New piperazine and piperidine compounds selectively binding...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 405/12 (2006.01) A61K 31/44 (2006.01) A61K 31/47 (2006.01) A61K 31/495 (2006.01) A61K 31/55 (2006.01) C07D 401/14 (2006.01) C07D 405/14 (2006.01) C07D 409/14 (2006.01) C07D 411/14 (2006.01) C07D 413/12 (2006.01) C07D 413/14 (2006.01)

Patent

CA 2247734

The invention relates to a group of new substituted pyridylmethylpiperazine and piperidine derivatives (a) selectively binding dopamine and serotonin receptors, their preparation and their use for treating central nervous system (CNS) disorders such as Parkinson's disease, aggression, anxiety disorders, autism, vertigo, depression, disturbances of cognition or memory and in particular schizophrenia and other psychotic disorders (see formula I) wherein - A represents a heterocyclic group of 5-7 ring atoms wherein 1- 3 heteroatoms from the group O, N and S are present, - R1 is hydrogen or fluoro, - R2 is C1-4-alkyl, C1-4-alkoxy or an oxo group, and p is 0, 1 or 2, - Z represents carbon or nitrogen, and the dotted line is a single bond when Z is nitrogen, and a single or double bond when Z is carbon, - R3 and R4 independently are hydrogen or C1-4-alkyl, - n has the value 1 or 2, - R5 is 2-pyridyl, 3-pyridyl or 4-pyridyl substituted at the meta-position with respect to the methylene bridge with a group Y, and optionally substituted with (R6)q, - Y is phenyl, furanyl or thienyl, which groups may be substituted with 1-3 substituents of the group hydroxy, halogen, CF3, C1-4-alkoxy, C1-4-alkyl, cyano, aminocarbonyl, mono- or di-C1-4-alkylaminocarbonyl, - R6 is halogen, hydroxy, C1-4-alkoxy or C1-4-alkyl, and q is 0, 1, 2 or 3 and salts thereof.

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