Phosphonic acid derivatives and use thereof

Details Phosphonic acid derivatives and use thereof Phosphonic acid derivatives and use thereof

1996-07-12

1998-09-01

Richter, Johann

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

514 80, 514118, 548414, 558171, C07F 922, A61K 3342

Patent

active

RE0358860

ABSTRACT:
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., "Inhbitions of Biological Actions of Big Endothelin-1 by Phosphoramidon" vol. 172, No. 2, pp. 390-395, 1990.
Grobelny et al, "Binding Enregetics of Phosphorus-containingInhibitors of Thermolysin", Biochemistry, vol. 28, No. 12 pp. 4948-4951, 1989.
Wakimasu, Rule 132 Declaration, Paper #10, File Wrapper of U.S. Patent No. 5,330,978 (admissions).
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.
Kam et al, "Inhibition of Thermolysin and Carboxypeptidase A by Phosphamidates", Biochemistry, vol. 18, No. 14, pp. 3032-3038, 1979.
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McMahon et al., "Phosphoramidon Blocks The Pressor Activity of Porcine Big Endothelin-1-(1-39) In Vivo and Conversion of Big Endothelin-1-(1-39), 2 Endothelin-1-(1-21) In Vitro", Proceedings National Academy of Science, vol. 88 (Feb. 1991), pp. 703-777.
Rich, H. David, "Peptidase Inhibitors" in Comprehensive Medicinal Chemistry The Rational Design, Mechanistic Study & Therapeutic Application of Chemical Compounds, vol. 2 (Pergamon Press PLC), pp. 391-496 (not continuous), 1990.
Carey, et al., "Reaction and Synthesis": Chapter 11 entitled Multistep Synthesis at pp. 539-553, Advanced Organic Chemicstry, Second Ed. Part B (New York Plenum Press, 1983).
Merz, et al., "Free Perturbation Simulations of the Inhibition of Thermolysin: Prediction of the Free Energy of Binding of a New Inhibitor", J. Am. Chem. Soc., vol. 111, No. 15 (1989), pp. 5649-5658.

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