首页> 外国专利> TETRAHYDROQUINOLINE DERIVATIVES, PROCESS FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS THEREOF AND THEIR USE FOR THE PREPARATION OF THERAPEUTIC AGENTS FOR ANTAGONISING THE EFFECTS OF EXCITATORY AMINO ACIDS ON THE NMDA RECEPTOR COMPLEX

TETRAHYDROQUINOLINE DERIVATIVES, PROCESS FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS THEREOF AND THEIR USE FOR THE PREPARATION OF THERAPEUTIC AGENTS FOR ANTAGONISING THE EFFECTS OF EXCITATORY AMINO ACIDS ON THE NMDA RECEPTOR COMPLEX

机译：四氢喹啉衍生物，其制备方法，其药物成分及其在制备治疗性药物中的作用，以拮抗刺激性氨基酸对NMDA受体复合物的作用

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Compounds of formula (I), or a salt or a non toxic metabolically labile esters thereof, wherein Y represents a carbon atom; Z is the group CH which is linked to the group Y via a double bond and X is CH or Z is methylene or NR11 and X is a carbon atom linked to the group Y via a double bond; A represents a C1-2alkylene chain and which chain may be substituted by one or two groups selected from C1-6alkyl optionally substituted by hydroxy, amino, C1-4alkyl amino or C1-4dialkyl amino or which chain may be substituted by the group =0; R represents a halogen atom or C1-4alkyl group; R1 represents a hydrogen, a halogen atom or C1-4alkyl group; R2 represents optionally substituted phenyl, a 5 membered heteroaryl group containing 1 to 3 heteroatoms selected from oxygen, sulphur and nitrogen or 6 membered heteroaryl group containing 1 to 3 nitrogen atoms, processes for their preparation and their use as glycine antagonists.

机译：式（I）的化合物或其盐或无毒的代谢不稳定的酯，其中Y表示碳原子; Z为通过双键与基团Y连接的CH基团，X为CH或Z为亚甲基或NR 11，X为通过双键与基团Y连接的碳原子。 A代表C 1-2亚烷基链，并且该链可以被选自C 1-6烷基的一个或两个基团取代，该基团任选地被羟基，氨基，C 1-4烷基氨基或C 1-4二烷基氨基取代，或者该链可以被基团= 0取代; R表示卤原子或C1-4烷基。 R1代表氢，卤原子或C1-4烷基。 R 2表示任选取代的苯基，含有1-3个选自氧，硫和氮的杂原子的5元杂芳基或含有1-3个氮原子的6元杂芳基，其制备方法及其用作甘氨酸拮抗剂的用途。

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公开/公告号IL140062B

专利类型
公开/公告日2007-05-15

原文格式PDF
申请/专利权人 GLAXO WELLCOME SPA;
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申请/专利号IL140062
发明设计人
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申请日2000-12-04
分类号A61K31/47;A61K31/4709;A61K31/495;A61P9/00;A61P25/00;A61P25/04;A61P25/28;A61P43/00;C07Dnull/null;C07D215/02;C07D401/00;C07D401/04;C07D401/14;
国家 IL
入库时间 2022-08-21 20:58:43

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