derivados de alquil-piperazinil-benzoxazolona e alquil-piperidinil-benzoxazolona, e método para preparar os mesmos

• Main Authors: GUSTAAF J. M. SCHARRENBURG, ANNE G. TOOROP, JOHANNES A, STEPHEN K. LONG, GERBEN M. VISSER, CORNELIS G. KRUSE, JOHANNES MOS, M. VAN DER HEIJDEN, GERRIT P. TOOROP, ROELOF W. FEENSTRA
• Format: Patent
• Language: Portuguese
• Published: 01.11.2011
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The invention relates to a group of novel piperazine and piperidine derivatives of formula (I), wherein: S1 is hydrogen, halogen, alkyl (1-3C), CN, CF3, OCF3, SCF3, alkoxy (1-3C), amino or mono- or dialkyl (1-3C) substituted amino, or hydroxy; X represents NR3, S, CH2, O, SO or SO2, wherein R3 is H or alkyl (1-3C); . . . Z represents =C or -N; -R1 independently represent H or alkyl (1-3C), or R1 and R2 together can form a bridge 2 or 3 C-atoms; R4 is hydrogen or alkyl (1-3C); Q is methyl, ethyl, ethyl substituted with one or more fluorine atoms, cyclopropyl-methyl, optionally substituted with one or more fluorine atoms, and salts and prodrugs thereof. It has been found that these compounds have both partial dopamine D2-receptor agonism and partial serotonin 5-HT1A-receptor agonism mediated activities.