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US 5,843,997 AGranted
Excitatory amino acid receptor antagonists
AssigneeEli Lilly and Company
InventorsLawrence J. Heinz, William H.W. Lunn, Darryle Darwin Schoepp
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Abstract
The present invention provides novel compounds that affect excitatory amino acid receptors and are useful in the treatment of neurological disorders. This invention also provides synthetic methods for the preparation of the novel compounds.
Claims13
A compound of the formula ##STR21## wherein:
- Z is NR.sup.5, O, or S;
- W is CH.sub.(3-p), --(CH.sub.2).sub.q --, --(CH.sub.2).sub.q CH.sub.(3-p), --(CH.sub.2).sub.q CO--, --(CH.sub.2).sub.q O--, --(CH.sub.2).sub.q CH.dbd.CH(CH.sub.2).sub.q --, --(CH.sub.2).sub.q CH.dbd.CH--, --CH.dbd.CHCO--, --CH.dbd.CHCOR.sup.6, --(CH.sub.2).sub.q CHOHR.sup.6, --(CH.sub.2).sub.q CHOH--, --(CH.sub.2).sub.q COR.sup.6, --O(CH.sub.2).sub.q --, NR.sup.5, O, S, SO, or SO.sub.2 ;
- n is 0 or 1;
- m is 0 or 1;
- p is 0, 1, 2, or 3;
- q is 0-6;
- r is 1 or 2;
- s is 0 or 1, provided that the sum of n, m, p and s is at least 1, and that p is 1 if n is 1, s is 0 and m is 0 or if m is 1 and W is --(CH.sub.2).sub.q --, --(CH.sub.2).sub.q CO--, --(CH.sub.2).sub.q O--, --(CH.sub.2).sub.q CH.dbd.CH(CH.sub.2).sub.q --, --CH.sub.2).sub.q CH.dbd.CH--, --CH.dbd.CHCO--, --(CH.sub.2).sub.q CHOH--, --O(CH.sub.2).sub.q --, NR5, O, S, SO or SO.sub.2 ;
- R.sup.1 and R.sup.2 are independently aryl, substituted aryl, heterocycle, or substituted heterocycle;
- R.sup.3 is hydrogen or a carboxy protecting group;
- R.sup.4 is hydrogen or a carboxy protecting group;
- R.sup.5 is hydrogen, C.sub.1 -C.sub.10 alkyl, acyl, or
- CO.sub.2 (C.sub.1 -C.sub.4 alkyl);
- R.sup.6 is C.sub.1 -C.sub.10 alkyl;
- provided that when n is 0 and s is 1, then R.sup.1 is selected from the group consisting of tetrazolyl, triazolyl, pyridazinyl, pyrimidinyl, pteridinyl, 1,2,4-triazine-3,5-dionyl, pyrazolonyl, 7H-purinyl, xanthinyl, 3-ethyl-5-hydroxy-1,2,4-thiadiazolyl, 3-hydroxy-1,2,4-thiadiazolyl, rhodaninyl, hydantoinyl, and pseudothiohydantoinyl;
- further provided that when n is 1, m is 1, and W is NR.sup.5, O, S, SO, or SO.sub.2, then s is 1;
- and when n is 0 and s is 0, then m is 1 and W is --(CH.sub.2).sub.q CO--, --(CH.sub.2).sub.q O--, --CH.dbd.CHCO--, --CH.dbd.CHCOR.sup.6, --(CH.sub.2).sub.q CHOHR.sup.6, --(CH.sub.2).sub.q CHOH--, --(CH.sub.2).sub.q COR.sup.6, --O(CH.sub.2).sub.q --, NR.sup.5, O, S, SO, or SO.sub.2 ;
- or a pharmaceutically-acceptable salt thereof.
15 more elements
Dependencies are inferred from the claim text.