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    Substituted diaza-spiro-[4.5]-decane derivatives and their use as neurokinin antagonists
    62.
    发明专利
    Substituted diaza-spiro-[4.5]-decane derivatives and their use as neurokinin antagonists 未知

    公开(公告)号：AU2005231984B2

    公开(公告)日：2011-03-03

    申请号：AU2005231984

    申请日：2005-04-04

    Applicant: JANSSEN PHARMACEUTICA NV

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

    IPC: C07D471/10

    Abstract: 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.

    ПРОИЗВОДНЫЕ ДИАЗА-СПИРО-[4,4]НОНАНА В КАЧЕСТВЕ АНТАГОНИСТОВ НЕЙРОКИНИНА (NK1)
    63.
    发明专利
    ПРОИЗВОДНЫЕ ДИАЗА-СПИРО-[4,4]НОНАНА В КАЧЕСТВЕ АНТАГОНИСТОВ НЕЙРОКИНИНА (NK1) 未知

    公开(公告)号：EA014239B1

    公开(公告)日：2010-10-29

    申请号：EA200701898

    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: Данноеизобретениеотноситсяк замещенномупроизводномудиаза-спиро-[4,4]нонанаобщейформулы (I) иегофармацевтическиприемлемымкислотно- илиосновно-аддитивнымсолям, стереохимическимизомернымформами N-оксидам, гдевсезаместителиимеютопределения, указанныев п.1, обладающемуантагонистическойактивностьюпоотношениюк нейрокинину, вчастности, антагонистическойактивностьюпоотношениюк NK, кспособуполученияданногопроизводного, ккомпозиции, содержащейуказанноепроизводное, ик егоприменениюв качествелекарственногосредства, вособенностидлялеченияи/илипрофилактикишизофрении, рвоты, тревогии депрессии, синдромараздраженнойкишки (IBS), нарушенийциркодианногоритма, преэклампсии, ноцицепции, висцеральнойи невропатическойболи, панкреатита, нейрогенноговоспаления, астмы, хроническогообструктивногозаболеваниялегких (COPD) инарушениймочеиспускания, такихкакнедержаниемочи.

    Diaza-spiro-[4.4]-nonane derivatives as neurokinin (NK1) antagonists
    65.
    发明专利
    Diaza-spiro-[4.4]-nonane derivatives as neurokinin (NK1) antagonists 未知

    公开(公告)号：NZ556628A

    公开(公告)日：2009-09-25

    申请号：NZ55662806

    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: A61P25/00 ,  A61K31/407 ,  A61K31/435 ,  A61K31/4523 ,  C07D211/58 ,  C07D487/10

    Abstract: Disclosed is a diaza-spiro-[4.4]-nonane derivative according to 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 of formula -O-, -S- or ûNR3-; Q is O or NR3; each R3 independently from each other, is hydrogen or alkyl; R1 is selected from the group ofAr1, Ar1-alkyl and di(Ar1)-alkyl; m and n are both equal to 1; Z is a covalent bond or a bivalent radical of formula ûCH2- or >C(=O); the spiro moiety has the formula (f6) or (f8) wherein "a" denotes the piperidinyl-moiety and "b" denotes the Alk-Y-Alk-L moiety; T is =O in an alpha-position relative to the N-atom and t is an integer, equal to 0 or 1; each Alk represents, independently from each other, a covalent bond; a bivalent straight or branched, saturated or unsaturated hydrocarbon radical having from 1 to 6 carbon atoms; or a cyclic saturated or unsaturated hydrocarbon radical having from 3 to 6 carbon atoms; each radical optionally substituted on one or more carbon atoms with one or more, phenyl, halo, cyano, hydroxy, formyl and amino radicals; Y is a covalent bond or a bivalent radical of formula -C(=O)-, -SO2- >C=CH-R or >C=N-R, wherein R is H, CN or nitro; L is selected from the group of hydrogen, alkyl, alkenyl, alkyloxy, alkyloxyalkyloxy, alkylcarbonyloxy, alkyloxycarbonyl, mono- and di(alkyl)amino, mono- and di(alkyloxycarbonyl)amino, mono- and di(alkylcarbonyl)amino, mono-and di(Ar3)amino, mono-and di(Ar3alkyl)amino, mono- and di(Het2)amino, mono- and di(Het2alkyl)amino, alkylsulfonyl, norbornyl, adamantyl, tricycloundecyl, Ar3, Ar3-oxy, Ar3carbonyl, Het2, Het-oxy, Her2carbonyl and mono- and di(Het2carbonyl)amino; The remaining substituents are defined herein. Also disclosed is the use of the above compounds for the manufacture of a medicament for treating tachykinin mediated conditions, and also for the treatment and/or prophylaxis of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (lBS), 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.

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