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5-arylpyrid 2,3-e 1,4 thiazepinone derivatives with mitochondrial sodium / calcium exchanger blocking activity

机译:5-芳基吡啶[2,3-e] [1,4]噻嗪酮衍生物具有线粒体钠/钙交换剂阻断活性

摘要

5-arylpyrid [2,3-e] [1,4] thiazepinone derivatives with mitochondrial sodium / calcium exchanger blocking activity. # {IMAGE-01} # The present invention relates to compounds of general formula (I), and its use in the manufacture of useful medicines for the treatment of neurodegenerative diseases, stroke, epilepsy, diabetes or, in general, any disease or pathology caused by altered biological functions where the mitochondrial sodium / calcium exchanger is involved. These diseases have been described as having mitochondrial dysfunction and an alteration of homeostasis of Ca {sup, 2 +} in neurons. Therefore, the compounds of the general formula (I) have the Na {sup, +} / Ca {sup, 2 +} exchanger of the mitochondria as biological targets. In addition, given the lack of potent and selective pharmacological tools to study the Na {sup, +} / Ca {sup, 2 +} exchanger of mitochondria, the compounds of the invention are useful for studying the physiology and pathophysiology of this target. biological in processes where its role has been discovered, or in future experimental observations. The present invention can be framed in the field of the pharmaceutical industry.
机译:5-芳基吡啶[2,3-e] [1,4]噻嗪酮衍生物具有线粒体钠/钙交换剂的阻断活性。 #{IMAGE-01}#本发明涉及通式(I)的化合物,及其在制备用于治疗神经退行性疾病,中风,癫痫,糖尿病或一般而言任何疾病或病理的药物中的用途由涉及线粒体钠/钙交换剂的生物学功能改变引起的。这些疾病被描述为具有线粒体功能障碍和神经元中Ca {sup,2 +}的体内稳态改变。因此,通式(I)的化合物具有线粒体的Na {sup,+} / Ca {sup,2 +}交换体作为生物靶标。另外,由于缺乏有效的和选择性的药理学工具来研究线粒体的Na {sup,+} / Ca {sup,2 +}交换子,本发明的化合物可用于研究该靶标的生理学和病理生理学。在发现其作用的过程中还是在未来的实验观察中具有生物学意义。本发明可以在制药工业领域中实现。

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