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    HELICASE-PRIMASE INHIBITORS FOR USE IN A METHOD OF TREATING ALZHEIMER'S DISEASE
    7.
    发明申请
    HELICASE-PRIMASE INHIBITORS FOR USE IN A METHOD OF TREATING ALZHEIMER'S DISEASE 审中-公开
    用于治疗阿尔茨海默病的方法中使用的初次使用抑制剂

    公开(公告)号：US20150374676A1

    公开(公告)日：2015-12-31

    申请号：US14767163

    申请日：2014-02-12

    申请人： AICURIS GMBH & CO. KG

    发明人： Ruth ITZHAKI

    IPC分类号： A61K31/4439 ,  A61K31/185 ,  A61K9/14

    CPC分类号： A61K31/4439 ,  A61K9/14 ,  A61K31/185 ,  A61K31/426 ,  A61K31/427

    摘要： The present invention relates to the use of helicase-primase inhibitors in a method of treating Alzheimer's Disease (AD). Particularly, the present invention relates to the use of helicase-primase inhibitors in a method of treating AD in a subject that is having HSV-1 infection and is having AD or is having HSV-1 infection and is suspected of having AD.The provided antiviral helicase-primase inhibitors affect the accumulation of the key AD proteins amyloid beta and abnormally phosphorylated tau that occur during HSV-1 infection.

    摘要翻译： 本发明涉及在治疗阿尔茨海默病（AD）的方法中使用解旋酶抑制剂。 特别地，本发明涉及在具有HSV-1感染并且具有AD或具有HSV-1感染并且怀疑具有AD的受试者中治疗AD的方法中使用解旋酶抑制剂。 所提供的抗病毒解旋酶启动子酶抑制剂影响在HSV-1感染期间发生的关键AD蛋白淀粉样蛋白β和异常磷酸化tau的积累。

    CRYSTALLINE N-[5-(AMINOSULFONYL)-4-METHYL-1,3-THIAZOL-2-YL]-N-METHYL-2-[4-(2-PYRIDINYL)PHENYL]ACETAMIDE MONO MESYLATE MONOHYDRATE HAVING A SPECIFIC PARTICLE SIZE DISTRIBUTION RANGE AND A SPECIFIC SURFACE AREA RANGE FOR USE IN PHARMACEUTICAL FORMULATIONS
    8.
    发明申请
    CRYSTALLINE N-[5-(AMINOSULFONYL)-4-METHYL-1,3-THIAZOL-2-YL]-N-METHYL-2-[4-(2-PYRIDINYL)PHENYL]ACETAMIDE MONO MESYLATE MONOHYDRATE HAVING A SPECIFIC PARTICLE SIZE DISTRIBUTION RANGE AND A SPECIFIC SURFACE AREA RANGE FOR USE IN PHARMACEUTICAL FORMULATIONS 有权
    N- [5-（氨基甲酰基）-4-甲基-1,3-噻唑-2-基] -N-甲基-2- [4-（2-吡啶基）苯基]乙酰胺单甲酸酯单磺酸盐具有特定颗粒尺寸 分配范围和用于制药配方的特定面积范围

    公开(公告)号：US20150366849A1

    公开(公告)日：2015-12-24

    申请号：US14840763

    申请日：2015-08-31

    申请人： AICURIS GMBH & CO. KG

    发明人： Wilfried SCHWAB ,  Alexander BIRKMANN ,  Kerstin PAULUS ,  Kurt VOGTLI ,  Dieter HAAG ,  Stephan MAAS ,  Kristian RUEPP

    IPC分类号： A61K31/4439 ,  A61K9/16 ,  A61K45/06

    CPC分类号： A61K31/4439 ,  A61K9/145 ,  A61K9/16 ,  A61K31/10 ,  A61K45/06 ,  C07D417/12 ,  Y10T428/2982

    摘要： The present invention relates to the crystalline mono mesylate monohydrate salt of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide in a definite particle size range, particle size distribution and a specific surface area range, which has demonstrated increased long term stability and release kinetics from pharmaceutical compositions, as well as to pharmaceutical compositions containing said crystalline N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide mono mesylate monohydrate having the afore-mentioned particle size range, particle size distribution and specific surface area range. Moreover, the present invention relates to the pharmacokinetic and pharmacodynamic in vivo profiles of the resultant free base of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]-acetamide after administration of the afore-mentioned crystalline N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]-acetamide mono mesylate monohydrate salt to a subject in need thereof.

    摘要翻译： 本发明涉及N- [5-（氨基磺酰基）-4-甲基-1,3-噻唑-2-基] -N-甲基-2- [4-（2-吡啶基） 苯基]乙酰胺，其具有确定的粒度范围，粒度分布和比表面积范围，其已经证明了药物组合物的长期稳定性和释放动力学的增加，以及含有所述N- [5-（氨基磺酰基） ）-4-甲基-1,3-噻唑-2-基] -N-甲基-2- [4-（2-吡啶基）苯基]乙酰胺单甲磺酸酯一水合物，具有上述粒度范围，粒度分布和 比表面积范围。 此外，本发明涉及得到的N- [5-（氨基磺酰基）-4-甲基-1,3-噻唑-2-基] -N-甲基-2-吡咯烷酮的游离碱的体内药代动力学和药效学特征， [4-（2-吡啶基）苯基] - 乙酰胺在给予上述N- [5-（氨基磺酰基）-4-甲基-1,3-噻唑-2-基] -N-甲基-2- [4-（2-吡啶基）苯基] - 乙酰胺单甲磺酸盐一水合物盐。

    Salts of a dihydroquinazoline derivative
    9.
    发明申请
    Salts of a dihydroquinazoline derivative 有权
    二氢喹唑啉衍生物的盐

    公开(公告)号：US20150045371A1

    公开(公告)日：2015-02-12

    申请号：US14381625

    申请日：2013-02-28

    申请人： AiCuris GmbH & Co. KG

    发明人： Welljanne Maertens ,  Christian Schickaneder

    IPC分类号： C07D239/84 ,  C07C309/30 ,  C07C309/29

    CPC分类号： C07D239/84 ,  C07C309/29 ,  C07C309/30

    摘要： The invention relates to besylate and tosylate salts of {8-fluoro-2-[4-(3-methoxyphenyl)piperazin-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-3,4-dihydroquinazolin-4-yl}acetic acid and solvates thereof, to the use thereof in a method of treating and/or preventing virus infections, and to the use thereof to produce drugs for use in treating and/or preventing diseases, in particular use as antiviral agents, in particular against cytomegaloviruses.

    摘要翻译： 本发明涉及{8-氟-2- [4-（3-甲氧基苯基）哌嗪-1-基] -3- [2-甲氧基-5-（三氟甲基）苯基] -3,4-苯并噻喃的苯磺酸盐和甲苯磺酸盐， 二氢喹唑啉-4-基}乙酸及其溶剂化物，用于治疗和/或预防病毒感染的方法及其用途，用于制备用于治疗和/或预防疾病的药物，特别是用作 抗病毒剂，特别是针对巨细胞病毒。