C07K9/008

CYCLIC PEPTIDE-N-ACETYLGALACTOSAMINE (GALNAC) CONJUGATES FOR DRUG DELIVERY TO LIVER CELLS

A conjugate comprising a cyclic peptide scaffold and one or more N-acetylgalactosamine (GalNAc) moieties. The conjugate may further carry a diagnostic or therapeutic agent for use in delivering the agent to liver cells. In some embodiments, the cyclic peptide may have 4-10 amino acid residues. The GalNAc moieties can be covalently bound to the cyclic peptide scaffold via a first linker and the agent can be covalently bound to the cyclic peptide scaffold via a second linker.

VANCOMYCIN DERIVATIVE, PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE THEREOF
20190153036 · 2019-05-23 ·

Provided are a class of vancomycin derivatives with a structure as shown in the general formula below and pharmaceutically acceptable salts thereof, a preparation method, a pharmaceutical composition containing the compound thereof, and the use of these compounds in preparing drugs for treating and/or preventing bacterial infection diseases, in particular drugs for treating infection diseases caused by Gram-positive bacteria.

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Site-selective functionalization of glycopeptide antibiotics
10294275 · 2019-05-21 · ·

Site-selective functionalized glycopeptide antibiotics, methods of making and using are described herein. The compounds exhibit improved activity against methicillin-susceptible S. aureus (MSSA), methicillin-resistant S. aureus (MRSA), vancomycin-sensitive S. aureus (VSE), vancomycin-resistant enterococci (VRE), or combinations thereof. The compounds can be administered as the neutral free acid or free base or can be administered as a pharmaceutically acceptable acid-addition or base-addition salt. The compounds can be formulated with one or more pharmaceutically acceptable excipients to prepare pharmaceutical compositions. The compounds can be administered by a variety of routes of administration including enteral, parenteral, topical, or transmucosal.

NOVEL FORMULATION OF PEGYLATED-LIPOSOME ENCAPSULATED GLYCOPEPTIDE ANTIBIOTICS

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.

Superficially porous particle (SPP) chiral phases for liquid chromatography
10272364 · 2019-04-30 · ·

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.

Technology for the Preparation of Microparticles
20190060239 · 2019-02-28 ·

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.

USE OF TEICOPLANIN AGAINST EBOLA VIRUS
20180353568 · 2018-12-13 · ·

The present invention discloses a use of teicoplanin against Ebola virus, and discloses a drug inhibiting an envelope protein GP that comprises the teicoplanin.

Separation and purification method for vancomycin hydrochloride of high purity

Provided is a separation and purification method for vancomycin hydrochloride of high purity. The method comprises the following steps: (1) obtaining a vancomycin hydrochloride solution from a crude vancomycin product by ion exchange chromatography and obtaining a concentrate by nanofiltration desalination and concentration; (2) adjusting the concentrate with a hydrochloric acid solution and then performing a column chromatography using a reverse chromatography column for the adjusted concentrate; (3) collecting the chromatographic solution of vancomycin to obtain a mixed chromatographic solution; (4) adjusting the mixed chromatographic solution, and separating the solution and the salts by nanofiltration desalination and concentration to obtain a concentrate; and (5) obtaining a vancomycin dry powder with a chromatographic purity of up to 99% and a pure white appearance by dehydrating and drying the concentrate of step (4), or by solvent crystallization or salting-out crystallization.

MACROCYCLIC BROAD SPECTRUM ANTIBIOTICS

Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.

Selective arylation of dichalcogenides in biomolecules

Disclosed are chemical transformations for the conjugation of unprotected peptide biomolecules. The disclosed chemical transformations relate to methods of selective cysteine and selenocysteine functionalization of unprotected peptide and protein molecules. The processes feature several significant advantages over existing methods of peptide modification, including specificity towards selenocysteine over other nucleophiles (e.g., amines, hydroxyls), excellent functional group tolerance, and mild reaction conditions. Also disclosed are syntheses of arylated cysteine and arylated selenocysteine peptide compounds.