Torii & Co., Ltd.

Seizo Taira

Hiroyuki Kawamura

Setsuro Fujii

Toyoo Nakayama

Toshiyuki Okutome

Yojiro Sakurai

Ryoji Matsui

Masahiro Iwaki

Masaoki Shibuya

Amidinonaphthyl furancarboxylate derivatives of the formula I ##STR1## wherein A is a single bond or A denotes (a) a phenyl group, cyclopentyl group, or cyclohexyl group, (b) an alkenylphenyl group, alkylphenyl group, phenylalkenyl group, or phenylalkyl group wherein alkyl is C.sub.1 to C.sub.7 alkyl and alkenyl is C.sub.2 to C.sub.7 alkenyl, (c) a C.sub.1 to C.sub.18 alkyl or C.sub.2 to C.sub.7 alkenyl group which may be substituted by one or two substituents selected from C.sub.1 to C.sub.5 alkyl groups and quanidino groups, wherein an alkyl substituent together with the carbon atom to which it is attached may form a cycloalkyl ring having from 3 to 6 carbon atoms, or said C.sub.1 to C.sub.5 alkyl may itself be substituted by a C.sub.3 to C.sub.6 cycloalkyl ring, or (d) --(CH.sub.2).sub.n --NH--CO--(CH.sub.2).sub.n' wherein n and n' may be the same or different and represent an integer from 1 to 4; and wherein R denotes (e) a hydroxyl group, (f) a C.sub.1 to C.sub.7 alkoxy group which may be mono- or disubstituted by C.sub.1 to C.sub.5 alkyl, (g) a phenyl-C.sub.1 -C.sub.4 alkoxy group, (h) --OAl(OH).sub.2, (i) an amino group, (j) ##STR2## or (k) ##STR3## and pharmaceutically acceptable acid addition salts thereof, useful as pharmaceuticals.

Amidinonaphthyl furancarboxylate derivatives and acid addition salts

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:

Amino- or guanidino-phenylpropionic acid derivatives

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Chiba, Japan

Seizo Taira