公开(公告)号：NO20084819A

公开(公告)日：2008-11-17

申请号：NO20084819

申请日：2008-11-17

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ANDRES-GIL JOSE IGNACIO ,  ALCAZAR-VACA MANUEL JESUS ,  PASTOR-FERNANDEZ JOAQUIN ,  DRINKENBURG WILHELMUS HELENA I ,  VEGA-RAMIRO JUAN ANTONIO ,  SANTAMARINA JULEN OYARZABAL ,  MORENA MARIA LOURDES LINARES DE LA ,  GONZALEZ SONIA MARTINEZ ,  DELGADO-JIMENEZ FRANCISCA

IPC: C07D401/12 ,  A61K31/497 ,  A61P25/00

CPC classification number: C07D401/12 ,  C07D239/47 ,  C07D401/14 ,  C07D403/06 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14

公开(公告)号：MX2007007472A

公开(公告)日：2007-07-20

申请号：MX2007007472

申请日：2005-12-20

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ANDRES-GIL JOSE IGNACIO ,  ALCAZAR-VACA MANUEL JESUS ,  PASTOR-FERNANDEZ JOAQUIN ,  OYARZABAL-SANTAMARINA JULEN ,  VEGA-RAMIRO JUAN ANTONIO ,  DRINKENBURG WILHELMUS HELENA IGNATIUS MARIA ,  LANGLOIS XAVIER JEAN MICHEL

IPC: A61K31/4166 ,  A61P25/00 ,  C07D233/70 ,  C07D249/12 ,  C07D257/04 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D405/14

Abstract: La presente invencion concierne a derivados sustituido de triazolona, tetrazolona e imidazolona de acuerdo con la Formula general (I): (ver formula) una sal de adicion de acido o de base farmaceuticamente aceptable del mismo, una forma estereoquimicamente isomerica del mismo, una forma N-oxido del mismo o una sal de amonio cuaternario del mismo, donde las variables se definen en la reivindicacion 1, que tienen actividad antagonista selectiva del (2C-adrenorreceptor; tambien se refiere a su preparacion, a composiciones que los comprenden y a su uso como medicamento; los compuestos de acuerdo con la invencion son utiles para la prevencion y/o el tratamiento de desordenes del sistema nervioso central, desordenes del humor, desordenes de ansiedad, desordenes relacionados con el estres asociados con depresion y/o ansiedad, desordenes cognitivos, desordenes de la personalidad, desordenes esquizoafectivos, enfermedad de Parkinson, demencia de tipo Alzheimer, condiciones de dolor cronico, enfermedades neurodegenerativas, desordenes de adicion, desordenes del humor y disfuncion sexual.

公开(公告)号：NO20073760A

公开(公告)日：2007-07-19

申请号：NO20073760

申请日：2007-07-19

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： LANGLOIS XAVIER JEAN MICHEL ,  ANDRES-GIL JOSE IGNACIO ,  ALCAZAR-VACA MANUEL JESUS ,  PASTOR-FERNANDEZ JOAQUIN ,  DRINKENBURG WILHELMUS HELENA I ,  OYARZABAL-SANTAMARINA JULEN ,  VEGA-RAMIRO JUAN ANTONIO

IPC: C07D249/12 ,  A61K31/41 ,  A61K31/4166 ,  A61K31/4196 ,  A61P25/00 ,  C07D233/70 ,  C07D257/04 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D405/14

CPC classification number: C07D257/04 ,  C07D233/70 ,  C07D249/12 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D405/14

公开(公告)号：HU0303270A2

公开(公告)日：2004-01-28

申请号：HU0303270

申请日：2002-02-13

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ALCAZAR-VACA MANUEL JESUS ,  ANDRES-GIL JOSE IGNACIO ,  BAKKER MARGARETHA HENRICA MARI ,  CID-NUNEZ JOSE MARIA ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  HEYLEN GODELIEVE IRMA CHRISTIN ,  LANGLOIS XAVIER JEAN MICHEL ,  MEGENS ANTONIUS ADRIANUS HENDR ,  PASTOR-FERNANDEZ JOAQUIN ,  STECKLER THOMAS HORST WOLFGANG

IPC: A61K31/454 ,  A61K31/495 ,  A61K31/496 ,  A61K31/538 ,  A61P3/04 ,  A61P25/00 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  C07D261/20 ,  C07D498/04 ,  C07D498/14 ,  C07D519/00

