The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Dec. 09, 2008
Filed:
Aug. 19, 2003
José Ignacio Andrés-gil, Madrid, ES;
Manuel Jesús Alcázar-vaca, Toledo, ES;
Maria Encarnacion Matesanz-ballesteros, Toledo, ES;
Margaretha Henrica Maria Bakker, Alsbach-Haehnlein, DE;
Antonius Adrianus Hendrikus Petrus Megens, Beerse, BE;
José Ignacio Andrés-Gil, Madrid, ES;
Manuel Jesús Alcázar-Vaca, Toledo, ES;
Maria Encarnacion Matesanz-Ballesteros, Toledo, ES;
Margaretha Henrica Maria Bakker, Alsbach-Haehnlein, DE;
Antonius Adrianus Hendrikus Petrus Megens, Beerse, BE;
Janssen Pharmaceutica N.V., Beerse, BE;
Abstract
The invention concerns substituted tricyclic isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisoxazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on at least one of the C6- and C9-positions of the phenylpart of the tricyclic moiety with a selected radical, according to Formula (I) wherein X=CH, N—R, S or O, R, R, Rand Rare certain specific substituents, with the proviso that at least one of Rand Ris not hydrogen, Pir is preferably an optionally substituted piperidinyl or piperazinyl radical and Rrepresents 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, anxiety, movement disorders, psychosis, Parkinson's disease and body weight disorders. The compounds according to the invention have surprisingly been shown to have a serotonine (5-HT) reuptake inhibitor activity in combination with additional α-adrenoceptor antagonist activity and show a strong anti-depressant activity without being sedative. The invention also relates to novel combination of isoxazoline derivatives according to the invention with one or more other compounds selected from the group of antidepressants, anxiolytics, anti-psychotics and anti-Parkinson's disease drugs to improve efficacy and/or onset of action.