5-substituted 2,4-thiazolidinediones (thiohydantoins), pseudothiohydantoins, and propseudothiohydantoins for use as antiviral agents
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Publication Number
US-11202774-B2
Publication Date
2021-12-21
Expiration Date
Abstract
The present invention concerns the synthesis and use of formulations of 5-substituted 2, 4-thiazolidinediones, pseudothiohydantoins, and propseudothiohydantoins and 2, 4-thiazolidinediones metforminate salts for topical and systemic treatments of infections caused by herpes simplex viruses and varicella zoster viruses.
Core Innovation
The patent describes 5-substituted 2,4-thiazolidinediones, also referred to as thiohydantoins, and 5-substituted pseudothiohydantoins, also referred to as 2-iminothiohydantoins, and propseudothiohydantoins. The disclosed compounds include metforminates and omega-3 PUFA-derived derivatives and are characterized by the stated formula structures, including Formula I, Formula II, and Formula III. Example compound identities connected to these formulas include JIVA-0042, JIVA-005, JIVA-0043, JIVA-0048, and JIVA-0049.
The disclosure identifies viral infections caused by herpes simplex viruses HSV-1 and HSV-2 and varicella zoster virus VZV as the problem addressed. The patent presents these thiohydantoin and pseudothiohydantoin compound classes as antiviral agents, with reported in vitro antiviral and toxicity findings for specified JIVA compounds. The results include EC50, CC50, and selective index values in connection with HSV-1, HSV-2, and VZV.
The patent further describes pharmaceutical uses and formulation concepts for antiviral treatment using the disclosed compounds. Reported formulation concepts include topical and systemic treatment approaches, including ophthalmic solutions and gels or creams, as well as injection suspensions. The disclosure also includes comparative reference to acyclovir and example identity/formulation pairings for specific JIVA compounds, supporting therapeutic use against HSV-1, HSV-2, and VZV.
Claims Coverage
The independent claim covers a method of treating persons with viral infections caused by HSV1, HSV2, or VZV by administering a therapeutically effective amount of a pharmaceutically-acceptable formulation whose active ingredient is a compound of Formula (II) or a pharmaceutically-acceptable water soluble salt. Dependent claims refine the active compound definition, specific salt forms, chemical purity, and topical administration constraints, forming five inventive feature sets.
Treatment of HSV1/HSV2 or VZV with a Formula (II) antiviral formulation
A method of treating persons who have viral infections comprising administering to such persons having infections from herpes simplex viruses HSV1 or HSV2 or varicella zoster virus VZV a therapeutically effective amount of an antiviral agent as a pharmaceutically-acceptable formulation having as an active ingredient a compound of Formula (II) or pharmaceutically-acceptable water soluble salts thereof, where R and R1 are each independently defined and stereoisomers are included when R is H and R1 is not H.
High chemical purity of the active compound
The method wherein the compound has at least 95% chemical purity.
Metformin salt formulation for herpes simplex virus infections
A method for treating herpes simplex virus infections by administering a therapeutically effective amount of a pharmaceutically acceptable formulation of a metformin salt.
Specific pharmaceutically acceptable water soluble salt forms
The method wherein the pharmaceutically acceptable water soluble salt is selected from hydrochloride, sulfate, acetate, fumarate, maleate, succinate, or ascorbate salts.
Topical ocular herpes genitalis or shingles treatment as solution gel or cream
A method for treating ocular herpes, herpes genitalis, or shingles infections by topically applying a formulation as a solution, gel, or cream over infected areas.
The coverage centers on treating HSV1, HSV2, or VZV using a therapeutically effective amount of a pharmaceutically-acceptable formulation with a Formula (II) active ingredient, including pharmaceutically-acceptable water soluble salts. The dependent claim refinements emphasize specific salt forms, chemical purity, and topical administration for ocular herpes, herpes genitalis, or shingles using solution, gel, or cream formulations.
Stated Advantages
Documented Applications
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