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1. 发明授权

US4645773A .beta.-carboline-3-oxadiazolyl derivatives, and their use as psychotropic agents 失效
标题翻译： β-咔啉-3-恶二唑基衍生物及其作为精神药物的用途
公开(公告)号：US4645773A
公开(公告)日：1987-02-24
申请号：US734219
申请日：1985-05-15
申请人： Mogens Engelstoft , Tage Honore , Frank Watjen , Erling N. Petersen , Andreas Huth
发明人： Mogens Engelstoft , Tage Honore , Frank Watjen , Erling N. Petersen , Andreas Huth
IPC分类号： A61K31/435 , A61P25/00 , A61P25/20 , A61P39/02 , C07D471/04 , A61K31/395
CPC分类号： C07D471/04
摘要： New .beta.-carboline-3-oxadiazolyl derivatives have the general formula I: ##STR1## wherein X is ##STR2## and wherein R.sup.4, R.sup.A and R have specified meanings. These new compounds exhibit surprising psychotropic properties.
摘要翻译：新的β-咔啉-3-恶二唑基衍生物具有通式I：其中X是<和>，其中R4，RA和R具有特定含义。这些新化合物表现出惊人的精神药性。

2. 发明授权

US5414002A 5- or 6-substituted .beta.-carboline-3-carboxylic acid esters 失效
标题翻译： 5-或6-取代的β-咔啉-3-羧酸酯
公开(公告)号：US5414002A
公开(公告)日：1995-05-09
申请号：US416629
申请日：1989-10-03
申请人： Helmut Biere , Andreas Huth , Dieter Rahtz , Ralph Schmiechen , Dieter Seidelmann , Wolfgang Kehr , Herbert H. Schneider , Mogens Engelstoft , Bondo J. Hansen , Frank Waetjen , Tage Honore
发明人： Helmut Biere , Andreas Huth , Dieter Rahtz , Ralph Schmiechen , Dieter Seidelmann , Wolfgang Kehr , Herbert H. Schneider , Mogens Engelstoft , Bondo J. Hansen , Frank Waetjen , Tage Honore
IPC分类号： C07D487/04 , A61K31/435 , A61K31/437 , A61P25/18 , C07D471/04
CPC分类号： C07D471/04
摘要： 5- or 6-substituted .beta.-carboline-3-carboxylic acid esters of Formula I ##STR1## wherein R.sup.1 is hydrogen, nitrilo, halogen, lower alkyl or lower alkoxy, andR.sup.3 is a branched C.sub.3-6 alkyl group which is optionally substituted by halogen, or a C.sub.3-6 cycloalkyl group which is optionally methyl-substituted, are valuable pharmaceuticals.
摘要翻译：式I的5-或6-取代的β-咔啉-3-羧酸酯其中R1是氢，次氮基，卤素，低级烷基或低级烷氧基，R3是支链C 3-6烷基，其任选地被卤素或任选被甲基取代的C 3-6环烷基是有价值的药物。

3. 发明申请

US20100076037A1 Methods of Treating Neuropathic Pain with Agonists of PPAR-gamma 审中-公开
标题翻译：用PPAR-γ激动剂治疗神经性疼痛的方法
公开(公告)号：US20100076037A1
公开(公告)日：2010-03-25
申请号：US12513234
申请日：2007-11-01
申请人： Lillian W. Chiang , Tage Honore
发明人： Lillian W. Chiang , Tage Honore
IPC分类号： A61K31/255 , A61K31/421 , A61K31/192 , A61K31/335 , A61K31/427 , A61P25/00
CPC分类号： A61K31/4436 , A61K31/216 , A61K31/415
摘要： Embodiments of the invention relate to the treatment of neuropathic pain in mammals. Embodiments of the invention include methods for treating neuropathic pain as well as methods for preparing medicaments used in the treatment of mammalian pain. Preferably, methods of the invention comprise the use of PPARgamma agonists for the treatment of mammalian pain.
摘要翻译：本发明的实施方案涉及哺乳动物神经性疼痛的治疗。本发明的实施方案包括治疗神经性疼痛的方法以及用于治疗哺乳动物疼痛的药物的制备方法。优选地，本发明的方法包括使用PPARγ激动剂来治疗哺乳动物的疼痛。

4. 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。

5. 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。

6. 发明授权

US5308845A 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：US5308845A
公开(公告)日：1994-05-03
申请号：US914274
申请日：1992-07-15
申请人： Tage Honore , Poul Jacobsen , Flemming Nielsen , Lars Naerum
发明人： Tage Honore , Poul Jacobsen , Flemming Nielsen , Lars Naerum
IPC分类号： C07D241/52 , C07D471/04 , C07D491/06 , C07D487/04 , A61K31/495
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; and R.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 - 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; or R.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 - 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; 或者R 5和R 6独立地是羟基，氢，NO 2，卤素，CN，CF 3，C 1-4 - 烷氧基，乙酰基，SO 2 NHCOCO 2，SO 2 NR'R'或SO 2 R'，其中R'是氢或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。

7. 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.

8. 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.

9. 发明申请

US20140024692A1 Methods of Treating Neuropathic Pain with Benzimidazole Derivative Agonists of PPARgamma 审中-公开
标题翻译：用PPARγ的苯并咪唑衍生物激动剂治疗神经性疼痛的方法
公开(公告)号：US20140024692A1
公开(公告)日：2014-01-23
申请号：US14032529
申请日：2013-09-20
申请人： Lillian W. Chiang , Tage Honore
发明人： Lillian W. Chiang , Tage Honore
IPC分类号： C07D235/08
CPC分类号： C07D235/08 , A61K31/416
摘要： Embodiments of the invention relate to the treatment of neuropathic pain in mammals. Embodiments of the invention include methods for treating neuropathic pain with benzimidazole derivatives with PPARgamma agonist activity, as well as methods for preparing medicaments used in such treatments of mammalian pain.
摘要翻译：本发明的实施方案涉及哺乳动物神经性疼痛的治疗。本发明的实施方案包括用具有PPARγ激动剂活性的苯并咪唑衍生物治疗神经性疼痛的方法，以及用于制备哺乳动物疼痛治疗中使用的药物的方法。

10. 发明申请

US20110028527A1 Methods of Treating Neuropathic Pain with Benzimidazole Derivative Agonists of PPARgamma 有权
标题翻译：用PPARγ的苯并咪唑衍生物激动剂治疗神经性疼痛的方法
公开(公告)号：US20110028527A1
公开(公告)日：2011-02-03
申请号：US12845868
申请日：2010-07-29
申请人： Lillian W. Chiang , Tage Honore
发明人： Lillian W. Chiang , Tage Honore
IPC分类号： A61K31/4184 , A61P25/04
CPC分类号： C07D235/08 , A61K31/416
摘要： Embodiments of the invention relate to the treatment of neuropathic pain in mammals. Embodiments of the invention include methods for treating neuropathic pain with benzimidazole derivatives with PPARgamma agonist activity, as well as methods for preparing medicaments used in such treatments of mammalian pain.
摘要翻译：本发明的实施方案涉及哺乳动物神经性疼痛的治疗。本发明的实施方案包括用具有PPARγ激动剂活性的苯并咪唑衍生物治疗神经性疼痛的方法，以及用于制备哺乳动物疼痛治疗中使用的药物的方法。

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