Phenyl glycines for use in reducing neurotoxic injury
AssigneeG. D. Searle & Co.
InventorsAlex A. Cordi, Michael L. Vazquez
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Abstract
A class of phenyl glycine compounds is described for treatment to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a phenyl glycine compound alone or in a composition in an amount effective as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites.
Claims42
A method to control neuropathological processes and the neurodegenerative consequences thereof in mammals, which method comprises treating a mammal susceptible to neurologic injury with an effective amount of a compound of the formula ##STR16## wherein each of R.sup.1 through R.sup.4 is independently selected from hydrido, alkyl, cycloalkyl, aralkyl, aryl, haloalkyl, halo, cyano, nitro, and groups represented by --OR.sup.5, --SR.sup.5, ##STR17## wherein each R.sup.5 is independently selected from hydrido, alkyl, aryl, and aralkyl;
- and wherein each of R.sup.6 and R.sup.7 is independently selected from hydrido, alkyl, acyl, aryl, aralkyl and ##STR18## and wherein Z is selected from --OR.sup.5, --SR.sup.5, ##STR19## and ##STR20## wherein each of R.sup.5, R.sup.6 and R.sup.7 defined as before;
- with the proviso that R.sup.6 and R.sup.7 are not at the same time carbonyl-containing groups;
- and wherein R.sup.8 is selected from hydrido and alkyl;
- or a pharmaceutically-acceptable salt thereof.
The method of claim 36 wherein each of the substituents R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are hydrido.
A compound of the formula ##STR21## wherein each of R.sup.1 through R.sup.4 is independently selected from hydrido, alkyl, cycloalkyl, aralkyl, aryl, haloalkyl, halo, cyano, nitro, and groups represented by --OR.sup.5, --SR.sup.5 ##STR22## wherein each R.sup.5 is independently selected from hydrido, alkyl, aryl, and aralkyl;
- and wherein each of R.sup.6 and R.sup.7 is independently selected from hydrido, alkyl, acyl, aryl, aralkyl and ##STR23## and wherein Z is selected from --OR.sup.5, --SR.sup.5, ##STR24## and ##STR25## wherein each of R.sup.5, R.sup.6 and R.sup.7 is defined as before;
- with the proviso that R.sup.6 and R.sup.7 are not at the same time carbonyl-containing groups;
- and wherein R.sup.8 is selected from hydrido and alkyl;
- or a pharmaceutically-acceptable salt thereof.
A pharmaceutical composition comprising a therapeutically-effective amount of a compound and a pharmaceutically-acceptable carrier or diluent, said compound selected from a family of compounds of the formula ##STR26## wherein each of R.sup.1 through R.sup.4 is independently selected from hydrido, alkyl, cycloalkyl, aralkyl, aryl, haloalkyl, halo, cyano, nitro, and groups represented by --OR.sup.5, --SR.sup.5, ##STR27## wherein each R.sup.5 is independently selected from hydrido, alkyl, aryl, and aralkyl;
- and wherein each of R.sup.6 and R.sup.7 is independently selected from hydrido, alkyl, acyl, aryl, aralkyl and ##STR28## and wherein Z is selected from --OR.sup.5, --SR.sup.5, ##STR29## and ##STR30## wherein each of R.sup.5, R.sup.6 and R.sup.7 is defined as before;
- with the proviso that R.sup.6 and R.sup.7 are not at the same time carbonyl-containing groups;
- and wherein R.sup.8 is selected from hydrido and alkyl;
- or a pharmaceutically-acceptable salt thereof.
Dependencies are inferred from the claim text.