o-Phosphono(alkyl)-N-sulfonyl-phenyl-alanine derivatives useful as intermediates for preparation of phosphono-hydroisoquinolines
AssigneeG. D. Searle & Co.
InventorsAlexis A. Cordi, Michael L. Vazquez
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AssigneeG. D. Searle & Co.
InventorsAlexis A. Cordi, Michael L. Vazquez
Estimating the term…
A class of phosphono-hydroisoquinoline 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 phosphono-hydroisoquinoline 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. Compounds of most interest are those of Formula I: ##STR1## wherein each of R.sup.1 through R.sup.4 is hydrido, wherein each of Z.sup.1 and Z.sup.2 is hydroxyl, wherein W is a single bond connecting the phosphorus atom with the aromatic ring and wherein the A ring is aromatic. Also disclosed are two classes of intermediate compounds having a fully unsaturated A ring, which intermediate compounds are useful in methods to make product compounds of Formula I.
A compound of the formula ##STR33## wherein each of R.sup.1 through R.sup.3 is independently selected from hydrido, alkyl, haloalkyl, halo, cyano, nitro and groups represented by --OR.sup.5, --SR.sup.5, ##STR34## wherein each R.sup.5 is independently selected from hydrido, alkyl, aryl and aralkyl;
Dependencies are inferred from the claim text.