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    Substituted amino isoxazoline derivatives and their use as anti-depressants.
    123.
    发明专利
    Substituted amino isoxazoline derivatives and their use as anti-depressants. 未知

    公开(公告)号：ZA200407904B

    公开(公告)日：2005-10-20

    申请号：ZA200407904

    申请日：2004-09-30

    Applicant: JANSSEN PHARMACEUTICA NV

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

    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 ,  C07D ,  A61K ,  A61P

    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.

    СОЕДИНЕНИЯ ДЛЯ ЛЕЧЕНИЯ НАРУШЕННОЙ ФУНДАЛЬНОЙ РЕЛАКСАЦИИ
    124.
    发明专利
    СОЕДИНЕНИЯ ДЛЯ ЛЕЧЕНИЯ НАРУШЕННОЙ ФУНДАЛЬНОЙ РЕЛАКСАЦИИ 未知

    公开(公告)号：EA005760B1

    公开(公告)日：2005-06-30

    申请号：EA200300049

    申请日：2001-06-13

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： VAN EMELEN KRISTOF ,  DE BRUYN MARCEL FRANS LEOPOLD ,  ALCAZAR-VACA MANUEL JESIS ,  ANDRES-GIL JOSE IGNACIO ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  MATESANZ-BALLESTEROS MARIA ENC ,  BARTOLOME-NEBREDA JOSE MANUEL

    IPC: C07D491/056 ,  A61K31/435 ,  A61K31/436 ,  A61K31/4545 ,  A61K31/513 ,  A61K31/5383 ,  A61P1/00 ,  A61P1/14 ,  C07D411/04 ,  C07D491/04 ,  C07D491/052 ,  C07D491/06 ,  C07D497/04 ,  C07D498/04

    Abstract: Настоящееизобретениекасаетсясоединенийформулы (I), ихстереохимическиизомерныхформ, N-оксидныхформ, фармацевтическиприемлемыхаддитивныхсолейкислот, где -a=a-a=a- представляетбивалентныйрадикалформулы -N=CH-CH=CH- (a-1), -CH=N-CH=CH- (a-2), -CH=CH-N=CH- (a-3), -CH=CH-CH=N- (a-4), -N=CH-N=CH- (a-6), -Z-Z- представляетбивалентныйрадикалформулы -Y-CH(R)-CH- (b-1), Y-CH(R)-O- (b-2), -Y-CH(R)-CH-O- (b-3), -Y-CH(R)-CH-S- (b-4), -Y-CH(R)-CH-NH (b-5) или -Y-CH(R)-CH-CH- (b-6), где, есливозможно, необязательноодинилидваатомаводороданаодномилиразныхатомахуглеродаилиазотамогутбытьзамещены Cалкилом; Yпредставляеткислородилисеру; Alkпредставляет Cалкандиил; R, Rи R, каждыйнезависимо, выбранизводорода, Cалкилаилигалогена; Rпредставляетводород; -A- представляетбивалентныйрадикалформулы (c-1) или (c-2), где m равно 0 или 1; Alkпредставляет Cалкил, необязательнозамещенныйоднимилиболеегидрокси; Rпредставляетводород, гидрокси, гидрокси-Cалкил, Cалкилокси, Cалкилоксикарбонилилигидроксикарбонил; Rпредставляетрадикалформулы (d-1), где X представляеткислород; Rпредставляетводород, Cалкил, Cциклоалкил, фенилилифенилметил; и Q представляетбивалентныйрадикалформулы -CH-CH- (e-1), -CH-CH-CH- (e-2), -CH-CO- (e-5), -(CH)-CO- (e-7), гденеобязательноодинилидваатомаводороданаодномилиразныхатомахуглеродамогутбытьзаменены Cалкилом, гидроксиилифенилом. Раскрытыспособыполученияуказанныхпродуктов, фармацевтическиекомпозиции, содержащиеуказанныепродукты, иихприменениев качествелекарственныхсредств, вчастности, длялечениясостояний, которыеотносятсяк нарушеннойфундальнойаккомодации.

    125.
    发明专利
    未知

    公开(公告)号：BR0308309A

    公开(公告)日：2004-12-28

    申请号：BR0308309

    申请日：2003-03-27

    Applicant: JANSSEN PHARMACEUTICA NV

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

    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.

    Indole derivatives with an improved antipsychotic activity
    126.
    发明专利
    Indole derivatives with an improved antipsychotic activity 未知

    公开(公告)号：AU2004242802A1

    公开(公告)日：2004-12-09

    申请号：AU2004242802

    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 ,  C07D491/04

    Abstract: The present invention relates to a novel indol derivative according to Formula (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 R 1, R 2 , R 3 , R 4 , R 5 , p, a 1 -a 2 a 3 -a 4 , Z 1 -Z 2 , X and Y are defined as in claim 1 . Said derivative exhibit a binding affinity towards dopamine receptors, in particular towards dopamine D 2 , D 3 and D 4 receptors, with selective serotonin reuptake inhibition properties and acting as 5-HT 1A agonists or partial agonists. The invention also relates to pharmaceutical compositions comprising the compounds according 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 their production.

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