The title compds. I [R1-R3 = H, Me, OH, OMe, halo, CF3, CN or CO2H] having medical utility, in particular as modulators of dopamine and serotonin receptors, preferably the D3, 5HT1A and 5-HT2A receptor subtypes, and in particular useful for the treatment of neuropsychiatric disorders, including schizophrenia, were prepd. E.g., a multi-step synthesis of I [R1-R3 = H], starting from 6-methylquinoline, was given. The affinity of compds. I for the dopamine and serotonin receptor subtypes was detd. using std. receptor binding assays. Thus, compds. I were found to be selective for dopamine D3 and having a Ki in the subnanomolar range (no specific data given). Pharmaceutical compn. comprising the compd. I is claimed.
Preparation of aryl piperazine derivatives useful for the treatment of neuropsychiatric disorders / Campiani, Giuseppe; Butini, Stefania; Fattorusso, Caterina; Franceschini, Silvia; Thale, Zia Irene; Nielsen, Karin Sandager; Scheel Krueger, Joergen; Madsen, Lars S. i. i. m.. - (2008).
Preparation of aryl piperazine derivatives useful for the treatment of neuropsychiatric disorders
FATTORUSSO, CATERINA;
2008
Abstract
The title compds. I [R1-R3 = H, Me, OH, OMe, halo, CF3, CN or CO2H] having medical utility, in particular as modulators of dopamine and serotonin receptors, preferably the D3, 5HT1A and 5-HT2A receptor subtypes, and in particular useful for the treatment of neuropsychiatric disorders, including schizophrenia, were prepd. E.g., a multi-step synthesis of I [R1-R3 = H], starting from 6-methylquinoline, was given. The affinity of compds. I for the dopamine and serotonin receptor subtypes was detd. using std. receptor binding assays. Thus, compds. I were found to be selective for dopamine D3 and having a Ki in the subnanomolar range (no specific data given). Pharmaceutical compn. comprising the compd. I is claimed.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
