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    • 3. 发明公开
    • ANTIGLUCOCORTICOID DRUG
    • 使用昆虫Feromonen的病理的糖皮质激素过剩引起的治疗
    • EP0896819A1
    • 1999-02-17
    • EP96902026.2
    • 1996-02-01
    • Burlakov, Sergei DmitrievichGenkin, Dmitry DmitrievichSurkov, Kirill GennadievichTets, Viktor Veniaminovich
    • Burlakov, Sergei DmitrievichGenkin, Dmitry DmitrievichSurkov, Kirill GennadievichTets, Viktor Veniaminovich
    • A61K31/045A61K31/075A61K31/11
    • A61K31/235A61K31/045A61K31/22
    • The invention is related to medicine and veterinary fields, in particular to nonsteroidal antiglucocorticoids. An aim of the invention is the establishment of a new class of drugs with low toxicity and high activity in regulation of sensitivity of mammalian cells to the glucocorticoid hormones. There is a naval application of an insect pheromone with long-chain aliphatic nonsteroidal structure or its synthetic analog or derivative that is unsaturated aliphatic alcohol, aldehyde or ester, for specific inhibition of glucocorticoid hormone influence on mammalian cells. The aliphatic carbon chain length of these pheromones varies from 10 to 21 carbon atoms. There is also a possibility of combining application of two or more pheromones and/or their synthetic analogs and derivatives for enhancement of therapeutic activity, selection being made on the basis of different hydrophobic properties proportional to the aliphatic carbon chain length. Difference in lengths of these chains must be no loss than five carbon atoms. Example of preparation of the pharmaceutical forms and results of comparative experiments that show their high activity are disclosed.
    • 本发明涉及医药和兽医领域,特别是对非甾体antiglucocorticoids。 本发明的一个目的是建立一个新的一类药物与在哺乳动物细胞中糖皮质激素的激素敏感性调节低毒性和高活性的。 存在与长链脂肪族的非甾体结构或其合成类似物或衍生物的昆虫信息素的海军应用确实是不饱和脂醇,醛或酯,用于在哺乳动物细胞上的糖皮质激素激素影响特异性抑制。 合成信息素的脂族碳链长度而变化,从10到21个碳原子。 因此,存在两个或更多个信息激素和/或合成的类似物的组合应用的可能性和衍生它们的用于增强的治疗活性的,正比于脂肪族碳链长度不同的疏水性能的基础上作出的选择。 差在链论文的长度必须不超过5个碳原子的损失。 制备的药物形式和对比实验的结果的例子并显示它们的高活性是游离缺失盘。