首页> 外国专利> PYRAZOLO1,5-aPYRIMIDINE COMPOUNDS, PHARMACEUTICAL COMPOSITION SHOWING ABILITY TO INHIBIT GABAA RECEPTORS, AND DRUG FOR TREATING AND PREVENTING DISORDERS ASSOCIATED WITH GABAA RECEPTOR INHIBITION

PYRAZOLO1,5-aPYRIMIDINE COMPOUNDS, PHARMACEUTICAL COMPOSITION SHOWING ABILITY TO INHIBIT GABAA RECEPTORS, AND DRUG FOR TREATING AND PREVENTING DISORDERS ASSOCIATED WITH GABAA RECEPTOR INHIBITION

机译:吡唑并[1,5-a]嘧啶化合物,具有抑制GABA A 受体能力的药物组合物以及用于治疗和预防与GABA A 受体抑制剂相关的疾病的药物

摘要

FIELD: medicine, pharmaceutics.;SUBSTANCE: pyrazolo[1,5-a]-pyrimidine compounds according to the invention are specified in a group consisting of: N-{2-fluor-5-[3-nitro-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylacetamide, N-{2-fluor-5-[3-cyano-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylacetamide, N-{2-chlor-5-[3-nitro-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylacetamide, N-{2-chlor-5-[3-cyano-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylacetamide, N-{2-fluor-5-[3-nitro-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-ethylmethanesulphonamide; {2-fluor-5-[3-cyano-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylmethanesulphonamide, N-{2-chlor-5-[3-nitro-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylmethanesulphonamide, N-{2-chlor-5-[3-cyano-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylmethanesulphonamide, N-{2-fluor-5-[3-cyano-2-methyl-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylacetamide, N-{2-chlor-5-[3-cyano-2-methyl-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylacetamide, N-{2-fluor-5-[3-cyano-2-methyl-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methyl-methanesulphonamide, N-{2-chlor-5-[3-cyano-2-methyl-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methyl-methanesulphonamide, N-{2-methyl-5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylacetamide, N-{2-methoxy-5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylacetamide, N-{2,4-difluor-5-[3-(thiophene_2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylacetamide and N-{5-fluor-2-methoxy-3-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylacetamide.;EFFECT: preparing pyrazolo[1,5-a]pyrimidine compounds, their pharmaceutically acceptable salts and hydrates showing an ability to inhibit GABAA receptors, and applicable for treating and preventing anxiety, epilepsy and sleeping disorders, including insomnia, as well as for inducing a sedative-hypnotic, analgesic and sleeping effects and myorelaxation.;14 cl, 6 tbl, 4 dwg, 22 ex
机译:物质:本发明的吡唑并[1,5-a]-嘧啶化合物在由N- {2-氟-5- [3-硝基-吡唑并[1], 5-a]嘧啶-7-基]-苯基} -N-甲基乙酰胺,N- {2-氟-5- [3-氰基-吡唑并[1,5-a]嘧啶-7-基]-苯基}- N-甲基乙酰胺,N- {2-氯-5- [3-硝基-吡唑并[1,5-a]嘧啶-7-基]-苯基} -N-甲基乙酰胺,N- {2-氯-5- [ 3-氰基吡唑并[1,5-a]嘧啶-7-基]-苯基} -N-甲基乙酰胺,N- {2-氟-5- [3-硝基吡唑并[1,5-a]嘧啶- 7-基]-苯基} -N-乙基甲磺酰胺; {2-氟-5- [3-氰基-吡唑并[1,5-a]嘧啶-7-基]-苯基} -N-甲基甲磺酰胺,N- {2-氯-5- [3-硝基-吡唑并[ 1,5-a]嘧啶-7-基]-苯基} -N-甲基甲磺酰胺,N- {2-氯-5- [3-氰基-吡唑并[1,5-a]嘧啶-7-基]-苯基} -N-甲基甲磺酰胺,N- {2-氟-5- [3-氰基-2-甲基-吡唑并[1,5-a]嘧啶-7-基]-苯基} -N-甲基乙酰胺,N- {2 -氯-5- [3-氰基-2-甲基-吡唑并[1,5-a]嘧啶-7-基]-苯基} -N-甲基乙酰胺,N- {2-氟-5- [3-氰基- 2-甲基-吡唑并[1,5-a]嘧啶-7-基]-苯基} -N-甲基-甲磺酰胺,N- {2-氯-5- [3-氰基-2-甲基-吡唑并], 5-a]嘧啶-7-基]-苯基} -N-甲基-甲磺酰胺,N- {2-甲基-5- [3-(噻吩-2-羰基)-吡唑并[1,5-a]嘧啶- 7-基]-苯基} -N-甲基乙酰胺,N- {2-甲氧基-5- [3-(噻吩-2-羰基)-吡唑并[1,5-a]嘧啶-7-基]-苯基}- N-甲基乙酰胺,N- {2,4-二氟-5- [3-(噻吩_2-羰基)-吡唑并[1,5-a]嘧啶-7-基]-苯基} -N-甲基乙酰胺和N- {5 -氟-2-甲氧基-3- [3-(噻吩-2-羰基)-吡喃佐洛[1,5-a]嘧啶-7-基]-苯基} -N-甲基乙酰胺。效果:制备吡唑并[1,5-a]嘧啶化合物,其药学上可接受的盐和水合物具有抑制GABA < Sub> A 受体,适用于治疗和预防焦虑症,癫痫病和睡眠障碍,包括失眠症,以及诱导镇静催眠,镇痛和睡眠作用以及髓鞘松弛。; 14 cl,6 tbl,4 dwg,22 ex

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