首页> 外国专利> Mesylate Salt Compound (S) - 2 - (4 - (3 - fluoro - Benzyloxy) - (Benzylamino) - propionamide, polymorphic form (nf6), Pharmaceutical Composition and Use thereof for the preparation of a Drug and its Preparation Process

Mesylate Salt Compound (S) - 2 - (4 - (3 - fluoro - Benzyloxy) - (Benzylamino) - propionamide, polymorphic form (nf6), Pharmaceutical Composition and Use thereof for the preparation of a Drug and its Preparation Process

机译:甲磺酸盐化合物(S)-2-(4-(3-氟-苄氧基)-(苄氨基)-丙酰胺,多晶型物(nf6),药物组合物及其在制备药物中的用途及其制备方法

摘要

1. Dihydrate (s) - 2 - [4 - (3-fluoro-benzene-benzene-benzene) - benzene The second requirement: the compound is consistent with the first requirement, and its crystal transformation nf6 is characterized by the XRD peak value of 17.9 degrees,Page: 1Page: 120.7 degrees and 23.0 seconds (using 2teta of cu-kalfa1 radiation + - 0.1 degrees to - 5 degrees Celsius). The third requirement: according to any requirement 1 to 2, the compound is characterized by XRD powder peak value of 7.9 degrees,Page: 1Page: 1Page: 120.1%20.7 degreesPage: 1Page: 123.5 ° and 24.8 ° (in 2theta using Cu-Kalfa1 radiation, + - 0.1 ° to -5 ° C). Claim 4: The compound according to any of claims 1 to 3, characterized by the following XRD data according to table (1). Claim 7: A pharmaceutical composition according to claim 6 comprising 1% to 99% mesylate anhydrate of (S) -2- [4- (3-fluoro-benzyloxy) -benzylamino] -propionamide in its NF6 crystalline modification of according to any of claims 2 to 5 and 1% to 99% of mesylate anhydrate of (S) -2- [4- (3-fluoro-benzyloxy) -benzylamino] -propionamide in its crystalline modification A1, characterized by XRD peaks comprising 18.6 °,20.3 degrees20.6 degrees and 22.8 degrees (using cu-kalfa1 radiation + - 0.1 degrees)Preference, characterized by a peak XRD of 7.8 degrees,12.0 degrees 15.6 degrees17.7 degrees18.6 degreesPage: 120.3 degrees20.6 degrees22 8 y 29 0 (en 2theta usando radiacion Cu-Kalfa1 2B- 0 1) e incluso con mayor preferencia caracterizado por los siguientes datos de XRD segun la tabla (2) Reivindicacion 9 Uso de un compuesto de acuerdo con cualquiera de las reivindicaciones 1 Monoamine oxidase B inhibitors and / or dopamine reabsorption inhibitors. Item 11: drugs provided in accordance with item 10 labor requirements for the treatment and / or prevention of certain physiological conditions and / or physiological pathology, including: central nervous system disorders, epilepsy, Parkinson's disease, neurodegenerative process, depression, spasm, hypnosis, Anal sex, chronic pain, neuralgia, dizziness, immigration, headache, concussion, cluster