Abstract: The invention concerns substituted isoxazolines derivatives according to Formula (I): wherein X=CH?2#191, N-R 7 , S or O, R 1 , R 2 and R 3 are certain specific substituents, Pir is an optionally substituted piperidyl or piperazyl radical and R3 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 serotonine (5-HT) reuptake inhibitor activity in combination with additional alpha2-adrenoceptor antagonist activity and show a strong anti-depressant activity without being sedative. Compounds according to the invention arc also suitable for treating patients with anxiety disorders and disorders of body weight. The invention also relates to novel combination of substituted isoxazolines derivatives having anti-depressant activity and/or anxiolytic activity and/or body weight control activity with antidepressants, anxiolytics and/or antipsychotics to improve efficacy and/or onset of action

公开(公告)号：NO20033700L

公开(公告)日：2003-10-21

申请号：NO20033700

申请日：2003-08-20

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： MEGENS ANTONIUS ADRIANUS HENDRIKUS PETRUS ,  ALCAZAR-VACA MANUEL JESUS ,  ANDRES-GIL JOSE IGNACIO ,  CID-NUNEZ JOSE MARIA ,  PASTOR-FERNANDEZ JOAQUIN ,  HEYLEN GODELIEVE IRMA CHRISTINE ,  LANGLOIS XAVIER JEAN MICHEL ,  BAKKER MARGARETHA HENRICA MARIA ,  STECKLER THOMAS HORST WOLFGANG ,  FERNANDEZ-GADEA FRANCISCO JAVIER

IPC: C07D498/04 ,  A61K31/454 ,  A61K31/495 ,  A61K31/496 ,  A61K31/538 ,  A61P3/04 ,  A61P25/00 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  C07D261/20 ,  C07D498/14 ,  C07D519/00 ,  A61K31/423 ,  A61K31/424

Abstract: The invention concerns substituted isoxazolines derivatives according to Formula (I): wherein X=CH?2#191, N-R 7 , S or O, R 1 , R 2 and R 3 are certain specific substituents, Pir is an optionally substituted piperidyl or piperazyl radical and R3 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 serotonine (5-HT) reuptake inhibitor activity in combination with additional alpha2-adrenoceptor antagonist activity and show a strong anti-depressant activity without being sedative. Compounds according to the invention arc also suitable for treating patients with anxiety disorders and disorders of body weight. The invention also relates to novel combination of substituted isoxazolines derivatives having anti-depressant activity and/or anxiolytic activity and/or body weight control activity with antidepressants, anxiolytics and/or antipsychotics to improve efficacy and/or onset of action

公开(公告)号：NO20033700D0

公开(公告)日：2003-08-20

申请号：NO20033700

申请日：2003-08-20

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ANDRES-GIL JOSE IGNACIO ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  ALCAZAR-VACA MANUEL JESUS ,  CID-NUNEZ JOSE MARIA ,  PASTOR-FERNANDEZ JOAQUIN ,  MEGENS ANTONIUS ADRIANUS HENDR ,  HEYLEN GODELIEVE IRMA CHRISTIN ,  LANGLOIS XAVIER JEAN MICHEL ,  BAKKER MARGARETHA HENRICA MARI ,  STECKLER THOMAS HORST WOLFGANG

IPC: A61K31/454 ,  A61K31/495 ,  A61K31/496 ,  A61K31/538 ,  A61P3/04 ,  A61P25/00 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  C07D261/20 ,  C07D498/04 ,  C07D498/14 ,  C07D519/00 ,  C07D

Abstract: The invention concerns substituted isoxazolines derivatives according to Formula (I): wherein X=CH?2#191, N-R 7 , S or O, R 1 , R 2 and R 3 are certain specific substituents, Pir is an optionally substituted piperidyl or piperazyl radical and R3 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 serotonine (5-HT) reuptake inhibitor activity in combination with additional alpha2-adrenoceptor antagonist activity and show a strong anti-depressant activity without being sedative. Compounds according to the invention arc also suitable for treating patients with anxiety disorders and disorders of body weight. The invention also relates to novel combination of substituted isoxazolines derivatives having anti-depressant activity and/or anxiolytic activity and/or body weight control activity with antidepressants, anxiolytics and/or antipsychotics to improve efficacy and/or onset of action

公开(公告)号：EA022012B1

公开(公告)日：2015-10-30

申请号：EA201290878

申请日：2011-03-08

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： BARTOLOME-NEBREDA JOSE MANUEL ,  CONDE-CEIDE SUSANA ,  MACDONALD GREGOR JAMES ,  PASTOR-FERNANDEZ JOAQUIN ,  VAN GOOL MICHIEL LUC MARIA ,  MARTIN-MARTIN MARIA LUZ ,  VANHOOF GRETA CONSTANTIA PETER

