| abstract |
"ISOXAZOLINE DERIVATIVES AS ANTIDEPRESSANTS". The invention relates to substituted isoxazoline derivatives according to Formula (1): wherein X = CH ~ 2 ~, NR ~ 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 fully hydrogenated hydrocarbon chain of up to 6 atoms with which the ring system is attached to the radical Pir 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 drug, in particular for the treatment of depression and / or anxiety and body weight disorders. The compounds according to the invention have surprisingly been shown to have a serotonin uptake inhibitory activity (5-HT) in combination with the additional α2 -adrenoceptor antagonistic activity and show strong non-sedative antidepressant activity. The compounds according to the invention are also suitable for treating patients with anxiety disorders and body weight disorders. The invention also relates to the novel combination of substituted isoxazoline derivatives having antidepressant activity and / or anxiolytic activity and / or body weight control activity with antidepressants, anxiolytics and / or antipsychotics to improve efficacy and / or principle of action. |