Phosphonate and phosphonamide endopeptidase inhibitors

Details Phosphonate and phosphonamide endopeptidase inhibitors Phosphonate and phosphonamide endopeptidase inhibitors

1989-01-17

1990-10-16

Shen, Cecilia

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

558170, 558171, A61K 3166, C07F 909

Patent

active

049635395

ABSTRACT:
Compounds of the formula ##STR1## wherein Y is O or NH and X is ##STR2## will inhibit the action of neutral endopeptidase. As a result, such compounds produce diuresis, natriuresis, and lower blood pressure as well as being useful in the treatment of congestive heart failure, relieving pain, and diarrhea when administered to a mammalian host.

REFERENCES:
patent: 4432971 (1984-02-01), Karanewsky et al.
patent: 4432972 (1984-02-01), Karanewsky et al.
patent: 4452790 (1984-06-01), Karanewsky et al.
patent: 4616005 (1986-10-01), Karanewsky et al.
patent: 4749688 (1988-06-01), Haslanger et al.
patent: 4853476 (1989-08-01), Petrakis et al.
Bartlett et al., "Phosphonamidates As Transition-State Analogue Inhibitors of Thermolysin, Biochemistry," vol. 22, p. 4618-4624 (1983).
Bartlett et al., "An Anaysis Of The Enzyme Inhibitor Binding Interactions . . . Thermolysin, Phosphorus and Sulfur," vol. 30, p. 537-543 (1987).

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