Phosphono/biaryl substituted dipetide derivatives

Details Phosphono/biaryl substituted dipetide derivatives Phosphono/biaryl substituted dipetide derivatives

1992-10-09

1994-03-15

Lee, Mary C.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514382, 514340, 548119, 546 22, A61K 3141, A61K 3144, C07F 906

Patent

active

052946320

ABSTRACT:
The invention relates to the N-phosphonomethyl-biaryl substituted dipeptide derivatives of formula I ##STR1## and tetrazole derivatives of the formula Ia ##STR2## wherein A represents a direct bond, lower alkylene, phenylene or cyclohexylene; m represents 1 or zero, provided that m represents 1 when A is a direct bond; R.sub.2 represents hydrogen, hydroxy, lower alkyl, aryl-lower alkyl, C.sub.5 -C.sub.7 -cycloalkyl-lower alkyl, amino-lower alkyl, hydroxy-lower alkyl, lower alkylthio-lower alkyl, lower alkoxy-lower alkyl, aryl-lower alkylthio-lower alkyl or aryl-lower alkoxy-lower alkyl; biaryl represents phenyl substituted by carbocyclic or heterocyclic aryl; and pharmaceutically acceptable mono-, di- or tri-ester derivatives thereof in which one, two or three of the acidic hydroxy groups of the carboxyl and/or phosphono functional groups are esterified in form of a mono-, di- or tri-pharmaceutically acceptable ester; and pharmaceutically acceptable amide derivatives thereof wherein the carboxyl group is derivatized in form of a pharmaceutically acceptable amide; and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising said compounds; methods for the preparation of said compounds and for the preparation of intermediates; and methods of treating disorders in mammals which are responsive to the inhibition of neutral endopeptidases by administration of said compounds to mammals in need of such treatment.

REFERENCES:
patent: 4053505 (1977-10-01), Dutra
patent: 4618708 (1986-10-01), Roques et al.
patent: 4721726 (1988-01-01), Berger
patent: 4749688 (1988-06-01), Haslanger et al.
patent: 4939261 (1990-07-01), Ksander
patent: 4963539 (1990-10-01), Delaney
patent: 5021430 (1991-06-01), Ksander
patent: 5155100 (1992-10-01), Erion et al.
Res. Comm. in Chem. Pathology and Pharmacology, vol. 52, 81 (1986).
Medicinal Research Reviews, vol. 5, 483-531 (1985).

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