Abstract: The present invention provides agents having high antimicrobial activity for preventing and treating infectious diseases. Thus, the present invention provides novel cyano-(substituted)-methylenepiperidinophenyl oxazolidinone derivatives, processes for making the compounds, as well as antimicrobial compositions containing said derivatives as active ingredients and methods of treating bacterial infections with the said derivatives.

Abstract: The invention relates to the new arginine salt forms of RS-(±)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, S-(?)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, R-(+)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, a process for their preparation and pharmaceutical formulations which comprise those arginine salt forms as the active ingredient for its use in treating microbial infections.

Abstract: The present invention provides agents having high antimicrobial activity for preventing and treating infectious diseases. Thus, the present invention provides novel cyanoalkylpiperidinophenyl oxazolidinone derivatives having antimicrobial activity, favourable pharmacokinetic and safety profiles, processes for making the compounds, as well as antimicrobial compositions containing said derivatives as active ingredients and methods of treating microbial infections with the said derivatives.

Abstract: This invention relates to topical compositions of an antibacterial benzoquinolizine-2-carboxylic acid, incorporated either as the single therapeutic ingredient in hitherto undescribed pharmaceutical compositions, or as an ingredient in novel combination with at least one agent selected from a retinoid, an antifungal agent, another antibacterial compound and/or a steroid/non-steroid anti-inflammatory agent, to processes for preparation of the compositions, to use of the compositions in preparation of a medicament, and to a method of therapeutic or prophylactic use of such a composition for the treatment of dermal, ophthalmic, otic and nasal infections, with or without attendant inflammation.

Abstract: The present invention relates to a pharmaceutical composition in aqueous solution form useful for parenteral application to a subject for treatment or prevention of infective disease. In particular the present invention relates to such a composition having as an active agent S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid 0.2 hydrate or S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid arginine salt or a benzoquinolizine-2-carboxylic acid antibiotic drug. The field of the invention also includes processes for the preparation of such a composition, the use of such a composition in preparation of a medicament, and to the therapeutic or prophylactic use of such a composition.

Abstract: A unit-dose pharmaceutical composition for the treatment of non-insulin dependent diabetes mellitus includes a combination of glimepiride and a thiazolidinedione insulin sensitizer, providing for the simultaneous release of each drug at rates substantially similar to those obtained with the separate administration of immediate release dosage forms of glimepiride and the thiazolidinedione. In addition, processes for the preparation of such combination unit-dose compositions and the use of such compositions for improving glycemic control are described.

Abstract: The invention relates to the new arginine salt forms of RS-(±)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, R-(+)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, a process for their preparation and pharmaceutical formulations which comprise those arginine salt forms as the active ingredient for its use in treating microbial infections.

Abstract: The present invention provides agents having high antimicrobial activity for preventing and treating infectious diseases. Thus, the present invention provides novel cyano-(substituted)-methylenepiperidinophenyl oxazolidinone derivatives, processes for making the compounds, as well as antimicrobial compositions containing said derivatives as active ingredients and methods of treating bacterial infections with the said derivatives.

Abstract: The invention relates to the new arginine salt forms of RS-(±)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, R-(+)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, a process for their preparation and pharmaceutical formulations which comprise those arginine salt forms as the active ingredient for its use in treating microbial infections.

Abstract: A stable unit-dose combination composition for the simultaneous delivery of a short-acting oral hypoglycemic biologically active agent (such as, for example, repaglinide or nateglinide), and a long-acting oral hypoglycemic biologically active agent (such as, for example, metformin). Such a composition can be used for the treatment of non-insulin dependent diabetes mellitus (NIDDM) and the improvement of glycemic control.

Abstract: The invention relates to the new arginine salt forms of RS-(±)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, R-(+)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, a process for their preparation and pharmaceutical formulations which comprise those arginine salt forms as the active ingredient for its use in treating microbial infections.

Abstract: A pharmaceutical composition suitable for a once-a-day dosing regimen includes a combination of a biguanide and a sulfonylurea in the form of a multiparticulate, polyphasic system for the treatment of non-insulin dependent diabetes mellitus (NIDDM) and for improving glycemic control.

Abstract: An oral delivery system for the treatment of non-insulin dependent diabetes mellitus in humans includes a pharmaceutically effective amount of a biguanide and a water-insoluble polymeric carrier, providing for a controlled release of the biguanide independent of environmental pH. In addition, a layer including a glitazone or sulfonylurea can be included in the oral delivery system, while still providing for a pH-independent, controlled release of biguanide over an extended period of time.

Abstract: A ready-to use, stable, gelled polymer droplet-in-oil dispersion is described which helps in in-situ formation of a multitude of small solid, semisolid, or gelled microcarriers. The dispersion is placed into a body in a semisolid form and cures to form the delivery system in-situ. The process for making such a dispersion comprises the steps of (i) dissolving a polymer in a biocompatible solvent at an elevated temperature to form a polymer solution, (ii) preparing a second oil phase solution of a biocompatible oil and a biocompatible emulsifier at an elevated temperature, (iii) mixing the polymer solution with the oil phase solution at an elevated temperature and subsequently cooling to refrigeration temperature. Placing the gelled dispersion within a body produces the microcarrier delivery system in-situ.