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    • 3. 发明授权
    • Amino- or guanidino-phenylpropionic acid derivatives
    • 氨基或胍基 - 苯基丙酸衍生物
    • US4182897A
    • 1980-01-08
    • US917232
    • 1978-06-20
    • Setsuro FujiiHiroyuki KawamuraSeizo TairaRyoji MatsuiYojiro SakuraiToshiyuki Okutome
    • Setsuro FujiiHiroyuki KawamuraSeizo TairaRyoji MatsuiYojiro SakuraiToshiyuki Okutome
    • C07C205/56C07C279/18A61K31/24C07C101/447C07C129/12
    • C07C279/18C07C205/56Y10S514/822
    • 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:HO--R.sup.2to an esterification in the conventional manner to obtain a nitrocinnamic ester derivative, then reducing the latter compound to obtain an aminophenylpropionic ester derivative and, if desired, reacting it with cyanamide to obtain a guanidino-phenylpropionic ester derivative and, if desired, further converting the reaction product to an acid addition salt.
    • 由下式表示的氨基或胍基 - 苯基丙酸酯衍生物:其中R是-NH 2或R 1是氢或低级烷基,R 2是未取代的或低级烷基 - 羧基烷基 - 低级 - 烷氧基 - ,低级烷氧基羰基或卤素取代的苯基或未取代的或卤素取代的萘基,其酸加成盐是对蛋白水解酶具有特异性酶抑制活性的新化合物,因此它们是有用的 作为由这些酶的异常活化引起的疾病的治疗剂。 上述化合物可以通过将下式所示的硝基肉桂酸衍生物和由式HO-R2表示的酚衍生物或萘酚衍生物以常规方式进行酯化而制得,得到硝基肌氨酸酯 衍生物,然后还原后一种化合物以获得氨基苯基丙酸酯衍生物,并且如果需要,可与氰酰胺反应,得到胍基 - 苯基丙酸酯衍生物,如果需要,将反应产物进一步转化成酸加成盐。