Therapeutic peptide derivatives

A peptide derivative consisting of:

• a biologically active peptide moiety having a free amino group, and at least one substituent attached to said peptide moiety, wherein said substituent is selected from the group consisting of Compounds I, II, and III, wherein Compound I is:
• ##STR20## wherein:
• R.sub.0 is O, S, or NR.sub.5, wherein R.sub.5 is H or (C.sub.1 -C.sub.6) alkyl;
• each R.sub.1 and R.sub.2, independently, is H, (CH.sub.2).sub.m OR.sub.6, or CH(OR.sub.7)CH.sub.2 OR.sub.8, wherein R.sub.6 is H or (C.sub.2 -C.sub.7) acyl, and each R.sub.7 and R.sub.8, independently, is H, (C.sub.2 -C.sub.7) acyl, or C(R.sub.9)(R.sub.10), wherein each R.sub.9 and R.sub.10, independently, is H or C.sub.1 -C.sub.6 alkyl;
• or R.sub.1 and R.sub.2 in combination are .dbd.CHCH.sub.2 OR.sub.11, R.sub.11 is H or (C.sub.2 -C.sub.7) acyl, and m is an integer between 1 and 5, inclusive;
• and
• one of R.sub.3 and R.sub.4 is (CH.sub.2).sub.n R.sub.12 or (CH.sub.2).sub.n CH(OH)R.sub.12, wherein R.sub.12 is CO, CH.sub.2 or SO.sub.2, and n is an integer between 1 and 5, inclusive;
• and the other of R.sub.3 and R.sub.4 is H, (C.sub.1 -C.sub.6) hydroxyalkyl, or (C.sub.2 -C.sub.7) acyl;
• and
• Compound II is:
• ##STR21## wherein:
• each R.sub.13, R.sub.14, and R.sub.15, independently, is H or (C.sub.2 -C.sub.24) acyl;
• R.sub.16 is NH or absent;
• R.sub.17 is CO, O, or absent;
• R.sub.18 is CO, CH.sub.2, SO.sub.2, or absent;
• m is an integer between 1 and 5, inclusive;
• n is an integer between 1 and 5, inclusive;
• and
• Compound III is:
• ##STR22## wherein:
• R.sub.19 is H, NH.sub.2, an aromatic functional group, OH, (C.sub.1 -C.sub.6) hydroxyalkyl, H(R.sub.27)(R.sub.28), SO.sub.3 H, or absent;
• wherein each R.sub.27 and R.sub.28, independently, is H or (C.sub.1 -C.sub.6) alkyl;
• R.sub.20 is O or absent;
• R.sub.21 is (C.sub.1 -C.sub.6) alkyl or absent;
• R.sub.22 is N, O, C, or CH;
• R.sub.23 is (C.sub.1 -C.sub.6) alkyl or absent;
• R.sub.24 is N, CH, or C;
• R.sub.25 is NH, O, or absent;
• R.sub.26 is SO.sub.2, CO, or CH.sub.2 ;
• m is an integer between 0 and 5, inclusive;
• n is an integer between 0 and 5, inclusive;
• p is an integer between 0 and 5, inclusive;
• and
• q is an integer between 0 and 5, inclusive;
• wherein said peptide moiety is attached to said substituent at R.sub.12, R.sub.18, or R.sub.26 by a CO--N, CH.sub.2 --N, or SO.sub.2 --N bond between said substituent and said free amino group.