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    SUBSTITUTED OXA-DIAZA-SPIRO-[5.5]-UNDECANONE DERIVATIVES AND THEIR USE AS NEUROKININ ANTAGONISTS
    1.
    发明申请
    SUBSTITUTED OXA-DIAZA-SPIRO-[5.5]-UNDECANONE DERIVATIVES AND THEIR USE AS NEUROKININ ANTAGONISTS 审中-公开
    取代的OXA-DIAZA-SPIRO- [5.5] - 十一酮衍生物及其作为神经激肽原拮抗剂的用途

    公开(公告)号：WO2006094934A8

    公开(公告)日：2006-12-07

    申请号：PCT/EP2006060419

    申请日：2006-03-03

    Applicant: JANSSEN PHARMACEUTICA NV ,  JANSSENS FRANS EDUARD ,  COUPA SOPHIE ,  PONCELET ALAIN PHILIPPE ,  SCHOENTJES BRUNO

    Inventor： JANSSENS FRANS EDUARD ,  COUPA SOPHIE ,  PONCELET ALAIN PHILIPPE ,  SCHOENTJES BRUNO

    IPC: C07D498/10 ,  A61K31/537 ,  A61P25/18 ,  A61P25/24

    CPC classification number: C07D498/10 ,  B82Y5/00

    Abstract: This invention concerns substituted oxa-diaza-spiro-[5.5]-undecanone derivatives having neurokinin antagonistic activity, in particular an NK 1 antagonistic activity, an NK 3 antagonistic activity, a combined NK 1 /NK 2 antagonistic activity and a combined NK 1 /NK 2 /NK 3 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 incont inence. 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.

    Abstract translation: 本发明涉及具有神经激肽拮抗活性，特别是NK 1拮抗活性，NK 3拮抗活性， 联合NK 1 / NK 2 拮抗活性和组合的NK 1 / NK 2 / NK 3 拮抗活性，它们的制备，包含它们的组合物以及它们作为药物的用途，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， - 惊厥，疼痛，尤其是内脏和神经性疼痛，胰腺炎，神经原性炎症，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）表示并且还包含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。

    Diaza-spiro-[4.4]-nonane derivatives as neurokinin (NK1) antagonists
    3.
    发明专利
    Diaza-spiro-[4.4]-nonane derivatives as neurokinin (NK1) antagonists 未知

    公开(公告)号：AU2006221984C1

    公开(公告)日：2012-02-09

    申请号：AU2006221984

    申请日：2006-03-03

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： JANSSENS FRANS EDUARD ,  PONCELET ALAIN PHILIPPE ,  SCHOENTJES BRUNO ,  COUPA SOPHIE ,  SIMONNET YVAN RENE FERDINAND

    IPC: C07D487/08 ,  A61K31/435 ,  A61P25/00

    Abstract: This invention concerns substituted diaza-spiro-[4.4]-nonane derivatives having neurokinin antagonistic activity, in particular NK1 antagonist ic 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, nocicept ion, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, chronic obstructive pulmonary disease (COPD) and micturition disorders such as urinary incont inence. 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

    Substituted oxa-diaza-spiro-(5.5)-undecanone derivatives and their use as neurokinin antagonists
    4.
    发明专利
    Substituted oxa-diaza-spiro-(5.5)-undecanone derivatives and their use as neurokinin antagonists 未知

    公开(公告)号：AU2006222061B2

    公开(公告)日：2011-04-28

    申请号：AU2006222061

    申请日：2006-03-03

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： SCHOENTJES BRUNO ,  PONCELET ALAIN PHILIPPE ,  JANSSENS FRANS EDUARD ,  COUPA SOPHIE

    IPC: C07D498/10 ,  A61K31/537 ,  A61P25/18 ,  A61P25/24

    Abstract: This invention concerns substituted oxa-diaza-spiro-[5.5]-undecanone derivatives having neurokinin antagonistic activity, in particular an NK1 antagonistic activity, an NK3 antagonistic activity, a combined NK1/NK2 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.

    Substituted diaza-spiro-[5.5]-undecane derivatives and their use as neurokinin antagonists
    5.
    发明专利
    Substituted diaza-spiro-[5.5]-undecane derivatives and their use as neurokinin antagonists 未知

    公开(公告)号：AU2005231985B2

    公开(公告)日：2011-03-03

    申请号：AU2005231985

    申请日：2005-04-04

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： SIMONNET YVAN RENE FERDINAND ,  COUPA SOPHIE ,  JANSSENS FRANS EDUARD ,  PONCELET ALAIN PHILIPPE ,  SCHOENTJES BRUNO

    IPC: C07D471/10 ,  A61K31/438 ,  A61P29/00

    Abstract: 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.

    DERIVADOS SUSTITUIDOS DE OXA-DIAZA-ESPIRO-[5.5]-UNDECANONA Y SU USO COMO ANTAGONISTAS DE LA NEUROCININA.
    7.
    发明专利
    DERIVADOS SUSTITUIDOS DE OXA-DIAZA-ESPIRO-[5.5]-UNDECANONA Y SU USO COMO ANTAGONISTAS DE LA NEUROCININA. 未知

    公开(公告)号：MX2007010728A

    公开(公告)日：2007-10-12

    申请号：MX2007010728

    申请日：2006-03-03

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： COUPA SOPHIE ,  PONCELET ALAIN PHILIPPE ,  JANSSENS FRANS EDUARD ,  SCHOENTJES BRUNO

    IPC: C07D498/10 ,  A61K31/537 ,  A61P25/18 ,  A61P25/24

    Abstract: Esta invencion se relaciona con derivados sustituidos de oxa-diaza-espiro-[5.5]-undecanona que tienen actividad antagonista de la neurocinina, en particular una actividad antagonista de NK1, una actividad antagonista de NK3, una actividad antagonista combinada de NK1/NK2 y una actividad antagonista combinada de NK1/NK2/NK3, su preparacion, composiciones que los comprenden y su uso como una medicina, en particular para el tratamiento y/o profilaxis de la esquizofrenia, emesis, ansiedad y depresion, sindrome del intestino irritable (IBS), perturbaciones del ritmo circadiano, preeclampsia, nocicepcion, dolor, en particular dolor visceral y neuropatico, pancreatitis, inflamacion neurogenica, asma, enfermedad pulmonar obstructiva cronica (COPD) y trastornos de la miccion, tales como incontinencia urinaria; los compuestos de acuerdo con la invencion pueden representarse por la formula general (I) (ver formula general (I)) y comprenden tambien las sales de adicion de acido o base farmaceuticamente aceptables de los mismos, las formas estereoquimicamente isomericas de los mismos, la forma de N oxido de los mismo y profarmacos de los mismos, en donde todos los sustituyentes se definen como en la reivindicacion 1.

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