Isoxazoline derivatives as anti-depressants

摘要

A compound or a process preparing a compound according to the general Formula(I), the pharmaceutically acceptable acid or base addition salts of this formula, the stereochemically isomeric forms of this formula and the N-oxide form. Where; X is CH2,N-R7, S or O ; R7 is selected from the group of hydrogen, alkyl, phenyl, phenylalkyl, alkylcarbonyl, alkyloxycarbonyl and mono-and dialkylaminocarbonyl, the phenyl and alkyl groups being optionally substituted with one or more halo atoms; Rl and R2 are each, independently from each other, selected from the group of hydrogen, hydroxy, cyano, halo,OS02H, OS02CH3, phenyl, phenylalkyl, alkyloxy, alkyloxyalkyloxy, alkyloxyalkyloxyalkyloxy, tetrahydrofuranyloxy, alkylcarbonyloxy, alkylthio, alkyloxyalkylcarbonyloxy, pyridinylcarbonyloxy, alkylcarbonyloxyalkyloxy, alkyloxycarbonyloxy, alkenyloxy, alkenyl carbonyloxy and mono-and dialkylaminoalkyloxy, the alkyl and aryl radicals being optionally substituted with one or more hydroxy or halo atoms or amino groups; or Rl and R2 may be taken together to form a bivalent radical-R'-R2-selected from the group of-CH2-CH2-O-,-O-CH2-CH2-,-O-CH2-O-,-CH2-O-CH2-and -O-CH2-CH2-O-; a and b are asymmetric centers ;(CH2) m is a straight hydrocarbon chain of m carbon atoms, m being an integer ranging from 1 to 4; Pir is an optionally substituted radical where; Each R8 is independently from each other, selected from the group of hydrogen, hydroxy, amino, nitro, cyano, halo and alkyl ; n is an integer ranging from 1 to 5; R9 is selected from the group of hydrogen, alkyl and formyl ; and R3 represents an optionally substituted aromatic homocyclic or heterocyclic ring system together with an optionally substituted and partially or completely hydrogenated hydrocarbon chain of 1 to 6 atoms long with which said ring system is attached to the Pir radical and of which may contain one or more heteroatoms selected from the group of O, N and S. This compound can be used as a medicament to treat depression, anxiety and body weight disorders when a therapeutic amount of this compound is used with a pharmaceutically acceptable carrier.