BENZOXAZINE COMPOUNDS FOR ENHANCING SYNAPTIC RESPONSE Russian patent published in 2005 - IPC

FIELD: organic chemistry, medicine.

SUBSTANCE: invention relates to new biologically active benzoxazine compounds and describes derivatives of benzoxazine of the following structure: wherein X¹ and X² are taken independently among hydrogen atom (H), -OR⁴, -CH₂OR⁴; or X¹ and X² taken in common represent -O-CR52

O- or -O-CR52CR52O-, or -O-CR52=CR52O-; Z represents oxygen atom (O) or sulfur atom (S); each R¹ represents independently hydrogen atom (H) or (C₁-C₆)-alkyl; each R² represents independently hydrogen atom (H) or (C₁-C₆)-alkyl, (C₁-C₃)-fluoroalkyl; each R⁴ represents independently hydrogen atom (H) or (C₁-C₆)-alkyl; each R⁵ represents hydrogen atom (H) or (C₁-C₆)-alkyl; n = 2, 3 or 4. Also, invention describes a method for preparing compound by cl. 1 with enantiomeric excess above 80% and relates to pharmaceutical composition for enhancing the synaptic response mediated by AMPA-receptors based on compounds by cl. 1. Pharmaceutical composition is useful for treatment of schizophrenia, schizophrenia-like behavior or depression in humans in necessary for carrying out such treatment based on compounds by cl. 1 wherein this pharmaceutical composition is useful for the memory improvement and comprising compound by cl. 1. Invention provides preparing new compounds eliciting useful biological properties.

EFFECT: valuable medicinal properties of compounds.

107 cl, 2 dwg, 2 tbl, 10 ex