Certain hetero phosphonic acid derivatives of 2-piperidine or 2-

Details Certain hetero phosphonic acid derivatives of 2-piperidine or 2- Certain hetero phosphonic acid derivatives of 2-piperidine or 2-

1986-02-28

1988-05-24

Rotman, Alan L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

546 22, 546 23, 546 24, 548413, C07F 958, C07F 965, A61K 31675

Patent

active

047466537

ABSTRACT:
The present invention is concerned with the phosphonic acids of formula I ##STR1## wherein one or both of the acidic hydroxy groups of the phosphonic acid moiety may be functionalized in form of pharmaceutically acceptable mono- or di-esters; wherein Y represents optionally substituted 2-carboxypyrrolidinyl, 2-carboxy-2,5-dihydropyrrolyl, 2-carboxy-1,2,3,6-tetrahydropyridinyl, 2-carboxy-1,2,5,6-tetrahydropyridinyl, 2-carboxypiperidinyl, 2-carboxytetrahydroquinolinyl or 2-carboxyperhydroquinolinyl, 2-carboxy-2,3-dihydroindolyl, 2-carboxyperhydroindolyl, and in each of which the carboxy group may be functionalized in form of a pharmaceutically acceptable ester or amide; A represents B--X--D wherein B represents a direct bond, or straight chain or branched lower alkylene; X represents O, S, SO, SO.sub.2, CO--NR.sub.b, R.sub.b N--CO or N--Ra; Ra represents hydrogen, lower alkyl, aryl, aryl-lower alkyl or acyl; R.sub.b represents hydrogen, lower alkyl or aryl-lower alkyl; D represents straight chain or branched lower alkylene; and pharmaceutically acceptable salts thereof; which are useful in mammals as antagonists of the N-methyl-D-aspartate sensitive excitatory amino acid receptor.

REFERENCES:
patent: 4477391 (1984-10-01), Collins
patent: 4483853 (1984-11-01), Collins
Simon, R. P. et al., Science, 226, 850-852, (1984).
Neuroscience Abstracts, 11, 106, (1985).
Epilepsia, 25, (Supple. 2), S140-S149, (1984).
Neuropharmacology, 23, 467-472, (1984).
Tetrahedron Letters, 1979, 4929-4930, (1979).
Medicinal Research Reviews, 2, 1-41, (1982).
Chem. Pharmaceutical Bulletin, 32, 3918-3925, (1984).

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