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1. 发明授权

US5153195A Quinoxaline compounds and their preparation and use 失效
标题翻译：喹喔啉化合物及其制备和用途
公开(公告)号：US5153195A
公开(公告)日：1992-10-06
申请号：US794262
申请日：1991-11-15
申请人： Tage Honore , Poul Jacobsen , Flemming E. Nielsen , Lars Naerum
发明人： Tage Honore , Poul Jacobsen , Flemming E. Nielsen , Lars Naerum
IPC分类号： C07D241/52 , C07D471/04 , C07D491/06
CPC分类号： C07D241/52 , C07D471/04 , C07D491/06
摘要： Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R.sup.1 is hydroxy; andR.sup.5 and R.sup.6 together form a fused phenyl, cyclohexyl or pyridyl ring, which is optionally substituted with halogen or CN; and R.sup.7 and R.sup.8 independently are hydrogen, hydroxy, NO.sub.2, halogen, CN, CF.sub.3, C.sub.1-4 -alkoxy, acetyl, SO.sub.2 NHCOCO.sub.2 Et, SO.sub.2 NR'R' or SO.sub.2 R', wherein R' is hydrogen or C.sub.1-4 -alkyl; orR.sup.5 and R.sup.6 independently are hydroxy, hydrogen, NO.sub.2, halogen, CN, CF.sub.3, C.sub.1-4 -alkoxy, acetyl, SO.sub.2 NHCOCO.sub.2 Et, SO.sub.2 NR'R' or SO.sub.2 R', wherein R' is hydrogen or C.sub.1-4 -alkyl; and R.sup.7 and R.sup.8 together form a fused phenyl, cyclohexyl or pyridyl ring which is optionally substituted with halogen or CN.The invention also relates to a method of preparing the compounds, pharmaceutical compositions thereof, and their use.The compounds are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters, particularly the quisqualate receptors, and especially as neuroleptics.
摘要翻译：具有式“IMAGE”的杂环二羟基喹喔啉化合物，其中R 1是羟基; 并且R 5和R 6一起形成稠合的苯基，环己基或吡啶环，其任选被卤素或CN取代; 并且R 7和R 8独立地是氢，羟基，NO 2，卤素，CN，CF 3，C 1-4 - 烷氧基，乙酰基，SO 2 NHCOCO 2Et，SO 2 NR'R'或SO 2 R'，其中R'是氢或C 1-4烷基; 或R 5和R 6独立地为羟基，氢，NO 2，卤素，CN，CF 3，C 1-4 - 烷氧基，乙酰基，SO 2 NHCOCO 2 Et，SO 2 NR'R'或SO 2 R'，其中R'为氢或C 1-4 - 烷基; 并且R 7和R 8一起形成任选被卤素或CN取代的稠合的苯基，环己基或吡啶基环。本发明还涉及制备化合物的方法，其药物组合物及其用途。该化合物可用于治疗由兴奋性神经递质特别是quisqualate受体的多动症引起的适应症，特别是作为精神安定药物。

2. 发明授权

US4812458A 6,7-disubstituted-2,3-dihydroxyquinoxaline compounds, pharmaceutical compositions thereof, and their use as neuroleptics 失效
标题翻译： 6,7-二取代-2,3-二羟基喹喔啉化合物及其药物组合物及其作为精神安定药的用途
公开(公告)号：US4812458A
公开(公告)日：1989-03-14
申请号：US92034
申请日：1987-09-02
申请人： Tage Honore , Jorgen Drejer , Poul Jacobsen , Flemming E. Nielsen
发明人： Tage Honore , Jorgen Drejer , Poul Jacobsen , Flemming E. Nielsen
IPC分类号： C07D241/44 , A61K31/495
CPC分类号： C07D241/44
摘要： Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R.sup.1 is halogen, CN, CF.sub.3, ethynyl, or N.sub.3 andR.sup.2 is SO.sub.2 C.sub.1-3 -alkyl, CF.sub.3, NO.sub.2, ethynyl, or CN.The invention also relates to a method of preparing the compounds, pharmaceutical compositions thereof, and their use.The compounds are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters, particularly the quisqualate receptors, and especially as neuroleptics.
摘要翻译：其中R 1是卤素，CN，CF 3，乙炔基或N 3和R 2的具有式“IMAGE”的杂环二羟基喹喔啉化合物是SO 2 C 1-3 - 烷基，CF 3，NO 2，乙炔基或CN。本发明还涉及制备化合物的方法，其药物组合物及其用途。该化合物可用于治疗由兴奋性神经递质特别是quisqualate受体的多动症引起的适应症，特别是作为精神安定药物。

