Phosphonyl amine derivative, process of its preparation and pharmaceutical preparation in which the derivative is comprised

摘要

In the present invention there are disclosed compounds of the general formula I, in which R represents alkyl, aryl or arylalkyl group, wherein the aryl is phenyl, naphthyl or heterocycle; Ri1 and Ri2, which can be identical or different represent hydrogen atoms or alkyl groups; Ri3 denotes aryl or arylalkyl group, wherein the aryl is as defined above; Ri4 represents a heterocycle being optionally substituted with a heterocycle or phenyl, or a phenyl group being substituted with a heterocycle, with exception of imidazole and indole; X represents a bond or -OCONH- or -CONH-. Further claimed are processes of their preparation and pharmaceutical preparations in which they are comprised. The compounds of the general formula I exhibit dual inhibition activity on ACE and NEP, and are therefore usable for treating cardiovascular diseases.