Abbott Laboratories Corporation

Robert Hallas

Daniel T Chu

John S Tadanier

Jerry R Martin

Jacob J Plattner

Yat Sun Or

Ly Tam Phan

Michael D Tufano

Leslie A Freiberg

Richard L Elliott

David J Bacino

Kenneth P Spina

Compounds, or pharmaceutically acceptable salts and esters thereof, of the formula:

Tricyclic erythromycin derivatives

Quinobenzothiazine derivatives of the formula ##STR1## as well as the pharmaceutically acceptable salts, esters, amides and prodrugs thereof are disclosed, wherein R.sup.1 is hydrogen or acarboxy-protecting group, R.sup.2 and R.sup.3 are substitutents, A is oxygen, sulfur, or carbon, Z is a halogen or a nitrogen-containing group, X is hydrogen, halogen or alkyl, and W is hydrogen, alkyl, amino or halogen. The compounds have potent antineoplastic activity.

Quinobenzothiazine antineoplastic agents

Quinobenzoxazine, derivatives of the formula ##STR1## as well as the pharmaceutically acceptable salts, esters, amides and prodrugs thereof are disclosed, wherein R.sup.1 is hydrogen or a carboxy-protecting group, R.sup.2 and R.sup.3 are substitutents, A is oxygen, Z is a halogen or a nitrogen-containing group, X is hydrogen, halogen or alkyl, and W is hydrogen, alkyl, amino or halogen. The compounds have potent antineoplastic activity.

Quinobenzoxazine, antineoplastic agents

7-(3-A-amino-1-pyrrolidinyl) substituted naphthyridine and quinoline compounds wherein A is a solubilizing group selected from an amino acid residue or polypeptide chain.

7-(peptidylpyrolidinyl)naphthyridine antibacterial compounds

Dipeptide quinolone derivatives

Described is a method for the preparation of 6'-modified fortimicin compounds including 6'-epi fortimicin by converting 1,2-di-N-protected fortimicin B into 4,6'-di-N-substituted alkoxycarbonyl-1,2'-di-N-protected fortimicin B which is further converted to 1,2'-di-substituted fortimicin B-4,5-carbamate, a compound whose substitution pattern is particularly suited to modification at the 6'-amino group and novel compounds thereof.

6'-Modified fortimicin compounds

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.

3-Amino-3-demethoxyfortimicins, pharmaceutical compositions thereof and

What is described is 2-epi-fortimicin A, 2-epi-fortimicin B or a 2-epi-fortimicin B derivative represented by the formula: ##STR1## wherein R.sub.1 is hydrogen or loweralkyl; R.sub.2 is hydrogen or hydroxy; R.sub.3 is methyl or hydrogen; and R.sub.4 is selected from the group consisting of hydrogen, loweralkyl, aminoloweralkyl, diaminoloweralkyl, N-loweralkylaminoalkyl, N,N-diloweralkylaminoloweralkyl, hydroxyloweralkyl, aminohydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl, N,N-diloweralkylaminohydroxyloweralkyl, acyl of the formula ##STR2## wherein R.sub.5 is loweralkyl, aminoacyl, diaminoacyl, hydroxyacyl, N-loweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl or an amino acid residue other than those defined above and the pharmaceutically acceptable salts thereof useful in the treatment of infections.

2-Epi-fortimicin A and derivatives

A 4'-O-sulfonyl erythromycin derivative of the following structural formula: ##STR1## where R is selected from the group consisting of oxygen, oxime, and substituted oxime, R.sub.1 is hydrogen or hydroxy and R.sub.2 is selected from the group consisting of phthalimide, substituted amides, benzamides, substituted benzamides, sulfonamides, substituted sulfonamides, amines, substituted amines, phenylurea, substituted phenylurea, phenylthiourea, substituted phenylthiourea, thiophenol and substituted thiophenol, phenoxides and substituted phenoxides and R.sub.3 is hydrogen or methyl. The present sulfonyl derivatives of erythromycin A, B and C are useful as antibiotics.

Growing community of inventors

Kenosha, WI, United States of America

Robert Hallas