Gabaergic receptor subtype selective ligands and their uses

摘要

Described herein are α3 or α2 or α2/α3 GABAergic receptor subtype selective ligands, pharmaceutical compositions, and methods of use of such ligands and compositions in treatment of anxiety disorders, epilepsy and schizophrenia with reduced sedative and ataxic side effects. In embodiments, such as α3 or α2 or α2/α3 GABAergic receptor subtype selective ligands lack ester linkages and may be thus relatively insensitive to hydrolysis by esterases.

主权项

1. A compound of formula (I): or a salt thereof, wherein: R is —H or —Si(Me)3; X is CH, CF, CCl or N; and R′ is selected from the group consisting of —CHF2, —CH2CF2CH3, —CF2CHF2,CF2CF2CH3, —CH2OCH3, —CF2CH2OCH3, —CF2OCH2CH3, —CH2OCH2CH3, —CH2OH, —CH2SCH3, —CF2CH2CH3, —CH2OCH2OCH3, —COCH2CH3, —C(CF2)OCH2CH3, —CH(CF3)OCH2CH3, —CH(CF3)NHCH2CH3,—CHO and —CH2CF2CH3, or
R′ is selected from the group consisting of: wherein each R1 is independently selected from the group consisting of —CH3, —CH2CH3 and —CH(CH3)2.