The present invention provides compounds that block calcium channels and have the Formula I: ##STR1##and pharmaceutically acceptable salts, esters, and pro-drugs thereof, whereinR.sup.1 and R.sup.2 are independently H, phenylcyclopentylcarbonyl, C.sub.1 -C.sub.7 alkyl, cyclohexylmethyl, benzyl, C.sub.1 -C.sub.5 alkylbenzyl, or C.sub.1 -C.sub.5 alkoxybenzyl,A is --C(O)-- or --CH.sub.2 --;R.sup.3 is H or --CH.sub.3 ;R.sup.4 is C.sub.1 -C.sub.4 alkyl or piperidin-1-ylethyl;R.sup.5 is phenyl-(CH.sub.2).sub.n --, C.sub.1 -C.sub.4 alkylphenyl-(CH.sub.2).sub.n --, or halophenyl-(CH.sub.2).sub.n --; andn is 1 or 2.The present invention also provides pharmaceutical compositions containing the compounds of Formula I and methods of using them to treat stroke, cerebral ischemia, head trauma, and epilepsy.

Warner-Lambert Company

Tyrosine-derived compounds as calcium channel antagonists

The present invention provides compounds that block calcium channels and have the Formula I: ##STR1##and pharmaceutically acceptable salts, esters, and pro-drugs thereof, whereinR.sup.1 and R.sup.2 are independently H, phenylcyclopentylcarbonyl, C.sub.1 -C.sub.7 alkyl, cyclohexylmethyl, benzyl, C.sub.1 -C.sub.5 alkylbenzyl, or C.sub.1 -C.sub.5 alkoxybenzyl,A is --C(O)-- or --CH.sub.2 --;R.sup.3 is H or --CH.sub.3 ;R.sup.4 is C.sub.1 -C.sub.4 alkyl or piperidin-1-ylethyl;R.sup.5 is phenyl-(CH.sub.2).sub.n --, C.sub.1 -C.sub.4 alkylphenyl-(CH.sub.2).sub.n --, or halophenyl-(CH.sub.2).sub.n --; and n is 1 or 2.The present invention also provides pharmaceutical compositions containing the compounds of Formula I and methods of using them to treat stroke, cerebral ischemia, head trauma, and epilepsy.

epilepsy/tyrosine

Tyrosine-derived compounds as calcium channel antagonists

Tyrosine-derived compounds as calcium channel antagonists

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