺

    公开(公告)号：US4167574A

    公开(公告)日：1979-09-11

    申请号：US954709

    申请日：1978-10-25

    申请人： Frans Janssens

    发明人： Frans Janssens

    IPC分类号： C07D211/58 ,  C07D257/04 ,  C07D401/06 ,  A61K31/445

    CPC分类号： C07D257/04 ,  C07D211/58

    摘要： Novel compounds of the series of N-phenyl-N-(4-piperidinyl)amides having a (4,5-dihydro-4-R-5-oxo-1H-tetrazol-1-yl)alkyl or (4,5-dihydro-4-R-5-thioxo-1H-tetrazol-1-yl)alkyl substituent group in the 1-position of the piperidine nucleus, said compounds being useful as analgesic agents.

    摘要翻译： 具有（4,5-二氢-4-R-5-氧代-1H-四唑-1-基）烷基的N-苯基-N-（4-哌啶基）酰胺系列的新型化合物或（4,5- 二氢-4-R-5-硫代-1H-四唑-1-基）烷基取代基，所述化合物可用作止痛剂。