Bridged tricyclic analogs of 2-(carboxycyclopropyl)glycine as inhibitors of glutamate transport

   
   

This invention provides compounds of the formula: ##STR1## wherein X is (CH.sub.2).sub.n, O, S, SO, SO.sub.2 or CR.sup.1 R.sup.2 ; n is 1 or 2; R.sup.1 and R.sup.2 are H, halogen, hydroxy, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, or R.sup.1 and R.sup.2, taken together form cycloalkyl of 3 to 6 carbon atoms, an alkylidene of up to 6 carbon atoms or a carbonyl; R.sup.3, R.sup.4 and R.sup.5 are H or alkyl of 1 to 6 carbon atoms; Z is H, alkyl of 1 to 6 carbon atoms, alkanoyl of 1 to 6 carbon atoms or alkoxycarbonyl of 2 to 7 carbon atoms; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods for their use in treating or preventing characterized by glutamate hypofunction, including schizophrenia, schizoaffective disorder and schizophreniform disorder, and for the treatment of cognitive deficits due to aging, stroke, Alzheimer's disease or other neurodegenerative diseases.

Esta invención proporciona los compuestos del fórmula: ## del ## STR1 en donde es X (CH.sub.2).sub.n, O, S, ASÍ PUES, SO.sub.2 o CR.sup.1 R.sup.2; n es 1 o 2; R.sup.1 y R.sup.2 son H, halógeno, hydroxy, alkyl de 1 a 6 átomos de carbón, alkoxy de 1 a 6 átomos de carbón, o R.sup.1 y R.sup.2, tomados juntos forman el cycloalkyl de 3 a 6 átomos de carbón, de un alkylidene de hasta 6 átomos de carbón o de un carbonyl; R.sup.3, R.sup.4 y R.sup.5 son H o alkyl de 1 a 6 átomos de carbón; Z es H, alkyl de 1 a 6 átomos de carbón, alkanoyl de 1 a 6 átomos de carbón o alkoxycarbonyl de 2 a 7 átomos de carbón; o una sal farmacéutico aceptable de eso, tan bien como las composiciones y los métodos farmacéuticos para su uso en tratar o la prevención caracterizada por el hypofunction del glutamato, incluyendo esquizofrenia, el desorden schizoaffective y el desorden del schizophreniform, y para el tratamiento del déficit cognoscitivo debido al envejecimiento, al movimiento, a la enfermedad de Alzheimer o a otras enfermedades neurodegenerative.

 
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