Compositions and methods for reducing body fat
Inventors
Grosskreutz, Cynthia L. • Pasquale, Louis R. • Singer, Michael S. • Kalayoglu, Murat V.
Assignees
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Publication Number
US-10285995-B2
Publication Date
2019-05-14
Expiration Date
Abstract
The present invention relates to compositions, such as bimatoprost, latanoprost and travoprost, and methods to reduce fat in the body of an individual, for example, by topical administration, injection, and/or implantation of such compositions.
Core Innovation
The invention relates to compositions and methods for reducing fat in the body of a subject using a compound of Formula (I), or a pharmaceutically acceptable salt thereof. The compound is defined by structural variables including dashed bonds represent a single or double bond that can be in the cis or trans configuration, and specific substituent definitions for radicals A, B, X, Z, and R group substituents, with defined constraints on whether substituents such as R1 and R2 are oxygen, hydroxyl, or -O(CO)R6.
The invention further encompasses related compound embodiments defined by additional formula sets, including Forms II–VIII and specified analogs and esters, with stereochemical conventions such as cis/trans configuration and α/β configuration, and conditional exclusions for certain structural combinations. The compounds are asserted to act through prostaglandin/prostaglandin-like receptor agonism consistent with prostamide and prostaglandin F2α receptor agonists, with described effects including reduced fat cell viability and/or number, reduced fat cell volume, reduced maturation, and/or dedifferentiation.
The method is implemented by administering the compound to the skin of the subject in a localized, non-systemic manner. Documented administration modes include topical to the skin, injection into fat deposits, and implantation of an implantable depot, supported by formulation and dosage form concepts such as ointment, lotion, cream, patch, transdermal system, and sustained-release depots.
Claims Coverage
The document provides one independent claim directed to a method of reducing fat by administering a Formula (I) compound to skin, with multiple dependent claims that narrow compound definitions and localized administration parameters. Across the independent claim, the key inventive concept is the specific Formula (I) structural definition combined with skin administration for fat reduction, with dependent claims further refining the structural scope and delivery and area constraints.
Skin administration of a Formula (I) fat-reducing compound
A method for reducing fat in the body of a subject, the method comprising administering to the skin of the subject a compound of Formula (I) or a pharmaceutically acceptable salt thereof, where the structural features include cis/trans configuration for dashed bonds and defined radicals A, B, X, and Z, with specified R-substituent definitions and constraints including the relationship between R1 and R2 and Z/X conditional possibilities.
Topical, injection, or depot delivery for localized fat reduction
The skin-administered method includes delivering the compound by topical application to the skin, injection into the skin, or implantation of a depot containing the compound.
Localized area selection from defined body regions
The skin-administered method further includes administering the compound to a localized area selected from a listed set of body regions.
Overall, claim coverage centers on reducing body fat via skin administration of a Formula (I) compound with constrained substituent definitions and cis/trans structural options. Dependent claim refinements include specific delivery modalities and defined localized body-area selection.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Obesity.
Cushing syndrome fat deposits.
HIV lipodystrophy.
Local cosmetic fat reduction.
Graves’ orbitopathy.
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