1-N-aminohydroxyacyl derivatives of gentamicin B
AssigneeSchering Corporation
InventorsPeter J. L. Daniels, Tattanahalli L. Nagabhushan
Life of this patent
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Abstract
1-N-(R-.beta.-amino-.alpha.-hydroxypropionyl) gentamicin B, 1-N-(R-.gamma.-amino-.alpha.-hydroxybutyryl) gentamicin B, 1-N-(R-.delta.-amino-.alpha.-hydroxyvaleryl) gentamicin B and the corresponding diastereoisomers derived from the respective S-aminohydroxy acids and the acid addition salts thereof exhibit substantial antibacterial activity, especially against strains of bacteria which are resistant to gentamicin B and acid addition salts thereof.
Claims11
A compound selected from the group consisting of 1-N-(R-.beta.-amino-.alpha.-hydroxypropionyl-gentamicin B, 1-N-(R-.gamma.-amino-.alpha.-hydroxybutyryl) gentamicin B, 1-N-(R-.delta.-amino-.alpha.-hydroxyvaleryl) gentamicin B, the respective R,S diastereoisomeric mixtures of said compounds and the non-toxic pharmaceutically acceptable acid addition salts thereof.
The R,S-diastereoisomeric mixture 1-N-(R,S-.beta.-amino-.alpha.-hydroxypropionyl) gentamicin B.
The R,S-diastereoisomeric mixture 1-N-(R,S-.gamma.-amino-.alpha.-hydroxybutyryl) gentamicin B.
The R,S-diastereoisomeric mixture 1-N-(R,S-.delta.-amino-.alpha.-hydroxyvaleryl) gentamicin B.
Dependencies are inferred from the claim text.