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    Glutamate (ampa/kainate) receptor antagonists: N-substituted fused azacycloalkylquinoxalinediones
    1.
    发明授权
    Glutamate (ampa/kainate) receptor antagonists: N-substituted fused azacycloalkylquinoxalinediones 失效
    谷氨酸（ampa / kainate）受体拮抗剂：N-取代的稠合氮杂环烷基喹喔啉

    公开(公告)号：US6057313A

    公开(公告)日：2000-05-02

    申请号：US869515

    申请日：1997-06-05

    申请人： Christopher Franklin Bigge ,  Thomas Charles Malone ,  Robert Michael Schelkun ,  Chung Stephen Yi

    发明人： Christopher Franklin Bigge ,  Thomas Charles Malone ,  Robert Michael Schelkun ,  Chung Stephen Yi

    IPC分类号： C07D217/02 ,  C07D217/04 ,  C07D217/06 ,  C07D471/04 ,  A61K31/495 ,  C07D487/04

    CPC分类号： C07D471/04 ,  C07D217/02 ,  C07D217/04 ,  C07D217/06

    摘要： Novel N-substituted azacycloalkyl ring fused 2,3-quinoxalinediones are disclosed represented by the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.1 is hydrogen, alkyl or W-alkyl; X and Y are independently hydrogen, halogen, nitro, cyano, trifluoromethyl, SO.sub.2 CF.sub.3, SO.sub.2 R.sup.4, SO.sub.2 NR.sup.4 R.sup.5, alkyl, alkenyl, (CH.sub.2).sub.z CONR.sup.4 R.sup.5, (CH.sub.2).sub.z COOR.sup.4, or NHCOR.sup.4, wherein R.sup.4 and R.sup.5 are independently hydrogen, alkyl having 1 to 6 carbon atoms, cycloalkyl or W-alkyl, and z is an integer from 0 to 4; R.sup.2 is benzoyl, W, W-alkyl, COcycloalkyl, COalkyl-W, CONR.sup.3 alkyl, CONR.sup.3 -W, CONR.sup.3 alkyl-W, CSNR.sup.3 alkyl, CSNR.sup.3 alkyl-W, ##STR2## or a moiety derived from a common amino acid by removal of the --OH from the carboxyl group which is alpha to the amino, wherein --W is aryl, heteroaryl, or the heterocycles piperidinyl, piperazinyl, morpholinyl or pyrrolidinyl, wherein R.sup.3 is hydrogen, alkyl or W-alkyl; and m and n are independently 0, 1 or 2 provided that m+n is >1; provided that when R.sup.2 is benzoyl, ##STR3## or X is nitro, Y and R.sup.1 are H, m is 2 and n is 1;when R.sup.2 is ##STR4## X is nitro, Y and R.sup.1 are H and m is 2 and n is 1; or when R.sup.2 is ##STR5## X is bromo, Y and R.sup.1 are H, m is 1 and n is 2. The novel N-substituted azacycloalkyl ring fused 2,3-quinoxalinediones may be used, for example, as neuroprotective agents, for treatment of chronic neurodegenerative disorders, as anticonvulsants and in the treatment of schizophrenia, epilepsy, anxiety, pain and drug addiction.

    摘要翻译： 公开了由下式表示的新的N-取代的氮杂环烷基环稠合的2,3-喹喔啉二醇：或其药学上可接受的盐，其中R 1是氢，烷基或W-烷基; X和Y独立地是氢，卤素，硝基，氰基，三氟甲基，SO 2 CF 3，SO 2 R 4，SO 2 NR 4 R 5，烷基，烯基，（CH 2）z CONR 4 R 5，（CH 2）z COOR 4或NHCOR 4，其中R 4和R 5独立地是氢， 6个碳原子，环烷基或W-烷基，z是0-4的整数; R 2是苯甲酰基，W，W-烷基，CO环烷基，CO烷基-W，CONR 3烷基，CONR 3 -W，CONR 3烷基-W，CSNR 3烷基，CSNR 3烷基-W，或通过从羧基中除去-OH而衍生自常见氨基酸的部分 其中-W是芳基，杂芳基或杂环哌啶基，哌嗪基，吗啉基或吡咯烷基，其中R 3是氢，烷基或W-烷基; m和n独立地为0,1或2，条件是m + n大于1; 条件是当R 2为苯甲酰基或X为硝基时，Y和R 1为H，m为2且n为1; 当R 2为硝基时，Y和R 1为H，m为2，n为1; 或当R 2为X时，Y和R 1为H，m为1且n为2.新的N-取代的氮杂环烷基环稠合2,3-喹喔啉酮可用作例如神经保护剂，用于治疗慢性 神经退行性疾病，抗惊厥药和治疗精神分裂症，癫痫，焦虑，疼痛和药物成瘾。

    Quinoxalinedione derivatives, their preparation and use
    3.
    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。