Alicyclic[c] benzopyrone derivatives and uses thereof

摘要

Disclosed are alicyclic[c]benzopyrone derivatives and use thereof. The alicyclic[c]benzopyrone derivatives are compounds represented by formula I or their salts. The present compounds not only significantly improve high activity induced by MK-801, but also effectively improve clambering symptom induced by Apomorphine and do not cause EPS within effective dose. These in vitro targets and in vivo pharmacological models are closely related to diseases of the nervous system caused by dopamine dysfunction, especially schizophrenia. Therefore the present compounds can be used for the treatment of central nervous system diseases, especially schizophrenia. ED50 is lower and effect is stronger in two animal models i.e. high activity induced by MK-801 and clambering symptom induced by Apomorphine, while ED50 is higher and therapeutic index is greater in animal models of catalepsy.;

主权项

1. A compound of formula I or a salt thereof:Wherein:
n1 is 1, 2 or 3; n2 is 3, 4 or 5; X is CH or N; Ar has formula II or formula III:Wherein:
Q is O or S; and R1, R2, R3, R4 and R5 are each independently H, halogen, unsubstituted C1-C5 alkyl, C1-C5 alkyl substituted by halogen, unsubstituted C1-C5 alkoxy, or C1-C5 alkoxy substituted by halogen.