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1. 发明授权

US5968928A Excitatory amino acid antagonists: fused-azacyclic quinoxalinediones and immunoassays thereof 失效
标题翻译：兴奋性氨基酸拮抗剂：融合 - 氮杂环喹诺酮和其免疫测定
公开(公告)号：US5968928A
公开(公告)日：1999-10-19
申请号：US909471
申请日：1997-08-11
申请人： Christopher Franklin Bigge , Gerald David Nordblom , Chung Stephen Yi
发明人： Christopher Franklin Bigge , Gerald David Nordblom , Chung Stephen Yi
IPC分类号： C07D471/04 , C07D519/00 , A61K31/495 , A61K31/55 , C07D487/14
CPC分类号： C07D471/04 , Y10S436/815
摘要： The invention discloses novel fused-azacylic quinoxalinediones. These compounds may be employed as excitatory amino acid antagonists and as analogs for use in immunological assays. The invention is also directed to both a radioimmunoassay and enzyme immunoassay for detecting and quantitating 1,4,7,8,9,10,-hexahydro-9-methyl-6-nitropyrido[3,4-f]-quinoxaline-2,3-dione PNQX and analogs thereof.
摘要翻译：本发明公开了新型稠合氮酰喹啉喹啉。这些化合物可以用作兴奋性氨基酸拮抗剂和用作免疫测定中的类似物。本发明还涉及用于检测和定量1,4,7,8,9,10-六氢-9-甲基-6-硝基吡啶并[3,4-f] - 喹喔啉-2的放射免疫测定和酶免疫测定， 3-二酮PNQX及其类似物。

2. 发明授权

US6057313A Glutamate (ampa/kainate) receptor antagonists: N-substituted fused azacycloalkylquinoxalinediones 失效
标题翻译：谷氨酸（ampa / kainate）受体拮抗剂：N-取代的稠合氮杂环烷基喹喔啉
公开(公告)号：US6057313A
公开(公告)日：2000-05-02
申请号：US869515
申请日：1997-06-05
申请人： Christopher Franklin Bigge , Thomas Charles Malone , Robert Michael Schelkun , Chung Stephen Yi
发明人： Christopher Franklin Bigge , Thomas Charles Malone , Robert Michael Schelkun , Chung Stephen Yi
IPC分类号： C07D217/02 , C07D217/04 , C07D217/06 , C07D471/04 , A61K31/495 , C07D487/04
CPC分类号： C07D471/04 , C07D217/02 , C07D217/04 , C07D217/06
摘要： Novel N-substituted azacycloalkyl ring fused 2,3-quinoxalinediones are disclosed represented by the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.1 is hydrogen, alkyl or W-alkyl; X and Y are independently hydrogen, halogen, nitro, cyano, trifluoromethyl, SO.sub.2 CF.sub.3, SO.sub.2 R.sup.4, SO.sub.2 NR.sup.4 R.sup.5, alkyl, alkenyl, (CH.sub.2).sub.z CONR.sup.4 R.sup.5, (CH.sub.2).sub.z COOR.sup.4, or NHCOR.sup.4, wherein R.sup.4 and R.sup.5 are independently hydrogen, alkyl having 1 to 6 carbon atoms, cycloalkyl or W-alkyl, and z is an integer from 0 to 4; R.sup.2 is benzoyl, W, W-alkyl, COcycloalkyl, COalkyl-W, CONR.sup.3 alkyl, CONR.sup.3 -W, CONR.sup.3 alkyl-W, CSNR.sup.3 alkyl, CSNR.sup.3 alkyl-W, ##STR2## or a moiety derived from a common amino acid by removal of the --OH from the carboxyl group which is alpha to the amino, wherein --W is aryl, heteroaryl, or the heterocycles piperidinyl, piperazinyl, morpholinyl or pyrrolidinyl, wherein R.sup.3 is hydrogen, alkyl or W-alkyl; and m and n are independently 0, 1 or 2 provided that m+n is >1; provided that when R.sup.2 is benzoyl, ##STR3## or X is nitro, Y and R.sup.1 are H, m is 2 and n is 1;when R.sup.2 is ##STR4## X is nitro, Y and R.sup.1 are H and m is 2 and n is 1; or when R.sup.2 is ##STR5## X is bromo, Y and R.sup.1 are H, m is 1 and n is 2. The novel N-substituted azacycloalkyl ring fused 2,3-quinoxalinediones may be used, for example, as neuroprotective agents, for treatment of chronic neurodegenerative disorders, as anticonvulsants and in the treatment of schizophrenia, epilepsy, anxiety, pain and drug addiction.
摘要翻译：公开了由下式表示的新的N-取代的氮杂环烷基环稠合的2,3-喹喔啉二醇：或其药学上可接受的盐，其中R 1是氢，烷基或W-烷基; X和Y独立地是氢，卤素，硝基，氰基，三氟甲基，SO 2 CF 3，SO 2 R 4，SO 2 NR 4 R 5，烷基，烯基，（CH 2）z CONR 4 R 5，（CH 2）z COOR 4或NHCOR 4，其中R 4和R 5独立地是氢， 6个碳原子，环烷基或W-烷基，z是0-4的整数; R 2是苯甲酰基，W，W-烷基，CO环烷基，CO烷基-W，CONR 3烷基，CONR 3 -W，CONR 3烷基-W，CSNR 3烷基，CSNR 3烷基-W，或通过从羧基中除去-OH而衍生自常见氨基酸的部分其中-W是芳基，杂芳基或杂环哌啶基，哌嗪基，吗啉基或吡咯烷基，其中R 3是氢，烷基或W-烷基; m和n独立地为0,1或2，条件是m + n大于1; 条件是当R 2为苯甲酰基或X为硝基时，Y和R 1为H，m为2且n为1; 当R 2为硝基时，Y和R 1为H，m为2，n为1; 或当R 2为X时，Y和R 1为H，m为1且n为2.新的N-取代的氮杂环烷基环稠合2,3-喹喔啉酮可用作例如神经保护剂，用于治疗慢性神经退行性疾病，抗惊厥药和治疗精神分裂症，癫痫，焦虑，疼痛和药物成瘾。

3. 发明授权

US06197771B1 Glutamate (ampa/kainate) receptor antagonists: N-substituted fused azacycloalkylquinoxalinediones 失效
标题翻译：谷氨酸（ampa / kainate）受体拮抗剂：N-取代的稠合氮杂环烷基喹喔啉
公开(公告)号：US06197771B1
公开(公告)日：2001-03-06
申请号：US09499475
申请日：2000-02-07
申请人： Christopher Franklin Bigge , Thomas Charles Malone , Robert Michael Schelkun , Chung Stephen Yi
发明人： Christopher Franklin Bigge , Thomas Charles Malone , Robert Michael Schelkun , Chung Stephen Yi
IPC分类号： A61K3147
CPC分类号： C07D471/04 , C07D217/02 , C07D217/04 , C07D217/06
摘要： Novel N-substituted azacycloalkyl ring fused 2,3-quinoxalinediones represented by the formula: or a pharmaceutically acceptable salt thereof, are disclosed, wherein the formula variables R1, R2, X, Y, m and n are as defined herein. Also disclosed are methods of treatment using the same and intermediate compounds useful in the preparation thereof.
摘要翻译：公开了由下式表示的新型N-取代的氮杂环烷基环稠合的2,3-喹喔啉二盐或其药学上可接受的盐，其中式变量R1，R2，X，Y，m和n如本文所定义。还公开了使用可用于其制备的相同和中间体化合物的治疗方法。

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