Composition comprising selenazol or thiazolone derivatives and silver and method of treatment therewith

Inventors

Holmgren, ArneLu, Jun

Assignees

Thioredoxin Systems AB

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Publication Number

US-10058542-B1

Patent

Publication Date

2018-08-28

Expiration Date


Abstract

A method for treating a prokaryotic infection in an animal or human by administering a pharmaceutically acceptable composition, comprising administering a source of silver ions and a benzoisoselenazol derivative, e.g., an ebselen derivative.

Core Innovation

The invention relates to a composition for treating a prokaryotic infection in an animal or human. The composition includes a unit dosage form adapted for administration enterally or by application to skin or mucous membranes, and the unit dosage form comprises at least one compound according to Formula I or a pharmaceutically acceptable salt thereof in an amount of at least 25 mg.

The compound according to Formula I is an inhibitor of prokaryotic thioredoxin reductase having an IC50 of less than about 25 bcM. The composition further comprises an effective amount of a source of at least one metal ion, and the composition is arranged so that a dose-dependent 33% reduction in the inhibitory concentration (IC50) for E. coli thioredoxin reductase is achieved for the at least one compound in the absence of the source of the at least one metal ion.

The composition is defined such that the at least one compound according to Formula I is synergistic with the source of the at least one metal ion with respect to inhibition of prokaryotic thioredoxin reductase. The at least one compound and the metal-ion source are each present in a sufficient amount to treat the prokaryotic infection by administration of the unit dosage form, and the composition also includes a pharmaceutically acceptable carrier.

Claims Coverage

One independent claim is provided, centered on a Formula I thioredoxin reductase inhibitor combined with a synergistic metal-ion source for treating prokaryotic infection.

Prokaryotic infection treatment using Formula I thioredoxin reductase inhibitors with metal-ion synergy

A composition for treating a prokaryotic infection in an animal or human with a unit dosage form adapted for administration enterally or by application to skin or mucous membranes, comprising at least one compound according to Formula I or a pharmaceutically acceptable salt thereof in an amount of at least 25 mg, wherein the compound is an inhibitor of prokaryotic thioredoxin reductase having an IC50 of less than about 25 bcM, and further comprising an effective amount of a source of at least one metal ion to achieve a dose-dependent 33% reduction in IC50 for E. coli thioredoxin reductase, where the compound is synergistic with the metal-ion source with respect to inhibition, with both present in sufficient amounts to treat the prokaryotic infection, and a pharmaceutically acceptable carrier.

The claim coverage combines a Formula I thioredoxin reductase inhibitor and a metal-ion source in a unit dosage form for treatment of prokaryotic infection, with stated synergy and a dose-dependent reduction in IC50.

Stated Advantages

A dose-dependent 33% reduction in IC50 for E. coli thioredoxin reductase is achieved with the compound being synergistic with the metal-ion source.

Documented Applications

Treating a prokaryotic infection in an animal or human using a unit dosage form adapted for administration enterally or by application to skin or mucous membranes.

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