3. 发明授权

US5061706A 2,3-quinoxalinediones for use as neuroleptics 失效
标题翻译：用作神经元的2,3-喹唑啉二醛
公开(公告)号：US5061706A
公开(公告)日：1991-10-29
申请号：US452029
申请日：1989-12-15
申请人： Tage Honoree , Poul Jacobsen , Flemming E. Nielsen , Lars Nafrim
发明人： Tage Honoree , Poul Jacobsen , Flemming E. Nielsen , Lars Nafrim
IPC分类号： A61K31/495 , A61P25/00 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/28 , C07D241/52
CPC分类号： C07D241/52
摘要： Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R.sup.1 is hydroxy, alkoxy, aryloxy, aralkyloxy, cycloalkylalkoxy, cycloalkoxy, or acyloxy; andR.sup.5, R.sup.6, R.sup.7 and R.sup.8 independently are hydrogen, NO.sub.2, halogen CN, SO.sub.2 NR'R', SO.sub.2 R', CF.sub.3, or OR', wherein R' is hydrogen or C.sub.1-4 -alkyl;The invention also relates to a method of preparing the compounds, pharmaceutical compositions thereof, and their use.The compounds are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters, particularly the quisqualate receptors, and especially as neuroleptics.

4. 发明授权

US5026704A Benzo[f]quinoxaline-2,3(1H,4H)-diones 失效
标题翻译：苯并[f]喹喔啉-2,3（1H，4H） - 二酮
公开(公告)号：US5026704A
公开(公告)日：1991-06-25
申请号：US456325
申请日：1989-12-26
申请人： Tage Honore , Poul Jacobsen , Flemming E. Nielsen , Lars Naerum
发明人： Tage Honore , Poul Jacobsen , Flemming E. Nielsen , Lars Naerum
IPC分类号： A61K31/495 , A61P25/00 , A61P25/08 , A61P25/28 , C07D20060101 , C07D241/38 , C07D241/44 , C07D241/52 , C07D403/06
CPC分类号： C07D241/38 , C07D241/44 , C07D241/52 , C07D403/06
摘要： Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R.sup.1 is C.sub.1-12 -alkyl, which may optionally be substututed by hydroxy, formyl, carboxy, carboxylic esters, amides or amines, C.sub.3-8 -cycloalkyl, aryl, aralkyl; and wherein R.sup.6 is, hydrogen, halogen, CN, CF.sub.3, NO.sub.2, or OR', wherein R' is C.sub.1-4 -alkyl and R.sup.5, R.sup.7 and R.sup.8 is hydrogen, provided R.sup.6 is not CF.sub.3, OCH.sub.3, NO.sub.2, Cl or Br when R.sup.1 is CH.sub.3 ; orR.sup.6 and R.sup.7 independently are NO.sub.2, halogen, CN, CF.sub.3, or OR', wherein R' is C.sub.1-4 -alkyl, and R.sup.5 and R.sup.8 are each hydrogen; orR.sup.5 and R.sup.6 together form a further fused aromatic ring, which may be substituted with halogen, NO.sub.2, CN, CF.sub.3 or OR', wherein R' is C.sub.1-4 -alkyl, and R.sup.7 and R.sup.8 independently are hydrogen, halogen, CN, CF.sub.3, NO.sub.2 or OR', wherein R' is C.sub.1-4 - alkyl; orR.sup.7 and R.sup.8 together form a further fused aromatic ring, which may be substituted with halogen, NO.sub.2, CN, CF.sub.3 or OR', wherein R' is C.sub.1-4 -alkyl, and R.sup.5 and R.sup.6 independently are hydrogen, halogen, CN, CF.sub.3, NO.sub.2 or OR', wherein R' is C.sub.1-4 -alkyl.The invention also relates to a method of preparing the compounds, pharmaceutical compositions thereof, and their use.The compounds are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters, particularly the quisqualate receptors, and especially as neuroleptics.

