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1. 发明申请

WO1997019934A1 QUINOXALINE COMPOUNDS, PHARMACEUTICAL PREPARATIONS CONTAINING THEM AND A PROCESS FOR THE PREPARATION THEREOF 审中-公开
标题翻译：喹啉化合物，含有它们的药物制剂及其制备方法
公开(公告)号：WO1997019934A1
公开(公告)日：1997-06-05
申请号：PCT/HU1996000072
申请日：1996-11-28
申请人： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT. , BATA, Imre , BATORI, Sándor , BENCE, Judit , BÖCSKEI, Zsolt , CSIKOS, Éva , ERDO"e;, Sándor , GÖNCZI, Csaba , HERMECZ, István , HÉJA, Gergely , LAKICS, Viktor , MAJLATH, Csilla , MOLNAR, Péter , PODANYI, Benjamin , RITZ, Imola , SANTANÉ, Csutor, Andrea , SZO"e;KÉNÉ, Szappanos, Andrea , SZVOBODA, Györgyné
发明人： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT.
IPC分类号： C07D241/44
CPC分类号： C07D241/54 , C07D241/44
摘要： The invention relates to compounds of general formula (I) and salts, tautomeric forms and N-oxides thereof in which formula: Z means hydrogen, hydroxy, C1-4 alkyl, C7-9 phenylalkyl, optionally substituted phenyl, COOC1-4 alkyl, C2-14 acyl, C1-4 alkylsulphonyl, trifluoromethyl-sulphonyl, optionally substituted benzoyl, optionally substituted phenyl-sulphonyl group; Y means hydrogen, or optionally substituted amino group, or Y and Z form together a -CO-O- group, where Y and Z mean together a valency bond, or Y and Y mean together a valency bond, and at the same time Z means hydrogen, hydroxy, C1-4 alkyl, C7-9 phenylalkyl, optionally substituted phenyl, COOC1-4 alkyl, C2-14 acyl, C1-4 alkylsulphonyl, trifluoromethyl-sulphonyl, optionally substituted benzoyl, optionally substituted phenyl-sulphonyl group; X and X mean together =O, or =S, or X means hydrogen, -NHR or -WR groups, and at the same time X means hydrogen, or X and X together form a valency bond, X means hydrogen, C1-4 alkyl, C7-9 phenylalkyl, optionally substituted phenyl, R and R mean hydrogen, halogen, C1-4 alkyl, trifluoromethyl, ciano, mercapto or sulphonylamido group, R means hydrogen or nitro group, R means hydrogen or hydroxy group, R means hydrogen, C1-4 alkyl, C7-9 phenylalkyl group, W means oxygen or sulfur with the proviso, that a) if at least one of the substituents of R , R and R is different from hydrogen or b) if the meaning of Z and Z is hydrogen and R means 6-chloro, R means hydrogen, R has a different meaning from 7-chloro, or R means 6-methyl, R means hydrogen, R has a different meaning from 7-methyl; compounds of general formula (I) show a significant activity at the glycine binding site of the NMDA-receptor, therefore they can be used as active ingredients of pharmaceutical compositions.
摘要翻译：本发明涉及通式（I）的化合物及其盐，互变异构形式和N-氧化物，其中式：Z 1表示氢，羟基，C 1-4烷基，C 7-9苯基烷基，任选取代的苯基，COOC1- C 1-4烷基磺酰基，三氟甲磺酰基，任选取代的苯甲酰基，任选取代的苯基磺酰基; Y 1表示氢或任选取代的氨基，或Y 1和Z 1一起形成-CO-O-基团，其中Y 2和Z 2表示价键，或 Y 1和Y 2均表示价键，同时Z 2表示氢，羟基，C 1-4烷基，C 7-9苯基烷基，任选取代的苯基，COOC 1-4烷基， 14酰基，C 1-4烷基磺酰基，三氟甲基磺酰基，任选取代的苯甲酰基，任选取代的苯基磺酰基; X 1和X 2均表示= O或= S或X 1表示氢，-NHR 4或-WR 5基团，同时X 2表示氢或X 2和X 3一起形成价键，X 3表示氢，C 1-4烷基，C 7-9苯基烷基，任选取代的苯基，R 1和R 2表示氢，卤素，C 1-4烷基，三氟甲基，碳原子，巯基或磺酰氨基，R 3表示氢或硝基，R 4表示氢或羟基，R 5表示氢，C 1-4烷基， 9苯基烷基，W表示氧或硫，条件是a）如果R 1，R 2和R 3的至少一个取代基不同于氢或b）如果Z的含义 1和Z 2是氢，R 1表示6-氯，R 3表示氢，R 2与7-氯不同，或者R 1表示6-甲基， R 3表示氢，R 2与7-甲基具有不同的含义; 通式（I）的化合物在NMDA受体的甘氨酸结合位点显示出显着的活性，因此它们可以用作药物组合物的活性成分。

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