Amino- or guanidino-phenylpropionic acid derivatives

Details Amino- or guanidino-phenylpropionic acid derivatives Amino- or guanidino-phenylpropionic acid derivatives

1978-06-20

1980-01-08

Rollins, Alton D.

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

Organic compounds

Carboxylic acid esters

560 34, 560 50, 424308, 424309, A61K 3124, C07C101447, C07C12912

Patent

active

041828976

ABSTRACT:
Amino- or guanidino-phenylpropionic ester derivatives represented by the formula: ##STR1## wherein R is --NH.sub.2 or ##STR2## R.sup.1 is hydrogen or a lower alkyl group, and R.sup.2 is an unsubstituted or a lower-alkyl-, carboxyalkyl-, lower-alkoxy-, lower-alkoxycarbonyl- or halogen-substituted phenyl group or an unsubstituted or a halogen-substituted naphthyl group, and acid addition salts thereof are novel compounds exhibiting a specific enzyme-inhibitory activity to proteolytic enzymes and, therefore, they are useful as the therapeutic agent of diseases induced by abnormal activation of these enzymes. The above-mentioned compounds can be produced by subjecting a nitrocinnamic acid derivative represented by the formula: ##STR3## and a phenol derivative or a naphthol derivative represented by the formula:

REFERENCES:
patent: 3520918 (1970-07-01), Chase et al.
patent: 4021472 (1977-05-01), Fujii et al.
N. Kayama et al., Gendai Iryo, 6, 1010-1016 (1974).
P. Walsmann et al., Pharmazie, 29, H. 5, 333-336 (1974).

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