5. 发明授权

US4912108A Pyridoquinoxaline compounds and their preparation and use as glutamate antagonists 失效
标题翻译：吡啶喹喔啉化合物及其制备和用作谷氨酸拮抗剂
公开(公告)号：US4912108A
公开(公告)日：1990-03-27
申请号：US347141
申请日：1989-05-03
申请人： Poul Jacobsen , Flemming E. Nielsen , Tage Honore
发明人： Poul Jacobsen , Flemming E. Nielsen , Tage Honore
IPC分类号： C07D241/38 , C07D471/04
CPC分类号： C07D241/38 , C07D471/04
摘要： Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein --A-- together with the two carbon atoms denoted as 1 and 2 is selected from ##STR2## R.sup.1, R.sup.2 and R.sup.3 are independently H, halogen, CN, NH.sub.2, NO.sub.2, SO.sub.3 H, SO.sub.2 NH.sub.2, or CONH.sub.2The invention also relates to a method of preparing the compounds, pharmaceutical compositions thereof, and their use.The compounds are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters.

6. 发明授权

US5532236A [1,2,4]triazolo[4,3-a]quinoxaline compounds 失效
标题翻译： [1,2,4]三唑并[4,3-a]喹喔啉化合物
公开(公告)号：US5532236A
公开(公告)日：1996-07-02
申请号：US237518
申请日：1994-05-03
申请人： Poul Jacobsen , Flemming E. Nielsen , Lone Jeppesen
发明人： Poul Jacobsen , Flemming E. Nielsen , Lone Jeppesen
IPC分类号： A61K31/495 , A61P21/02 , A61P25/00 , A61P25/08 , A61P25/20 , A61P25/28 , C07D487/04 , C07D487/14 , A61K31/505 , A61K31/54 , C07D417/14
CPC分类号： C07D487/04
摘要： The present invention relates to [1,2,4]triazolo[4,3-a quinoxaline derivatives of formula I ##STR1## wherein one of R.sup.1 and R.sup.2 is a 5- or 6-membered nitrogen-containing heterocyclic ring which is optionally substituted with one, two or three substituents, wherein each substituent is independently phenyl or C.sub.1-6 -alkyl, or one of R.sup.1 and R.sup.2 is a fused ring system comprising a 5- or 6-membered nitrogen-containing heterocyclic ring and a benzene, pyridine, pyrimidine or pyrazine ring, wherein the fused ring system is optionally substituted with phenyl or C.sub.1-6 -alkyl; and the other of R.sup.1 and R.sup.2 is hydrogen, C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, halogen, NO.sub.2, NH.sub.2, CN, CF.sub.3, COC.sub.1-6 -alkyl or SO.sub.2 NR'R", wherein R' and R" are independently hydrogen or C.sub.1-6 -alkyl; and X is O or S; and pharmaceutically acceptable salts thereof. The compounds have affinity for the AMPA receptors and are antagonists in connection with this type of receptors which makes them useful in the treatment of CNS ailments, especially in the treatment of any of the numerous indications caused by hyperactivity of excitatory amino acids.
摘要翻译：本发明涉及式Ⅰ化合物[1,2,4]三唑并[4,3-a喹喔啉衍生物，其中R 1和R 2之一为5-或6-元含氮杂环，其中任选地被一个，两个或三个取代基取代，其中每个取代基独立地是苯基或C 1-6 - 烷基，或者R 1和R 2中的一个是包含5或6元含氮杂环的稠环体系和苯，吡啶，嘧啶或吡嗪环，其中稠环体系任选被苯基或C 1-6 - 烷基取代; R 1和R 2中的另一个为氢，C 1-6 - 烷基，C 1-6 - 烷氧基，卤素，NO 2，NH 2，CN，CF 3，COC 1-6 - 烷基或SO 2 NR'R“ '独立地是氢或C 1-6 - 烷基; X为O或S; 及其药学上可接受的盐。这些化合物对AMPA受体具有亲和力，并且是与这种类型的受体有关的拮抗剂，这使得它们可用于治疗CNS疾病，特别是在治疗由兴奋性氨基酸的多动症引起的许多适应症中的任何一种。

