John S Tadanier

43606660, Nov 23, 1982

May 22, 1981

6/266030

John S. Tadanier - Waukegan IL
Jerry R. Martin - Waukegan IL
Paulette Collum - Zion IL

Abbott Laboratories - North Chicago IL

C07N 1522

536 161

2-Deoxyfortimicin A, 2-deoxy-4-N-alkyl fortimicins and 2-deoxy-4-N-acyl fortimicins represented by the formula ##STR1## wherein R is selected from the group consisting of acyl, aminoacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, an amino acid residue, hydroxyacyl, loweralkyl, aminoloweralkyl, N-monoloweralkylaminoloweralkyl, hydroxyloweralkyl, N-N-diloweralkylaminoloweralkyl or hydroxy-substituted aminoloweralkyl, and the pharmaceutically acceptable salts thereof; intermediates therefor; and pharmaceutical compositions containing the compounds of this invention.

43606687, Nov 23, 1982

May 22, 1981

6/266266

Jerry R. Martin - Waukegan IL
John S. Tadanier - Waukegan IL
Paulette Collum - Zion IL

Abbott Laboratories - North Chicago IL

C07H 1522

536 161

2-Deoxyfortimicin, A, 2-deoxy-4-N-alkyl fortimicins and 2-deoxy-4-N-acyl fortimicins represented by the formula ##STR1## wherein R is selected from the group consisting of acyl, aminoacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, an amino acid residue, hydroxyacyl, loweralkyl, aminoloweralkyl, N-monoloweralkylaminoloweralkyl, hydroxyloweralkyl, N-N-diloweralkylaminoloweralkyl or hydroxy-substituted aminoloweralkyl, and the pharmaceutically acceptable salts thereof; intermediates therefor; and pharmaceutical compositions containing the compounds of this invention.

42319242, Nov 4, 1980

Jan 10, 1979

6/002436

John S. Tadanier - Waukegan IL
Jerry R. Martin - Waukegan IL
Paul Kurath - Waukegan IL

Abbott Laboratories - North Chicago IL

C07C10352
C07H 1522

2601125R

This invention provides 4-N-acylfortimicin B derivatives of the structure ##STR1## wherein R is acyl, aminoacyl, N-monoloweralkylminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, or substituted aminoacyl of the formula ##STR2## where R. sup. 1 is an acyl radical derived from an amino acid or a short peptide, and the pharmaceutically acceptable salts thereof. The compounds are useful as intermediates for preparing 4-N-alkyl or substituted alkylfortimicin B derivatives. In addition to their utility as intermediates, some of the compounds of this invention are also useful as antimicrobial agents.

44276621, Jan 24, 1984

Apr 9, 1982

6/366798

John S. Tadanier - Waukegan IL
Robert Hallas - Kenosha WI
Leslie A. Freiberg - Waukegan IL
David J. Bacino - Waukegan IL

Abbott Laboratories - North Chicago IL

A61K 3171
C07H 1522

424180

Disclosed herein are fortimicin derivatives represented by the formula: ##STR1## wherein R is hydrogen, loweralkyl, aminoloweralkyl, diaminoloweralkyl, N-loweralkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl, hydroxyloweralkyl, aminohydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl, N,N-diloweralkylaminohydroxyloweralkyl, loweracyl, aminoloweracyl, diaminoloweracyl, hydroxyloweracyl, N-loweralkylaminoloweracyl, N,N-diloweralkylaminoloweracyl, or aminohydroxyloweracyl, and the pharmaceutically acceptable salts thereof. Also disclosed are intermediates useful in the preparation of these compounds and compositions of these compounds together with a pharmaceutically acceptable carrier and/or diluent.

41247566, Nov 7, 1978

Dec 27, 1976

5/754670

Jerry R. Martin - Waukegan IL
John S. Tadanier - Waukegan IL

Abbott Laboratories - North Chicago IL

C07H 1522

536 17

Described are 3-de-O-methylfortimicins A and B and 4-N-acyl and 4-N-alkyl-3-de-O-methylfortimicin B derivatives, and their preparation, which compounds are useful as antibiotics or as intermediates for preparing other useful derivatives having antibacterial activity. The compounds have the following structural formula ##STR1## wherein R is hydrogen, acyl, aminoacyl, N-monoloweralkylaminoacyl, N. N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, alkyl, aminoalkyl, N-monoloweralkylaminoalkyl, N. N-diloweralkylaminoalkyl or hydroxy-substituted aminoalkyl and the pharmaceutically acceptable salts thereof, for example, salts formed from hydrochloric, sulfuric, and phosphoric acids.

42321476, Nov 4, 1980

Sep 26, 1979

6/079143

John S. Tadanier - Waukegan IL
Jerry R. Martin - Waukegan IL

Abbott Laboratories - North Chicago IL

C07H 1700

536 4

4-N-acylfortimicin B-1,5-carbamates represented by the formula ##STR1## wherein R is acyl and R. sub. 1 is hydrogen or benzyloxycarbonyl.

42699703, May 26, 1981

Sep 26, 1979

6/079138

John S. Tadanier - Waukegan IL
Jerry R. Martin - Waukegan IL

Abbott Laboratories - North Chicago IL

C07H 1522
C07D41302

536 17R

A 1,2-carbamate of fortimicin B and derivatives represented by the formula: ##STR1## wherein: R is hydrogen or monocyclicaryloxycarbonyl, R. sub. 1 is hydrogen or monocyclicaryloxycarbonyl; and R. sub. 2 is selected from the group consisting of loweralkyl, loweralkoxycarbonyl aminoloweralkyl, hydroxyloweralkyl, hydroxy-substituted aminolowerakyl, an amino acid residue, and N-protected amino acid residue, or when R and R. sub. 1 are hydrogen, R. sub. 2 can also be hydrogen; and the acid addition salts thereof when R,R. sub. 1 or R. sub. 2 are hydrogen or an unprotected aminoacid residue.

41559029, May 22, 1979

Mar 20, 1978

5/888085

John S. Tadanier - Waukegan IL
Jerry R. Martin - Waukegan IL
Paul Kurath - Waukegan IL

Abbott Laboratories - North Chicago IL

C07C10352

2601125R

This invention provides 4-N-acylfortimicin B derivatives of the structure ##STR1## wherein R is acyl, aminoacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, or substituted aminoacyl of the formula ##STR2## where R. sup. 1 is an acyl radical derived from an amino acid or a short peptide, and the pharmaceutically acceptable salts thereof. The compounds are useful as intermediates for preparing 4-N-alkyl or substituted alkylfortimicin B derivatives. In addition to their utility as intermediates, some of the compounds of this invention are also useful as antimicrobial agents.