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Novel thyroid receptor ligands
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一种甲氧基、化合物的技术，应用在新化合物领域，能够解决效能和耐受性未知等问题
Inactive Publication Date: 2007-07-04
KARO BIO AB
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In Graves' hyperthyroidism, glucocorticoids can reduce thyroid secretion of T 4 , but efficacy and tolerability unknown
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[0080] (a) Add sodium acetate (7.0 g, 83 mmol) to a mixture of 5-hydroxy-1-indanone (5.6 g, 38 mmol), acetic acid (260 ml) and 4-5 drops of water, then add dropwise Bromine (13.3 g, 83 mmol) in acetic acid (60 mL). The reaction mixture was stirred at room temperature for 18 hours, and the precipitate was filtered and dried. 8.4 g (72%) of 4,6-dibromo-5-hydroxy-1-indanone were obtained as a solid, which was used directly in the next experiment without further purification.
[0081] (b) In a mixture containing bis-(3-isopropyl-4-methoxyphenyl)iodonium tetrafluoroborate (6.25 g, 12.2 mmol), bronze (1.02 g) and dichloromethane (25 mL ) in a stirred suspension system containing 4,6-dibromo-5-hydroxyl-1-indanone (2.50 g, 8.17 mmol) and triethylamine (1.00 g, 8.99 mmol) in nitrogen at room temperature Dichloromethane solution (25 mL). The reaction mixture was stirred for 48 hours in the dark ...
[0088] 4-Fluorobenzyl bromide (15 mg, 0.080 mmol) and ethyl[4,6-dibromo-5-(3-isopropyl-4-hydroxyphenoxy)indanyl-1]acetate (20 mg, 0.039 mmol) was coupled and then worked up according to the procedure described in Example 1. Obtained 5.3 mg (23%) of {4,6-dibromo-5-[4-(4-fluorobenzyloxy)-3-isopropylphenoxy]indanyl-1}acetic acid. LC-MS (ES) m / z 591 (M-1).
Embodiment 3
[0090] {4,6-Dibromo-5-[3-isopropyl-4-(5-methylisoxazolyl-3-methoxy)phenoxy]indanyl-1}acetic acid ethyl[4 , 6-dibromo-5-(3-isopropyl-4-hydroxyphenoxy)indanyl-1] acetate (20 mg, 0.039 mmol), potassium carbonate (11 mg, 0.080 mmol) The mixture with acetonitrile (0.75 mL) was stirred at room temperature for 30 minutes. 3-Chloromethyl-5-methylisoxazole (10.5 mg, 0.080 mmol) and a catalytic amount of potassium iodide in acetonitrile (0.25 mL) were added, and the reaction mixture was stirred at 80°C. After 16 hours, the reaction mixture was purified on a short column (SPE-silica, 1 g / 6 mL, n-heptane / ethyl acetate 65:35), the resulting filtrate was concentrated, the residue and THF (0.50 mL) and Lithium hydroxide (0.5 mL, 1N) was stirred at room temperature for 16 hours. The reaction mixture was filtered through an SCX-column (strong cation exchanger: silane benzenesulfonate, 1 g / 3 ml, eluting with methanol), and the filtrate was concentrated. The filter residue was dissolved with ...
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Abstract
This invention relates to novel compounds according to the general formula: which are thyroid receptor ligands, preferably antagonists, partial antagonists or partial agonists and to methods for using such compounds in the treatment of cardiac and metabolic disorders, such as cardiac arrhythmias, thyro-toxicosis, subclinical hyperthyrodism and liver diseases.
Description
technical field [0001] The present invention relates to novel compounds which are thyroxine receptor ligands, preferably antagonists, and methods of using these compounds in the treatment of cardiac and metabolic disorders such as arrhythmias, thyrotoxicosis, subclinical hyperthyroidism and liver disease . Background technique [0002] Nuclear hormone receptors are a class of intracellular, ligand-regulated transcription factors, including thyroid hormone receptors. Thyroid hormones play an important role in mammalian growth, development and homeostasis. They regulate important genes in the gut, skeletal and cardiac muscle, liver and central nervous system, affect overall metabolic rate, cholesterol and triglyceride levels, heart rate, and influence mood and physical state. [0003] There are two major subtypes of thyroid hormone receptors, TRα and TRβ, expressed from two different genes. Distinct RNA processing results in at least two isoforms for each gene. TRα 1 , TR...
Claims
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