Treatment of adipocytes
Inventors
Reaume, Andrew G. • Cong, Weina • Greenway, Frank • Coulter, Ann
Assignees
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Publication Number
US-12064432-B2
Publication Date
2024-08-20
Expiration Date
Abstract
The present disclosure provides compositions comprising a lyn kinase activator and TRPM8 agonist, and to methods of: reducing blood glucose levels, weight gain, or fat depot levels; treating metabolic syndrome, Syndrome X, obesity, prediabetes, type II diabetes, type I diabetes; treating hypercholesterolemia, hypertension, coronary heart disease, diabetic neuropathy, lipodystrophy, diabetic retinopathy, erectile dysfunction, kidney disease, dyslipidemia, dyslipoproteinemia, a peroxisome proliferator activated receptor-associated disorder, septicemia, a thrombotic disorder, or pancreatitis; inducing the beiging of adipocytes; and preventing pancreatic beta cell degeneration.
Core Innovation
The patent describes lyn kinase activator compounds and their use in combination with a TRPM8 agonist for treating mammals. The TRPM8 agonist is menthol, and other TRPM8 agonists are also described as alternatives, including icilin, WS3, and WS23. The lyn kinase activator is described by a broad structural formula, including pharmaceutically acceptable salts and related variants such as stereoisomers, diastereomers, optical stereoisomers, prodrugs, hydrates, solvates, and isotopes.
The combination is presented as a pharmaceutical composition comprising a therapeutically effective amount of one or more lyn kinase activators and one or more TRPM8 agonists, together with pharmaceutically acceptable carriers and excipients. Representative combinations include Compound 102 together with menthol, and the document also describes lyn kinase activator compound examples including WS 3 and WS 23.
The document further states that the combination is used in treating a mammal in need thereof. Explicit therapeutic indications include hypertension, coronary heart disease, diabetic neuropathy, lipodystrophy, and pancreatitis, with overlap among the independent claims.
Claims Coverage
The consolidated document provides two independent method claims covering treatment by administering an effective amount of a lyn kinase activator and a TRPM8 agonist, where the TRPM8 agonist is menthol and the lyn kinase activator is defined by a formula or a pharmaceutically acceptable salt. Across the independent claims, the inventive features center on the defined lyn kinase activator, menthol as the TRPM8 agonist, and specified therapeutic indications in a mammal.
Treatment by co-administering a lyn kinase activator and menthol
A method of treating hypertension, coronary heart disease, diabetic neuropathy, lipodystrophy, or pancreatitis in a mammal in need thereof, comprising administering an effective amount of a lyn kinase activator and a TRPM8 agonist, wherein the TRPM8 agonist is menthol.
Defined lyn kinase activator by formula or pharmaceutically acceptable salt
The lyn kinase activator is of formula or a pharmaceutically acceptable salt thereof.
Treatment by co-administering a lyn kinase activator and menthol for a narrowed indication set
A method of treating hypertension, coronary heart disease, diabetic neuropathy, or lipodystrophy in a mammal in need thereof, comprising administering an effective amount of a lyn kinase activator and a TRPM8 agonist, wherein the TRPM8 agonist is menthol.
The independent claims center on administering an effective amount of a formula-defined lyn kinase activator, or pharmaceutically acceptable salt, together with menthol as the TRPM8 agonist for treating specified cardiovascular, metabolic, and related conditions in mammals.
Stated Advantages
The document describes in vitro and in vivo support for effects on fasting glucose and body weight loss.
The document describes associations with beige adipocyte-related gene/protein expression and TRPM8 receptor involvement.
The document describes synergy between menthol and Compound 102.
Documented Applications
Treating hypertension in a mammal.
Treating coronary heart disease in a mammal.
Treating diabetic neuropathy in a mammal.
Treating lipodystrophy in a mammal.
Treating pancreatitis in a mammal.
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