1-BENZOYL-PIPERAZINE DERIVATIVES AS GLYCINE UPTAKE INHIBITORS FOR THE TREATMENT OF PSYCHOSES.

摘要

The invention relates to compounds of formula (I) wherein Ar is substituted aryl or unsubstituted or substituted 6-membered heteroaryl, containing one, two or three nitrogen atoms, and wherein the aryl and the heteroaryl groups may be substituted by one or more substituents selected from the group consisting of hydroxy, halogen, CN, (C1 -C6)-alkyl, (C1-C6)-alkyl substituted by halogen, (C1-C6)-alkoxy, (C1-C6)-alkoxy substituted by halogen, NR7R8, C(O)R9 or SO2R10; R1 is hydrogen or (C1-C6)-alkyl; R2 is halogen, (C1-C6) -alkyl, (C2-C6) -alkenyl, wherein a hydrogen atom may be replaced by CN, C(O)-R9 or (C1-C6)-alkyl, or is (C2-C6) -alkynyl, (C1-C6)-alkyl substituted by halogen, -(CH2)n-(C3-C7)-cycloalkyl, -(CH2)n-heterocycloalkyl, -C(O)-R9, -(CH2)n-aryl or -(CH2)n-5 or -6 -membered heteroaryl containing one, two or three heteroatoms, selected from the group consisting of oxygen, sulphur or nitrogen wherein aryl, cycloalkyl, heterocycloalkyl and heteroaryl are unsubstituted or substituted by one or more substituents selected from the group consisting of hydroxy, halogen, (C1-C6)-alkyl, (C1-C6)-alkyl substituted by halogen or (C1-C6) alkoxy; R3, R4 and R6 independently from each other are hydrogen, hydroxy, halogen, (C1-C6)-alkyl or (C1-C6)-alkoxy; R5 is NO2, CN, C(O)R9, SO2R10 or NR11R12 ; R7 and R8 independently from each other are hydrogen or (C1-C6)-alkyl; the other substituents are defined in the claims; and to pharmaceutically acceptable acid addition salts thereof for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.