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1. 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。

2. 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.

3. 发明授权

US5079250A Tricyclic heterocyclic diols and their preparation and use 失效
标题翻译：三环杂环二醇及其制备与使用
公开(公告)号：US5079250A
公开(公告)日：1992-01-07
申请号：US572172
申请日：1990-08-23
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 --N.dbd.CR.sup.3 --CR.sup.3 .dbd.N--, --NH--CR.sup.3 .dbd.CR.sup.3 --CR.sup.3 .dbd.N--, 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.

4. 发明授权

US5057516A 7,8-dihydroxy-1H-pyrazolo[3,4-f]quinoxalines 失效
标题翻译： 7,8-二羟基-1H-吡唑并（3,4-F）喹唑啉
公开(公告)号：US5057516A
公开(公告)日：1991-10-15
申请号：US570903
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 --NR.sup.3 --N=CR.sup.3 -- and --CR.sup.3 =N--NR.sup.3 --, 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.

5. 发明授权

US4977155A 1,2,3-triazolo compounds 失效
标题翻译： 1,2,3-三唑并
公开(公告)号：US4977155A
公开(公告)日：1990-12-11
申请号：US369762
申请日：1989-06-22
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 --N.dbd.N--N.sup.3 --,--NR.sup.3 --N.dbd.N--,.dbd.N--NR.sup.3 --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.

6. 发明授权

US6124285A Indole-2,3-dione-3-oxime derivatives 失效
标题翻译：吲哚-2,3-二酮-3-肟衍生物
公开(公告)号：US6124285A
公开(公告)日：2000-09-26
申请号：US77554
申请日：1998-06-01
申请人： Frank Watjen , Jorgen Drejer
发明人： Frank Watjen , Jorgen Drejer
IPC分类号： A61K20060101 , A61K31/00 , A61K31/40 , A61K31/407 , A61K31/435 , A61K31/47 , A61K31/4738 , A61K31/4745 , A61K31/55 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/28 , A61P25/30 , A61P43/00 , C07D20060101 , C07D209/40 , C07D471/04 , C07D487/04 , A61K31/4375 , A61K31/5375 , C07D417/12
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention relates to novel indole-2,3-dione-3-oxime derivatives capable of antagonising the effect of excitatory amino acids, such as glutamate. More specifically the novel indole-2,3-dione-3-oxime derivatives of the invention may be described by general formula (I), wherein R.sup.3 represents "Het", or a group of formula (II), wherein "Het" represents a saturated or unsaturated, 4 to 7 membered, monocyclic, heterocyclic ring, at least one of R.sup.31, R.sup.32, and R.sup.33 independendy represents hydrogen, alkyl, or hydroxyalkyl, and at least one of R.sup.31, R.sup.32, and R.sup.33 independently represents (CH.sub.2).sub.n R.sup.34 ; wherein R.sup.34 represents hydroxy, carboxy, alkoxycarbonyl, alkenyloxycarbonyl, alkynyloxycarbonyl, cycloalkoxycarbonyl, cycloalkyl-alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, CONR.sup.35 R.sup.36, or "Het"; wherein n is 0, 1, 2, or 3; and R.sup.5 represents phenyl, naphthyl, thienyl, or pyridyl, all of which may be substituted. "A" represents a ring of five to seven atoms fused with the benzo ring at the positions marked "a" and "b", and formed by the following bivalent radicals: a-NR.sup.6 --CH.sub.2 --CH.sub.2 -b; a-CH.sub.2 --NR.sup.6 --CH.sub.2 -b; a-CH.sub.2 --CH.sub.2 --NR.sup.6 -b; a-NR.sup.6 --CH.sub.2 --CH.sub.2 --H.sub.2 -b; a-CH.sub.2 --NR.sup.6 --CH.sub.2 --CH.sub.2 -b; a--CH.sub.2 --CH.sub.2 --NR.sup.6 --CH.sub.2 -b; a-CH.sub.2 --CH.sub.2 --CH.sub.2 --NR.sup.6 -b; a-NR.sup.6 --CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2 -b; a-CH.sub.2 --NR.sup.6 --CH.sub.2 --CH.sub.2 --CH.sub.2 -b; a-CH.sub.2 --CH.sub.2 --NR.sup.6 --CH.sub.2 --CH.sub.2 -b; a-CH.sub.2 --CH.sub.2 --CH.sub.2 --NR.sup.6 --CH.sub.2 -b; or a-CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2 --NR.sup.6 -b; wherein R.sup.6 represents hydrogen, alkyl or CH.sub.2 CH.sub.2 OH; or a pharmaceutically acceptable salt thereof.
摘要翻译： PCT No.PCT / DK97 / 00418 Sec。 371日期1998年6月1日 102（e）日期1998年6月1日PCT 1997年10月1日PCT PCT。公开号WO98 / 14447 日期：1998年4月9日本发明涉及能够拮抗兴奋性氨基酸如谷氨酸的作用的新的吲哚-2,3-二酮-3-肟衍生物。更具体地，本发明的新的吲哚-2,3-二酮-3-肟衍生物可以由通式（I）描述，其中R 3表示“Het”，或式（II）的基团，其中“Het”表示饱和或不饱和的4至7元单环杂环，R 31，R 32和R 33独立的至少一个表示氢，烷基或羟基烷基，并且R 31，R 32和R 33中的至少一个独立地表示（CH 2） nR34; 其中R34表示羟基，羧基，烷氧基羰基，烯氧基羰基，炔氧基羰基，环烷氧基羰基，环烷基 - 烷氧基羰基，芳氧基羰基，芳烷氧羰基，CONR35R36或“Het”。其中n为0,1,2或3; 并且R 5表示苯基，萘基，噻吩基或吡啶基，它们都可以被取代。 “A”表示在标记为“a”和“b”的位置与苯并环稠合的5至7个原子的环，由以下二价基团形成：a-NR6-CH2-CH2-b; a-CH2-NR6-CH2-b; a-CH2-CH2-NR6-b; a-NR6-CH2-CH2-H2-b; a-CH2-NR6-CH2-CH2-b; a-CH2-CH2-NR6-CH2-b; a-CH2-CH2-CH2-NR6-b; a-NR6-CH2-CH2-CH2-CH2-b; a-CH 2 -NR 6 -CH 2 -CH 2 -CH 2 -B; a-CH2-CH2-NR6-CH2-CH2-b; a-CH2-CH2-CH2-NR6-CH2-b; 或a-CH2-CH2-CH2-CH2-NR6-b; 其中R6表示氢，烷基或CH2CH2OH; 或其药学上可接受的盐。

