The present invention relates to compounds that are cationic vancomycin analogs and their compositions. Method of making the compounds and their use as medicament for the treatment of bacterial infection are also disclosed.

The present invention provides a glycopeptide compound or pharmaceutically acceptable salt thereof as shown in Formula (I) or (II), and a method for preparing same, and pharmaceutical compositions and applications thereof, wherein the definition of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 is the same as that of the specification. The glycopeptide compound of the present invention has in-vitro antibacterial activity and has important significance for development of new antibacterial agents. ##STR00001##

Microspheres are produced by contacting a solution of a macromolecule or small molecule in a solvent with an antisolvent and a counterion, and chilling the solution. The microspheres are useful for preparing pharmaceuticals, nutraceuticals, cosmetic products and the like of defined dimensions.

The invention is directed to glycopeptide antibiotics and their aglycones that are engineered to overcome bacterial resistance by replacement of a single, specific peptide carboxamide group in the core peptide of the glycopeptide antibiotic with an amidine group. The amidine pseudopeptide analog of the glycopeptide is effective in killing vancomycin-resistant bacteria at therapeutically achievable concentrations in a patient. For example, a [[C(NH)NH]Tpg.sup.4]-vancomycin aglycon designed to exhibit the dual binding to D-Ala-D-Ala and D-Ala-D-Lac needed to reinstate activity against vancomycin-resistant bacteria has been shown to overcome a common mode of bacterial resistance to the last resort antibiotics of the glycopeptide class. The pseudopeptide amidine analogs can be prepared from corresponding pseudopeptide thioamide analogs, which can be prepared synthetically, semi-synthetically, or biosynthetically.

The present invention discloses a cyclopeptide glass and a pharmaceutical composition glass containing a cyclopeptide. The cyclopeptide glass of the present invention can simultaneously exert efficacy and function as a drug adjuvant. Compared with crystals and traditional drug dosage forms or adjuvants, the cyclopeptide glass effectively increases a drug dissolution rate, improves drug bioavailability, and may be widely used in the fields of drug delivery and sustained release for resistance to tumors, resistance to viruses/bacteria, blood sugar control, immune regulation, neuromodulation, etc.

This invention is directed to a novel method of treating an individual suffering from a bacterial infection, such as bacterial infections of various tissues or organs of an individual. In general, the method of treatment involves administering to an individual a pharmaceutical formulation that comprises a liposome-encapsulated antimicrobial agent, wherein polyethylene glycol (PEG) molecules are covalently attached to the surface of the liposomes.

The invention concerns agents with antibacterial activity, their production and use in the treatment of bacterial infections in animals, including man. The agents are derivatives of vancomycin-type antibiotics, of structure XW-L-V, wherein X is hydrogen, acetyl or a lipophilic membrane-insertive element, W is a basic peptide or basic amino acid; L is a linking group and V is a glycopeptide moiety which inhibits peptidoglycan biosynthesis in bacteria.

The present invention relates to a novel stationary phase support for liquid chromatographic chiral separations. The specific combination of the special underlying support material and certain classes of known chiral selectors according to the invention produces far superior chiral (enantiomeric) separations than those obtained on any conventionally known supports. These chiral (enantiomeric) separations are enhanced in terms of significantly higher efficiencies (theoretical plate numbers), higher resolutions (R.sub.s), shorter retention times and either equivalent or slightly higher selectivities than those obtained on conventional supports.

The invention provides methods for drying dalbavancin. The method includes providing wet dalbavancin that includes dalbavancin, water, and a solvent. The wet dalbavancin is dried at at a temperature of about 30 C. or less, at a vacuum pressure of about 50 mbar or less, until the water level of the wet dalbavancin is less than about 20% (w/w). Water is then added to the dalbavancin and the resulting wet dalbavancin is dried at least once more at a temperature of about 30 C. or less, at a vacuum pressure of about 50 mbar or less, until the solvent level of the dalbavancin is less than about 3.0% (w/w).

Drug substance preparations of oritavancin having high purity are disclosed, along with pharmaceutical compositions comprising such oritavancin drug substance preparations, and drug products or dosage forms comprising such pharmaceutical compositions.