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22 条记录 (耗时 0.015 秒)

    Indole-derivatives, method of treatment therewith, and pharmaceutical compositions comprising such compounds
    1.
    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

    申请人： Frank Watjen ,  Jorgen Drejer ,  Leif H. Jensen

    发明人： Frank Watjen ,  Jorgen Drejer ,  Leif H. Jensen

    IPC分类号： C07D209/40 ,  A61K31/40 ,  C07D403/12

    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
    2.
    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

    申请人： Frank Watjen ,  Jorgen Drejer ,  Leif H. Jensen

    发明人： Frank Watjen ,  Jorgen Drejer ,  Leif H. Jensen

    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。

    Isatine derivatives, their preparation and use
    3.
    发明授权
    Isatine derivatives, their preparation and use 失效
    伊马替尼衍生物，其制备和用途

    公开(公告)号：US5198461A

    公开(公告)日：1993-03-30

    申请号：US710790

    申请日：1991-06-05

    申请人： Frank Watjen ,  Jorgen Drejer ,  Leif H. Jensen

    发明人： Frank Watjen ,  Jorgen Drejer ,  Leif H. Jensen

    IPC分类号： C07D209/40

    CPC分类号： C07D209/40

    摘要： A method of treatment with compounds having the formula ##STR1## R.sup.1 is hydrogen, C.sub.1-6 -alkyl which may be branched, C.sub.3-7 -cycloalkyl, benzyl, phenyl which may be substituted, acyl, hydroxy, C.sub.1-6 -alkoxy, CH.sub.2 CO.sub.2 R' wherein R' is hydrogen or C.sub.1-6 -alkyl which may be branched, CH.sub.2 CN, CH.sub.2 CONR.sup.IV R.sup.V wherein R.sup.IV and R.sup.V independently are hydrogen or C.sub.1-6 -alkyl, or CH.sub.2 C(.dbd.NOH)NH.sub.2 ; R.sup.2 is hydrogen, benzyl, C.sub.1-6 -alkyl which may be branched, or C.sub.3-7 -cycloalkyl; R.sup.4, R.sup.5, R.sup.6, R.sup.7 independently are hydrogen, C.sub.1-6 -alkyl which may be branched, phenyl, halogen, C.sub.1-6 -alkoxy, NO.sub.2, CN, CF.sub.3, OCF.sub.3, or SO.sub.2 NR"R'" wherein R" and R'" independently are hydrogen, aralkoxy, aralkyl, or C.sub.1-6 -alkyl; or R.sup.6 and R.sup.7 together form an additional 4 to 7 membered ring which may be aromatic or partial saturated and which may be substituted with halogen, NO.sub.2, CF.sub.3, CN, OCF.sub.3, SO.sub.2 NR" R"' wherein R" and R"' independently are hydrogen, aralkoxy, aralkyl, or C.sub.1-6 -alkyl, and R.sup.4 and R.sup.5 have the meanings set forth above, are disclosed, as well as pharmaceutical compositions thereof. Certain of the compounds are novel.The compounds and pharmaceutical compositions containing the compounds are useful in the treatment of central nervous system disorders and especially conditions sensitive to excitatory amino acids.

    摘要翻译： 具有下式的化合物的方法是氢，可以是支链的C 1-6 - 烷基，C 3-7 - 环烷基，苄基，可被取代的苯基，酰基，羟基，C 1-6 - 烷氧基， CH2CO2R'其中R'是氢或可以是支链的C 1-6 - 烷基，CH 2 CN，CH 2 CONRIVRV其中RIV和RV独立地是氢或C 1-6 - 烷基或CH 2 C（= NOH）NH 2; R2是氢，苄基，可以是支链的C 1-6 - 烷基或C 3-7 - 环烷基; R4，R5，R6，R7独立地是氢，可以是支链的C1-6烷基，苯基，卤素，C1-6烷氧基，NO2，CN，CF3，OCF3或SO2NR''R“ '和R“独立地是氢，芳烷氧基，芳烷基或C 1-6 - 烷基; 或R6和R7一起形成另外的4至7元环，其可以是芳族或部分饱和的并且可以被卤素，NO 2，CF 3，CN，OCF 3，SO 2 NR“R”取代，其中R“和R' 独立地是氢，芳烷氧基，芳烷基或C 1-6 - 烷基，并且R 4和R 5具有上述含义，以及其药物组合物。 某些化合物是新颖的。 含有这些化合物的化合物和药物组合物可用于治疗中枢神经系统疾病，特别是对兴奋性氨基酸敏感的病症。

    Method of antagonizing excitatory amino acids by administration of imidazobenzodiazepine compounds
    4.
    发明授权
    Method of antagonizing excitatory amino acids by administration of imidazobenzodiazepine compounds 失效
    通过施用咪唑并二氮杂化合物拮抗兴奋性氨基酸的方法

