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    HYDROCHLORIDE SALT OF AN AZABICYCLO[3.2.1]OCTANE DERIVATIVE
    22.
    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
    24.
    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
    25.
    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。

    Indole-derivatives, method of treatment therewith, and pharmaceutical compositions comprising such compounds
    27.
    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
    29.
    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
    30.
    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。