2-N-acyl and alkyl 6-epi-fortimicin B and derivatives

Drug – bio-affecting and body treating compositions – Conjugate or complex of monoclonal or polyclonal antibody,... – Conjugated via claimed linking group – bond – chelating agent,...

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536 4, 536 17R, A61K 3171, C07H 1522

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active

041872967

ABSTRACT:
2'-N-Acyl and alkyl-6'-epi-fortimicin B and fortimicin B derivatives represented by the formula ##STR1## wherein: R is acyl, hydroxyacyl, aminoacyl, N-monoloweralkylamino, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, an amino acid residue, loweralkyl, aminoloweralkyl, hydroxyloweralkyl, N-loweralkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl, aminohydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl or N,N-diloweralkylaminohydroxyloweralkyl; and R.sub.1 is acyl, aminoacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, an amino acid residue, hydroxyacyl loweralkyl, aminoloweralkyl, hydroxyloweralkyl, N-loweralkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl, aminohydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl, N,N-diloweralkylaminohydroxyloweralkyl or hydrogen; R.sub.2 is loweralkyl; and R.sub.3 is hydrogen or loweralkyl; and the pharmaceutically acceptable salts thereof; pharmaceutical compositions containing the compounds; and methods of making and using the compounds. The compounds are antibiotics.

REFERENCES:
patent: 3931400 (1976-01-01), Nara et al.
patent: 3976768 (1976-08-01), Nara et al.
patent: 4060682 (1977-11-01), Umezawa et al.

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