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    Substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives
    1.
    发明申请
    Substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives 失效
    取代的咪唑并[1,5-a] [1,2,4]三唑并[1,5-d] [1,4]苯并二氮杂衍生物

    公开(公告)号：US20060079507A1

    公开(公告)日：2006-04-13

    申请号：US11245736

    申请日：2005-10-07

    申请人： Henner Knust ,  Heinz Stadler ,  Andrew Thomas

    发明人： Henner Knust ,  Heinz Stadler ,  Andrew Thomas

    IPC分类号： A61K31/551 ,  C07D487/14

    CPC分类号： A61K31/5517 ,  C07D487/14

    摘要： The present invention is concerned with a method of treating a disease selected from the group consisting of cognitive disorders, anxiety, Alzheimer's disease, and schizophrenia comprising administering a therapeutically effective amount of a substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of the following formula wherein R1 is halogen, lower alkyl, lower alkynyl, cycloalkyl, lower alkoxy, OCF3, —NHR, —NHC(O)R or —NHSO2R; R2 is hydrogen, methyl or aryl which is unsubstituted or substituted by one or two substituents selected from the group consisting of halogen and lower alkoxy; R3 is hydrogen, lower alkyl, lower alkenyl, cycloalkyl, lower alkoxy, —O(CH2)n+1—O-lower alkyl, —(CH2)n-aryl which is optionally substituted by lower alkyl or halogen, heteroaryl, —NHR, —N(R)2, wherein each R can be the same or different, —NHCH2C≡CH, or pyrrolidin-1-one; R is hydrogen, lower alkyl, lower alkyl substituted by halogen, heteroaryl, —(CH2)nO-lower alkyl, —NH-lower alkyl, cycloalkyl or aryl, and n is 0, 1, 2 or 3; and with their pharmaceutically acceptable acid addition salts. The invention also provides novel compounds of formula I-A and pharmaceutical compositions containing them. The most preferred indication is Alzheimer's disease.

    摘要翻译： 本发明涉及治疗选自认知障碍，焦虑，阿尔茨海默氏病和精神分裂症的疾病的方法，其包括给予治疗有效量的取代的咪唑并[1,5-a] [1,2， 4]具有下式的三唑并[1,5-d] [1,4]苯并二氮杂其中R 1是卤素，低级烷基，低级炔基，环烷基，低级烷氧基，OCF 3 -NHR，-NHC（O）R或-NHSO 2 R; R 2是未被取代的或被一个或两个选自卤素和低级烷氧基的取代基取代的氢，甲基或芳基; R 3是氢，低级烷基，低级烯基，环烷基，低级烷氧基，-O（CH 2 CH 2）n + 1 -O-低级 烷基， - （CH 2）n - 芳基，其任选被低级烷基或卤素取代，杂芳基，-NHR，-N（R）2 - 其中每个R可以相同或不同，-NHCH 2C≡CH或吡咯烷-1-酮; R为氢，低级烷基，被卤素取代的低级烷基，杂芳基， - （CH 2）n - 低级烷基，-NH-低级烷基，环烷基或芳基， 并且n为0,1,2或3; 和其药学上可接受的酸加成盐。 本发明还提供新颖的式I-A化合物和含有它们的药物组合物。 最优选的指征是阿尔茨海默病。

    Aryl-isoxazole-4-carbonyl-indole-carboxylic acid amide derivatives
    6.
    发明申请
    Aryl-isoxazole-4-carbonyl-indole-carboxylic acid amide derivatives 失效
    芳基异恶唑-4-羰基 - 吲哚羧酸酰胺衍生物

    公开(公告)号：US20070082936A1

    公开(公告)日：2007-04-12

    申请号：US11543178

    申请日：2006-10-04

    申请人： Bernd Buettelmann ,  Bo Han ,  Henner Knust ,  Matthias Nettekoven ,  Andrew Thomas

    发明人： Bernd Buettelmann ,  Bo Han ,  Henner Knust ,  Matthias Nettekoven ,  Andrew Thomas

    IPC分类号： A61K31/42 ,  C07D413/02

    CPC分类号： C07D413/14

    摘要： The present invention is concerned with aryl-isoxazole-4-carbonyl-indole-carboxylic acid amide derivatives of formula I wherein R1, R2, R3, R4, and R5 are as defined in the specification and claims and with their pharmaceutically acceptable acid addition salts. The invention also relates to methods for preparing such compounds. This class of compounds has a high affinity and selectivity for GABA A α5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease. Thus, the invention also is concerned with pharmaceutical compositions containing compounds of formula I or their pharmaceutically acceptable acid addition salts and methods for the treatment of GABA A α5 mediated diseases, including Alzheimer's disease.

