首页>
外国专利>
Treating mitochondrial diseases, e.g. Parkinson's or Alzheimer's disease or retinitis pigmentosa, using fumaric acid derivative, e.g. mono- or dialkyl fumarate, having succinate dehydrogenase stimulating activity
Treating mitochondrial diseases, e.g. Parkinson's or Alzheimer's disease or retinitis pigmentosa, using fumaric acid derivative, e.g. mono- or dialkyl fumarate, having succinate dehydrogenase stimulating activity
The use of fumaric acid derivatives (I) (including their mixtures) is claimed for the production of a pharmaceutical composition for the treatment of mitochondrial diseases. - ACTIVITY : Antiparkinsonian; neuroprotective; nootropic; ophthalmological; antiinflammatory; cerebroprotective. - MECHANISM OF ACTION : Succinate dehydrogenase (SDH) stimulant. SDH is a component of mitochondrial membranes, which catalyzes the conversion of succinic acid into fumaric acid (as part of the citrate cycle) and is associated with oxidative phosphorylation, deficiency of which causes mitochondrial diseases. In tests in fibroblasts, dimethyl fumarate (Ia) at 0.75 m equivalents/l increased SDH activity 838%.
展开▼
机译：要求保护富马酸衍生物（I）（包括其混合物）在生产用于治疗线粒体疾病的药物组合物中的用途。 -活动：Antiparkinsonian;神经保护促智眼科的消炎（药;脑保护。 -作用机理：琥珀酸脱氢酶（SDH）刺激物。 SDH是线粒体膜的成分，它催化琥珀酸向富马酸的转化（作为柠檬酸盐循环的一部分），并与氧化磷酸化有关，氧化磷酸化不足会导致线粒体疾病。在成纤维细胞的测试中，浓度为0.75 m / l的富马酸二甲酯（Ia）可将SDH活性提高838％。
展开▼
