Antagonists of specific excitatory amino acid neurotransmitter r

Details Antagonists of specific excitatory amino acid neurotransmitter r Antagonists of specific excitatory amino acid neurotransmitter r

1987-03-04

1988-08-02

Evans, J. E.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Phosphorus containing other than solely as part of an...

2605025G, 514112, 558190, 558192, C07F 938, A61K 3113, A61K 31195, A61K 31045

Patent

active

047614056

ABSTRACT:
The invention pertains to novel, potent anticonvulsants, analgesics, cognition enhancers and neuroprotectants achieving their action through the antagonism of specific excitatory amino acid neurotransmitter receptors. In particular, the invention is directed to .omega.-[2-(phosphonoalkylenyl)-cycloalkyl]-2-aminoalkanoic acids having general formula: ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and are selected from the group consisting of hydrogen, lower alkyl (C.sub.1 to C.sub.6), alkyl (C.sub.7 to C.sub.12), fatty acid chain (C.sub.13 to C.sub.24), aryl, aralkyl, hydroxyl; the stereoisomers being in their resolved or racemic form; n and m=0,1,2 or 3; z=0,1 or 2; the cycloalkyl ring being replaced with the cycloalkenyl ring; and the pharmaceutically acceptable salts and derivatives thereof.

REFERENCES:
patent: 4147780 (1979-04-01), Dingwall et al.
patent: 4477391 (1984-10-01), Collins
patent: 4483853 (1984-11-01), Collins et al.
patent: 4656298 (1987-04-01), Dingwall et al.
patent: 4657899 (1987-04-01), Rzeszotarski et al.
Matoba et al., Chem. Pharm. Bull., vol. 32, No. 10, 1984, pp. 3918-3925.

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