Certain phosphonic acids and derivatives useful for the treatmen

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...

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548413, 546 22, 546 23, C07F 9572, A61K 3140

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active

050575066

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 represent 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-carboxyetrahydroquinolinyl or 2-carboxyperhydroquinolinyl, 2-carboxyl-2,3-dihydroindolyl or 2-carboxyperhydroindolyl as described herein, and in each of which the carboxy group may be functionalized in form of a pharmaceutical acceptable ester or amide; A represents a direct bond, lower alkenylene, lower alkylidene or lower alkylene provided that A does not represent a direct bond when Y represents 2-carboxypyrolidinyl; and pharmaceutically acceptable salts thereof; which are useful for the treatment of nervous system disorders in mammals and as antagonists of the N-methyl-D-aspartate sensitive excitatory amino acid receptor.

REFERENCES:
patent: 4898854 (1990-02-01), Hutchison et al.
patent: 4906621 (1990-03-01), Hutchison et al.
Chem. Abstracts, vol. 104 (9), Abst. No. 104:69130-a Mar. 3, 1986.
Chem. Abstracts, vol. 108(13), Abst. No. 108: 112,734-X, Mar. 28, 1988.
Tetrahedron Letters No. 51, pp. 4929-2930 E. Petrilla Jr. and E. R. Spitz Miller.
Chem. Pharm. Bull. 32 391814 25 (1984).
Phosphorus and Sulfur 1984 vol. 20 pp. 313-321.

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