Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...
Patent
1992-06-03
1994-07-19
Springer, David B.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Phosphorus containing other than solely as part of an...
514118, 548414, 558171, C07F 922, A61K 3342
Patent
active
053309782
ABSTRACT:
A phosphonic acid derivative compound represented by formula [I ] or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 each represent hydrocarbon groups which may be substituted, except cases in which (1) R.sub.2 is unsubstituted methyl, ( 2 ) R.sub.3 is an unsubstituted hydrocarbon group having 1 to 3 carbon atoms, and (3) R.sub.1 is benzyloxycarbonylaminomethyl, R.sub.2 is isobutyl and R.sub.3 is isobutyl or phenylmethyl, which has endothelin-converting enzyme inhibiting activity and is useful as pharmaceutical drugs such as therapeutic agents for hypertension, cardiac or cerebral circulatory diseases and renal diseases.
REFERENCES:
patent: 4379146 (1983-04-01), Greenlee et al.
patent: 4432972 (1984-02-01), Karanewsky et al.
Proc. Natl. Acad. Sci. USA--"Phosphorus-containing Inhibitors of Antiotensin-converting Enzyme", vol. 79, pp. 2176-2180, Apr. 1982.
Biochemistry, "Phosphonamidates as Transition-State Analogue Inhibitors of Thermolysin"--22, 4618-4624 (1982).
Biochemical and Biophysical Res. Comm., "Inhibition of Biological Actions Of Big Endothelin-1 by Phosphoramidon", vol. 172, No. 2, pp. 390-395 (1990).
Grobelny, et al., "Binding Energetics of phosphorus-containing inhibitors of Thermolysin", Biochemistry, vol. 28, No. 12, 1989, pp. 4948-4951.
Morgan et al., "Differential binding energy: A detailed evaluation of the influence of hydrogen-bonding and hydrophobic groups on the inhibition of thermolysin by phosphorus-containing inhibitors", Journal of The American Chemical Society, vol. 113, No. 1, 1991, pp. 297-307.
Kam et al., "Inhibition of thermolysin and carboxypeptidase A by phosphoramidates", Biochemstry, vol. 18, No. 14, 1979, pp. 3032-3038.
Kawada Akira
Mori Masaaki
Wakimasu Mitsuhiro
Conlin David G.
Neuner George W.
Springer David B.
Takeda Chemical Industries Ltd.
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