    摘要翻译： 本发明涉及式I的芳基 - 异恶唑-4-羰基 - 吲哚 - 羧酸酰胺衍生物，其中R 1，R 2，R 3， R 4，R 4和R 5如说明书和权利要求书及其药学上可接受的酸加成盐所定义。 本发明还涉及制备这些化合物的方法。 这类化合物对GABA Aα5受体结合位点具有高亲和力和选择性，可能作为认知增强剂或治疗阿尔茨海默病等认知障碍。 因此，本发明还涉及含有式I化合物或其药学上可接受的酸加成盐的药物组合物和用于治疗包括阿尔茨海默氏病在内的GABA Aα5介导的疾病的方法。

    Isoxazolo derivatives
    7.
    发明申请
    Isoxazolo derivatives 失效
    异恶唑衍生物

    公开(公告)号：US20070066668A1

    公开(公告)日：2007-03-22

    申请号：US11520394

    申请日：2006-09-13

    申请人： Bernd Buettelmann ,  Bo Han ,  Henner Knust ,  Matthias Nettekoven ,  Andrew Thomas

    发明人： Bernd Buettelmann ,  Bo Han ,  Henner Knust ,  Matthias Nettekoven ,  Andrew Thomas

    IPC分类号： A61K31/42 ,  C07D413/02

    CPC分类号： C07D413/14 ,  C07D413/06 ,  C07D451/06

    摘要： The present invention is concerned with aryl-isoxazole-4-carbonyl-pyrrole-2-carboxylic acid amide derivatives of formula wherein R1, R2, R3, R4, and R5, and m are as defined herein and with their pharmaceutically acceptable acid addition salts. This class of compounds have high affinity and selectivity for GABA A α5 receptor binding sites and therefore may be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.

    摘要翻译： 本发明涉及下式的芳基 - 异恶唑-4-羰基 - 吡咯-2-羧酸酰胺衍生物其中R 1，R 2，R 3， R 4，R 4和R 5，m如本文所定义，并与其药学上可接受的酸加成盐反应。 这类化合物对GABA Aα5受体结合位点具有高亲和力和选择性，因此可用作认知增强剂或治疗认知障碍如阿尔茨海默病。

    Isoxazolo-pyrazine derivatives
    8.
    发明授权
    Isoxazolo-pyrazine derivatives 有权
    异恶唑并吡嗪衍生物

    公开(公告)号：US07902201B2

    公开(公告)日：2011-03-08

    申请号：US12788338

    申请日：2010-05-27

    申请人： Bernd Buettelmann ,  Roland Jakob-Roetne ,  Henner Knust ,  Andrew Thomas

    发明人： Bernd Buettelmann ,  Roland Jakob-Roetne ,  Henner Knust ,  Andrew Thomas

    IPC分类号： A61K31/4965

    CPC分类号： C07D413/12 ,  C07D413/14

    摘要： The invention relates to isoxazolo-pyrazine derivatives and their pharmaceutically acceptable salts having affinity and selectivity for the GABA A α5 receptor binding site, their manufacture, and pharmaceutical compositions containing them. The compounds of the present invention are inverse agonists of GABAAα5. The invention also relates to methods for enhancing cognition and for treating cognitive disorders like Alzheimer's disease.

    摘要翻译： 本发明涉及异恶唑并吡嗪衍生物及其药学上可接受的盐，其对GABA Aα5受体结合位点具有亲和力和选择性，其制备和含有它们的药物组合物。 本发明的化合物是GABAAα5的反向激动剂。 本发明还涉及增强认知和治疗认知障碍如阿尔茨海默病的方法。

    ISOXAZOLO-PYRAZINE DERIVATIVES
    10.
    发明申请
    ISOXAZOLO-PYRAZINE DERIVATIVES 审中-公开
    ISOXAZOLO-PYRAZINE DORIVATIVES

    公开(公告)号：US20100041886A1

    公开(公告)日：2010-02-18

    申请号：US12581192

    申请日：2009-10-19

    申请人： Bernd Buettelmann ,  Roland Jakob-Roetne ,  Henner Knust ,  Andrew Thomas

    发明人： Bernd Buettelmann ,  Roland Jakob-Roetne ,  Henner Knust ,  Andrew Thomas

    IPC分类号： C07D413/02

    CPC分类号： C07D413/12 ,  C07D413/14

    摘要： The invention relates to isoxazolo-pyrazine derivatives and their pharmaceutically acceptable salts having affinity and selectivity for the GABA A α5 receptor binding site, their manufacture, and pharmaceutical compositions containing them. The compounds of present invention are inverse agonists of GABA A α5. The invention also relates to methods for enhancing cognition and for treating cognitive disorders like Alzheimer's disease.

    摘要翻译： 本发明涉及异恶唑并吡嗪衍生物及其药学上可接受的盐，其对GABA Aα5受体结合位点具有亲和性和选择性，其制备和含有它们的药物组合物。 本发明的化合物是GABA Aα5的反向激动剂。 本发明还涉及增强认知和治疗认知障碍如阿尔茨海默病的方法。