Ohio University

University of Tennessee Research Foundation

Douglas Goetz

Stephen Bergmeier

Frank L Schwartz

Mark C McMills

Kelly D McCall

Leonard D Kohn

Giorgio Napolitano

Ramiro Malgor

Norikazu Harii

Uruguaysito Benavides-Peralta

Mariana Gonzalez-Murguiondo

Christopher J Lewis

Crina M Orac

Stephen C Bergmeier

Mohammad F Kiani

Cina M Orac

Cesidio Giuliani

Nilesh D Dagia

Mark C Mcmills

Compounds having General Formula (I) or General Formula (II): in which Ris chosen from Cto Caliphatic or heteroaliphatic groups, optionally substituted with one or more aryl groups, substituted aryl groups, heteroaryl groups, substituted heteroaryl groups, or combination thereof, Ris chosen from aromatic moieties, substituted aromatic moieties, heteroaromatic moieties, substituted heteroaromatic moieties, and coumarin; Ris chosen from &#x2014;H, Cto Caliphatic or heteroaliphatic groups, phenyl, or substituted phenyl, wherein the aliphatic or heteroaliphatic groups are optionally substituted with one or more phenyl groups, aryl groups, heteroaryl groups, substituted heteroaryl groups, or combination thereof, and wherein the aliphatic or heteroaliphatic groups are optionally bonded to Rto form a ring; X is S or O; and Y is S or NH, may be used in pharmaceutical compositions that modify of biological signaling processes or as reagents for biological assays.

Imidazole and thiazole compositions for modifying biological signaling

Compounds having General Formula (I) or General Formula (II): in which Ris chosen from Cto Caliphatic or heteroaliphatic groups, optionally substituted with one or more aryl groups, substituted aryl groups, heteroaryl groups, substituted heteroaryl groups, or combination thereof; Ris chosen from aromatic moieties, substituted aromatic moieties, heteroaromatic moieties, substituted heteroaromatic moieties, and coumarin; Ris chosen from &#x2014;H, Cto Caliphatic or heteroaliphatic groups, phenyl, or substituted phenyl, wherein the aliphatic or heteroaliphatic groups are optionally substituted with one or more phenyl groups, aryl groups, heteroaryl groups, substituted heteroaryl groups, or combination thereof, and wherein the aliphatic or heteroaliphatic groups are optionally bonded to Rto form a ring; X is S or O; and Y is S or NH, may be used in pharmaceutical compositions that modify of biological signaling processes or as reagents for biological assays.

Methods for preventing, treating, and/or reducing the risk of developing non-alcoholic fatty liver disease in a subject in need thereof and pharmaceutical compositions for the prevention or treatment of non-alcoholic fatty liver disease. Methods for inhibiting excessive accumulation of fat in liver tissue. The methods include administering to the subject or contacting the liver tissue with a therapeutically effective amount of at least one compound of General Formula (I) or General Formula (II): or pharmaceutically-acceptable salts or solvates thereof. The pharmaceutical composition includes at least one compound of the General Formula (I) or the General Formula (II) for administration to a subject for the prevention or treatment of non-alcoholic fatty liver disease. 

Prevention and treatment of non-alcoholic fatty liver disease

Compounds having General Formula (I) or General Formula (II): in which Ris chosen from Cto Caliphatic or heteroaliphatic groups, optionally substituted with one or more aryl groups, substituted aryl groups, heteroaryl groups, substituted heteroaryl groups, or combination thereof; Ris chosen from aromatic moieties, substituted aromatic moieties, heteroaromatic moieties substituted heteroaromatic moieties, and coumarin; Ris chosen from &#x2014;H, Cto Caliphatic or heteroaliphatic groups, phenyl, or substituted phenyl, wherein the aliphatic or heteroaliphatic groups are optionally substituted with one or more phenyl groups, aryl groups, heteroaryl groups, substituted heteroaryl groups, or combination thereof, and wherein the aliphatic or heteroaliphatic groups are optionally bonded to Rto form a ring; X is S or O; and Y is S or NH, may be used in pharmaceutical compositions that modify of biological signaling processes or as reagents for biological assays. 

Methods for preventing, treating, and/or reducing the risk of developing non-alcoholic fatty liver disease in a subject in need thereof and pharmaceutical compositions for the prevention or treatment of non-alcoholic fatty liver disease. The methods include administering a therapeutically effective amount of phenylmethimazole, methimazole derivatives, and/or tautomeric cyclic thiones to the subject. The pharmaceutical composition includes phenylmethimazole, methimazole derivatives, and/or tautomeric cyclic thiones formulated for administration to a subject for the prevention or treatment of non-alcoholic fatty liver disease.

Treatment of autoimmune and/or inflammatory diseases associated with overexpression of Toll-like receptor 3 (TLR3) as well as Toll-like receptor 4 (TLR4) and/or TLR3/TLR4 signaling in nonimmune cells, monocytes, macrophages, and/or dendritic cells in association with related pathologies. The use of phenylmethimazoles, methimazole derivatives, and tautomeric cyclic thiones for the treatment of autoimmune and inflammatory diseases associated with TLR3 as well as TLR4 and/or TLR3/TLR4 cellular signaling in association with related pathologies is disclosed. Methods of treating a subject having a disease or condition associated with abnormal TLR-3 as well as TLR-4 and/or TLR3/TLR4 cellular signaling in association with related pathologies are also disclosed. The present disclosure also relates to the treatment of autoimmune-inflammatory pathologies and chemokine and cytokine-mediated diseases associated with TLR overexpression and signaling. The disclosure also relates to pharmaceutical formulations capable of inhibiting the IRF-3/Type 1 IFN/STAT/ISRE/IRF-1 pathway associated with Toll-like receptor overexpression or signaling.

Use of phenylmethimazoles, methimazole derivatives, and tautomeric cyclic thiones for the treatment of autoimmune/inflammatory diseases associated with toll-like receptor overexpression

Methods of ameliorating episodes of accute or chronic colitis are provided by using methimazole derivatives and tautomeric cyclic thiones in combination with another pharmaceutical compound.

Methods for the amelioration of episodes of acute or chronic ulcerative colitis

The present invention provides a biomolecular carrier of pharmaceuticals, comprising: a biomolecule carrier bearing molecules that bind to a cellular adhesion molecule expressed on endothelial cell; and a pharmaceutical. The present invention also provides a method of treating a pathophysiological state in an individual in need of such treatment, comprising the steps of: irradiating a target tissue or organ in said individual; and administering to said individual the biomolecular carrier disclosed herein.

Growing community of inventors

Athens, OH, United States of America

Douglas Goetz