摘要 |
Certain new phosphonoalkanoylamino acids of the formula (I) herein and their pharmaceutically acceptable salts exhibit improved antihypertensive properties and are particularly useful for the reduction of angiotensin related hypertension. <CHEM> in which R1 and R2, which are the same or different, are each selected from the group consisting of a hydrogen atom, an optionally substituted lower alkyl, a lower alkenyl, an optionally substituted aryl and an optionally substituted aralkyl radical; n is 0 or 1; R3 is a hydrogen atom, an optionally substituted lower alkyl, a lower alkenyl, an optionally substituted aryl or an optionally substituted aralkyl group; and (a) R4 is a hydrogen atom, a lower alkyl or a phenyl-lower alkyl radical; R5 and R6, which are the same or different, are each selected from the group consisting of a hydrogen atom, an optionally substituted lower alkyl or an aryl radical; and R7 is selected from the group consisting of -OR8, -NR9 or -SR10, wherein R8 and R10 are each selected from the group consisting of a hydrogen atom, a lower alkyl, an optionally substituted aryl, or an optionally substituted aralkyl radical and R9 is a hydrogen atom, a hydroxy or lower alkyl radical or the residue of an - amino acid; or (b) R4 and R5 are part of a four-, five- or six-membered optionally substituted heterocyclic ring as a connected bridge of 2 to 4 atoms of carbon or carbon and either nitrogen, sulphur or oxygen; and R6 and R7 are each as defined in (a); with the proviso that when R3 is a hydrogen atom, n is 0, the heterocyclic ring is an unsubstituted pyrrolidine, R6 is a hydrogen atom, and R7 is OR8, at least one of R1, R2 and R8 is an optionally substituted aryl radical; or (c) R5 and R6 are selected to form a side chain of alpha -amino acid, where N(R4) CR5R6COR7 is an alpha -amino acid residue; with the proviso that (i) when R3 is hydrogen and n is 0, the
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