Therapeutic thyroid hormone ligand patents 1998 – 2003

Abstract

This review aims to cover the intense patenting activity in the thyroid hormone field during the past 5 years. The prospects for the use of new thyromimetic agents in medicinal therapy are highly promising if adverse effects can be minimised or eliminated. Prior attempts to utilise thyroid hormones pharmacologically to treat medicinal disorders have been limited by manifestations of hyperthyroidism and, in particular, by cardiovascular toxicity. The scientific literature suggests that most of the effects of thyroid hormones on the heart are mediated through the thyroid hormone receptor (TR)α, whilst most actions of the hormones on the liver and other tissues are mediated through TRβ. Consequently, it is envisaged that useful examples may be found for safe treatment of diseases involving genes that are regulated by TRβ. Accordingly, treatment of metabolic diseases, such as hyperlipidaemia, hypercholesterolaemia, obesity and diabetes, are claimed in most patents. Biological data are very seldom revealed in the patents but are rather just stated to have been generated. Almost every conceivable variation of the endogenous hormones 3,5,3′-triiodo-L-thyronine and 3,5,3′,5′-tetraiodo-L-thyronine has been claimed at the present date. There is no doubt that the future will hold a significant potential for thyromimetic agents in selective medical interventions, especially in the field of metabolic diseases.

• cardiac arrhythmia
• dyslipidaemia
• hyperthyroidism
• hypothyroidism
• metabolic disease
• obesity
• thyroid hormone agonist
• thyroid hormone antagonist