Abstract: A compound having the formula selected from the group consisting of a compound of formula I a compound of formula II a compound of formula III as well as and pharmaceutically acceptable salts, esters, solvates, metabolites, and prodrugs thereof, are useful in treating bacterial infections. Also provided are pharmaceutically acceptible compositions, methods of treating bacterial infections, and processes for the preparation of the compounds.

Abstract: Novel 2-halo-6-O-substituted ketolide derivatives and pharmaceutically acceptable salts and esters thereof having antibacterial activity having a formula ##STR1## compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier, a method for treating bacterial infections by administering to a mammal a pharmaceutical composition containing a therapeutically-effective amount of a compound of the invention, and processes for their preparation.

Abstract: The claimed invention relates to a novel process of preparing N-demethyl-N-alkyl-4"-deoxy erythromycin A and B. The process comprises protecting the 2'-hydroxy or the 2'- and 11-hydroxy of a N-demethyl-4"-deoxy erythromycin derivative having the formula: ##STR1## where R.sub.b is H or OH, with a silyl protecting group and alkylating the N-position of the desosamine sugar.

Abstract: Antimicrobial compounds having the formula ##STR1## as well as the pharmaceutically acceptable salts, esters and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.

Abstract: Antimicrobial compounds having the formula as well as pharmaceutically acceptable sats, esters or prodrugs thereof, pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.

Abstract: The instant invention provides novel macrolide compounds and compositions useful in treating bacterial infections. Also provided are processes for preparing same.

Abstract: Novel 6,11-bridged erythromycin compounds and pharmaceutically acceptable salts and esters thereof having antibacterial activity having a formula ##STR1## compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier, a method for treating bacterial infections by administering to a mammal a pharmaceutical composition containing a therapeutically-effective amount of a compound of the invention, and processes for their preparation.

Abstract: A process for the preparation of 4"-deoxyerythromycins, having the formula: ##STR1## wherein R is H or OH, R.sup.1 is H or loweralkyl, and R.sup.2 is H or CH.sub.3 by treatment of the starting material, 2'-O-acetyl-4"-imidazolylthiocarbamoyl-erythromycin, with a hypophosphite reagent, in a water-miscible protic solvent optionally comprising a phase transfer agent. In a preferred embodiment, the water-miscible solvent is an alcohol and the starting material is reacted with sodium hypophosphite, ACVA and tetra-n-butylammonium hydroxide.

Abstract: The present invention provides a tablet for the controlled release of an active agent comprising (a) a matrix layer comprising an active agent embedded in a non-swelling, non-gelling hydrophobic matrix; (b) a first barrier layer laminated to a single face of the matrix layer; and (c) an optional second barrier layer laminated to the opposite face of the matrix layer and oppositely disposed to the first barrier layer; wherein the matrix comprises up to about 80% active agent and from about 5% to about 80% by weight of nonswellable waxes or polymeric material insoluble in aqueous medium, and the first and second barrier layers independently comprise (1) polymeric material exhibiting a high degree of swelling and gelling in aqueous medium or (2) nonswellable wax or polymeric material insoluble in aqueous medium.

Abstract: Novel 3'-N-modified 6-O-substituted erythromycin ketolide compounds and pharmaceutically acceptable salts and esters thereof having antibacterial activity having a formula ##STR1## compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier, as well as a method for treating bacterial infections by administering to a mammal a pharmaceutical composition containing a therapeutically-effective amount of a compound of the invention.

Abstract: Antimicrobial compounds having the formula ##STR1## as well as pharmaceutically acceptable salts, esters or prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.

Abstract: Disclosed are 3'-N-desmethyl-3'-N-susbstituted-6-O-methyl-11-deoxy-11,12-cyclic carbamate erythrolide A derivatives which are antagonists of luteinizing hormone-releasing hormone (LHRH). Also disclosed are pharmaceutical compositions comprising the compounds, to methods of using the compounds and to the process of making the same.

Abstract: Disclosed is a pharmaceutical composition for extended release of an erythromycin derivative in the gastrointestinal environment. The composition comprises an erythromycin derivative and a pharmaceutically acceptable polymer so that, when ingested orally, the composition induces statistically significantly lower C.sub.max in the plasma than an immediate release composition of the erythromycin derivative while maintaining bioavailability and minimum concentration substantially equivalent to that of the immediate release composition of the erythromycin derivative upon multiple dosing. The compositions of the invention have an improved taste profile and reduced gastrointestinal side effects as compared to those for the immediate release composition.

Abstract: Antibacterial compounds having the formula ##STR1## and the pharmaceutically acceptable salts, esters and amides thereof, as well as pharmaceutical compositions containing such compounds and the use of the same in the treatment of bacterial infections.

Abstract: Disclosed are 3',3'-N-bisdesmethyl-3',3'-N-bis-substituted-6-O-methyl-11-deoxy-11,12-cyc lic carbamate erythromycin A derivatives which are antagonists of lutenizing hormone-releasing hormone (LHRH). Also disclosed are pharmaceutical compositions comprising the compounds, to methods of using the compounds and to the process of making the same.

Abstract: Disclosed are 3'-N-desmethyl-3'-N-substituted-6-O-methyl-11-deoxy-11,12-cyclic carbamate erythromycin A derivatives which are antagonists of lutenizing hormone-releasing hormone (LHRH). Also disclosed are pharmaceutical compositions comprising the compounds, to methods of using the compounds and to the process of making the same.

Abstract: A power transmission mechanism which is adapted to completely interrupt power transmission when a torque exceeds a predetermined value, and which has a simple configuration and is manufactured at low cost, and which is bidirectionally rotatable. When a torque, whose magnitude is not more than the predetermined value, is transmitted from a pulley (1) to a shaft (4), each of three elastic members is accommodated in such a manner as to extend over both of a holding portion (3) of the pulley and a holding part (6) of a hub (5). When an excessive torque, whose magnitude exceeds the predetermined value, is applied to the pulley, deformation of each of the elastic members is gradually enhanced by a compressive force applied from the pulley in a radial direction, so that each of the elastic members moves in the radial direction. Then, each of the elastic members further advances and is detached from a corresponding one of the holding portion of the pulley.

Abstract: The present invention concerns the novel antiobiotic 6-O-methylerythromycin A form O solvate, a process for its preparation, pharmaceutical compositions comprising this compound and a method of use as a therapeutic agent.

Abstract: A process of preparing a 6-O-alkyl derivative of 9-oxime erythromycin B is provided. Intermediates used in the preparation of a 6-O-alkyl 9-oxime erythromycin B are also provided. Pharmaceutical compositions containing a 6-O-alkyl derivative of 9-oxime erythromycin B and the use of those compositions to treat bacterial infections are also provided.

Abstract: Disclosed are 9-hydrazone erythromycin and 9-azine erythromycin derivatives and the processes for making the same. The compounds are useful intermediates for conversion into 6-O-alkyl erythromycin. Also disclosed are the processes for converting the compounds into 6-O-alkyl erythromycin.