7. 发明授权

US5504085A Triazolo quinoxalines and their preparation and use 失效
标题翻译：三氮唑喹喔啉及其制备和使用
公开(公告)号：US5504085A
公开(公告)日：1996-04-02
申请号：US285598
申请日：1994-08-03
申请人： Poul Jacobsen , Flemming E. Nielsen
发明人： Poul Jacobsen , Flemming E. Nielsen
IPC分类号： A61K31/495 , A61P25/00 , C07D487/04 , C07D241/52
CPC分类号： C07D487/04
摘要： Quinoxaline compounds represented by formulas I or II, ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen, C.sub.1-6 -alkyl, halogen, NO.sub.2, NH.sub.2, CN, CF.sub.3, SO.sub.2 NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are independently hydrogen or C.sub.1-6 -alkyl, or COR.sup.6 wherein R.sup.6 is C.sub.1-6 -alkyl; and R.sup.3 is hydrogen, C.sub.1-6 -alkyl or CF.sub.3, compositions thereof and methods of preparing the compounds are described.The compounds are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters.
摘要翻译：由式I或II表示的喹喔啉化合物，其中R 1和R 2独立地是氢，C 1-6 - 烷基，卤素，NO 2，NH 2，CN，CF 3，SO 2 NR 4 R 5，其中R 4和R 5 独立地是氢或C 1-6 - 烷基，或COR 6，其中R 6是C 1-6 - 烷基; 和R 3为氢，C 1-6 - 烷基或CF 3，其组成和制备该化合物的方法。该化合物可用于治疗由兴奋性神经递质的多动症引起的适应症。

8. 发明授权

US5109001A Fused 2,3-dihydroxydiazolo compounds and their preparation and use 失效
标题翻译：熔融的2,3-二羟基二唑化合物及其制备和使用
公开(公告)号：US5109001A
公开(公告)日：1992-04-28
申请号：US570819
申请日：1990-08-22
申请人： Poul Jacobsen , Flemming E. Nielsen , Tage Honore , Jorgen Drejer
发明人： Poul Jacobsen , Flemming E. Nielsen , Tage Honore , Jorgen Drejer
IPC分类号： A61K31/00 , A61K31/495 , A61K31/55 , A61P25/00 , A61P43/00 , C07D487/04 , C07D495/04 , C07D498/04 , C07D513/04 , C07D517/04
CPC分类号： C07D487/04 , C07D495/04 , C07D513/04 , C07D517/04
摘要： Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R.sup.2 is hydrogen, NO.sub.2, NH.sub.2, CN, halogen, or SO.sub.2 NH.sub.2 ;--X--Y--Z-- is selected from .dbd.N-Se--N.dbd., .dbd.N--O--N.cuberoot., .dbd.N--S--N.dbd.;wherein R.sup.3 is hydrogen, lower alkyl, or CF.sub.3.The invention also relates to a method of preparing the compounds, pharmaceutical compositions thereof, and their use.The compounds are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters.

