;in form of free base and salts with pharmaceutically accepted acids, as well as racemate, individual optical isomers or mixture thereof. In formula R1, R2, R3, R4, Y and Z are as described in specification. Compounds of present invention are capable to potentiate (positively modulate) AMPA/KA glutamate receptors and simultaneously to block transmembrane currents induced by activation of NMDA glutamate receptors. Also disclosed are method for production of said compounds, including optical isomers; pharmaceutical composition; method for investigation of glutamatergic system, and method for Alzheimer's disease, treatment; as well as method for extreme retentiveness of memory by administering of effective amount of claimed compounds.;EFFECT: new pharmaceutically active compounds for Alzheimer's disease treatment.;23 cl, 1 tbl, 11 ex"/> S-SUBSTITUTED (HETERO)ARYLALKYLISOTHIOUREAS, PRODUCTION THEREOF, PHARMACEUTICAL COMPOSITION, INVESTIGATION OF GLUTAMATERGIC SYSTEM, TREATMENT METHODS (VARIANTS)
首页> 外国专利> S-SUBSTITUTED (HETERO)ARYLALKYLISOTHIOUREAS, PRODUCTION THEREOF, PHARMACEUTICAL COMPOSITION, INVESTIGATION OF GLUTAMATERGIC SYSTEM, TREATMENT METHODS (VARIANTS)

S-SUBSTITUTED (HETERO)ARYLALKYLISOTHIOUREAS, PRODUCTION THEREOF, PHARMACEUTICAL COMPOSITION, INVESTIGATION OF GLUTAMATERGIC SYSTEM, TREATMENT METHODS (VARIANTS)

机译:S取代的[(杂)芳基]烷基异硫氰酸盐,其生产,药物成分,谷氨酸系统的研究,治疗方法(多种)

摘要

FIELD: organic chemistry, pharmaceutical industry, medicine.;SUBSTANCE: invention relates to new derivatives of S-substituted N-1-[(hetero)aryl]alkyl-N'-1-[(hetero)aryl]alkylisothioureas of general formula I; ;in form of free base and salts with pharmaceutically accepted acids, as well as racemate, individual optical isomers or mixture thereof. In formula R1, R2, R3, R4, Y and Z are as described in specification. Compounds of present invention are capable to potentiate (positively modulate) AMPA/KA glutamate receptors and simultaneously to block transmembrane currents induced by activation of NMDA glutamate receptors. Also disclosed are method for production of said compounds, including optical isomers; pharmaceutical composition; method for investigation of glutamatergic system, and method for Alzheimer's disease, treatment; as well as method for extreme retentiveness of memory by administering of effective amount of claimed compounds.;EFFECT: new pharmaceutically active compounds for Alzheimer's disease treatment.;23 cl, 1 tbl, 11 ex
机译:技术领域本发明涉及通式I的S-取代的N-1-[(杂)芳基]烷基-N'-1-[[(杂)芳基]烷基]异硫脲的新衍生物; ;以游离碱和与药学上可接受的酸形成的盐以及外消旋体,单个旋光异构体或其混合物的形式。式R 1 ,R 2 ,R 3 ,R 4 ,Y和Z如规范中所述。本发明的化合物能够增强(正调节)AMPA / KA谷氨酸受体,同时阻断由NMDA谷氨酸受体的活化引起的跨膜电流。还公开了制备所述化合物的方法,所述化合物包括旋光异构体。药物组合物;谷氨酸能系统的研究方法以及阿尔茨海默氏病的治疗方法;以及通过施用有效量的所要求保护的化合物来极度保持记忆的方法。效果:用于治疗阿尔茨海默氏病的新型药物活性化合物; 23 cl,1 tbl,11 ex

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