Abbott Laboratories Corporation

Paul A Lartey

Larry L Klein

Ramin Faghih

David J Grampovnik

Hugh N Nellans

Clarence J Maring

Ming Clinton Yeung

Sheela A Thomas

David A Riley

David A Degoey

William Rosenbrook, Jr

Christina Louise Leone

Daniel T Chu

James B McAlpine

Leslie A Freiberg

Jill E Hochlowski

Richard J Pariza

Marianna Jackson

Carla M Edwards

Leping Li

Clinton M Yeung

Neal S Burres

Lisa A Alder

Shari DeNinno

Albert Christian Petersen

Hugh Nerby Nellans

Cynthia Burnell Curty

4'-Deoxy derivatives of erythromycin having the Formula (I) ##STR1## and pharmaceutically acceptable salts thereof, which are enhancers of gastric motility but have minimal antibacterial activity, as well as pharmaceutical compositions containing the same and methods for their use and preparation.

4'-deoxyerythromycin derivatives

A process for preparing a compound having the formula: ##STR1## wherein R is selected from the group consisting of C.sub.3 -C.sub.6 -cycloalkyl, C.sub.3 -C.sub.6 -cycloalkylmethyl, C.sub.1 -C.sub.6 -alkyl, allyl and 2-methoxyethyl, by reacting: ##STR2## under defined conditions with subsequent stepwise reactions of the respective intermediate compounds with a malonic acid diester, POCl.sub.3, and by heating the final intermediate in a high boiling solvent.

Process for preparing 1-substituted

Novel antifungal agents having the formula: ##STR1## wherein R is hydrogen or --C(O)--R.sub.1 wherein R.sub.1 is alkenyl, C.sub.2 -C.sub.12 -alkyl, aryl, arylalkenyl, arylalkyl, aryl-aryl-, arylalkoxy-aryl-, aryloxyl-aryl-, aryl-aryl-aryl- or arylalkoxy-aryl-aryl-, or pharmaceutically acceptable salts, esters or prodrugs thereof, as well as (i) pharmaceutical compositions comprising such compounds, (ii) methods of treatment using such compounds, and (iv) methods and fungal cultures useful in making the same.

Antifungal fusacandins

Novel macrocyclic 13-membered ring-contracted compounds derived from erythromycins A and B having the Formula (I) ##STR1## and pharmaceutically acceptable salts thereof, wherein R, R.sup.1, R.sup.2, R.sup.3 and X are specifically defined, having use in treating gastrointestinal disorders associated with hypermotilinemia, pharmaceutical compositions thereof, a method of treating gastrointestinal disorders associated with hypermotilinemia with said pharmaceutical compositions, and processes for the preparation thereof.

Macrocyclic 13-membered ring derivatives of erythromycins A and B

Disclosed are novel antifungal agents having the formula: ##STR1## or a pharmaceutically acceptable acid, ester or prodrug thereof, wherein preferred compounds include those compounds wherein R.sub.1 is selected from the group consisting of --NH.sub.2 ; R.sub.2 is selected from the group consisting of hydrogen, fluoro, and hydroxyl; R.sub.3 is selected from the group consisting of --CH.sub.2 (p-C.sub.6 H.sub.4).sub.3 O(CH.sub.2).sub.3 CH.sub.3, --CH.sub.2 (p-C.sub.6 H.sub.4)O(CH.sub.2).sub.6 CH.sub.3, --COO(p-C.sub.6 H.sub.4)O(CH.sub.2).sub.6 CH.sub.3, --CO(Piperazinyl)(p-C.sub.6 H.sub.4).sub.2 OCH.sub.3, --CO(p-C.sub.6 H.sub.4)O(CH.sub.2).sub.6 CH.sub.3, --CO(p-C.sub.6 H.sub.4)(Piperazinyl)(p-C.sub.6 H.sub.4)O(CH.sub.2).sub.4 CH.sub.3, --CO(p-C.sub.6 H.sub.4)(Piperazinyl)(p-C.sub.6 H.sub.4)O(CH.sub.2).sub.6 CH.sub.3, --CO(p-C.sub.6 H.sub.4)(Piperazinyl)(p-C.sub.6 H.sub.4)OCH.sub.3, and --CO(p-C.sub.6 H.sub.4)(Piperazinyl)O(CH.sub.2).sub.6 CH.sub.3 ; and R.sub.4 is selected from the group consisting of --CH(OH)CH.sub.3, --CH.sub.2 OH, --CH.sub.2 CH.sub.3, --CH.sub.2 CH.sub.2 CH.sub.2 NH.sub.2, --CH.sub.2 (CH.sub.2)NH.sub.2, --CH.sub.2 NH.sub.2, --CH.sub.2 (CH.sub.2).sub.2 (NH)C.dbd.(NH)--NH.sub.2, --CH.sub.3, --CH.sub.2 (Ph)OH, hydrogen, --CH.sub.2 CH.sub.2 COOH, and --CH.sub.2 COOH. Also disclosed are pharmaceutical compositions containing such compounds and the use of the same in the treatment of fungal infections.

Amino-lipopetide antifungal agents

Process for preparing 4-deoxyerythromycin derivatives

Antibacterial compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein Y is selected from ##STR2## and X is selected from the group consisting of --C(O)--, --C(S)--, --CH.sub.2 --, --CH.sub.2 CH.sub.2 -- and --C(CH.sub.3).sub.2 --; also disclosed are processes and intermediates useful in the preparation of the above compounds, as well as compositions containing the same and methods for their use.

Erythromycin derivatives

Antibacterial compounds are disclosed having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sup.1 is --NR.sup.4 R.sup.6, where R.sup.4 and R.sup.6 are independently selected from the group consisting of hydrogen, loweralkyl and arylalkyl or, together, R.sup.4 and R.sup.6 form a nitrogen-containing heterocycle attached at the nitrogen atom; R.sup.2 is selected from the group consisting of hydrogen, --OH and, when R.sup.3 is methylene, oxygen so as to form an epoxide; and R.sup.3 is selected from the group consisting of --CH.sub.2 OH, --NR.sup.4 R.sup.6, --(CH.sub.2).sub.n NR.sup.4 R.sup.6 and, when R.sup.2 is oxygen, methylene so as to form an epoxide, where n is 1-4 and R.sup.4 and R.sup.6 are as previously defined, with the proviso that when R.sup.2 is --OH, R.sup.3 may not be --NR.sup.4 R.sup.6 ; or R.sup.2 and R.sup.3 together are.dbd.CH.sub.2. Also disclosed are processes and intermediates useful in the preparation of the above compounds, as well as compositions containing the same and methods for their use.

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

Semisynthetic antibiotics with improved therapeutic properties are disclosed. In particular, 9-R-azacyclic derivatives of erythromycin, its derivatives, and their salts and esters show superior antimicrobial activity compared to other macrolide compounds.

9-R-azacyclic erythromycin antibiotics

Aminodeoxy derivatives of 3-deoxy-D-manno-2-octulosonic acid (KDO) are potent inhibitors of bacterial enzymes and a novel class of antibacterial agents.

Amino D-manno-2-octulopyranosidonate containing compounds,

Derivatives of 3-deoxy-D-manno-2-octulosonic acid (KDO) are potent inhibitors of bacterial enzymes and a novel class of antibacterial agents.

D-manno-2-octulosonic acid derivatives, pharmaceutical compositions and

Described is a method of O-demethylating a fortimicin compound using hydriodic acid or tri-methylsilyiodide as an O-demethylating agent.

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Wadsworth, IL, United States of America

Paul A Lartey