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36 条记录 (耗时 0.062 秒)

    Certain cycloalkyl and azacycloalkyl pyrrolopyridines; a new class of gaba rain receptor ligands
    21.
    发明授权
    Certain cycloalkyl and azacycloalkyl pyrrolopyridines; a new class of gaba rain receptor ligands 失效
    某些环烷基和氮杂环烷基吡咯并吡啶; 一类新的gaba雨受体配体

    公开(公告)号：US5367077A

    公开(公告)日：1994-11-22

    申请号：US866802

    申请日：1992-04-08

    申请人： Charles A. Blum ,  Alan J. Hutchison ,  Raynmond F. Horvath

    发明人： Charles A. Blum ,  Alan J. Hutchison ,  Raynmond F. Horvath

    IPC分类号： C07D471/04 ,  C07D471/14 ,  C07D491/113 ,  C07D491/20

    CPC分类号： C07D471/04 ,  C07D471/14

    摘要： The present invention encompasses compounds of the formula: ##STR1## and pharmaceutically acceptable non-toxic salts thereof wherein: A represents nitrogen or C--H, andB represents nitrogen or C--H, with the proviso that when A is nitrogen, B is C--H, and when B is nitrogen, A is C--H;n is 0, 1, or 2;Y represents nitrogen or carbon, each of which is substituted with various organic or inorganic substituents;W represents an aromatic group unsubstituted or substituted with various organic or inorganic substituents; andR1 and R2 are the same or different and represent hydrogen or lower alkyl.These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine type drugs, and enhancement of alertness.

    摘要翻译： 本发明包括下式的化合物及其药学上可接受的无毒盐，其中：A表示氮或CH，B表示氮或CH，条件是当A为氮时，B为CH，当为 B为氮，A为CH; n为0,1或2; Y表示氮或碳，各自被各种有机或无机取代基取代; W表示未被取代或被各种有机或无机取代基取代的芳基; 并且R 1和R 2相同或不同，表示氢或低级烷基。 这些化合物是用于GABAa脑受体或其前药的高度选择性激动剂，拮抗剂或反向激动剂，并且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并提高警觉性。

    Aryl-Substituted Benzo[D]Isothiazol-3-Ylamine Analogues
    25.
    发明申请
    Aryl-Substituted Benzo[D]Isothiazol-3-Ylamine Analogues 审中-公开
    芳基取代的苯并[D]异噻唑-3-基胺类似物

    公开(公告)号：US20080125466A1

    公开(公告)日：2008-05-29

    申请号：US10564263

    申请日：2004-07-09

    申请人： Charles A. Blum ,  Xiaozhang Zheng

    发明人： Charles A. Blum ,  Xiaozhang Zheng

    IPC分类号： A61K31/4439 ,  C07D417/10 ,  A61P3/04 ,  A61P25/00 ,  A61P11/00

    CPC分类号： C07D275/06 ,  C07D417/04

    摘要： Aryl-substituted benzo[d]isothiazol-3-ylamine analogues) are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

    摘要翻译： 提供了芳基取代的苯并[d]异噻唑-3-基胺类似物），其中变量如本文所述。 这些化合物是可用于在体内或体外调节特异性受体活性的配体，并且特别可用于治疗与人类，驯养伴侣动物和家畜中的病理受体激活相关的病症。 还提供了使用这些化合物治疗这种病症的药物组合物和方法，以及使用这些配体进行受体定位研究的方法。

    Heteroaryl Substituted Piperazinyl-Pyridine Analogues
    26.
    发明申请
    Heteroaryl Substituted Piperazinyl-Pyridine Analogues 审中-公开
    杂芳基取代的哌嗪基 - 吡啶类似物

    公开(公告)号：US20080124384A1

    公开(公告)日：2008-05-29

    申请号：US11795651

    申请日：2006-01-19

    申请人： Charles A. Blum

    发明人： Charles A. Blum

    IPC分类号： A61K9/70 ,  C07D239/24 ,  A61K31/506 ,  C07D295/00 ,  C12N1/00 ,  A61P31/00 ,  A61P13/02 ,  A61P43/00 ,  A61P17/02 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/397

    CPC分类号： C07D401/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

    摘要： Substituted biaryl piperazinyl-pyridine analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

    摘要翻译： 提供了下式的取代的联芳基哌嗪基 - 吡啶类似物：其中变量如本文所述。 这些化合物是可用于在体内或体外调节特异性受体活性的配体，并且特别可用于治疗与人类，驯养伴侣动物和家畜中的病理受体激活相关的病症。 还提供了使用这些化合物治疗这种病症的药物组合物和方法，以及使用这些配体进行受体定位研究的方法。

    Substituted aryl and cycloalkyl imidazolones; a new class of GABA brain receptor ligands
    29.
    发明授权
    Substituted aryl and cycloalkyl imidazolones; a new class of GABA brain receptor ligands 失效
    取代的芳基和环烷基咪唑啉酮; 一类新的GABA脑受体配体

    公开(公告)号：US5849927A

    公开(公告)日：1998-12-15

    申请号：US872542

    申请日：1997-06-10

    申请人： Robert W. DeSimone ,  Charles A. Blum

    发明人： Robert W. DeSimone ,  Charles A. Blum

    IPC分类号： C07D413/04 ,  C07D417/04 ,  C07D263/58

    CPC分类号： C07D413/04 ,  C07D417/04

    摘要： Disclosed are compounds of the formula: ##STR1## wherein: T is NH, O, or S; X is hydrogen, hydroxyl, lower alkyl, or an optionally substituted amide; the W ring is an optionally substituted aryl or heteroaryl group; and ##STR2## represents an optionally substituted benzo group or an optionally substituted 5, 6, 7, or 8 membered ring. 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. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.

    摘要翻译： 公开了下式的化合物：其中：T是NH，O或S; X是氢，羟基，低级烷基或任意取代的酰胺; W环是任选取代的芳基或杂芳基; 并且表示任选取代的苯并基或任选取代的5,6,7或8元环。 这些化合物是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，睡眠和癫痫发作，用苯二氮卓类药物过量并用于记忆增强。

    Substituted aryl and cycloalkyl imidazolones; a new class of GABA brain receptor ligands
    30.
    发明授权
    Substituted aryl and cycloalkyl imidazolones; a new class of GABA brain receptor ligands 失效

    公开(公告)号：US5637725A

    公开(公告)日：1997-06-10

    申请号：US462674

    申请日：1995-06-05

    申请人： Robert W. DeSimone ,  Charles A. Blum

    发明人： Robert W. DeSimone ,  Charles A. Blum

    IPC分类号： C07D413/04 ,  C07D417/04 ,  C07D263/58

    CPC分类号： C07D413/04 ,  C07D417/04

    摘要： Disclosed are compounds of the formula: ##STR1## wherein: T is NH, O, or S;X is hydrogen, hydroxyl, lower alkyl, or an optionally substituted amide;the W ring is an optionally substituted aryl or heteroaryl group; and ##STR2## represents an optionally substituted benzo group or an optionally substituted 5, 6, 7, or 8 membered ring.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. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.