Abbott Laboratories Corporation

Paulette Johnson

Jerry R Martin

John S Tadanier

Alex M Nadzan

A 1,2-modified fortimicin A or B represented by the formulae I, II and III: ##STR1## wherein R is hydrogen or loweralkyl; and R.sub.1 is selected from the group consisting of hydrogen, loweralkyl, aminoloweralkyl, diaminoloweralkyl, N-lower-alkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl, hydroxyloweralkyl, amino hydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl, N-N-diloweralkylaminohydroxyloweralkyl, acyl, aminoacyl, hydroxy-substituted aminoacyl, diaminoacyl, hydroxyacyl, hydroxy-substituted diaminoacyl, N-loweralkylaminoacyl, N, N-diloweralkylaminoacyl, hydroxysubstituted-N-loweralkylaminoacyl and hydroxy-substituted-N, N-diloweralkylaminoacyl, and the pharmaceutically acceptable salts thereof. The compounds are broad spectrum antibiotics.

1,2-Modified fortimicins A and B, intermediates therefor and method for

A 1,2-modified fortimicin A or B represented by the formulae I, II and III: ##STR1## wherein R is hydrogen or loweralkyl.

The present invention provides 2-deoxy-3-O-demethyl-fortimcins A and B and the 4-N-acyl and alkyl derivatives thereof, represented by the formula: ##STR1## wherein R is selected from the group consisting of hydrogen, acyl, aminoacyl,diaminoacyl,N-monoloweralkylaminoalkyl,N,N-diloweralkylaminoalky l, hydroxy-substituted aminoacyl,loweralkyl, aminoloweralkyl, N-monoloweralkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl and hydroxy-substituted aminoloweralkyl and the pharmaceutically acceptable salts thereof.

2-Deoxy-3-O-Demethylfortimicins

Disclosed are 2-deoxy-2-substituted fortimicin A and B derivatives represented by the formula ##STR1## wherein R is hydrogen glycyl, .beta.-alanyl, acetyl, or .beta.-amino lower alkyl, R.sub.1 is hydrogen, amino, azido, halo, glycylamido, .beta.-alanyl amido or 2-O-methanesulfonyl and R.sub.2 is hydrogen or halo and their pharmaceutically acceptable salts. The compounds are active antibacterial agents.

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Zion, IL, United States of America

Paulette Johnson