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    • 1. 发明申请
    • PHARMACEUTICALLY USEFUL SALTS OF CARBOXYLIC ACID DERIVATES
    • 羧甲酸衍生物的药用有效的盐
    • WO2004110984A1
    • 2004-12-23
    • PCT/SE2004/000964
    • 2004-06-16
    • ASTRAZENECA ABAURELL, Carl-JohanDAHLSTRÖM, MikaelLINDSTEDT-ALSTERMARK, Eva-LotteMINIDIS, AnnaOHLSSON, BengtSTÅHLE, Erica
    • AURELL, Carl-JohanDAHLSTRÖM, MikaelLINDSTEDT-ALSTERMARK, Eva-LotteMINIDIS, AnnaOHLSSON, BengtSTÅHLE, Erica
    • C07C235/20
    • C07C235/20C07B2200/07
    • A compound selected from one or more of the following: a ( 1 R ,2 S )-2-hydroxyindan-1-amine salt of (2 S )-2-ethoxy-3-(4-{2-[hexyl(2-phenylethyl)amino]-2-oxoethoxy}phenyl)propanoic acid; an L-arginine salt of (2 S )-2-ethoxy-3-(4-{2-[hexyl(2-phenylethyl)amino-2-oxoethoxyphenyl)propanoic acid; a tert -butylamine salt of (2 S )-2-ethoxy-3-(4-{2-[hexyl(2-phenylethyl)amino-2-oxoethoxyphenyl)propanoic acid; a choline salt of (2 S )-2-ethoxy-3-(4-{2-[hexyl(2-phenylethyl)amino]-2-oxoethoxy}phenyl)propanoic acid; an adamantylamine salt of (2 S )-2-ethoxy-3-(4-{2-[hexyl(2-phenylethyl)amino]-2-oxoethoxy}phenyl)propanoic acid; a N -benzyl-2-phenylethanaminium salt of (2 S )-2-ethoxy-3-(4-{2-[hexyl(2-phenylethyl)amino]-2-oxoethoxy}phenyl)propanoic acid; a N -benzyl-2-(benzylamino) ethanaminium salt of (2 S )-2-ethoxy-3-(4-{2-[hexyl(2-phenylethyl)amino]-2-oxoethoxy}phenyl)propanoic acid; or a tris(hydroxymethyl)methylamine salt of (2 S )-2-ethoxy-3-(4-{2-[hexyl(2-phenylethyl)amino]-2-oxoethoxy}phenyl)propanoic acid.
    • 选自下列一种或多种的化合物:(2S)-2-乙氧基-3-(4- {2- [己基(2-苯基乙基) 氨基] -2-氧代乙氧基}苯基)丙酸; (2S)-2-乙氧基-3-(4- {2- [己基(2-苯基乙基)氨基-2-氧代乙氧基苯基)丙酸的L-精氨酸盐; (2S)-2-乙氧基-3-(4- {2- [己基(2-苯基乙基)氨基-2-氧代乙氧基苯基)丙酸的叔丁基胺盐; (2S)-2-乙氧基-3-(4- {2- [己基(2-苯基乙基)氨基] -2-氧代乙氧基}苯基)丙酸的胆碱盐; (2S)-2-乙氧基-3-(4- {2- [己基(2-苯基乙基)氨基] -2-氧代乙氧基}苯基)丙酸的金刚烷基胺盐; (2S)-2-乙氧基-3-(4- {2- [己基(2-苯基乙基)氨基] -2-氧代乙氧基}苯基)丙酸的N-苄基-2-苯基乙胺盐; (2S)-2-乙氧基-3-(4- {2- [己基(2-苯基乙基)氨基] -2-氧代乙氧基}苯基)丙酸的N-苄基-2-(苄基氨基)乙胺盐; 或(2S)-2-乙氧基-3-(4- {2- [己基(2-苯基乙基)氨基] -2-氧代乙氧基}苯基)丙酸的三(羟甲基)甲胺盐。
    • 4. 发明申请
    • NOVEL HEMIFUMARATE SALT OF ISOINDOLE COMPOUND ACTING AS BACE INHIBITOR
    • 新型化合物作为化合物抑制剂的盐酸盐
    • WO2011142716A1
    • 2011-11-17
    • PCT/SE2011/050592
    • 2011-05-11
    • ASTRAZENECA ABBERGSTRÖM, Per-OlovMINIDIS, AnnaSTRANNE, Robert, Ulf, JohanWERNERSSON, Mikael
    • BERGSTRÖM, Per-OlovMINIDIS, AnnaSTRANNE, Robert, Ulf, JohanWERNERSSON, Mikael
    • C07D401/14A61K31/506A61P25/28
    • C07D401/14C07D213/50C07D401/04
    • 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.
    • 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。