headache, neurons, hemispheric, facial pain, spider ophthalmia, severe headache, restless leg symptoms, addiction, exercise anxiety, tickling, burning,Tension, substance abuse, severe alcoholism, under reward syndrome, cognitive impairment, autism, dyslexia, attention deficit, hypertension, anxiety, schizophrenia, obsessive-compulsive dementia, psychosis, bipolar disorder, Tourette syndrome, moderate cognitive impairment and disorder Learning in children, adolescents and adults, age-related memory changes, age-related cognitive decline, Alzheimer's disease, Down's syndrome, traumatic brain injury, Huntington's disease, progressive paralysis, HIV, cerebrovascular accidents, vascular diseases,Pick or Creutzfeldt-Jacob disease, multiple sclerosis. Claim 15: Process for preparing the NF6 crystalline modification of (S) -2- [4- (3-fluoro-benzyloxy) -benzylamino] -propionamide mesylate anhydrate according to any of claims 2 to 5 comprising the steps of : (a) incubate mesylate anhydrate of (S) -2- [4- (3-fluoro-benzyloxy) -benzylamino] -propionamide crystalline modification A1 at = 0 ° C for one or several milliseconds or seconds or minutes or hours or days,O (b) incubate dihydroacid (s) - 2 - [4 - (3-fluoro-benzene) - benzene] Propionamide, as a component of the mixture, which contains at least one additional A lt component; = 0 milliseconds or seconds or minutes or days.
机译:1.二水合物-2-[4--(3-氟-苯-苯-苯)-苯]第二个要求:该化合物与第一个要求一致,并且其晶体转化nf6的特征在于XRD峰值17.9度,页:1页:120.7度和23.0秒(使用cu-kalfa1辐射的2teta +-0.1度到-5摄氏度)。第三个要求:根据要求1至2,该化合物的特征在于XRD粉末峰值为7.9度,页:1页:1页:120.1%20.7度页:1页:123.5°和24.8°(在2θ中使用Cu-Kalfa1辐射,+-0.1°至-5°C)。权利要求4:根据权利要求1至3中任一项的化合物,其特征在于根据表(1)的以下XRD数据。 7.根据权利要求6所述的药物组合物,所述药物组合物包含1至99%的(S)-2- [4-(3-氟-苄氧基)-苄基氨基]-丙酰胺的甲磺酸盐无水物,其具有根据以下任一项的NF6结晶修饰。权利要求2至5和1%至99%的(S)-2- [4-(3-氟-苄氧基)-苄氨基]-丙酰胺的甲磺酸盐无水物的结晶变体A1,其特征在于XRD峰包括18.6°,20.3 20.6度和22.8度(使用cu-kalfa1辐射+-0.1度)是首选参数,其特征是XRD峰值为7.8度,12.0度15.6度17.7度18.6度页面:120.3度20.6度22 8 y 29 0( en 2theta usando radiacion Cu-Kalfa1 2B- 0 1)包括XRD枪支的XRD枪支(2)补充剂9丙酮酸的抗氧化剂和单酚/二胺1胺或多巴胺重吸收抑制剂。第11项:根据第10项劳动要求提供的药物,用于治疗和/或预防某些生理状况和/或生理病理,包括:中枢神经系统疾病,癫痫,帕金森氏病,神经退行性疾病,抑郁症,痉挛,催眠,肛交,慢性疼痛,神经痛,头晕,移民,头痛,脑震荡,丛集性头痛,神经元,半球,面部疼痛,蜘蛛眼病,严重头痛,不安的腿部症状,成瘾,运动焦虑,发痒,燃烧,紧张,滥用药物,严重酗酒,奖励综合征,认知障碍,自闭症,阅读障碍,注意力缺陷,高血压,焦虑症,精神分裂症,强迫症,精神病,双相情感障碍,图雷特综合征,中度认知障碍和障碍儿童,青少年和成人的学习,年龄相关的记忆变化,年龄相关的认知能力下降,阿尔茨海默氏病,唐氏综合症,脑外伤ry,亨廷顿舞蹈病,进行性瘫痪,HIV,脑血管意外,血管疾病,Pick或Creutzfeldt-Jacob病,多发性硬化症。 15.根据权利要求2至5中任一项所述的制备(S)-2- [4-(3-氟-苄氧基)-苄氨基]-丙酰胺甲磺酸酯无水物的NF6结晶修饰的方法,其包括以下步骤:(a)在<= 0°C下孵育(S)-2- [4-(3-氟-苄氧基)-苄氨基]-丙酰胺结晶修饰A1的甲磺酸盐一毫秒或几毫秒或几秒钟或几分钟或几小时或几天,O( b)孵育作为混合物组分的二氢酸-2- [4-(3-氟-苯)-苯]丙酰胺,该丙酸至少含有一种另外的A lt组分; = 0毫秒或秒或分钟或天。

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