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109 条记录 (耗时 0.048 秒)

    Substituted imidazo [1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives
    102.
    发明授权
    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：US07671048B2

    公开(公告)日：2010-03-02

    申请号：US11245736

    申请日：2005-10-07

    申请人： Henner Knust ,  Heinz Stadler ,  Andrew William Thomas

    发明人： Henner Knust ,  Heinz Stadler ,  Andrew William Thomas

    IPC分类号： A61P25/28 ,  A61K31/5517 ,  C07D487/12

    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]三唑并[1,5-d] [1,4]苯并二氮杂衍生物其中R1是卤素，低级烷基，低级炔基，环烷基，低级烷氧基，OCF3，-NHR，-NHC（O） NHSO2R; R2是氢，甲基或芳基，其未被取代或被一个或两个选自卤素和低级烷氧基的取代基取代; R3是氢，低级烷基，低级烯基，环烷基，低级烷氧基，-O（CH2）n + 1-O-低级烷基， - （CH2）n-芳基，其任选被低级烷基或卤素，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 O-低级烷基，-NH-低级烷基，环烷基或芳基，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。

    Substitued imidazo [1,5-A][1,2,4]triazolo[1,5-D][1,4]benzodiazepine derivatives
    104.
    发明授权
    Substitued 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：US07432256B2

    公开(公告)日：2008-10-07

    申请号：US11297691

    申请日：2005-12-08

    申请人： Bernd Buettelmann ,  Henner Knust ,  Andrew William Thomas

    发明人： Bernd Buettelmann ,  Henner Knust ,  Andrew William Thomas

    IPC分类号： A61P25/28 ,  A61K31/551 ,  C07D487/12

    CPC分类号： C07D487/14

    摘要： The present invention is concerned with substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of the formula I wherein R1 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, nitro, cycloalkyl, —O(CH2)mO(CH2)mOH or —C≡C—R′; R2 is hydrogen or methyl; R3 is lower alkyl, lower alkyl substituted by halogen, lower alkenyl, lower alkenyl substituted by halogen, lower alkynyl, —(CH2)n-cycloalkyl, —(CR′R″)m—CH3, phenyl that is unsubstituted or substituted by halogen, pyridinyl or thienyl each of which is unsubstituted or substituted by lower alkyl, —(CH2)n—NH-cycloalkyl, lower alkenyl-cycloalkyl, lower alkynyl-(CR′R″)mOH, or lower alkynyl-phenyl wherein the phenyl ring is unsubstituited or substituted by halogen, CF3, lower alkyl or lower alkoxy; R′ is hydrogen or lower alkyl; R″ is hydrogen, hydroxy or lower alkyl; n is 0, 1 or 2; m is 1, 2 or 3; and o is 1 or 2; and pharmaceutically acceptable acid addition salts thereof. This class of compounds have high affinity and selectivity for GABA A α5 receptor binding sites. Thus, the invention also relates to methods of enhancing cognition and treating cognitive disorders like Alzheimer's disease.

    摘要翻译： 本发明涉及式I的取代的咪唑并[1,5-a] [1,2,4]三唑并[1,5-d] [1,4]苯并二氮杂衍生物，其中R 1， >是氢，卤素，低级烷基，被卤素取代的低级烷基，低级烷氧基，被卤素取代的低级烷氧基，硝基，环烷基，-O（CH 2 CH 2）m O （CH 2）2 OH或-C≡C-R'; R 2是氢或甲基; R 3是低级烷基，被卤素取代的低级烷基，低级烯基，被卤素取代的低级链烯基，低级炔基， - （CH 2 SO 2）n

    Aryl-isoxazol-4-yl-imidazole derivatives
    105.
    发明授权
    Aryl-isoxazol-4-yl-imidazole derivatives 失效
    芳基异恶唑-4-基 - 咪唑衍生物

    公开(公告)号：US07414061B2

    公开(公告)日：2008-08-19

    申请号：US11640622

    申请日：2006-12-18

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

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

    IPC分类号： A61K31/506 ,  A61K31/4439 ,  A61K31/42 ,  C07D413/14

    CPC分类号： C07D413/04

    摘要： The present invention is concerned with aryl-isoxazol-4-yl-imidazole derivatives of formula I: wherein R1 to R6 are as defined in the specification and pharmaceutically acceptable acid addition salts thereof. This class of compounds has 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.

