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US 5,670,516 AGranted
Excitatory amino acid receptor antagonists
AssigneeEli Lilly and Company
InventorsM. Brian Arnold, Nancy K. Augenstein, William H. W. Lunn, Paul L. Ornstein, Darryle D. Schoepp
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Abstract
This invention provides novel decahydroisoquinoline compounds which are useful as excitatory amino acid receptor antagonists and in the treatment of neurological disorders. This invention also provides synthetic methods for preparing decahydroisoquinolines, as well as, novel intermediates in the synthesis thereof.
Claims42
A compound of the formula ##STR87## wherein:
- R.sup.1 is hydrogen, C.sub.1 -C.sub.10 alkyl, arylalkyl, alkoxycarbonyl or acyl;
- R.sup.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, substituted alkyl, cycloalkyl, or arylalkyl;
- R.sup.3 is CO.sub.2 H, SO.sub.3 H, CONHSO.sub.2 R.sup.8, or a group of formula ##STR88## W is (CH.sub.2).sub.n, S, SO, SO.sub.2 ;
- Y is CHR.sup.7, NR.sup.4, O, S, SO, or SO.sub.2 ;
- Z is NR.sup.6, CHR.sup.7, or CH;
- or
- W and Y together are HC.dbd.CH or C.tbd.C, or Y and Z together are HC.dbd.CH or C.tbd.C;
- R.sup.4 is hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl, or acyl;
- R.sup.5 is hydrogen, C.sub.1 -C.sub.4 alkyl, CF.sub.3, phenyl, hydroxy, amino, bromo, iodo, or chloro;
- R.sup.6 is acyl;
- R.sup.7 is independently hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl, or substituted phenyl;
- R.sup.8 is C.sub.1 -C.sub.4 alkyl or tetrazole-5-yl;
- and
- n is 0, 1, or 2;
- provided that when Y is NR.sup.4, O, S, SO, or SO.sub.2, W is (CH.sub.2).sub.n and Z is CHR.sup.7 or CH;
- further provided that when W is S, SO, or SO.sub.2, Y is CHR.sup.7, Z is CHR.sup.7 or CH, or Y and Z together are HC.dbd.CH or C.tbd.C;
- further provided that when W and Z are CH.sub.2, Y is not S;
- further provided that when W and Y together are HC.dbd.CH or C.tbd.C, Z is CHR.sub.7 ;
- or a pharmaceutically acceptable salt thereof.
16 more elements
Dependencies are inferred from the claim text.