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    Novel isatineoxime derivatives, their preparation and use
    2.
    发明公开
    Novel isatineoxime derivatives, their preparation and use 失效
    Isatinoxim-Derivate，ihre Herstellung und Verwendung。

    公开(公告)号：EP0633262A1

    公开(公告)日：1995-01-11

    申请号：EP94610036.9

    申请日：1994-06-29

    申请人： NEUROSEARCH A/S

    发明人： Wätjen, Frank ,  Dahl, Bjarne Hugo ,  Drejer, Jorgen ,  Jensen, Leif Helth

    IPC分类号： C07D471/04 ,  A61K31/40 ,  A61K31/435

    CPC分类号： C07D471/04

    摘要： A compound having the formula

    or a pharmaceutically acceptable salt thereof
    wherein
    R⁴ and R⁵ independently are hydrogen, halogen, CF₃, CN, NO₂ or SO₂NR¹R² wherein R¹ is hydrogen or alkyl, and R² is hydrogen or alkyl, or wherein R¹ and R² together represent -(CH₂) n -A-(CH₂) m -, wherein A is O, S, CH₂ or NR I , wherein R I is H, alkyl, n is 0,1,2,3,4,5 and m is 0,1,2,3,4,5;
    R II is hydrogen, benzyl, (C=O)CF₃, C₁₋₆-carboxylic acid acyl, alkoxy, or alkyl, CH₂CO₂R VI wherein R VI is hydrogen or alkyl;
    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CHEM的化合物或其药学上可接受的盐，其中R 4和R 5独立地是氢，卤素，CF 3，CN，NO 2或SO 2 NRR R 2，其中R 1是 氢或烷基，R 2是氢或烷基，或其中R 1和R 2一起表示 - （CH 2）n -A（CH 2）m - ，其中A是O，S，CH 2或NR 其中R 1是H，烷基，n是0,1,2,3,4,5，m是0,1,2,3,4,5; R II是氢，苄基，（C = O）CF 3，C 1-6 - 羧酸酰基，烷氧基或烷基，CH 2 CO 2 R VI其中R VI是氢或烷基; 以及与谷氨酸和天冬氨酸受体阻断有关的哺乳动物包括人的病症的方法。

    Indole derivatives as glutamate antagonists
    3.
    发明公开
    Indole derivatives as glutamate antagonists 失效
    Indol Derivate als Glutamat Antagonisten。

    公开(公告)号：EP0629615A1

    公开(公告)日：1994-12-21

    申请号：EP94610030.2

    申请日：1994-06-01

    申请人： NEUROSEARCH A/S

    发明人： Wätjen, Frank ,  Drejer, Jorgen ,  Jensen, Leif Helth

    IPC分类号： C07D209/40 ,  A61K31/40

    CPC分类号： C07D209/40

    摘要： The present patent application discloses compounds having the formula

    or a pharmaceutically acceptable salt thereof
    wherein
    R²¹ and R²² each independently are alkyl; and
    R¹, R², R³, R⁴, R¹¹, R¹², R¹³, and R¹⁴ each independently are hydrogen, halogen, CF₃, CN, or NO₂.
    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CHEM的化合物或其药学上可接受的盐，其中R 2和R 2各自独立地是烷基; 和R 1，R 2，R 3，R 4，R 1，R 1，R 3，和R 1， 4各自独立地为氢，卤素，CF 3，CN或NO 2。 该化合物可用作体内活性谷氨酸拮抗剂。

    Novel isatinoxime derivatives, their preparation and use
    5.
    发明公开
    Novel isatinoxime derivatives, their preparation and use 失效
    Isatinoximderivate，ihre Herstellung und Anwendung。

    公开(公告)号：EP0529636A1

    公开(公告)日：1993-03-03

    申请号：EP92114654.4

    申请日：1992-08-27

    申请人： NEUROSEARCH A/S

    发明人： Wätjen, Frank ,  Dahl, Bjarne Hugo ,  Drejer, Jorgen ,  Jensen, Leif Helth

    IPC分类号： C07D487/04 ,  C07D471/04 ,  C07D491/048 ,  C07D495/04 ,  A61K31/40 ,  A61K31/435 ,  A61K31/55

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

    摘要： A compound having the formula

    wherein
    R⁴ and R⁵ independently are hydrogen, halogen, CF₃, CN, NO₂ or SO₂NR¹R² wherein
    R¹ is hydrogen or straight, C₁₋₆-alkyl which may be branched or cyclic,
    R² is hydrogen or straight, C₁₋₆-alkyl which may be branched or cyclic,
    or wherein R¹ and R² together represent -(CH₂) n -A-(CH₂) m -,
    wherein A is O, S, CH₂ or NR I , wherein R I is H, C₁₋₆-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, O;
    Z = O, S, N-R II ,

