| abstract |
The present invention relates to a compound of formula (I) or a pharmaceutically active salt thereof comprising all stereoisomeric forms of the compounds of formula (I), individual diastereomers or enantiomers, or racemic and non-racemic mixtures thereof: [Formula I] Where Ar is aryl or 5- or 6-membered heteroaryl; Is a 6 to 9 membered mono or bi-heterocyclic group, wherein X is an additional hetero atom selected from the group consisting of carbon atoms, SO 2 , or N or O; If X is a carbon atom, O, SO 2 or unsubstituted N, R 1 is hydrogen, hydroxy, cyano,-(CH 2 ) q -OH,-(CH 2 ) q -NRR '-(CH 2 ) q -CN, lower alkyl, -S (O) 2 -lower alkyl, -NR-S (O) 2 -lower alkyl, -C (O) -lower alkyl, -NR-C (O) -lower alkyl, phenyl Or a heterocyclic group selected from piperidinyl-2-one; If X is an N-atom substituted by R 1 , then R 1 is hydrogen, — (CH 2 ) q —OH, — (CH 2 ) q —NRR ′, — (CH 2 ) q—CN, lower alkyl, — S (O) 2 -lower alkyl, aryl, 5- or 6-membered heteroaryl or -C (O) -lower alkyl, provided q is 2 or 3; R / R 'are independently of each other hydrogen or lower alkyl; R 2 is hydrogen, halogen, lower alkyl, cyano, lower alkoxy substituted with halogen, lower alkyl substituted with halogen, or 5- or 6-membered heteroaryl; R 3 is hydrogen or halogen; R 4 is hydrogen or lower alkyl; n is 1 or 2; when n is 2, R 1 may be the same or different; o is 1 or 2; when o is 2, R 2 may be the same or different; p is 1 or 2; when p is 2, R 3 may be the same or different; q is 1, 2 or 3; s is 0, 1, 2, 3 or 4. The compounds of the present invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety or attention deficit hyperactivity disorder (ADHD). |