METHOD OF PRODUCING AMINOACYL OR PEPTIDE DERIVATIVES OF PHOSPHONIC OR PHOSPHINIC ACID OR SALTS THEREOF

1533239 Antibacterial compositions containing peptides ROCHE PRODUCTS Ltd 26 Jan 1976 [27 Jan 1975 20 Nov 1975] 3417/75 and 47787/75 Heading A5B [Also in Divisions C2 and C3] Antibacterial compositions for oral, parenteral and rectal administration comprise a carrier and a compound of formula I or pharmaceutically acceptable salt thereof wherein n is 0, 1, 2, or 3; R1 is H, or a C 1-6 alkyl, C 3-6 cycloalkyl, (C 3-6 cycloalkyl)-(C 1-6 alkyl), aryl, or aryl-(C 1-6 alkyl) group, said groups being optionally substituted by one or more amino, hydroxy, mercapto, methylthio, carboxy, or guanidino groups so as to form the charactering residue of an α-amino acid R1CH(NH 2 )CO 2 H of the type found in proteins; and any "aryl" moiety being optionally substituted by hydroxy, halogen, nitro, C 1-6 alkyl, or C 1-6 alkoxy; each R2 (independently) and R3 is the characterising residue of an α-amino acid R2CH(NH 2 )CO 2 H or R3CH(NH 2 )CO 2 H of the type found in proteins, with the proviso that when n is O and R1 is H or Ph then R3 is other than H; R1 3 is H or R3 and R1 3 together form the characterising residue of a cyclic α-amino acid of the type found in proteins; and R4 is Me or OH. When asymmetric, the configuration at * is L and at ** is R. Also included may be an anti-biotic (e.g. amoxycillin, cephradine, D- cycloserine) whose activity is "potentiated" by the above compounds.