IPC: C07D487/04 ,  A61K31/4985 ,  A61P3/00 ,  A61P25/00

Abstract: Изобретениеотноситсяк новымпроизводнымимидазо[1,2-а]пиразинаформулы (I), которыеявляютсяингибиторамиферментафосфодиэстераза 10 (PDE10) иприменимыдлялеченияилипрофилактикиневрологических, психиатрическихи метаболическихрасстройств, вкоторыевовлеченфермент PDE10. Крометого, изобретениенаправленонафармацевтическиекомпозиции, включающиеуказанныесоединения, наспособыполученияуказанныхсоединенийи композиций, наприменениетакихсоединенийилифармацевтическихкомпозицийдляпрофилактикиилилеченияневрологических, психиатрическихи метаболическихрасстройстви заболеваний.

公开(公告)号：EA020847B1

公开(公告)日：2015-02-27

申请号：EA201290244

申请日：2010-10-27

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： PASTOR-FERNANDEZ JOAQUIN ,  BARTOLOME-NEBREDA JOSE MANUEL ,  MACDONALD GREGOR JAMES ,  CONDE-CEIDE SUSANA ,  DELGADO-GONZALEZ OSCAR ,  VANHOOF GRETA CONSTANTIA PETER ,  VAN GOOL MICHIEL LUC MARIA ,  MARTIN-MARTIN MARIA LUZ ,  ALONSO-DE DIEGO SERGIO-ALVAR ,  SWINNEY KELLY ANN ,  LEYS CARINA ,  WEERTS JOHAN ERWIN EDMOND

IPC: C07D487/04 ,  A61K31/5025 ,  A61P3/00 ,  A61P25/00

Abstract: Изобретениеотноситсяк новымпроизводнымимидазо[1,2-b]пиридазинаформулы (I), которыеявляютсяингибиторамиферментафосфодиэстеразы 10 (PDE10) икоторыеявляютсяполезнымидлялеченияилипредупрежденияневрологических, психиатрическихи метаболическихрасстройств, вкоторыевовлеченфермент PDE10. Изобретениетакженаправленонафармацевтическиекомпозиции, содержащиетакиесоединения, наспособыполучениятакихсоединенийи композиций, наприменениетакихсоединенийилифармацевтическихкомпозицийприпредупрежденииилилеченииневрологических, психиатрическихи метаболическихрасстройстви заболеваний.

公开(公告)号：EA020010B1

公开(公告)日：2014-07-30

申请号：EA201290534

申请日：2010-12-16

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： MACDONALD GREGOR JAMES ,  TRESADERN GARY JOHN ,  TRABANCO-SUAREZ ANDRES AVELINO ,  PASTOR-FERNANDEZ JOAQUIN

IPC: C07D513/04 ,  A61K31/428 ,  A61K31/429 ,  A61P25/18

Abstract: Настоящееизобретениеотноситсяк новымбициклическимтиазоламформулы (I)которыепредставляютсобойположительныеаллостерическиемодуляторыметаботропногоглутаматногорецептораподтипа 5 (mGluR5) икоторыеявляютсяпригоднымидлялеченияилипредотвращениязаболеваний, связанныхс дисфункциейглутамата, изаболеваний, вкоторыхучаствует mGluR5 подтипрецептора. Настоящееизобретениетакжеотноситсяк фармацевтическимкомпозициям, содержащимданныесоединения, кспособамполученияданныхсоединенийи композицийи кприменениюданныхсоединенийи композицийдляпредотвращенияи лечениязаболеваний, вкоторыхучаствует mGluR5.

公开(公告)号：AU2010332811B2

公开(公告)日：2014-07-24

申请号：AU2010332811

申请日：2010-12-16

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： MACDONALD GREGOR JAMES ,  TRABANCO-SUAREZ ANDRES AVELINO ,  CONDE-CEIDE SUSANA ,  TRESADERN GARY JOHN ,  BARTOLOME-NEBREDA JOSE MANUEL ,  PASTOR-FERNANDEZ JOAQUIN

IPC: C07D513/04 ,  A61K31/428 ,  A61K31/429 ,  A61P25/18

Abstract: The present invention relates to novel bicyclic thiazoles of formula (I) which are positive allosteric modulators of the metabotropic glutamate receptor subtype 5 ("mGluR5") and which are useful for the treatment or prevention of disorders associated with glutamate dysfunction and diseases in which the mGluR5 subtype of receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which mGluR5 is involved.