首页> 外国专利> 2,4-DIAMINOPYRIDINE DERIVATIVES, A PHARMACEUTICAL COMPOSITION AND A MEDICINAL AGENT WHICH ARE BASED THEREON AND USED FOR TREATING OR PREVENTING DISEASES AND DISTURBANCES CAUSED BY THE HYPERACTIVATION OF NMDA-RECEPTORS AND/OR IN THE FORM OF COGNITIVE FUNCTION STIMULATORS AND A METHOD FOR THE USE THEREOF

2,4-DIAMINOPYRIDINE DERIVATIVES, A PHARMACEUTICAL COMPOSITION AND A MEDICINAL AGENT WHICH ARE BASED THEREON AND USED FOR TREATING OR PREVENTING DISEASES AND DISTURBANCES CAUSED BY THE HYPERACTIVATION OF NMDA-RECEPTORS AND/OR IN THE FORM OF COGNITIVE FUNCTION STIMULATORS AND A METHOD FOR THE USE THEREOF

机译:2,4-二氨基吡啶类衍生物,一种药物组合物和一种医药剂,它们被用于治疗或预防因过度激活NMDA受体和/或以指定方式表达而引起的疾病和干扰。使用

摘要

The invention relates to novel 2,4-diaminopyridine derivatives, pharmaceutically acceptable salts and /or solvates thereof, to compositions and medicinal agents containing the novel 2,4-diaminopyridine derivatives and to the use thereof as the NMDA-receptor blockers and cognitive function stimulators. The novel derivatives combine the properties of highly affine NMDA-receptor antagonist with the properties of moderate acetylcholinesterase inhibitors and with the properties of highly affine agonists of nicotine cholinoreceptors and sympathomimetics, whereby determining the comprehensive normalising action thereof on the disballance of several neurotransmitting systems, including glytamatergic, cholinergic and adrenergic systems without undesirable side effects which were previously observed in the known NMDA-antagonists. They not only do not cause the disturbance of intellectual abilities, attention and memory that is typical for the known NMDA-receptor antagonists, but, in addition, can be useful for treating and preventing a range of diseases and disturbances related to disturbed cognitive functions and learning ability. The method for treating or preventing diseases and disorders caused by the incresed activation of the glutamatergic system and/or by the damage of intellectual mnestic functions.
机译:本发明涉及新颖的2,4-二氨基吡啶衍生物,其药学上可接受的盐和/或溶剂化物,涉及包含新颖的2,4-二氨基吡啶衍生物的组合物和药物,及其作为NMDA受体阻滞剂和认知功能刺激剂的用途。 。新型衍生物将高度亲和的NMDA受体拮抗剂的特性与中度乙酰胆碱酯酶抑制剂的特性以及尼古丁胆碱受体和拟交感神经药的高度亲和性激动剂的特性相结合,从而确定了其对几种神经递质系统(包括以前没有在已知的NMDA拮抗剂中观察到的不希望有的副作用的地格能,胆碱能和肾上腺素能系统。它们不仅不会引起已知NMDA受体拮抗剂常见的智力,注意力和记忆障碍,而且还可以用于治疗和预防一系列与认知功能和精神障碍有关的疾病和障碍。学习能力。该方法用于治疗或预防由谷氨酸能系统的激活增加和/或智力记忆功能受损引起的疾病和病症。

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