9. 发明授权

US5559106A Heterocyclic compounds, their use and preparation 失效
标题翻译：杂环化合物，其使用和制备
公开(公告)号：US5559106A
公开(公告)日：1996-09-24
申请号：US350744
申请日：1994-12-07
申请人： Poul Jacobsen , Flemming E. Nielsen , Lone Jeppesen
发明人： Poul Jacobsen , Flemming E. Nielsen , Lone Jeppesen
IPC分类号： A61K31/495 , A61P9/10 , A61P25/00 , A61P25/28 , C07D487/04 , C07F9/6561 , A61K31/675 , C07F9/6524
CPC分类号： C07D487/04 , C07F9/6561
摘要： Quinoxaline compounds of the general formula ##STR1## wherein R.sup.1 is COX', POX'X" or alkyl substituted with COX' or POX'X", and X' and X" independently are hydroxy or alkoxy, and R.sup.6, R.sup.7, R.sup.8 and R.sup.9 independently are hydrogen, alkyl, halogen, NH.sub.2, NO.sub.2, CN, CF.sub.3, SO.sub.2 NY'Y" or COZ' wherein Z' is NY'Y" or alkyl and Y' and Y" independently are hydrogen or alkyl, triazolyl, imidazolyl, imidazolyl substituted with phenyl or alkyl, or R.sup.6 and R.sup.7, or R.sup.8 and R.sup.9, together form a further fused ring, are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters.
摘要翻译：其中R1是COX'，POX'X“或被COX'或POX'X”取代的烷基的喹喔啉化合物，X'和X“独立地是羟基或烷氧基，R6，R7 ，R8和R9独立地是氢，烷基，卤素，NH2，NO2，CN，CF3，SO2NY'Y“或COZ”，其中Z'是NY'Y“或烷基，Y'和Y'独立地是氢或烷基，三唑基，咪唑基，被苯基或烷基取代的咪唑基，或R6和R7或R8和R9一起形成另外的稠环，可用于治疗由兴奋性神经递质的多动症引起的适应症。

10. 发明授权

US5081123A Quinoxaline compound and their preparation and use 失效
标题翻译：喹啉化合物及其制备和使用
公开(公告)号：US5081123A
公开(公告)日：1992-01-14
申请号：US451382
申请日：1989-12-15
申请人： Tage Honore , Poul Jacobsen , Flemming E. Nielsen , Lars Naerum
发明人： Tage Honore , Poul Jacobsen , Flemming E. Nielsen , Lars Naerum
IPC分类号： A61K31/495 , A61P25/00 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/28 , C07D241/52 , C07D471/04 , C07D487/04 , C07D491/06
CPC分类号： C07D241/52 , C07D471/04 , C07D491/06
摘要： Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R.sup.1 is hydroxy, alkoxy, aryloxy, aralkyloxy, cycloalkylalkoxy, cycloalkoxy, or acyloxy;R.sup.5 and R.sup.6 together form a further fused ring, which is substituted with hydrogen, halogen or CN, and R.sup.7 and R.sup.8 independently are hydrogen, NO.sub.2, halogen, CN, SO.sub.2 NR'R', SO.sub.2 R', CF.sub.3, or OR', wherein R' is hydrogen or C.sub.1-4 -alkyl; orR.sup.7 and R.sup.8 together form a further fused ring, which is substituted with hydrogen, halogen or CN, and R.sup.5 and r.sup.6 independently are hydrogen, NO.sub.2, halogen, CN, SO.sub.2 NR'R', SO.sub.2 R', CF.sub.3, or OR', wherein R' is hydrogen or C.sub.1-4 -alkyl.The invention also relates to a method of preparing the compounds, pharmaceutical compositions thereof, and their use.The compounds are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters, particularly the quisqualate receptors, and especially as neuroleptics.

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