Aminophosponic acid derivative

Details Aminophosponic acid derivative Aminophosponic acid derivative

1993-05-04

1995-01-10

Dees, Jose G.

Organic compounds -- part of the class 532-570 series

Organic compounds

Phosphorus acids or salts thereof

562 17, C07F 908

Patent

active

053809211

ABSTRACT:
There are provided novel aminophosphonic acid derivatives of the general formula [I]: ##STR1## wherein n is an integer of 2 or 3; R.sup.1 is a phenyl, naphthyl, indolyl, benzothienyl, benzofuryl or benzoxazolyl group which may have 1 to 3 substituents selected from the group consisting of hydroxyl and lower alkyloxy groups, or a hydrogen atom; R.sup.2 is a lower alkyl group, a benzyl group, a 4-hydroxybenzyl group, a 3-indolylmethyl group or a .beta.-phenethyl group; and A is an optional residue of an amino acid selected from the group consisting of tryptophane, tyrosine, phenylalanine, homophenylalanine, naphthylalanine or N.sup..omega. -nitroarginine, and their pharmaceutically acceptable salts. The compounds according to the present invention and their pharmaceutically acceptable salts exhibit an inhibitory activity against endothelin-converting enzyme, and are expected to be useful as a drug treating various diseases with which endothelin is concerned.

REFERENCES:
Flynn et al, "The Synthesis of an Aminophosphonic Acid Converting Enzyme Inhibitor", Tetrahedron Letters, 27:1757-1758 (1986).
Bertenshaw et al, "Phosphorus-Containing Inhibitors of Endothelin Converting Enzyme; Effects of the Electronic Nature of Phosphorus on Inhibitor Potency", J. Med. Chem., 36:173-176 (1993).
Okada et al, Biochem. Biophys. Res. Commun., 171(3):1192-1198 (1990).

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