Treatment of adipocytes

Inventors

Reaume, Andrew G. • Cong, Weina • Greenway, Frank • Coulter, Ann

Assignees

Melior Pharmaceuticals I Inc • Louisiana State University

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 disclosure provides compositions comprising a LYN kinase activator and a TRPM8 agonist. The LYN kinase activator is described as a compound of a stated formula or a pharmaceutically acceptable salt thereof, and the TRPM8 agonist is menthol, with other TRPM8 agonists also mentioned as icilin, WS3, and WS23.

The disclosure states methods of administering an effective amount of a LYN kinase activator together with a TRPM8 agonist in a mammal. The outcomes explicitly include reducing blood glucose levels, weight gain, and fat depot levels, and treating metabolic syndrome, Syndrome X, obesity, prediabetes, type I and type II diabetes, hypercholesterolemia, and dyslipidemia.

The disclosure also includes inducing the beiging of adipocytes and preventing pancreatic beta cell degeneration. It further describes pharmaceutical compositions and kit formats comprising a therapeutically effective amount of a LYN kinase activator and a TRPM8 agonist, including menthol, with a pharmaceutically acceptable carrier, vehicle, or excipient.

Claims Coverage

The independent claims cover combination administration of a LYN kinase activator and a TRPM8 agonist, menthol, to achieve metabolic and cellular outcomes. Across the independent claims, the inventive features are combination administration of a formula-defined LYN kinase activator or pharmaceutically acceptable salt thereof with menthol, and therapeutic use for reducing metabolic measures, inducing adipocyte beiging, or preventing pancreatic beta cell degeneration.

The independent claims consistently require administering a LYN kinase activator defined by a stated formula or pharmaceutically acceptable salt thereof together with menthol as a TRPM8 agonist, with therapeutic purposes focused on metabolic improvements, adipocyte beiging, and prevention of pancreatic beta cell degeneration.

Stated Advantages

Documented Applications