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65 条记录 (耗时 0.02 秒)

    Oxadiazolyl imidazobenzodiazepine derivatives pharmaceutical compositions thereof, and method of treating therewith
    25.
    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

    申请人： Frank Watjen ,  Mogens Engelstoft ,  John B. Hansen ,  Leif H. Jensen

    发明人： Frank Watjen ,  Mogens Engelstoft ,  John B. Hansen ,  Leif H. Jensen

    IPC分类号： C07D20060101 ,  C07D271/06 ,  C07D487/04 ,  C07D487/14 ,  A61K31/555

    CPC分类号： C07D271/06 ,  C07D487/04 ,  C07D487/14

    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。

    HYDROCHLORIDE SALT OF AN AZABICYCLO[3.2.1]OCTANE DERIVATIVE
    27.
    发明申请
    HYDROCHLORIDE SALT OF AN AZABICYCLO[3.2.1]OCTANE DERIVATIVE 有权
    亚硫酸氢盐的盐酸盐[3.2.1]月桂衍生物

    公开(公告)号：US20100056561A1

    公开(公告)日：2010-03-04

    申请号：US12529502

    申请日：2008-02-28

    申请人： Trevor John Grinter ,  Peter Moldt ,  Frank Watjen

    发明人： Trevor John Grinter ,  Peter Moldt ,  Frank Watjen

    IPC分类号： A61K31/46 ,  C07D451/02 ,  A61P25/00

    CPC分类号： C07D451/02

    摘要： The invention relates to a hydrochloride salt of (1R,2R,3S,5S)-3-(3,4-dichlorophenyl)-2-[(methyloxy)methyl]-8-azabicyclo[3.2.1]octane, uses of the salt as a medicament in the treatment inter alia of disorders of the central nervous system and pharmaceutical compositions and dosage forms comprising the salt.

    摘要翻译： 本发明涉及（1R，2R，3S，5S）-3-（3,4-二氯苯基）-2 - [（甲氧基）甲基] -8-氮杂双环[3.2.1]辛烷的盐酸盐， 盐作为治疗特别是中枢神经系统病症的药物以及包含该盐的药物组合物和剂型。

    Quinoxalinedione derivatives, their preparation and use
    29.
    发明授权
    Quinoxalinedione derivatives, their preparation and use 失效
    喹喔啉二酮衍生物，其制备和用途

    公开(公告)号：US06703391B2

    公开(公告)日：2004-03-09

    申请号：US08443507

    申请日：1995-05-18

    申请人： Christopher Franklin Bigge ,  Thomas Charles Malone ,  Frank Watjen

    发明人： Christopher Franklin Bigge ,  Thomas Charles Malone ,  Frank Watjen

    IPC分类号： C07D48704

    CPC分类号： C07D471/04 ,  C07D217/04 ,  C07D487/04 ,  C07F9/6561

    摘要： A compound having the formula or a pharmaceutically acceptable salt thereof wherein R is hydrogen or hydroxy; R1 is hydrogen, alkyl, arylalkyl, (CH2)nOH, or (CH2)nNR7R8; R5 and R6 are each independently hydrogen, halogen, NO2, CN, CF3, SO2NR7R8, PO3R9R10, alkyl, alkenyl, alkynyl, (CH2)nCONR7R8, (CH2)nCO2R10, NHCOR11, A is a ring formed by the following: a-NR12—CHR13—CHR14-b, a-CHR13—CHR14—NR12-b, a-CHR13—NR12—CHR14-b, a-CHR14—CH2—NR12—CHR13-b, a-CHR13—NR12—CH2—CHR14-b, a-CH2—CH2—CHR13—NR12-b, a-NR12—CHR13—CHR12—CH2—CH2-b, a-CH2—CH2—NR12—CH2—CH2-b, a-CH2—CH2—CH2NR12—CH2-b, a-CH2—NR12—CH2—CH2-b a-CH2—CH2—CH2—CH2—NR12-b, a-NR12—CH2—CH2—CH2—CH2-b, The compounds are useful in the treatment of disorders responsive to the blockade of glutamic and aspartic acid receptors.

    摘要翻译： 具有下式的化合物或其药学上可接受的盐，其中R是氢或羟基; R 1是氢，烷基，芳基烷基，（CH 2）n OH或（CH 2）n NR 7 R 8; R 5和 R 6各自独立地为氢，卤素，NO 2，CN，CF 3，SO 2 NR 7，PO 3 R 9，烷基，烯基，炔基，（CH 2）n CONR 7 R 8 >，（CH 2）n CO 2 R 10，NHCOR 11，A是由以下形成的环：a-NR 12 -CHR 13 -CHR 14 - ，a-CHR 13 - CHR 14 -NR 12 -b，a-CHR 13 -NR 12 -CHR 14 -b，a-CHR 14 -CH 2 -NR 12 -CHR 13 - b，a-CHR 13 -NR 12 -CH 2 -CHR 14 -b，a-CH 2 -CH 2 -CHR 13 -NR 12 -b，-NR a R 12 -CHR -CH 2 -CH 2-b，a-CH 2 -CH 2 -NR 12 -CH 2 -CH 2 -B，a-CH 2 -CH 2 -CH 2 NR 12 -CH 2 -B，a-CH 2 - NR 12 -CH 2 -CH 2 -BA-CH 2 -CH 2 -CH 2 -CH 2 -NR 12 -b，a-NR 12 -CH 2 -CH 2 -CH 2 -CH 2 -B，该化合物可用于治疗 的阻滞谷氨酸和天冬氨酸受体的病症。

    Indole-2,3-dione-3-oxime derivatives
    30.
    发明授权
    Indole-2,3-dione-3-oxime derivatives 失效
    吲哚-2,3-二酮-3-肟衍生物

    公开(公告)号：US06693111B1

    公开(公告)日：2004-02-17

    申请号：US09584117

    申请日：2000-05-31

    申请人： Frank Watjen ,  Jorgen Drejer

    发明人： Frank Watjen ,  Jorgen Drejer

    IPC分类号： A61K315375

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： Indole-2,3-dione-3-oxime derivatives, for instance compounds represented by the formula are capable of antagonizing the effect of excitatory amino acids, such as glutamate. Also disclosed are methods of preparing the compounds, pharmaceutical compositions comprising them, and methods of treatment of disorders or diseases which are responsive to excitatory amino acid receptor antagonists.

    摘要翻译： 吲哚-2,3-二酮-3-肟衍生物，例如由下式表示的化合物能够拮抗兴奋性氨基酸如谷氨酸的作用。 还公开了制备化合物的方法，包含它们的药物组合物，以及治疗对兴奋性氨基酸受体拮抗剂有反应的病症或疾病的方法。