首页> 外国专利> 1,2,4-triazolo4,3-cquinazolin-3-ones and 1,2,4-triazolo4,3- c quinazolin-3-thiones

1,2,4-triazolo4,3-cquinazolin-3-ones and 1,2,4-triazolo4,3- c quinazolin-3-thiones

机译:1,2,4-三唑并[4,3-c]喹唑啉-3-酮和1,2,4-三唑并[4,3-c]喹唑啉-3-硫酮

摘要

The present invention encompasses structures of the Formula: ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: X is oxygen, H.sub.2, or sulfur;PPY is oxygen or sulfur; P PW is alkyl, arylalkyl, or heteroarylalkyl, each of which is optionally substituted; orPPW is aryl or heteroaryl; ##STR2## wherein: Z.sub.1, Z.sub.2, Z.sub.3, and Z.sub.4 independently represent nitrogen or C--R.sub.a, wherePP each R.sub.a independently is hydrogen, an inorganic substitutent or an optionally substituted aromatic group;PPn is 1, 2 or 3; andP PR.sub.b is hydrogen, alkyl, or an optionally substituted aromatic group,PPwhich 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 drugs, and enhancement of memory.
机译:本发明包括式的结构或其药学上可接受的无毒盐,其中:X是氧,H 2或硫; P是氧或硫; P是氧或硫。 W是烷基,芳基烷基或杂芳基烷基,它们各自任选地被取代;或P W为芳基或杂芳基;或## STR2 ##其中:Z.sub.1,Z.sub.2,Z.sub.3和Z.sub.4独立地代表氮或C–R.a。,其中

每个R a独立地为氢,无机取代基或任选取代的芳族基团; P n为1、2或3; P RB是氢,烷基或任选取代的芳族基团,该化合物是针对GABA a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,并且是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和增强记忆力。

著录项

  • 公开/公告号US5955465A

    专利类型

  • 公开/公告日1999-09-21

    原文格式PDF

  • 申请/专利权人 NEUROGEN CORPORATION;

    申请/专利号US19970946040

  • 发明设计人 PAUL CHEN;ALAN HUTCHISON;

    申请日1997-10-07

  • 分类号A01N43/54;C07D257/08;C07D487/00;C07D239/00;

  • 国家 US

  • 入库时间 2022-08-22 02:07:17

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