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NEW IMIDAZO (1,5-C) CHINAZOLINE; A NEW CLASS OF LIGANDS FOR GABA RECEPTORS IN BRAIN

机译:新的咪达唑(1,5-C)CHINAZOLINE;一类新的脑GABA受体配体

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.
机译:公开了具有下式的化合物的化合物:或其药学上可接受的无毒盐,其中:X为氧,H 2或硫Y为氢,或任选取代的烷基,烯基,(取代的)芳基烷基,芳基或杂芳基或被取代的羰基具有烷基,环烷基,芳基或氨基; W是烷基,芳基烷基或杂芳基烷基,其中每个芳基任选地被至多两个基团取代;或W为芳基,噻吩基,吡啶基或杂芳基,其各自任选地被取代; Z 1,Z 2,Z 3和Z 4分别代表氮或C-R 1,其中R 1为氢,卤素,羟基,氨基或苯基或吡啶基,可选地被卤素,羟基,低级烷基或低级烷氧基单或独立地双取代,这些化合物是针对GABA a脑受体的高选择性激动剂,拮抗剂或反向激动剂,或针对GABA a脑受体的激动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,睡眠和癫痫发作,苯二氮卓类药物过量以及增强记忆力。

著录项

  • 公开/公告号AT387447T

    专利类型

  • 公开/公告日2008-03-15

    原文格式PDF

  • 申请/专利权人 NEUROGEN CORPORATION;

    申请/专利号AT19970915905T

  • 发明设计人 CHEN PAUL;HUTCHISON ALAN;CAI GUOLIN;

    申请日1997-03-12

  • 分类号C07D487/04;A61K31/505;A61K31/519;A61P25/22;C07D401/14;C07D403/14;

  • 国家 AT

  • 入库时间 2022-08-21 20:05:06

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