Compounds for treatment of metabolic syndrome
Inventors
AGREDA NAVAJAS, Juan Carlos • Kassuya, Roberto Mikio
Assignees
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Publication Number
US-9440966-B2
Publication Date
2016-09-13
Expiration Date
Abstract
Present invention refers to new compounds of formula I or II, its synthesis and its use in the treatment of metabolic syndrome, particularly for the treatment of type I or type II diabetes and/or metabolic syndrome or metabolic disease or metabolic disorders.
Core Innovation
The invention relates to β-carbolinic compound scaffolds and pyrido[3,4-b]indole-3-carboxamide derivatives as agents for metabolic syndrome. The description provides general formula I and substitution definitions for R1–R8, and general formulas II and III are also mentioned, together with pharmaceutically acceptable salt forms and composition contexts.
The document discloses preferred embodiments by name, including 4a, 5a, 7a, 21a/21b/21e/23a–23f/26b, and other preferred compounds. It also describes hydrochloride salt embodiments, compounds bearing an N-(2-aminoethyl) substituent and aryl ring substituents such as hydroxy, methoxy, ethoxy, fluoro, methyl, and methoxyethyl, as well as compounds 25a/25b to HCl salts 26a/26b and products bearing an ethylenediamine functionality.
The invention further states that the compounds and pharmaceutically acceptable salts are used for treating and/or preventing metabolic syndrome and related conditions, including diabetes, hypertension, hyperlipidemia/hypercholesterolemia/hypertriglyceridemia, and obesity/overweight. Pharmaceutical, cosmetic, and functional food/nutraceutical compositions, medicament-related manufacturing uses, and composition contexts with optional inert carriers or excipients are described.
Claims Coverage
The independent claim coverage centers on 1 inventive feature: a compound of formula I and pharmaceutically, cosmetically or food grade acceptable salt forms. A dependent refinement adds a pharmaceutical composition context with an optional inert compound, carrier, or excipient.
β-Carbolinic compound of formula I with acceptable salt forms
A compound of formula I and any pharmaceutically, cosmetically or food grade acceptable salt thereof.
Pharmaceutical composition with optional inert carrier or excipient
A pharmaceutical composition comprising at least one compound according to formula I and/or pharmaceutically acceptable salts or combinations, and optionally an inert compound, carrier or excipient.
Overall, the claims cover β-carbolinic compounds and pyrido[3,4-b]indole-3-carboxamide derivatives defined by formula I and acceptable salt forms, with additional pharmaceutical composition coverage that optionally includes an inert carrier or excipient.
Stated Advantages
Used for treating and/or preventing metabolic syndrome and related conditions including diabetes, hypertension, hyperlipidemia/hypercholesterolemia/hypertriglyceridemia, and obesity/overweight.
Documented Applications
Therapeutic use as agents for treating and/or preventing metabolic syndrome and related conditions.
Formulation into pharmaceutical compositions for administration as medicaments.
Cosmetic uses of the compounds and acceptable salt forms.
Functional food and nutraceutical compositions using the compounds and acceptable salt forms.
Oral glucose tolerance tests for compound 7a (ANIS-BZ) and compound 4a (ANIS-NH2), with further in vivo efficacy readouts including blood pressure, plasma cholesterol levels, plasma triglyceride levels, and body weight.
Toxicity/safety studies in Drosophila and mice for the compounds described, with reported statistical outcomes.
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