Abbott Laboratories Corporation

Leslie A Freiberg

Carla M Edwards

Richard J Pariza

Hugh N Nellans

David J Bacino

John S Tadanier

Nicholas S Bodor

Jerry R Martin

Clarence J Maring

Larry L Klein

Paul A Lartey

Andre G Pernet

Robert Hallas

Daniel Ambrose Dunnigan

Clinton M Yeung

Prabhavathi Fernandes

Howard E Gracey

Macrocylic lactam compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof, wherein A is selected from ##STR2## also disclosed are synthetic processes and intermediates useful in the preparation of the compounds of the invention, as well as compositions containing the same and methods for their use in stimulating contractile motion of the gastrointestinal tract.

Macrocyclic lactam prokinetic agents

Macrocylic lactam compounds of formula (i) ##STR1## and pharmaceutically acceptable salts thereof, wherein A is selected from ##STR2## also disclosed are synthetic processes and intermediates useful in the preparation of the compounds of the invention, as well as compositions containing the same and methods for their use in stimulating contractile motion of the gastrointestinal tract.

Erythromycin derivatives

The present invention is directed to the production and utilization of novel antibiotic compounds. These compounds are derivatives of the antibacterial agents tylosin and rosaramicin and exert a broad spectrum antibiotic activity toward several bacterial strains. Pharmaceutical compositions and methods of treating bacterial infections are described.

Rosaramicin derivatives and method of treating bacterial infections

Disclosed herein are erythromycin derivatives of the formula ##STR1## wherein R.sub.1 is lower alkyl, aryl, alkene, aryl halide, alkylamino, hydroxyalkyl and furanyl, and pharmaceutically acceptable salts thereof. These compounds have improved oral absorption, reduced effects on gastrointestinal motility, increased acid stability and longer serum half-lives.

Erythromycin A 11,12-carbonates and method of use

An erythromycin A derivative with high antimicrobial activity and improved pharmacokinetics is disclosed. 4'-Deoxyerythromycin A 11,12-carbonate and derivatives show superior in vitro and in vivo antimicrobial activity compared to erythromycin A, and when administered to animals has a serum half-life much prolonged over that of erythromycin A.

Erythromycin A 11,12-carbonate and method of use

Erythromycin A derivatives with high antimicrobial activity are disclosed. 14-hydroxyerythromycin A and derivatives show superior in vitro antimicrobial activity compared to the parent compounds.

Erythromycin A derivatives and method of use

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

Highly water-soluble erythromycin A derivatives wherein the desosamine moiety is quaternized with an acyloxy-, benzoyloxy- or alkoxycarbonyl-(or carboxy)-acylmethyl iodide, bromine or chloride and esterified in the 2-position with loweralkyl or --(CH.sub.2).sub.n CO.sub.2 R', wherein R' is H, loweralkyl or substituted loweralkyl and n is an integer from 1-5. These new esters readily convert to erythromycin A upon administration to warm-blooded animals.

Salts of erythromycin A esters

Novel fortimicin antibiotics represented by the formula ##STR1## wherein R.sub.1 is loweralkyl, R.sub.2 is hydrogen or loweralkyl and R.sub.3 is selected from the group consisting of hydrogen, acyl, hydroxyacyl, aminoacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl or an aminoacid residue, loweralkyl, hydroxyloweralkyl, aminoloweralkyl, N-monoloweralkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl or hydroxy-substituted aminoloweralkyl; and the pharmaceutically acceptable salts thereof, intermediates useful in their preparation, compositions employing the compounds and methods of using the compounds.

6'N-Alkyl- and 6',6'-di-N-alkyl derivatives of fortimicins A and B

Covers the process for the conversion of niddamycin to known compounds such as carbomycin B, leucomycin A.sub.1 and A.sub.3, and other antibiotic compounds as well as novel 3-(O)-esters 3-(0)-esters and dimethyl acetal derivatives not obtained from natural sources. These compounds are represented by the general formula: ##SPC1## Wherein R is hydroxy or oxygen, R.sub.1 is hydrogen, HCO (formyl), CH.sub.3 CO (acetyl), CH.sub.3 CH.sub.2 CO (propionyl) or CH.sub.3 CH.sub.2 CH.sub.2 CO (butyryl); wherein R.sub.2 is hydrogen or equivalent to R.sub.1 and R.sub.3 is CHO or CH(OCH.sub.3).sub.2. These compounds are useful antimicrobial agents.

Process for the conversion of niddamycin to leucomycin A.sub.1,

Covers 9-dihydroniddamycin A compounds and related 3-(O)-esters, which are active antimicrobial agents, and the process for their preparation. These compounds are represented by the general formula: ##SPC1## Wherein R.sub.1 is hydrogen, HCO (formyl), CH.sub.3 CO (acetyl), C.sub.2 H.sub.5 CO (propionyl) or C.sub.3 H.sub.7 CO (butyryl); R.sub.2 is hydrogen or equal to R.sub.1 and R.sub.3 is CHO or CH(OCH.sub.3).sub.2.

Growing community of inventors

Waukegan, IL, United States of America

Leslie A Freiberg