J-series prostaglandin-ethanolamides as novel therapeutics for skin and/or oral disorders
Inventors
Assignees
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Publication Number
US-10960013-B2
Publication Date
2021-03-30
Expiration Date
Abstract
Provided is a method of preventing and/or treating a skin disorder and/or an oral disorder including administering to a subject in need thereof an effective amount of a compound of formula (I) or a prodrug or derivative thereof, and salts thereof.
Core Innovation
The document describes 15-deoxy Δ12,14-PGJ2-ethanolamide (15dPMJ2), its prodrugs and derivatives, and salts as endoplasmic reticulum (ER)-stress-inducing agents. The proposed approach uses elevated endogenous ER stress in diseased or tumor cells to cross a cell-death threshold, with the stated aim of selectively killing those cells while limiting harm to normal cells.
The claimed method treats melanoma by administering an effective amount of a compound of formula (I) or formula (II), a salt thereof, or a combination thereof. The document also describes ER-stress-related cell death and reports reduced melanoma tumor weight with increased CHOP10 expression in treated mice. The background section is not included in the provided content, so the problem it identifies is not explicitly described.
Claims Coverage
The provided relevant claims identify one independent claim directed to a method of treating melanoma, accompanied by six inventive features detailing administration and formulation specifics.
Treating melanoma with compounds of formula (I) or (II)
Claim 1 recites a method of treating melanoma by administering to a subject in need thereof an effective amount of a compound of formula (I) or formula (II), a salt thereof, or any combination thereof.
Topical administration
A dependent claim specifies topical administration.
Melanoma associated with ER stress
A dependent claim specifies melanoma caused by ER stress and/or exhibiting increased ER stress.
ER-stress-dependent cell death
A dependent claim specifies that the method induces cell death through an ER-stress-dependent mechanism.
Pharmaceutical composition with a carrier
A dependent claim specifies administration of a pharmaceutical composition comprising compound of formula (I) and a pharmaceutically acceptable carrier.
Formula (I) or a salt thereof
A dependent claim specifies the compound as formula (I) or a salt thereof.
The claim coverage centers on treating melanoma with formula (I) or formula (II), a salt, or a combination, with dependent refinements specifying topical administration, ER-stress conditions, an ER-stress-dependent cell-death mechanism, and formulation details.
Stated Advantages
Selective killing of diseased or tumor cells by exploiting their elevated endogenous ER stress, while limiting harm to normal cells.
Greater toxicity in tumorigenic than non-tumorigenic keratinocytes.
Significantly reduced melanoma tumor weight and increased CHOP10 expression in treated mice.
Documented Applications
Treatment of melanoma by administering a compound of formula (I) or formula (II), a salt thereof, or a combination thereof.
Topical treatment of human papillomavirus (HPV)-associated cutaneous papillomas.
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