利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

71 条记录 (耗时 0.034 秒)

    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。

    Substituted imidazo[1,5-A][1,2,4]triazolo[1,5-D][1,4]benzodiazepine derivatives
    2.
    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：US08293730B2

    公开(公告)日：2012-10-23

    申请号：US12618802

    申请日：2009-11-16

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

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

    IPC分类号： A61P25/00 ,  A61K31/55 ,  C07D487/14

    CPC分类号： A61K31/5517 ,  C07D487/14

    摘要： The present invention is concerned with a method of treating Alzheimer's disease by administering a therapeutically effective amount of a substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine of formula I wherein R1, R2, and R3 are as defined herein, and their pharmaceutically acceptable acid addition salts. The invention also provides novel compounds of formula I-A and pharmaceutical compositions containing them.

    摘要翻译： 本发明涉及通过施用治疗有效量的取代咪唑并[1,5-a] [1,2,4]三唑并[1,5-d] [1,4]苯并二氮杂治疗阿尔茨海默病的方法 其中R 1，R 2和R 3如本文所定义，并且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。

    SUBSTITUTED IMIDAZO[1,5-A][1,2,4]TRIAZOLO[1,5-D][1,4]BENZODIAZEPINE DERIVATIVES
    3.
    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]苯并恶嗪衍生物

    公开(公告)号：US20100075954A1

    公开(公告)日：2010-03-25

    申请号：US12618802

    申请日：2009-11-16

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

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

    IPC分类号： A61K31/551 ,  C07D243/10 ,  A61P25/28

    CPC分类号： A61K31/5517 ,  C07D487/14

    摘要： The present invention is concerned with a method of treating Alzheimer's disease by administering a therapeutically effective amount of a substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine of formula I wherein R1, R2, and R3 are as defined herein, and their pharmaceutically acceptable acid addition salts. The invention also provides novel compounds of formula I-A and pharmaceutical compositions containing them.

    摘要翻译： 本发明涉及通过施用治疗有效量的取代咪唑并[1,5-a] [1,2,4]三唑并[1,5-d] [1,4]苯并二氮杂治疗阿尔茨海默病的方法 其中R 1，R 2和R 3如本文所定义，并且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。

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

    Phenyl or pyridinyl-ethynyl derivatives
    6.
    发明授权
    Phenyl or pyridinyl-ethynyl derivatives 有权
    苯基或吡啶基 - 乙炔基衍生物

    公开(公告)号：US08772300B2

    公开(公告)日：2014-07-08

    申请号：US13443911

    申请日：2012-04-11

    申请人： Georg Jaeschke ,  Synese Jolidon ,  Lothar Lindemann ,  Antonio Ricci ,  Daniel Rueher ,  Heinz Stadler ,  Eric Vieira

    发明人： Georg Jaeschke ,  Synese Jolidon ,  Lothar Lindemann ,  Antonio Ricci ,  Daniel Rueher ,  Heinz Stadler ,  Eric Vieira

    IPC分类号： A01N43/54 ,  C07D239/42 ,  C07D401/04

    CPC分类号： C07D213/56 ,  C07D213/57 ,  C07D239/28 ,  C07D401/06 ,  C07D403/06 ,  C07D407/12 ,  C07D413/06

    摘要： The present invention relates to ethynyl derivatives of formula I wherein Y is N or C—R3; R3 is hydrogen, methyl, halogen or nitrile; R1 is phenyl or pyridinyl, each of which is optionally substituted by halogen, lower alkyl or lower alkoxy; R2/R2′ are each independently hydrogen, lower alkyl or lower alkyl substituted by halogen, or R2 and R2′ together with the N-atom to which they are attached form a morpholine ring, a piperidine ring or an azetidine ring, each of which is unsubstituted or substituted one or more substituents selected from lower alkoxy, halogen, hydroxy and methyl; R4/R4′ are each independently hydrogen or lower alkyl, or R4 and R4′ together form a C3-5 cycloalkyl-, tetrahydrofuran- or an oxetane-ring; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5).

    摘要翻译： 本发明涉及式I的乙炔基衍生物，其中Y是N或C-R3; R3是氢，甲基，卤素或腈; R1是苯基或吡啶基，其各自任选被卤素，低级烷基或低级烷氧基取代; R2 / R2'各自独立地为氢，被卤素取代的低级烷基或低级烷基，或R2和R2'与它们所连接的N-原子一起形成吗啉环，哌啶环或氮杂环丁烷环，其中每个 未取代或取代的一个或多个选自低级烷氧基，卤素，羟基和甲基的取代基; R 4 / R 4'各自独立地为氢或低级烷基，或者R 4和R 4'一起形成C 3-5环烷基，四氢呋喃或氧杂环丁烷环; 或其药学上可接受的酸加成盐，或其相应的对映异构体和/或其旋光异构体和/或立体异构体。 式I化合物是代谢型谷氨酸受体亚型5（mGluR5）的正变构调节剂（PAM）。