5-substituted 2,4-thiazolidinediones (thiohydantoins), pseudothiohydantoins, and propseudothiohydantoins for use as antiviral agents
Inventors
Assignees
Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-10646477-B1
Publication Date
2020-05-12
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 invention concerns antiviral therapy for persons having viral infections, including infections from herpes simplex viruses (HSV1 or HSV2) and varicella zoster virus (VZV). It is based on administering a therapeutically effective amount of an antiviral agent formulated with a compound of Formula (III), named propseudothiohydantoins, having defined substituent groups R and R1, and including pharmaceutically-acceptable water soluble salts.
Propseudothiohydantoins are defined by a structural formula in which R and R1 are each independently selected from specified groups, including H, F, Cl, CH3, CF3, C1-C6 straight-chain or branched alkyls, and C6-C10 aryl. When R is H and R1 is not H, both R- and S-stereoisomers are included, and water-soluble salts of Formula (III) are included as pharmaceutically acceptable forms.
The described scope includes formulations in pharmaceutically-acceptable forms and salt forms, with particular emphasis on administering the active ingredient as part of a pharmaceutical formulation. The partial content also describes specific compounds identified as JIVA-0042, JIVA-005, JIVA-0043/0044/0045/0046/0048/0049, and notes antiviral findings in vitro against HSV and VZV using plaque/yield reduction and cytotoxicity assays, along with formulation examples such as ophthalmic solution, topical clear gels/creams, ocular solutions, and injection.
Claims Coverage
The independent claim covers a method of treating persons with viral infections (HSV1, HSV2, or VZV) using a therapeutically effective amount of a pharmaceutical formulation whose active ingredient is a propseudothiohydantoin compound of Formula (III), including pharmaceutically-acceptable water soluble salts. The claim set refines this coverage with substituent/salt choices, administration/formulation type, and a chemical purity constraint (at least 95%).
Treating HSV1, HSV2, or VZV with propseudothiohydantoins of Formula (III)
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 (III), named as propseudothiohydantoins, with the specified substituent selections and stereoisomer inclusions, and pharmaceutically-acceptable water soluble salts of Formula (III).
Propseudothiohydantoin with R as H and R1 as F
The method wherein the Formula (III) compound has R as H and R1 as F.
Sodium salt of the selected Formula (III) compound
The method wherein a Formula (III) compound is used where R is H and R1 is F, specifically as its sodium salt.
Therapeutically effective topical, ophthalmic, or systemic formulation types
The method wherein a formulation is suitable for topical application as a clear gel or cream ointment, for use as an ophthalmic solution, or for systemic administration.
Ocular or topical dosage forms with pharmaceutically acceptable adjuvants, binders, diluents, and excipients
The method wherein the formulation is intended for ocular or topical administration and is provided as an ointment, liquid, injection, or related gel or cream forms containing one or more pharmaceutically acceptable adjuvants, binders, diluents, and excipients.
Active compound at least 95% chemical purity
The method wherein the compound has at least 95% chemical purity.
Across the claim set, the core coverage is a therapeutic method for HSV1, HSV2, or VZV that administers a therapeutically effective amount of a pharmaceutical formulation containing propseudothiohydantoins of Formula (III), including water-soluble salts. Dependent refinements narrow the substituent pattern (R=H, R1=F), specify a sodium salt, define topical, ophthalmic, or systemic formulation types, provide examples of ocular or topical dosage forms including excipients and adjuvants, and impose a chemical purity threshold of at least 95%.
Stated Advantages
Documented Applications
No documented applications found
Interested in licensing this patent?