    wherein R II , R III , R IV and R V independently are hydrogen, benzyl, C₁₋₆-acyl, C₁₋₆-alkoxy which may be branched or cyclic, or C₁₋₆-alkyl which may be branched or cyclic;
    X is -(CH₂) o - wherein o is 0, 1, 2, or 3;
    Y is -(CH₂) p - wherein p is 0, 1, 2 or 3;
    α and β 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CHEM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 R R 2，其中R 1是氢或直链，C1- 可以是支链或环状的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）n A- （CH 2）m - ，其中A是O，S，CH 2或NR I，其中R 1是H，可以是直链，支链或环状的C 1-6 - 烷基，n是0,1,2， 3，4，5和m是0,1,2,3,4,5; Q是NOH，O; Z = O，S，NR II，CHEM，其中R II，R III，R IV和R V独立地是氢，苄基，C 1-6 - 酰基，C 1-6 - 可以是支链或环状的烷氧基或可以是支链或环状的C1-6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。

    Novel isatineoxime derivatives, their preparation and use
    9.
    发明公开
    Novel isatineoxime derivatives, their preparation and use 失效
    Neue Isatineoxime Derivate，ihre Herstellung und Verwendung。

    公开(公告)号：EP0522494A1

    公开(公告)日：1993-01-13

    申请号：EP92111478.1

    申请日：1992-07-07

    申请人： NEUROSEARCH A/S

    发明人： Wätjen, Frank ,  Drejer, Jorgen ,  Jensen, Leif Helth

    IPC分类号： C07D209/60 ,  A61K31/40

    CPC分类号： C07D209/60

    摘要： A compound having the formula

    wherein
    R¹ is C₁₋₆-alkyl which may be branched or cyclic;
    R² is C₁₋₆-alkyl which may be branched or cyclic;
    or wherein R¹ and R² together represent -(CH₂) 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CHEM的化合物，其中R 1是可以是支链或环状的C 1-6 - 烷基; R 2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。一种治疗哺乳动物（包括人）的障碍的方法，其对谷氨酸的阻断和 天冬氨酸受体，同样。

    Isatine derivatives, their preparation and use
    10.
    发明公开
    Isatine derivatives, their preparation and use 失效
    ISATINE衍生物，其制备和使用

    公开(公告)号：EP0432648A3

    公开(公告)日：1991-09-25

    申请号：EP90123474.0

    申请日：1990-12-06

    申请人： NEUROSEARCH A/S

    发明人： Wätjen, Frank ,  Drejer, Jorgen ,  Jensen, Leif Helth

    IPC分类号： C07D209/40 ,  A61K31/40

    CPC分类号： C07D209/40

    摘要： A method of treatment with compounds having the formula

    wherein
    R¹ is hydrogen, C₁₋₆-alkyl which may be branched, C₃₋₇-cycloalkyl, benzyl, phenyl which may be substituted, acyl, hydroxy, C₁₋₆-alkoxy, CH₂CO₂R' wherein R' is hydrogen or C₁₋₆-alkyl which may be branched, CH₂CN, CH₂CONR IV R V wherein R IV and R V independently are hydrogen or C₁₋₆-alkyl, or CH₂C(=NOH)NH₂;
    R² is hydrogen, benzyl, C₁₋₆-alkyl which may be branched, or C₃₋₇-cycloalkyl;
    R⁴, R⁵, R⁶, R⁷ independently are hydrogen, C₁₋₆-alkyl which may be branched, phenyl, halogen, C₁₋₆-alkoxy, NO₂, CN, SO₂NR''R''' wherein R'' and R''' independently are hydrogen or C₁₋₆-alkyl, or CF₃; or R⁶ and R⁷ together form an additional 4 to 7 membered ring which may be aromatic or partial saturated and which may be substituted with halogen, NO₂, CF₃, CN, SO₂NR''R''' wherein R'' and R''' independently are hydrogen or C₁₋₆-alkyl, and R⁴ and R⁵ 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.