Amino- or guanidino-phenylpropionic acid derivatives
US4182897A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Jun 20, 1978 |
| Grant date | Jan 8, 1980 |
| Priority date | — |
| Expiry date | Jun 20, 1998 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07C205/56
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
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: EQU HO--R.sup.2 to 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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.