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    • 4. 发明申请
    • NOVEL POLYMORPHIC FORMS OF (S)-2-[-4-(3-FLUORO-BENZYLOXY)-BENZYLAMINO]-PROPIONAMIDE MESYLATE SALT AND PROCESSES OF MANUFACTURING THEREOF
    • (S)-2 - [ - 4-(3-氟 - 苄基) - 苯甲酰胺] - 丙二酰胺盐酸盐的新型多晶型及其制备方法
    • WO2011047767A1
    • 2011-04-28
    • PCT/EP2010/005824
    • 2010-09-23
    • MERCK PATENT GMBHSCHLUETER, DorisSAAL, ChristophKUEHN, ClemensSCHLUETER, Tobias
    • SCHLUETER, DorisSAAL, ChristophKUEHN, ClemensSCHLUETER, Tobias
    • C07C237/06A61K31/165A61P25/00
    • C07C237/06
    • The present invention relates to (S)-2-[4-(3-Fluoro-benzyloxy)-benzylamino]- propionamide mesylate anhydrate and crystalline modifications thereof. The present invention further relates to processes of manufacturing these crystalline modifications as well as their use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions selected from the group consisting of "central nervous system disorders, epilepsy, Parkinson's disease, neurodegenerative processes, depression, spasm, hypnosis, analgesia, chronic pain, neuropathic pain, head pain conditions, migraine, headache, cluster headache, neuralgia, hemicrania, facial pain, arachnoiditis, severe headache, restless legs syndrome, addictive disorders, motor restlessness, creeping, burning, pulling sensations, drug abuse, severe alcoholism, reward deficiency syndrome, cognitive disorders, autism, dyslexia, attention deficit hyperactivity disorder, anxiety, schizophrenia, obsessive compulsive disorders, psychosis, bipolar disorder, Tourette's syndrome, mild cognitive impairment and disorders of learning in children, adolescents and adults, age associated memory impairment, age associated cognitive decline, Alzheimer's disease, Down's Syndrome, traumatic brain injury Huntington's disease, progressive supranuclear Palsy, HIV, stroke, vascular diseases, Pick's or Creutzfeldt-Jacob diseases, multiple sclerosis".
    • 本发明涉及(S)-2- [4-(3-氟 - 苄氧基) - 苄氨基] - 丙酰胺甲磺酸盐水合物及其结晶修饰物。 本发明还涉及制造这些结晶修饰物的方法及其在治疗和/或预防选自“中枢神经系统疾病,癫痫,帕金森病,神经退行性过程中的生理和/或病理生理状况”中的用途 ,抑郁症,痉挛,催眠,镇痛,慢性疼痛,神经性疼痛,头痛症状,偏头痛,头痛,头痛,神经痛,血红素,面部疼痛,蛛网膜炎,严重头痛,不宁腿综合症,上瘾症,运动不安, 灼热,拉扯感觉,药物滥用,严重酒精中毒,奖励缺陷综合征,认知障碍,自闭症,阅读障碍,注意力缺陷多动障碍,焦虑症,精神分裂症,强迫症,精神病,双相情感障碍,Tourette综合征,轻度认知障碍和学习障碍 在儿童,青少年和成年人中,年龄与我相关 多发性神经损伤,年龄相关认知衰退,阿尔茨海默病,唐氏综合征,创伤性脑损伤亨廷顿舞蹈病,进行性核上性麻痹,艾滋病毒,中风,血管疾病,Pick's或Creutzfeldt-Jacob疾病,多发性硬化症“。