首页> 外国专利> AMORPHIC FORM OF N- {2-FLUOR-5- 3- (THIOFEN-2-CARBONIL) -PYRAZOLO 1,5-a PYRIMIDIN-7-IL -PHENYL} -N-METHYL-ACETAMIDE, METHOD FOR ITS PREPARATION, CONTAINING THE SPECIFIED AMORPHIC FORM PHARMACEUTICAL COMPOSITION (OPTIONS) AND MEDICINAL PRODUCT AND METHOD FOR TREATING AND / OR PREVENTION OF NERVOUS DISORDERS

AMORPHIC FORM OF N- {2-FLUOR-5- 3- (THIOFEN-2-CARBONIL) -PYRAZOLO 1,5-a PYRIMIDIN-7-IL -PHENYL} -N-METHYL-ACETAMIDE, METHOD FOR ITS PREPARATION, CONTAINING THE SPECIFIED AMORPHIC FORM PHARMACEUTICAL COMPOSITION (OPTIONS) AND MEDICINAL PRODUCT AND METHOD FOR TREATING AND / OR PREVENTION OF NERVOUS DISORDERS

机译:N- {2-氟-5- [3-(噻吩芬-2-碳)-吡唑并[1,5-a]吡唑啉-7-IL]-苯基] -N-甲基-乙酰胺的非晶体形式,其制备方法包含特定的非处方形式药物成分和药物的制备,治疗和/或预防神经疾病的方法

摘要

1. Amorphous form of N- {2-fluoro-5- [3- (thiophen-2-carbonyl) pyrazolo [1,5-a] pyrimidin-7-yl] phenyl} -N-methyl-acetamide. ! 2. The amorphous form according to claim 1, which shows the x-ray diffraction pattern shown in figure 1.! 3. The method of obtaining the amorphous form according to any one of claims 1 to 2, comprising dissolving N- {2-fluoro-5- [3- (thiophen-2-carbonyl) -pyrazolo [1,5-a] pyrimidin-7-yl ] -phenyl} -N-methyl-acetamide in dichloromethane, evaporating the solvent in vacuo and drying the resulting product to remove residual solvent. ! 4. The method according to claim 3, in which after dissolving N- {2-fluoro-5- [3- (thiophen-2-carbonyl) -pyrazolo [1,5-a] pyrimidin-7-yl] phenyl} - Charcoal is added to the resulting solution, the resulting mixture is heated to 30-50 ° C, stirred for 20-45 min, then the resulting suspension is cooled to 15-30 ° C, charcoal is removed from it by filtration, after which the solvent is evaporated under vacuum and the resulting product is dried under vacuum at 40-60 ° C to remove residual solvent. ! 5. The method according to claim 4, in which the mixture obtained after adding charcoal to a solution of N- {2-fluoro-5- [3- (thiophene-2-carbonyl) -pyrazolo [1,5-a] pyrimidin-7 -yl] -phenyl} -N-methyl-acetamide in dichloromethane, heated to 40 ° C (± 5 ° C). ! 6. The method according to claim 4, in which the mixture obtained after adding charcoal to a solution of N- {2-fluoro-5- [3- (thiophene-2-carbonyl) -pyrazolo- [1,5-a] pyrimidine- 7-yl] phenyl} -N-methyl-acetamide in dichloromethane, stirred for 30 minutes (± 5 minutes). ! 7. The method according to claim 4, in which the resulting suspension is cooled to 20-25 ° C. ! 8. The method according to claim 4, in which the product obtained after evaporation of the solvent under vacuum is dried at 50 ° C (± 5 ° C). ! 9. The use of an amorphous form according to claim
机译:1.N- {2-氟-5- [3-(噻吩-2-羰基)吡唑并[1,5-a]嘧啶-7-基]苯基] -N-甲基乙酰胺的无定形形式。 ! 2.根据权利要求1的无定形形式,其显示图1所示的x射线衍射图。 3.根据权利要求1-2中任一项的获得无定形形式的方法,包括溶解N- {2-氟-5- [3-(噻吩-2-羰基)-吡唑并[1,5-a]嘧啶在二氯甲烷中的-7-基]-苯基} -N-甲基-乙酰胺,真空蒸发溶剂,干燥所得产物以除去残留的溶剂。 ! 4.根据权利要求3的方法,其中在溶解N- {2-氟-5- [3-(噻吩-2-羰基)-吡唑并[1,5-a]嘧啶-7-基]苯基}-之后将木炭添加到所得溶液中,将所得混合物加热至30-50°C,搅拌20-45分钟,然后将所得悬浮液冷却至15-30°C,通过过滤从其中除去木炭,然后在真空下蒸发溶剂,并将得到的产物在40-60℃下真空干燥以除去残留的溶剂。 ! 5.根据权利要求4的方法,其中将木炭加到N- {2-氟-5- [3-(噻吩-2-羰基)-吡唑并[1,5-a]嘧啶在二氯甲烷中的-7-基]-苯基} -N-甲基-乙酰胺,加热至40°C(±5°C)。 ! 6.根据权利要求4的方法,其中将木炭添加到N- {2-氟-5- [3-(噻吩-2-羰基)-吡唑并-[1,5-a]]溶液中后获得的混合物。在二氯甲烷中,将嘧啶-7-基]苯基} -N-甲基-乙酰胺搅拌30分钟(±5分钟)。 ! 7.根据权利要求4的方法,其中将所得悬浮液冷却至20-25℃。 8.根据权利要求4的方法,其中在真空下蒸发溶剂后获得的产物在50℃(±5℃)下干燥。 ! 9.根据权利要求1的无定形形式的用途

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