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    DIAZA-SPIRO-[4.4]-NONANE DERIVATIVES AS NEUROKININ (NK1) ANTAGONISTS
    11.
    发明专利
    DIAZA-SPIRO-[4.4]-NONANE DERIVATIVES AS NEUROKININ (NK1) ANTAGONISTS 未知

    公开(公告)号：CA2599186C

    公开(公告)日：2014-12-09

    申请号：CA2599186

    申请日：2006-03-03

    Applicant: JANSSEN PHARMACEUTICA NV

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

    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 1.

    SUBSTITUTED DIAZA-SPIRO-[5.5]-UNDECANE DERIVATIVES AND THEIR USE AS NEUROKININ ANTAGONISTS
    13.
    发明专利
    SUBSTITUTED DIAZA-SPIRO-[5.5]-UNDECANE DERIVATIVES AND THEIR USE AS NEUROKININ ANTAGONISTS 未知

    公开(公告)号：MY142090A

    公开(公告)日：2010-09-15

    申请号：MYPI20051505

    申请日：2005-04-04

    Applicant: JANSSEN PHARMACEUTICA NV

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

    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, THIER 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), CIRACADIAN RHYTHM DISTURBANCES, PRE-ECLAMPSIA, NOCICEPTION, PAIN, IN PARTICULAR VISCERAL AND NEURAOPHATIC 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 (1) AND COMPRISES ALSO THE PHARMACEUTICALLY ACCEPTABLE ACID OR BASE ADDITION SALTS THEREOF, THE STREOCHEMICALLY ISOMERIC FORMS THEREOF, THE N-OXIDE FORM THEREOF AND PRODRUGS THEREOF, WHEREIN ALL SUBSTITUENTS ARE DEFINED AS IN CLAIM 1.

    Substituted oxa-diaza-spiro-[5.5]-undecanone derivatives and their use as neurokinin antagonists
    15.
    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：NZ556629A

    公开(公告)日：2010-04-30

    申请号：NZ55662906

    申请日：2006-03-03

    Applicant: JANSSEN PHARMACEUTICA NV

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

    IPC: C07D498/10 ,  A61K31/4468 ,  A61K31/4523 ,  A61K31/537 ,  A61P25/18 ,  A61P25/24 ,  C07D211/58

    Abstract: Disclosed are oxa-diaza-spiro-[5.5]-undecanone derivatives as represented by the general Formula (I), wherein: R2 is Ar2, Ar2-alkyl, di(Ar2)alkyl, Het1 or Het1-alkyl; X is a covalent bond or a bivalent radical selected from O, S, or NR3; Q is O or NR3; each R3 independently from each other, is hydrogen or alkyl; R1 is selected from the group of Ar1, Ar1-alkyl and di(Ar1)-alkyl; n is an integer, equal to 0, 1 or 2; m is an integer, equal to 1 or 2, provided that if m is 2. then n is 1; Z is a covalent bond or a bivalent radical selected from CH-2 or C(=O); A1, A2, A3 and A4 are each independently from each other selected from the group of CH2CH2, C(=O)O and OC(=O), provided that at least one of C(=O)O and OC(=O) is selected and that =O is in an alpha-position relative to the N-atom; and wherein the remaining substituents are as disclosed herein. Also disclosed is the use of a compound as defined above for the manufacture of a medicament for the treatment and / or prophylaxis of tachykinin mediated conditions, and conditions such as schizophrenia, emesis, anxiety and depression, irritable bowel syndrome. circadian rhythm disturbances, pre-eclampsia, nociceprion, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, chronic obstructive pulmonary disease and micturition disorders such as urinary incontinence.

    17.
    发明专利
    未知

    公开(公告)号：BRPI0608074A2

    公开(公告)日：2009-11-03

    申请号：BRPI0608074

    申请日：2006-03-03

    Applicant: JANSSEN PHARMACEUTICA NV

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

    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.

    DIAZA-SPIRO-[4.4]-NONANE DERIVATIVES AS NEUROKININ (NK1) ANTAGONISTS
    19.
    发明专利
    DIAZA-SPIRO-[4.4]-NONANE DERIVATIVES AS NEUROKININ (NK1) ANTAGONISTS 未知

    公开(公告)号：CA2599186A1

    公开(公告)日：2006-09-14

    申请号：CA2599186

    申请日：2006-03-03

    Applicant: JANSSEN PHARMACEUTICA NV

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

    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 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.

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