Indole derivatives as potassium channel blockers
    1.
    发明授权
    Indole derivatives as potassium channel blockers 失效
    吲哚衍生物作为钾通道阻滞剂

    公开(公告)号:US5158969A

    公开(公告)日:1992-10-27

    申请号:US748050

    申请日:1991-08-21

    IPC分类号: A61K31/40

    CPC分类号: A61K31/40

    摘要: A method of treating a disease in a mammal, including a human, responsive to blockade of potassium channels, which comprises administering to a mammal in need thereof an effective amount of a compound having the formula ##STR1## wherein R.sup.11, R.sup.12, R.sup.13, R.sup.14 and R.sup.15 independently of each other are hydrogen, CF.sub.3, NO.sub.2, NH.sub.2, OH, C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy or phenyl; andR.sup.4, R.sup.5, R.sup.6 and R.sup.7 independently of each other are hydrogen, halogen, CF.sub.3, C.sub.1-6 -alkyl, NO.sub.2, NH.sub.2, OH or C.sub.1-6 -alkoxy,and a method as above wherein 1-(4-methoxyphenyl)-indole is employed,and a method as above wherein depression, memory disorders, Alzheimers disease and diabetes 2 is treated,and further a method as above wherein the active ingredient is administered in the form of a pharmaceutical composition thereof, in which it is present together with a pharmaceutically-acceptable carrier or diluent.

    Oxadiazolyl imidazobenzodiazepine derivatives pharmaceutical
compositions thereof, and method of treating therewith
    7.
    发明授权
    Oxadiazolyl imidazobenzodiazepine derivatives pharmaceutical compositions thereof, and method of treating therewith 失效
    恶二唑基咪唑并二氮杂衍生物药物组合物及其处理方法

    公开(公告)号:US4670433A

    公开(公告)日:1987-06-02

    申请号:US837100

    申请日:1986-03-06

    摘要: New oxadiazolyl imidazobenzodiazepine derivatives having the formula ##STR1## wherein R.sup.3 has the formula ##STR2## wherein R" is hydrogen, C.sub.1-6 alkyl C.sub.1-6 alkoxymethyl or C.sub.3-6 - cycloalkyl;R.sup.4 is hydrogen;R.sup.5 is C.sub.1-6 alkyl or R.sup.4 and R.sup.5 together form a 2-4 membered alkylene bridge; and R.sup.A is C.sub.1-6 alkyl, C.sub.1-6 alkoxy, or C.sub.1-3 trifluoroalkyl, pharmaceutical compositions thereof, and method of treating therewith, are disclosed.The compounds and pharmaceutical compositions are useful in the amelioration, mitigation, or elimination of central nervous system disorders related to benzodiazepine receptors and especially as anticonvulsants, anxiolytics, hypnotics, and nootropics.

    摘要翻译: 具有式“IMAGE”的新的恶二唑基咪唑并二氮杂衍生物,其中R 3具有式“IMAGE”,其中R“是氢,C 1-6烷基C 1-6烷氧基甲基或C 3-6 - 环烷基; R4是氢; R5是C1-6烷基或R4和R5一起形成2-4元亚烷基桥; RA是C 1-6烷基,C 1-6烷氧基或C 1-3三氟烷基,其药物组合物及其处理方法。 化合物和药物组合物可用于改善,缓解或消除与苯二氮卓类受体相关的中枢神经系统疾病,特别是抗惊厥药,抗焦虑药,催眠药和嗜酸剂。

    Indole-derivatives, method of treatment therewith, and pharmaceutical
compositions comprising such compounds
    9.
    发明授权
    Indole-derivatives, method of treatment therewith, and pharmaceutical compositions comprising such compounds 失效
    吲哚衍生物,其治疗方法和包含这些化合物的药物组合物

    公开(公告)号:US5478859A

    公开(公告)日:1995-12-26

    申请号:US259016

    申请日:1994-06-13

    CPC分类号: C07D209/40

    摘要: The present patent application discloses compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sup.21 and R.sup.22 each independently are alkyl; andR.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.11, R.sup.12, R.sup.13, and R.sup.14 each independently are hydrogen, halogen, CF.sub.3, CN, or NO.sub.2.The compounds are useful as in vivo active glutamate antagonists.

    摘要翻译: 本专利申请公开了具有式“IMAGE”的化合物或其药学上可接受的盐,其中R 21和R 22各自独立地为烷基; 并且R 1,R 2,R 3,R 4,R 11,R 12,R 13和R 14各自独立地为氢,卤素,CF 3,CN或NO 2。 这些化合物可用作体内活性谷氨酸拮抗剂。

    Isatineoxime derivatives and their use
    10.
    发明授权
    Isatineoxime derivatives and their use 失效
    伊马替尼肟衍生物及其用途

    公开(公告)号:US5223527A

    公开(公告)日:1993-06-29

    申请号:US899620

    申请日:1992-06-16

    IPC分类号: C07D209/60

    CPC分类号: C07D209/60

    摘要: A compound having the formula ##STR1## wherein R.sup.1 is C.sub.1-6 -alkyl which may be branched or cyclic;R.sup.2 is C.sub.1-6 -alkyl which may be branched or cyclic; or wherein R.sup.1 and R.sup.2 together represent --(CH.sub.2).sub.n --, wherein n is 3, 4, 5.and a method of treating disorders of a mammal, including a human, responsive to the blockade of glutamic and aspartic acid receptors, with the same.

    摘要翻译: 具有式“IMAGE”的化合物,其中R 1是可以是支链或环状的C 1-6 - 烷基; R2是可以是支链或环状的C 1-6 - 烷基; 或其中R 1和R 2一起表示 - (CH 2)n - ,其中n为3,4,5。以及治疗对谷氨酸和天冬氨酸受体的封闭反应的哺乳动物(包括人)的病症的方法,其中 相同。