公开(公告)号：HK1065537A1

公开(公告)日：2005-02-25

申请号：HK04108329

申请日：2004-10-25

Applicant: JANSSEN PHARMACEUTICA NV

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

IPC: A61K20090101 ,  A61K31/454 ,  A61K31/495 ,  A61K31/496 ,  A61K31/538 ,  A61P20090101 ,  A61P3/04 ,  A61P25/00 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  C07D20090101 ,  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