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Hydrates of a phenoxypyridazinone compound and its use in the manufacture of a medicament for treating a disease characterized by resistance to thyroid hormone

机译:苯氧基哒嗪酮化合物的水合物及其在制备用于治疗以甲状腺激素抵抗性为特征的疾病的药物中的用途

摘要

The disclosure describes methods of synthesis of pyridazinone compounds as thyroid hormone analogs and their prodrugs. Preferred methods according to the disclosure allow for large-scale preparation of pyridazinone compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of pyridazinone compounds in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of a pyridazinone compound such as 2-(3,5-dichloro-4-((5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yl)oxy)phenyl)-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile, wherein the morphic form is a dihydrate.
机译:本公开描述了作为甲状腺激素类似物的哒嗪酮化合物的合成方法及其前药。根据本发明的优选方法允许大规模制备具有高纯度的哒嗪酮化合物。在一些实施方案中,根据本发明的优选方法还允许以比先前使用的制备此类化合物的方法更高的产率制备哒嗪酮化合物。还公开了哒嗪酮化合物的形态形式,例如2-(3,5-二氯-4-((5-异丙基-6-氧代-1,6-二氢哒嗪-3-基)氧基)苯基)-3,5 -二氧代-2,3,4,5-四氢-1,2,4-三嗪-6-腈,其中该形态为二水合物。

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