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Publication Number
US-9504695-B2
Publication Date
2016-11-29
Expiration Date
Abstract
Provided are methods, compositions, systems, and kits for treating metabolic syndrome or a disorder associated with metabolic syndrome, e.g., obesity, dyslipidemia, and/or a diabetic condition, comprising administering systemically to a subject one or more compounds of the Formula (I) and/or (II): or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, polymorph, tautomer, isotopically enriched derivative, or prodrug thereof, wherein , L, R1, R2, Z, X, A and B are defined herein.
Core Innovation
The invention relates to prostaglandin-like compounds defined by a compound formula and to a pharmaceutical composition comprising a compound of a prostaglandin-derivative scaffold, including named analogs and derivatives, and pharmaceutically acceptable salts thereof. The compound candidates are defined by Formula (I) and related sub-formulas, with variable substituent definitions including R1, R2, R3/R3′, X, Y, x, y, n, Z, and G.
The disclosed compound definitions include permissible structural variations, including salts, hydrates, solvates, stereoisomers, polymorphs, tautomers, isotopically enriched derivatives, and prodrugs. Double-bond cis/trans or single-bond substitutions are also permitted, and the document includes embodiments in which Z is O or S and G is O or S.
Named examples within the compound family include tafluprost and tafluprost free-acid, bimatoprost and bimatoprost free acid and related forms, travoprost and travoprost free acid, latanoprost and latanoprost free acid, fluprostenol isopropyl ester, AL-16082, AL-12182, and AL-12182 free acid. The document further identifies related subclasses through particular values assigned to y, x, and n, and through structural exemplars in Formula (I-a) through I-f and related variants.
Claims Coverage
The provided independent claim covers a method of reducing body fat by administering to the skin a pharmaceutical composition containing a compound of the specified formula, or a pharmaceutically acceptable salt, in an individual with excess body fat. Dependent claims further refine the eligible condition and the delivery or formulation modalities, including intradermal administration, implantable depot delivery, and sustained-release formulation.
Skin administration for reducing excess body fat
A method comprising administering to the skin of the individual a pharmaceutical composition comprising a compound of the formula, or a pharmaceutically acceptable salt thereof, wherein the individual suffers from an excess of body fat.
Obesity-specific application
The method wherein the individual suffers from obesity.
Subcutaneous fat specificity
The method wherein the body fat includes subcutaneous fat.
Intradermal administration
The pharmaceutical composition is administered intradermally.
Implantable depot delivery
The pharmaceutical composition is administered from an implantable depot.
Sustained-release formulation
The pharmaceutical composition is administered in a sustained-release formulation.
Overall, claim coverage is directed to skin administration of a prostaglandin-derivative formula compound, or pharmaceutically acceptable salt, for excess body fat, with dependent refinements to obesity, subcutaneous fat, intradermal administration, implantable depot delivery, and sustained-release formulation.
Stated Advantages
Reduced obesity or weight gain.
Improvements in serum lipid and glucose-related metrics.
Reducing adipocytes.
Improving serum triglycerides and LDL while increasing HDL.
Reducing serum glucose and improving glucose tolerance and insulin sensitivity.
Reducing body fat in an individual suffering from an excess of body fat.
Documented Applications
Treating or preventing metabolic syndrome and associated disorders.
Reducing body fat in an individual with excess body fat, including individuals suffering from obesity.
Delivery via transdermal administration, intradermal administration, and sustained-release or time-release formulations.
Systemic delivery aimed at metabolic syndrome and obesity outcomes.
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