Novel heterocyclic analogs of diphenylethylene compounds

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 277/34 (2006.01) A61K 31/357 (2006.01) A61K 31/385 (2006.01) A61K 31/39 (2006.01) A61K 31/4166 (2006.01) A61K 31/421 (2006.01) A61K 31/426 (2006.01) C07D 233/72 (2006.01) C07D 263/44 (2006.01) C07D 317/34 (2006.01) C07D 327/04 (2006.01) C07D 339/06 (2006.01)

Patent

CA 2410171

Novel diphenylethylene compounds and derivatives thereof containing thiazolidinedione or oxazolidinedione moieties are provided which are effective in lowering blood glucose level, serum insulin, triglyceride and free fatty acid levels in animal models of Type II diabetes. In contrast to previously reported thiazolidinedione compounds, known to lower leptin levels, the present compounds increase leptin levels and have no known liver toxicity. The compounds are disclosed as useful for a variety of treatments including the treatment of inflammation, inflammatory and immunological diseases, insulin resistance, hyperlipidemia, coronary artery disease, cancer and multiple sclerosis.

L'invention concerne des nouveaux composés de diphényléthylène et des dérivés de ceux-ci renfermant des fractions thiazolidinédione ou oxazolidinédione, ces composés étant efficaces pour faire baisser la glycémie, le taux d'insuline sérique, les taux de triglycérides et d'acides gras libres chez des modèles animaux atteints du diabète de type II. Contrairement aux composés thiazolidine connus jusqu'alors, capables de faire baisser les taux de leptine, les composés selon la présente invention font augmenter les taux de leptine et ne présentent pas de toxicité connue pour le foie. Les composés selon la présente invention sont utiles dans une palette de traitements, notamment le traitement d'inflammation, de maladies inflammatoires et immunologiques, de la résistance à l'insuline, de l'hyperlipidémie, de la coronaropathie, du cancer et de la sclérose en plaques.

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