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45 条记录 (耗时 0.045 秒)

    2-Substituted imidazo[1,2-A]pyridine derivatives
    25.
    发明授权
    2-Substituted imidazo[1,2-A]pyridine derivatives 失效
    2-取代的咪唑并[1,2-A]吡啶衍生物

    公开(公告)号：US06552037B2

    公开(公告)日：2003-04-22

    申请号：US09897837

    申请日：2001-06-29

    申请人： Guolin Cai ,  Kenneth Shaw

    发明人： Guolin Cai ,  Kenneth Shaw

    IPC分类号： C07D47104

    CPC分类号： C07D471/04 ,  G01N33/6896

    摘要： Disclosed are compounds of the formula: and the pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein X, A, B, C, D and W are defined herein, which compounds bind with high selectivity and high affinity to the benzodiazepine site of the GABAA receptors and are therefore useful in the treatment of certain central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples.

    摘要翻译： 公开了下式的化合物及其药学上可接受的盐，前药和溶剂化物，其中X，A，B，C，D和W在本文中定义，该化合物以高选择性和高亲和力结合GABAA的苯二氮卓位点 受体，因此可用于治疗某些中枢神经系统（CNS）疾病和作为组织样品中GABA A受体定位的探针。

    Imidazoloisoquinolines
    26.
    发明授权
    Imidazoloisoquinolines 失效
    咪唑并异喹啉

    公开(公告)号：US06528649B2

    公开(公告)日：2003-03-04

    申请号：US09867304

    申请日：2001-05-29

    申请人： Guolin Cai ,  Kenneth Shaw

    发明人： Guolin Cai ,  Kenneth Shaw

    IPC分类号： C07D47104

    CPC分类号： C07D471/04 ,  C07D217/24 ,  C07D237/32 ,  C07D487/04

    摘要： Disclosed are compounds of the formula: and the pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein n, R1, R2, R3, W, Q, and X are defined herein, which compounds bind with high selectivity and high affinity to the benzodiazepine site of the GABAA receptors and are therefore useful in the treatment of certain central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples.

    摘要翻译： 公开了下式的化合物及其药学上可接受的盐，前药和溶剂化物，其中n，R 1，R 2，R 3，W，Q和X在本文中定义，该化合物以高选择性和对苯并二氮杂位点的高亲和力 的GABA A受体，因此可用于治疗某些中枢神经系统（CNS）疾病和作为组织样品中GABA A受体定位的探针。

    Heterocyclic amino substituted heteroaryl fused pyridines; GABA brain receptor ligands
    27.
    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

    申请人： Guolin Cai ,  Gang Liu ,  Guoquing Chen ,  Pamela A. Albaugh

    发明人： Guolin Cai ,  Gang Liu ,  Guoquing Chen ,  Pamela A. Albaugh

    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。

    Imidazo�1,5-c! quinazolines; a new class of GABA brain receptor ligands
    28.
    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：US5792766A

    公开(公告)日：1998-08-11

    申请号：US614878

    申请日：1996-03-13

    申请人： Paul Chen ,  Alan Hutchison ,  Guolin Cai

    发明人： Paul Chen ,  Alan Hutchison ,  Guolin Cai

    IPC分类号： A61K31/519 ,  A61P25/22 ,  C07D401/14 ,  C07D403/14 ,  C07D487/04 ,  A61K31/505 ,  C07D403/07

    CPC分类号： C07D487/04

    摘要： Disclosed are compounds of compounds of the formula: ##STR1## or the pharmaceutically acceptable nontoxic salts thereof wherein: X is oxygen, H.sub.2 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 Z.sub.1, Z.sub.2, Z.sub.3, and Z.sub.4 independently represent nitrogen or C-R.sub.1 where R.sub.1 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： 公开了下式的化合物或其药学上可接受的无毒盐，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，芳基或氨基取代的羰基; W是烷基，芳烷基或杂芳基烷基，其中每个芳基任选被至多两个基团取代; 或W是芳基，噻吩基，吡啶基或杂芳基，其各自任选被取代; 并且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被二取代的吡啶基， 化合物是GABAa脑受体或GABAa脑受体的激动剂或反向激动剂前药的高选择性激动剂，拮抗剂或反向激动剂。 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。