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    SUBSTITUTED AMINO ISOXAZOLINE DERIVATIVES AND THEIR USE AS ANTI-DEPRESSANTS
    36.
    发明专利
    SUBSTITUTED AMINO ISOXAZOLINE DERIVATIVES AND THEIR USE AS ANTI-DEPRESSANTS 未知

    公开(公告)号：HRP20040871A2

    公开(公告)日：2005-04-30

    申请号：HRP20040871

    申请日：2004-09-21

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： ANDRES-GIL JOSE IGNACIO ,  ALCAZAR-VACA MANUEL JESUS ,  BAKKER MARGARETHA HENRICA MARI ,  DE LUCAS OLIVARES ANA ISABEL

    IPC: A61K31/496 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/55 ,  A61P3/04 ,  A61P25/00 ,  A61P25/02 ,  A61P25/04 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  C07D498/04 ,  C07D498/14 ,  C07D261/20 ,  A61K31/424

    Abstract: The invention concerns substituted amino isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisozazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on the phenylpart of the tricyclic moiety with primary, secondary and/or tertiary amino groups, according to Formula (I) wherein X=CH 2 , N-R 7 , S or O, R 1 , R 2 and R 3 are certain specific substituents, with the proviso that at least one of R 1 and R 2 is an amino radical of formula N-R 10 R 11 wherein R 10 and R 11 are each a variety of radicals, Pir is an optionally substituted piperidyl or piperazyl radical and R 3 represents an optionally substituted aromatic homocyclic or heterocyclic ring system including a partially or completely hydrogenated hydrocarbon chain of maximum 6 atoms long with which the ring system is attached to the Pir radical and which may contain one or more heteroatoms selected from the group of O, N and S; a process for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for the treatment of depression and/of anxiety and disorders of body weight. The compounds according to the invention have surprisingly been shown to have a serotonin (5-HT) reuptake inhibitor activity in combination with additional alpha 2 -adrenoceptor antagonist activity and show a strong anti-depressant activity without being sedative. Compounds according to the invention are also suitable for treating depression, anxiety and body weight disorders. The invention also relates to novel combination of substituted amino isoxazoline derivatives according to the invention with antidepressants, anxiolytics and/or antipsychotics to improve efficacy and/or onset of action.

    37.
    发明专利
    未知

    公开(公告)号：DE69632032T2

    公开(公告)日：2005-03-10

    申请号：DE69632032

    申请日：1996-01-30

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： VAN LOMMEN ROSALIA ,  ANDRES-GIL JOSE IGNACIO ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  MATESANZ-BALLESTEROS MARIA ENC

    IPC: A61K31/435 ,  A61P9/08 ,  A61P25/04 ,  A61P25/06 ,  C07D491/04 ,  C07D491/056

    Abstract: PCT No. PCT/EP96/00396 Sec. 371 Date Aug. 6, 1997 Sec. 102(e) Date Aug. 6, 1997 PCT Filed Jan. 30, 1996 PCT Pub. No. WO96/24596 PCT Pub. Date Aug. 15, 1996The present invention is concerned with compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein =a1-a2=a3-a4= is a bivalent radical of formula =N-CH=CH-CH= (a), =CH-N=CH-CH= (b), =CH-CH=N-CH= (c), =CH-CH=CH-N= (d), wherein one or two hydrogen atoms can be substituted by halo, hydroxy, C1-6alkyl or C1-6alkyloxy; R1 is hydrogen or C1-6alkyl; R2 is hydrogen or C1-6alkyl; R3 is hydrogen or C1-6alkyl; Alk1 is C1-5alkanediyl; Alk2 is C2-15alkanediyl; Q is a five- or six-membered heterocyclic ring containing at least one nitrogen atom or a radical of formula -C(NR5R6)=C-R4 wherein R4 is hydrogen, cyano, aminocarbonyl or C1-6alkyl; R5 is hydrogen, C1-6alkyl, C3-6alkenyl or C3-6alkynyl; R6 is hydrogen or C1-6alkyl; or R5 and R6 taken together may form a bivalent radical of formula -(CH2)4- or -(CH2)5-. Pharmaceutical compositions, preparations and use as a medicine are described.

    INDOLE DERIVATIVES WITH AN IMPROVED ANTIPSYCHOTIC ACTIVITY
    38.
    发明专利
    INDOLE DERIVATIVES WITH AN IMPROVED ANTIPSYCHOTIC ACTIVITY 未知

    公开(公告)号：CA2525282A1

    公开(公告)日：2004-12-09

    申请号：CA2525282

    申请日：2004-05-26

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： BARTOLOME-NEBREDA JOSE MANUEL ,  ANDRES-GIL JOSE IGNACIO

    IPC: C07D498/04 ,  A61K31/4355 ,  A61K31/436 ,  A61K31/5383 ,  A61P25/18 ,  C07D221/00 ,  C07D265/00 ,  C07D319/00 ,  C07D491/04

    Abstract: The present invention relates to a novel indol derivative according to Formu la (I), a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables R1, R2, R3, R4, R5, p, a1=a2a3=a4, Z1-Z2, X and Y are defined as in claim 1. Said derivative exhibi t a binding affinity towards dopamine receptors, in particular towards dopamin e D2, D3 and D4 receptors, with selective serotonin reuptake inhibition properties and acting as 5-HT1A agonists or partial agonists. The invention also relates to pharmaceutical compositions comprising the compounds accordi ng to the invention, the use thereof for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic disorders, most in particular schizophrenia and processes for thei r production.

    39.
    发明专利
    未知

    公开(公告)号：NO20044645L

    公开(公告)日：2004-10-27

    申请号：NO20044645

    申请日：2004-10-27

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： ANDRES-GIL JOSE IGNACIO ,  BAKKER MARGARETHA HENRICA MARIA ,  ALCAZAR-VACA MANUELL JESUS ,  OLIVARES ANA ISABEL DE LUCAS

    IPC: A61K31/496 ,  A61K31/497 ,  A61K31/5377 ,  C07D498/04 ,  A61K31/5383 ,  A61K31/55 ,  A61P3/04 ,  A61P25/00 ,  A61P25/02 ,  A61P25/04 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  C07D498/14

    Abstract: The invention concerns substituted amino isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisozazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on the phenylpart of the tricyclic moiety with primary, secondary and/or tertiary amino groups, according to Formula (I) wherein X=CH 2 , N-R 7 , S or O, R 1 , R 2 and R 3 are certain specific substituents, with the proviso that at least one of R 1 and R 2 is an amino radical of formula N-R 10 R 11 wherein R 10 and R 11 are each a variety of radicals, Pir is an optionally substituted piperidyl or piperazyl radical and R 3 represents an optionally substituted aromatic homocyclic or heterocyclic ring system including a partially or completely hydrogenated hydrocarbon chain of maximum 6 atoms long with which the ring system is attached to the Pir radical and which may contain one or more heteroatoms selected from the group of O, N and S; a process for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for the treatment of depression and/of anxiety and disorders of body weight. The compounds according to the invention have surprisingly been shown to have a serotonin (5-HT) reuptake inhibitor activity in combination with additional alpha 2 -adrenoceptor antagonist activity and show a strong anti-depressant activity without being sedative. Compounds according to the invention are also suitable for treating depression, anxiety and body weight disorders. The invention also relates to novel combination of substituted amino isoxazoline derivatives according to the invention with antidepressants, anxiolytics and/or antipsychotics to improve efficacy and/or onset of action.

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