首页> 外国专利> POLYMORPHIC MODIFICATION IN N- {5- 3- (THIOFEN-2-CARBONYL) -PYRAZOLO 1,5-a PYRIMIDIN-7-IL -2-FLUOR-Phenyl} -N-METHYL-ACETAMIDE (OPTIONS), CONTAINING ITS PHARMACEUTICAL COMPOSITION (OPTIONS), MEDICINAL PRODUCT, METHOD FOR OBTAINING THE SPECIFIED POLYMORPHIC MODIFICATION IN (OPTIONS) AND METHOD FOR TREATING AND / OR PREVENTION OF NERVOUS DISEASES

POLYMORPHIC MODIFICATION IN N- {5- 3- (THIOFEN-2-CARBONYL) -PYRAZOLO 1,5-a PYRIMIDIN-7-IL -2-FLUOR-Phenyl} -N-METHYL-ACETAMIDE (OPTIONS), CONTAINING ITS PHARMACEUTICAL COMPOSITION (OPTIONS), MEDICINAL PRODUCT, METHOD FOR OBTAINING THE SPECIFIED POLYMORPHIC MODIFICATION IN (OPTIONS) AND METHOD FOR TREATING AND / OR PREVENTION OF NERVOUS DISEASES

机译:N- {5- [3-(3-噻吩基-2-羰基)-吡唑并[1,5-a] PYRIMIDIN-7-IL] -2-氟-苯基} -N-甲基-乙酰胺中的多态性修饰(选项),包含其药物成分(选项),药物产品,在(选项)中进行特定多态修饰的方法以及治疗和/或预防神经疾病的方法

摘要

1. Polymorphic modification of N- {5- [3- (thiophen-2-carbonyl) -pyrazolo [1,5-a] pyrimidin-7-yl] -2-fluoro-phenyl} -N-methyl-acetamide, characterized by powder X-ray diffractometry curve having specific peaks at 20 = 7.1 ° (± 0.1 °) and 21.4 ° (± 0.1 °). ! 2. The polymorphic modification according to claim 1, characterized by a curve of powder x-ray diffractometry having specific peaks at 2θ = 7.1 ° (± 0.1 °), 11.8 ° (± 0.1 °), 12.3 ° ( ± 0.1 °), 12.6 ° (± 0.1 °), 13.7 ° (± 0.1 °), 14.7 ° (± 0.1 °), 15.5 ° (± 0 , 1 °), 19.0 ° (± 0.1 °), 20.8 ° (± 0.1 °), 21.4 ° (± 0.1 °), 22.0 ° (± 0.1 °), 22.3 ° (± 0.1 °), 22.6 ° (± 0.1 °), 23.4 ° (± 0.1 °), 23.9 ° (± 0.1 °) , 25.6 ° (± 0.1 °), 26.3 ° (± 0.1 °), 27.1 ° (± 0.1 °), 27.8 ° (± 0.1 °), 31 , 8 ° (± 0.1 °) and 36.5 ° (± 0.1 °). ! 3. Polymorphic modification of N- {5- [3- (thiophen-2-carbonyl) -pyrazolo [1,5-a] pyrimidin-7-yl] -2-fluoro-phenyl} -N-methyl-acetamide, characterized by Fourier transform Raman spectrum having characteristic signals at 3107 cm-1, 1605 cm-1, 1593 cm-1, 1538 cm-1, 1336 cm-1 and 102 cm-1. ! 4. Polymorphic modification of N- {5- [3- (thiophen-2-carbonyl) -pyrazolo [1,5-a] pyrimidin-7-yl] -2-fluoro-phenyl} -N-methyl-acetamide, characterized by differential scanning calorimetry having a melting peak of about 158 ° C. ! 5. The method of producing the polymorphic modification according to any one of claims 1 to 4, in which the polymorphic modification A of N- {5- [3- (thiophen-2-carbonyl) -pyrazolo [1,5-a] pyrimidin-7-yl is suspended ] -2-fluoro-phenyl} -N-methyl-acetamide at room temperature in a solvent selected from the group consisting of C1-C6 aliphatic alcohols, C1-C6 aliphatic ketones, C1-C4 alkyl esters of C1-C4 aliphatic acids, C4-C5 saturated cyclic ethers , C1-C6 aliphatic nitriles, aromatic hydrocarbons and water, and mixtures selected from the group consisting of C1-C6 aliphatic alcohol and C1-C6 aliphatic organic acid, water and C1-C6 aliphatic alcohol,
机译:1. N- {5- [3-(噻吩-2-羰基)-吡唑并[1,5-a]嘧啶-7-基] -2-氟-苯基} -N-甲基-乙酰胺的多晶型修饰,其特征在于通过粉末X射线衍射法测得的曲线在20 = 7.1°(±0.1°)和21.4°(±0.1°)具有特定峰。 ! 2.根据权利要求1所述的多晶型物修饰物,其特征在于粉末X射线衍射的曲线在2θ= 7.1°(±0.1°),11.8°(±0.1°),12.3°(±0.1°), 12.6°(±0.1°),13.7°(±0.1°),14.7°(±0.1°),15.5°(±0,1°),19.0°(±0.1°),20.8°(±0.1°), 21.4°(±0.1°),22.0°(±0.1°),22.3°(±0.1°),22.6°(±0.1°),23.4°(±0.1°),23.9°(±0.1°),25.6° (±0.1°),26.3°(±0.1°),27.1°(±0.1°),27.8°(±0.1°),31、8°(±0.1°)和36.5°(±0.1°)。 ! 3.N- {5- [3-(噻吩-2-羰基)-吡唑并[1,5-a]嘧啶-7-基] -2-氟-苯基} -N-甲基-乙酰胺的多晶型修饰,其特征在于通过傅里叶变换的拉曼光谱具有在3107 cm-1、1605 cm-1、1593 cm-1、1538 cm-1、1336 cm-1和102 cm-1处的特征信号。 ! 4. N- {5- [3-(噻吩-2-羰基)-吡唑并[1,5-a]嘧啶-7-基] -2-氟-苯基} -N-甲基-乙酰胺的多晶型修饰,其特征在于通过差示扫描量热法测定,其熔融峰为约158℃。 5.根据权利要求1-4中任一项的生产多晶型变体的方法,其中N- {5- [3-(噻吩-2-羰基)-吡唑并[1,5-a]的多晶型变体A。在室温下,在选自C 1 -C 6脂族醇,C 1 -C 6脂族酮,C 1 -C 4烷基酯的溶剂中,悬浮嘧啶丁-7-基] -2-氟-苯基} -N-甲基乙酰胺。 C1-C4脂族酸,C4-C5饱和环醚,C1-C6脂族腈,芳族烃和水,以及选自C1-C6脂族醇和C1-C6脂族有机酸的混合物,水和C1- C6脂肪醇

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