    公开(公告)号：US5270306A

    公开(公告)日：1993-12-14

    申请号：US703160

    申请日：1991-05-20

    申请人： Leif H. Jensen ,  Jorgen Drejer ,  Frank Watjen

    发明人： Leif H. Jensen ,  Jorgen Drejer ,  Frank Watjen

    IPC分类号： A61K31/55 ,  A01N43/62

    CPC分类号： A61K31/55

    摘要： A method of antagonizing the biological effects of an excitatory amino acid of a subject in need of such antagonization comprising the step of administering to said subject an effective amount of a compound having the formula ##STR1## wherein R.sup.3 is hydrogen, C.sub.1-8 -alkyl which may be branched, or cycloalkylmethyl;R.sup.7 and R.sup.8 are independently hydrogen, halogen, CF.sub.3, CN, NO.sub.2, NH.sub.2, C.sub.1-4 -alkyl or C.sub.1-4 -alkoxy; andR.sup.4 is hydrogen and R.sup.5 is hydrogen or C.sub.1-7 -alkyl; or R.sup.4 and R.sup.5 together signify (CH.sub.2).sub.n wherein n is an integer of 2-3.

    摘要翻译： 拮抗需要这种拮抗作用的受试者的兴奋性氨基酸的生物学作用的方法，包括向所述受试者施用有效量的具有下式的化合物（I）的步骤：其中R 3是氢，C1- 可以是支链的8-烷基或环烷基甲基; R 7和R 8独立地是氢，卤素，CF 3，CN，NO 2，NH 2，C 1-4 - 烷基或C 1-4 - 烷氧基; R4为氢，R5为氢或C1-7烷基; 或R 4和R 5一起表示（CH 2）n，其中n是2-3的整数。

    Isatinoxime derivatives, their preparation and use
    5.
    发明授权
    Isatinoxime derivatives, their preparation and use 失效
    伊马替尼衍生物，其制备和用途

    公开(公告)号：US5242918A

    公开(公告)日：1993-09-07

    申请号：US936579

    申请日：1992-08-27

    申请人： Frank Watjen ,  Bjarne H. Dahl ,  Jorgen Drejer ,  Leif H. Jensen

    发明人： Frank Watjen ,  Bjarne H. Dahl ,  Jorgen Drejer ,  Leif H. Jensen

    IPC分类号： C07C205/45 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04

    CPC分类号： C07D471/04 ,  C07C205/45 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04

    摘要： A compound having the formula ##STR1## wherein R.sup.4 and R.sup.5 independently are hydrogen, halogen, CF.sub.3, CN, NO.sub.2 or SO.sub.2 NR.sup.1 R.sup.2 whereinR.sup.1 is hydrogen or straight, C.sub.1-6 -alkyl which may be branched or cyclic,R.sup.2 is hydrogen or straight, 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 --A--(CH.sub.2).sub.m --, wherein A is O, S, CH.sub.2 or NR.sup.I, wherein R.sup.I is H, C.sub.1-6 -alkyl which may be straight, branched or cyclic, n is 0, 1, 2, 3, 4, 5 and m is 0, 1, 2, 3, 4, 5;Q is NOH or O;Z=O, S, N--R.sup.II, ##STR2## wherein R.sup.II, R.sup.III, R.sup.IV and R.sup.V independently are hydrogen, benzyl, C.sub.1-6 carboxylic acid-acyl, C.sub.1-6 -alkoxy which may be branched or cyclic, or C.sub.1-6 -alkyl which may be branched or cyclic;X is --(CH.sub.2).sub.o -- wherein o is 0, 1, 2, or 3;Y is --(CH.sub.2).sub.p -- wherein p is 0, 1, 2 or 3;.alpha. and .beta. indicate attachment points,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 4和R 5独立地是氢，卤素，CF 3，CN，NO 2或SO 2 NR 1 R 2，其中R 1是氢或直链，可以是支链或环状的C 1-6 - 烷基，R 2是氢或直链， 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）nA-（CH 2）m - ，其中A是O，S，CH 2或NRI，其中R 1是H，C 1-6 - 烷基，其可以是直链，支链或环状的，n为0,1,2,3,4,5，m为0,1,2,3,4,5; Q是NOH或O; Z = O，S，N-RII，其中RII，RIII，RIV和RV独立地是氢，苄基，C1-6羧酸 - 酰基，可以是支链或环状的C1-6 - 烷氧基或C1-6 可以是支链或环状的 - 烷基; X是 - （CH 2）o - ，其中o是0,1,2或3; Y是 - （CH 2）p - ，其中p是0,1,2或3; α和β表示连接点，以及一种治疗对谷氨酸和天冬氨酸受体的封闭有反应的哺乳动物（包括人）的病症的方法。

    Oxadiazolyl imidazobenzodiazepine derivatives pharmaceutical compositions thereof, and method of treating therewith
    6.
    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。