A61P31/10

HYBRID AMPHOTERICIN B DERIVATIVES WITH REDUCED TOXICITY
20230000891 · 2023-01-05 ·

Disclosed are C16 ester derivatives of C2′epi-amphotericin B (C2′epiAmB) characterized by improved clinical efficacy with reduced toxicity compared to AmB. Also disclosed are pharmaceutical compositions comprising the C16 ester derivatives of C2′epiAmB, therapeutic methods of using the C16 ester derivatives of C2′epiAmB, and methods of making the C16 ester derivatives of C2′epiAmB.

ACC INHIBITOR AND USE THEREOF

The present invention provides a compound suitable for use as an acetyl CoA carboxylase (ACC) inhibitor, specifically, a thienopyridine derivative, and use of the compound in the preparation of drugs for treating metabolic disorders, cancers or other proliferative disorders, and nonalcoholic steatohepatitis (NASH).

Hydrogen peroxide-producing bacterial composition
11564785 · 2023-01-31 · ·

The invention provides compositions that include isolated, non-pathogenic, hydrogen peroxide-producing bacterial strains and genetically engineered LDH-deficient bacterial strains, which can be used to whiten teeth and treat periodontal disease.

Peptides and compositions for prevention of cell adhesion and methods of using same
11566054 · 2023-01-31 · ·

Compositions comprising an isolated peptide, which may for example optionally comprise a sequence selected from the group consisting of FDYDWY (SEQ ID NO: 2), SFSQNKSVHSFDYDWYNVSDQADLKN (SEQ ID NO: 3) or CSFSQNKSVHSFDYDWYNVSDQADLKNC (SEQ ID NO: 1), or any cyclized version thereof, and methods of using same, including for treatment of or prevention of formation of microbial biofilms and against adhesion of a cell to a surface.

Compounds for use as inhibitors of alternative oxidase or cytochrome bc1 complex

The invention provides compounds for use in inhibiting a microbial alternative oxidase (AOX) and/or cytochrome bc.sub.1 complex. The invention extends to the use of such inhibitors in agrochemicals and in pharmaceuticals, for treating microbial infections, including fungal infections.

Modified polynucleotides for the production of cytoplasmic and cytoskeletal proteins
11564998 · 2023-01-31 · ·

The invention relates to compositions including polynucleotides encoding polypeptides which have been chemically modified by replacing the uridines with 1-methyl-pseudouridine to improve one or more of the stability and/or clearance in tissues, receptor uptake and/or kinetics, cellular access by the compositions, engagement with translational machinery, mRNA half-life, translation efficiency, immune evasion, protein production capacity, secretion efficiency, accessibility to circulation, protein half-life and/or modulation of a cell's status, function, and/or activity.

Immunorhelin compounds for intracellular infections

The present invention provides immune stimulating peptides (immunorhelins) capable of activating GnRH receptors when administered to animal or human patients or cells. These immunorhelins have utility in treating intracellular bacterial, fungal, and protozoal infections.

Chloroquine gel and preparation method and application thereof

A product for preventing and treating external genitalia infection and/or flat warts is provided, wherein the product comprises a chloroquine nanosphere. The chloroquine nanosphere comprises a water-soluble nanosphere carrier, and chloroquine or a chloroquine derivative. A mass ratio of the chloroquine or the chloroquine derivative to the water-soluble nanosphere carrier during preparation ranges from 1:3 to 1:5. A loading rate of the chloroquine or the chloroquine derivative in the prepared chloroquine nanosphere ranges from 3.0% to 21.6%. The water-soluble nanosphere carrier is water-soluble chitosan; a deacetylation degree of the water-soluble chitosan ranges from 80% to 95%, and a viscosity-average molecular weight thereof ranges from 3000 to 5000 g/mol. The chloroquine derivative is selected from one or more of hydroxychloroquine, chloroquine phosphate or chloroquine sulfate.

Chloroquine gel and preparation method and application thereof

A product for preventing and treating external genitalia infection and/or flat warts is provided, wherein the product comprises a chloroquine nanosphere. The chloroquine nanosphere comprises a water-soluble nanosphere carrier, and chloroquine or a chloroquine derivative. A mass ratio of the chloroquine or the chloroquine derivative to the water-soluble nanosphere carrier during preparation ranges from 1:3 to 1:5. A loading rate of the chloroquine or the chloroquine derivative in the prepared chloroquine nanosphere ranges from 3.0% to 21.6%. The water-soluble nanosphere carrier is water-soluble chitosan; a deacetylation degree of the water-soluble chitosan ranges from 80% to 95%, and a viscosity-average molecular weight thereof ranges from 3000 to 5000 g/mol. The chloroquine derivative is selected from one or more of hydroxychloroquine, chloroquine phosphate or chloroquine sulfate.

LIPID DEPOT FORMULATIONS

The present invention relates to pre-formulations comprising low viscosity, non-liquid crystalline, mixtures of: a) at least one neutral diacyl lipid and/or at least one tocopherol; b) at least one phospholipid; c) at least one biocompatible, oxygen containing, low viscosity organic solvent;
wherein at least one bioactive agent is dissolved or dispersed in the low viscosity mixture and wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. The preformulations are suitable for generating parenteral, non-parenteral and topical depot compositions for sustained release of active agents. The invention additionally relates to a method of delivery of an active agent comprising administration of a preformulation of the invention, a method of treatment comprising administration of a preformulation of the invention and the use of a preformulation of the invention in a method for the manufacture of a medicament.