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1. 发明授权

US06706710B2 Form of (R)-N-[5-methyl-8-(4-methylpiperazin-1-yl)-1,2,3,4-tetrahydro-2-naphthyl]-4-morpholinobenzamide 失效
标题翻译：（R）-N- [5-甲基-8-（4-甲基哌嗪-1-基）-1,2,3,4-四氢-2-萘基] -4-吗啉代苯甲酰胺
公开(公告)号：US06706710B2
公开(公告)日：2004-03-16
申请号：US10333286
申请日：2003-01-17
申请人： Per-Olov Bergström , Martin Hedberg , Mona Lindström , Erica Ståhle
发明人： Per-Olov Bergström , Martin Hedberg , Mona Lindström , Erica Ståhle
IPC分类号： A61K315327
CPC分类号： C07D295/135
摘要： This invention relates to a novel form of a scrotonin h5-HT1B-receptor antagonist, namely a novel form of a salt of (R)-N-[5-methyl-8-(4-methylpiperazin-1-yl)-1,2,2,4-tetrahydro-2-naphtyl]-4-morpholinobenzamide referred to as (R)-N-[5-methyl-8-(4-methylpiperazin-1-yl)-1,2,3,4-tetrahydro-2-naphtyl]-4-morpholinobenzamide monohydrobromide Form A. The invention also relates to processes for preparation of said of Form A, which form has a potential use after suitable pharmaceutical formulation in medical treatment, preferably in CNS disorders, over active bladder or vasospam, or growth control of tumors.
摘要翻译：本发明涉及一种新型形式的角质蛋白h5-HT1B受体拮抗剂，即（R）-N- [5-甲基-8-（4-甲基哌嗪-1-基）称为（R）-N- [5-甲基-8-（4-甲基哌嗪-1-基）-1,2,3,4-四氢-2-萘基] -4-吗啉代苯甲酰胺，四氢-2-萘基] -4-吗啉代苯甲酰胺单氢溴酸盐形式A.本发明还涉及制备所述形式A的方法，该形式在药物治疗中优选在CNS障碍中的适当药物制剂之后具有潜在用途，超过活性膀胱或血管紧张素，或肿瘤的生长控制。

2. 发明申请

US20110281894A1 HEMIFUMARATE SALT 审中-公开
标题翻译：高锰酸盐
公开(公告)号：US20110281894A1
公开(公告)日：2011-11-17
申请号：US13105569
申请日：2011-05-11
申请人： Per-Olov Bergström , Anna Minidis , Robert Ulf Johan Stranne , Mikael Wernersson
发明人： Per-Olov Bergström , Anna Minidis , Robert Ulf Johan Stranne , Mikael Wernersson
IPC分类号： A61K31/506 , A61P7/00 , C07D401/04 , A61P25/16 , C07D213/57 , A61P43/00 , C07D401/14 , 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 (1S)-1-(2-(difluoromethyl)pyridin-4-yl)-4-fluoro-1-(3-(pyrimidin-5-yl)phenyl)-1H-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 Aβ-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/或预防与疾病相关的疾病如唐氏综合征和淀粉样血管病，例如但不限于脑淀粉样血管病或遗传性脑出血的治疗方法，与认知障碍，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，与诸如阿尔茨海默病或痴呆的疾病相关的神经变性，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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