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1. 发明申请

WO2011142716A1 NOVEL HEMIFUMARATE SALT OF ISOINDOLE COMPOUND ACTING AS BACE INHIBITOR 审中-公开
标题翻译：新型化合物作为化合物抑制剂的盐酸盐
公开(公告)号：WO2011142716A1
公开(公告)日：2011-11-17
申请号：PCT/SE2011/050592
申请日：2011-05-11
申请人： ASTRAZENECA AB , BERGSTRÖM, Per-Olov , MINIDIS, Anna , STRANNE, Robert, Ulf, Johan , WERNERSSON, Mikael
发明人： BERGSTRÖM, Per-Olov , MINIDIS, Anna , STRANNE, Robert, Ulf, Johan , WERNERSSON, Mikael
IPC分类号： C07D401/14 , A61K31/506 , A61P25/28
CPC分类号： C07D401/14 , C07D213/50 , C07D401/04
摘要： The present invention relates to a hemifumarate salt of the compound (1 S )-1-(2- (difluoromethyl)pyridin-4-yl)-4-fluoro-1-(3-(pyrimidin-5-yl)phenyl)-1 H -isoindol-3-amine, Form A thereof and its pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Αβ-related pathologies such as Downs syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI ("mild cognitive impairment"), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.
摘要翻译：本发明涉及化合物（1S）-1-（2-（二氟甲基）吡啶-4-基）-4-氟-1-（3-（嘧啶-5-基）苯基）-1H的半富马酸盐 - 异吲哚-3-胺，其A型及其药物组合物。此外，本发明涉及用于治疗和/或预防ß相关病理学的治疗方法，例如唐氏综合征，β-淀粉样变性血管病，例如但不限于脑淀粉样血管病或遗传性脑出血，与认知相关的疾病损伤例如但不限于MCI（“轻度认知障碍”），阿尔茨海默病，记忆丧失，与阿尔茨海默病相关的注意力缺陷症状，与疾病如阿尔茨海默病或痴呆相关的神经变性，包括混合血管和退行性来源的痴呆老年性痴呆，老年性痴呆和与帕金森病相关的痴呆，进行性核上性麻痹或皮质基底变性。

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