| abstract |
The present invention provides compounds, compositions and methods for inhibiting glycine transporter 2 and for affecting glycine transporter-mediated neuronal activity. Useful compounds have the formula (I): Embedded image Wherein n is 0, 1, 2 or 3 and R is independently halogen, hydroxy, lower alkyl optionally substituted with halogen or lower alkoxy optionally substituted with halogen; X is O, S or N-R ', wherein R' is lower alkyl, aryl, heteroaryl, aryl-lower alkylene or heteroaryl-lower alkylene; Q can be absent or present, and if present, has the formula (Q): Embedded image Wherein n, R and X are as defined above; when Q is present, W is lower alkylene; and when Q is absent, W is optionally substituted lower. alkyl, aryl which may be substituted, heteroaryl which may be substituted (aryl which may be substituted) -X-CH 2 - or (heteroaryl which may be substituted) -X-CH 2 - (wherein, X is as defined above), or a pharmaceutically acceptable salt thereof. These compounds are useful for treating neurological and muscular diseases such as psychosis, pain, epilepsy, neurodegenerative diseases, stroke, head trauma, multiple sclerosis, diseases associated with increased muscle contraction such as convulsions and muscle clonus Or it is particularly useful for treating muscular disorders such as conditions. In addition, the compounds of the invention are useful for finding other agents that show improved activity in assays in which the compounds of the invention are effective. |