Aryl and heteroaryl substituted pyridino derivatives GABA brain receptor ligands
    7.
    发明授权
    Aryl and heteroaryl substituted pyridino derivatives GABA brain receptor ligands 失效
    芳基和杂芳基取代的吡啶衍生物GABA脑受体配体

    公开(公告)号:US06297256B1

    公开(公告)日:2001-10-02

    申请号:US09596031

    申请日:2000-06-15

    IPC分类号: G07D40104

    CPC分类号: C07D401/14 C07D495/04

    摘要: Disclosed are aryl and heteroaryl substitated pyridino compounds. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.

    摘要翻译: 公开了芳基和杂芳基取代的吡啶基化合物。 这些化合物是GABAA脑受体的高度选择性激动剂,拮抗剂或反向激动剂或GABAA脑受体的激动剂,拮抗剂或反向激动剂的前药,因此可用于诊断和治疗焦虑症,抑郁症,唐氏综合症,睡眠和癫痫发作障碍, 过量与苯二氮卓类药物和增强记忆。 还提供药物组合物,包括包装的药物组合物。 本发明的化合物也可用作组织样品中GABA A受体定位的探针。

    Substituted 4-oxo-napthyridine-3-carboxamides: GABA brain receptor ligands
    9.
    发明授权
    Substituted 4-oxo-napthyridine-3-carboxamides: GABA brain receptor ligands 失效
    取代的4-氧代 - 萘啶-3-甲酰胺:GABA脑受体配体

    公开(公告)号:US06646124B2

    公开(公告)日:2003-11-11

    申请号:US10114743

    申请日:2002-04-02

    IPC分类号: C07D41300

    CPC分类号: C07D471/04

    摘要: The present invention encompasses structures of the Formula or the pharmaceutically acceptable non-toxic salts thereof wherein: X is hydrogen, halogen, (un)substituted alkyl, (un)substituted alkoxy or amino; and Y is (un)substituted alkyl, aryl, or heteroaryl, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness.

    摘要翻译: 本发明包括式的药学上可接受的无毒盐的结构,其中:X是氢,卤素,(未)取代的烷基,(未)取代的烷氧基或氨基; 和Y是(未)取代的烷基,芳基或杂芳基,该化合物是GABAa脑受体的高选择性激动剂,拮抗剂或反向激动剂或GABAa脑受体的激动剂,拮抗剂或反向激动剂的前药。 这些化合物可用于诊断和治疗焦虑症,唐氏综合征,睡眠,认知和癫痫发作,以及用苯二氮卓类药物过量并提高警觉性。

    Heterocyclic amino substituted heteroaryl fused pyridines; GABA brain receptor ligands
    10.
    发明授权
    Heterocyclic amino substituted heteroaryl fused pyridines; GABA brain receptor ligands 失效
    杂环氨基取代的杂芳基稠合吡啶; GABA脑受体配体

    公开(公告)号:US06423711B1

    公开(公告)日:2002-07-23

    申请号:US09736497

    申请日:2000-12-13

    IPC分类号: C07D41304

    CPC分类号: C07D471/04 C07D495/04

    摘要: Disclosed are compounds of the formula or the pharmaceutically acceptable non-toxic salts thereof wherein: n is an integer from 0 to 3; the C ring is aryl or heteroaryl; X is CH, N, or O Z represents an electron pair, hydrogen, or (un)substituted heterocycle, aryl, or amido; W is (un)substituted alkyl, aryl, or heteroaryl; A and B are hydrogen or lower alkyl, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness.

    摘要翻译: 公开了下式的化合物或其药学上可接受的无毒盐,其中:n是0-3的整数; C环是芳基或杂芳基; X是CH,N或OZ表示电子对,氢或( 取代的杂环,芳基或酰氨基; W是(未)取代的烷基,芳基或杂芳基; A和B是氢或低级烷基,该化合物是GABAa脑受体或前药的高选择性激动剂,拮抗剂或反向激动剂 激动剂,拮抗剂或GA​​BAa脑受体的反向激动剂。 这些化合物可用于诊断和治疗焦虑症,唐氏综合征,睡眠,认知和癫痫发作,以及用苯二氮卓类药物过量并提高警觉性。