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45 条记录 (耗时 0.028 秒)

    Imidazo[1,5-c]quinazolines; A new class of GABA brain receptor ligands
    36.
    发明授权
    Imidazo[1,5-c]quinazolines; A new class of GABA brain receptor ligands 失效
    咪唑并[1,5-c]喹唑啉; 一类新的GABA脑受体配体

    公开(公告)号：US06297252B1

    公开(公告)日：2001-10-02

    申请号：US09619169

    申请日：2000-07-19

    申请人： Paul Chen ,  Alan Hutchison ,  Guolin Cai

    发明人： Paul Chen ,  Alan Hutchison ,  Guolin Cai

    IPC分类号： C07D40314

    CPC分类号： C07D487/04

    摘要： Disclosed are compounds of compounds of the formula: or the pharmaceutically acceptable nontoxic salts thereof wherein: X is oxygen, H2 or sulfur Y is hydrogen, or optionally substituted alkyl, alkenyl, (substituted)arylalkyl, aryl or heteroaryl, or a carbonyl group substituted with alkyl, cycloalkyl, aryl, or amino groups; W is alkyl, arylalkyl or heteroarylalkyl, where each aryl group is optionally substituted with up to two groups; or W is aryl, thienyl, pyridyl or heteroaryl, each of which is optionally substituted; and Z1, Z2, Z3, and Z4 independently represent nitrogen or C—R1 where R1 is hydrogen, halogen, hydroxy, amino, or phenyl or pyridyl optionally mono- or independently disubstituted with halogen, hydroxy, lower alkyl, or lower alkoxy, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine drugs, and enhancement of memory.

    摘要翻译： 公开了下式化合物或其药学上可接受的无毒盐的化合物，其中：X是氧，H 2或硫，Y是氢，或任选取代的烷基，烯基，（取代的）芳基烷基，芳基或杂芳基，或被 烷基，环烷基，芳基或氨基; W是烷基，芳基烷基或杂芳基烷基，其中每个芳基任选被至多两个基团取代; 或者W是芳基，噻吩基，吡啶基或杂芳基，其各自任选被取代; 和Z 1，Z 2，Z 3和Z 4独立地表示氮或C-R 1，其中R 1是氢，卤素，羟基，氨基或苯基或任选被卤素，羟基，低级烷基或低级烷氧基单取代或独立地取代的吡啶基， 用于GABAa脑受体的高选择性激动剂，拮抗剂或反向激动剂或激动剂的前药或GABAa脑受体的反向激动剂。 这些化合物可用于诊断和治疗焦虑，睡眠和癫痫发作，用苯二氮卓类药物过量使用，并增强记忆功能。

    4-(4-piperidylmethyhlamino) substituted heteroaryl fused pyridines: GABA brain receptor ligands
    37.
    发明授权
    4-(4-piperidylmethyhlamino) substituted heteroaryl fused pyridines: GABA brain receptor ligands 失效
    4-（4-哌啶基甲基氨基）取代的杂芳基稠合吡啶：GABA脑受体配体

    公开(公告)号：US6103903A

    公开(公告)日：2000-08-15

    申请号：US259150

    申请日：1999-02-26

    申请人： Guolin Cai ,  Gang Liu

    发明人： Guolin Cai ,  Gang Liu

    IPC分类号： A61P25/00 ,  C07D471/04 ,  C07D495/04 ,  C07D401/14 ,  C07D409/14

    CPC分类号： C07D471/04 ,  C07D495/04

    摘要： Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: R is hydrogen, alkyl, or(un)substituted alkoxy or amino; andW 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. The compounds of the invention 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：R是氢，烷基或（未）取代的烷氧基或氨基; W是（un）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。 本发明的化合物可用于诊断和治疗焦虑症，唐氏综合征，睡眠，认知和发作障碍，以及用苯二氮卓类药物过量并提高警觉性。

    Aryl fused substituted 4-oxy-pyridines
    40.
    发明授权
    Aryl fused substituted 4-oxy-pyridines 失效
    芳基稠合取代的4-氧 - 吡啶

    公开(公告)号：US07371752B2

    公开(公告)日：2008-05-13

    申请号：US11003195

    申请日：2004-12-03

    申请人： Guolin Cai ,  Pamela Albaugh ,  Jun Yuan

    发明人： Guolin Cai ,  Pamela Albaugh ,  Jun Yuan

    IPC分类号： A61K31/495 ,  A61K31/44 ,  C07D487/00 ,  C07D471/02

    CPC分类号： C07D215/233 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D471/04 ,  C07D495/04

    摘要： Disclosed are compounds of the formula: wherein X, Q, W and are as defined herein. These compounds are 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： 公开了下式的化合物：其中X，Q，W和如本文所定义。 这些化合物是用于GABA A A受体的激动剂，拮抗剂或反向激动剂或GABAAβ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，抑郁症，唐氏综合征，睡眠和癫痫发作障碍，用苯二氮卓类药物服用过量，并增加记忆力。 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 A受体定位的探针。