    摘要翻译： 本发明涉及式I的芳基 - 异恶唑-4-基 - 咪唑衍生物：其中R 1至R 6如本说明书和药学上可接受的酸所定义 其加成盐。 这类化合物对GABA Aα5受体结合位点具有高亲和力和选择性，可用作认知增强剂或用于治疗认知障碍如阿尔茨海默病。

    Aryl-4-ethynyl-isoxazole derivatives
    106.
    发明申请
    Aryl-4-ethynyl-isoxazole derivatives 失效
    芳基-4-乙炔基 - 异恶唑衍生物

    公开(公告)号：US20070287739A1

    公开(公告)日：2007-12-13

    申请号：US11805640

    申请日：2007-05-24

    申请人： Bernd Buettelmann ,  Henner Knust ,  Andrew Thomas

    发明人： Bernd Buettelmann ,  Henner Knust ,  Andrew Thomas

    IPC分类号： A61K31/42 ,  C07D261/06

    CPC分类号： C07D413/06 ,  C07D261/08 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04

    摘要： The present invention is concerned with aryl-4-ethynyl-isoxazole derivatives of formula I wherein R1 to R5 are as described in the specification and pharmaceutically acceptable salt thereof. This class of compounds has high affinity and selectivity for GABA A α5 receptor binding sites, being useful as a cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.

    摘要翻译： 本发明涉及式I的芳基-4-乙炔基 - 异恶唑衍生物，其中R 1至R 5如说明书及其药学上可接受的盐所述。 这类化合物对GABA Aα5受体结合位点具有高亲和力和选择性，可用作认知增强剂或用于治疗认知障碍如阿尔茨海默病。

    Aryl-isoxazolo-4-yl-oxadiazole derivatives
    107.
    发明申请
    Aryl-isoxazolo-4-yl-oxadiazole derivatives 失效
    芳基异恶唑-4-基 - 恶二唑衍生物

    公开(公告)号：US20070161686A1

    公开(公告)日：2007-07-12

    申请号：US11639695

    申请日：2006-12-15

    申请人： Bernd Buettelmann ,  Bo Han ,  Henner Knust ,  Andreas Koblet ,  Andrew Thomas

    发明人： Bernd Buettelmann ,  Bo Han ,  Henner Knust ,  Andreas Koblet ,  Andrew Thomas

    IPC分类号： A61K31/4245 ,  C07D413/02

    CPC分类号： C07D413/04 ,  C07D413/14

    摘要： The present invention is concerned with isoxazol-4-yl-oxadiazole derivatives of formula wherein R1, R2, and R3, are as defined in the specification and pharmaceutically acceptable acid addition salts thereof. This class of compounds has 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.

    摘要翻译： 本发明涉及下式的异恶唑-4-基 - 恶二唑衍生物其中R 1，R 2，R 3和R 3为 在本说明书中定义及其药学上可接受的酸加成盐。 这类化合物对GABA Aα5受体结合位点具有高亲和力和选择性，可用作认知增强剂或用于治疗认知障碍如阿尔茨海默病。

    Substituted imidazol[1,5-A][1,2,4]triazolo[1,5-D][1,4]benzodiazepine derivatives
    108.
    发明申请
    Substituted imidazol[1,5-A][1,2,4]triazolo[1,5-D][1,4]benzodiazepine derivatives 有权
    取代的咪唑[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：US20060084642A1

    公开(公告)日：2006-04-20

    申请号：US11252025

    申请日：2005-10-17

    申请人： Henner Knust ,  Andrew Thomas

    发明人： Henner Knust ,  Andrew Thomas

    IPC分类号： A61K31/551 ,  C07D487/14

    CPC分类号： C07D487/14

    摘要： The present invention is concerned with substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of formula I wherein R1 is hydrogen, halogen, lower alkyl, lower alkynyl, cycloalkyl, heterocycloalkyl, benzyl, cyano, lower alkoxy, OCF3, —NHR, —NHC(O)R or —NHSO2R; R2 is lower alkyl substituted by halogen; R3 is hydrogen, methyl or aryl; R is lower alkyl, cycloalkyl or aryl; and pharmaceutically acceptable acid addition salts thereof. Such compounds have 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, anxiety, schizophrenia or Alzheimer's disease.

    摘要翻译： 本发明涉及式I的取代咪唑并[1,5-a] [1,2,4]三唑并[1,5-d] [1,4]苯并二氮杂衍生物，其中R 1， 氰基，低级烷氧基，OCF 3，-NHR，-NHC（O）R或-NHSO 2，其中R 1是氢，卤素，低级烷基，低级炔基，环烷基，杂环烷基， SUB> R R 2是被卤素取代的低级烷基; R 3是氢，甲基或芳基; R是低级烷基，环烷基或芳基; 及其药学上可接受的酸加成盐。 这样的化合物对GABA Aα5受体结合位点具有高亲和力和选择性，并且可用作认知增强剂或治疗认知障碍，焦虑，精神分裂症或阿尔茨海默病。

    Substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives
    109.
    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。