7. 发明授权

US5436250A Isatineoxime derivatives, their preparation and use 失效
标题翻译：异恶嗪衍生物，其制备和用途
公开(公告)号：US5436250A
公开(公告)日：1995-07-25
申请号：US088328
申请日：1993-07-07
申请人： Frank Watjen , Bjarne H. Dahl , Jorgen Drejer , Lein H. Jensen
发明人： Frank Watjen , Bjarne H. Dahl , Jorgen Drejer , Lein H. Jensen
IPC分类号： C07C205/45 , C07D471/04 , C07D487/04 , C07D491/04 , C07D491/048 , C07D495/04 , A61K31/395
CPC分类号： C07C205/45 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04
摘要： A compound having the formula ##STR1## wherein R.sup.4 and R.sup.5 independently are hydrogen, halogen, CF.sub.3, CN, NO.sub.2 or SO.sub.2 NR.sup.1 R.sup.2 whereinR.sup.1 is hydrogen or C.sub.1-6 -alkyl which may be straight, branched or cyclic,R.sup.2 is hydrogen or C.sub.1-6 -alkyl which may be straight, branched or cyclic, or wherein R.sup.1 and R.sup.2 together represent --(CH.sub.2).sub.n --A--(CH.sub.2).sub.m --, wherein A is O, S, CH.sub.2 or NR.sup.I, wherein R.sup.I is H, C.sub.1-6 -alkyl which may be straight, branched or cyclic, n is 0, 1, 2, 3, 4, 5 and m is 0, 1, 2, 3, 4, 5;R.sup.II is hydrogen, benzyl, (C.dbd.O)CF.sub.3, C.sub.1-6 -carboxylic acid acyl, C.sub.1-6 -alkoxy which may be branched or cyclic, or C.sub.1-6 -alkyl which may be straight, branched or cyclic, CH.sub.2 CO.sub.2 R.sup.VI wherein R.sup.VI is hydrogen or C.sub.1-6 -alkyl which may be straight or branched;and a method of treating disorders of a mammal, including a human, responsive to the blockade of glutamic and aspartic acid receptors, with the same.
摘要翻译：具有式“IMAGE”的化合物，其中R4和R5独立地是氢，卤素，CF3，CN，NO2或SO2NR1R2，其中R1是氢或可以是直链，支链或环状的C1-6烷基，R2是氢或C1- 其可以是直链，支链或环状的，或其中R 1和R 2一起表示 - （CH 2）n -A（CH 2）m - ，其中A是O，S，CH 2或NRI，其中R 1是H，C 1-6 - 烷基，其可以是直链，支链或环状的，n为0,1,2,3,4,5，m为0,1,2,3,4,5; RII是氢，苄基，（C = O）CF 3，C 1-6 - 羧酸酰基，可以是支链或环状的C 1-6 - 烷氧基或可以是直链，支链或环状的C 1-6 - 烷基，CH 2 CO 2 RVI，其中 RVI是氢或可以是直链或支链的C1-6烷基; 以及治疗对谷氨酸和天冬氨酸受体的阻断作用的哺乳动物（包括人）的病症的方法。

8. 发明授权

US5158961A Piperidine compounds and their preparation and use 失效
标题翻译：哌啶化合物及其制备和用途
公开(公告)号：US5158961A
公开(公告)日：1992-10-27
申请号：US673933
申请日：1991-03-22
申请人： Palle Jakobsen , Jorgen Drejer
发明人： Palle Jakobsen , Jorgen Drejer
IPC分类号： C07D211/20 , C07D211/22 , C07D405/12 , C07D405/14 , C07D417/14
CPC分类号： C07D405/12 , C07D211/20 , C07D211/22 , C07D405/14 , C07D417/14
摘要： Novel piperidine compounds having the formula ##STR1## wherein the symbols have the same meaning as set forth in the specification, and salts thereof with a pharmaceutically acceptable acid, are disclosed.The novel compound are useful in the treatment of anoxia, migraine, ischemia and epilepsy.
摘要翻译：公开了具有式（I）的新颖的哌啶化合物，其中符号具有与说明书中所述相同的含义，以及其与药学上可接受的酸的盐。该新型化合物可用于治疗缺氧，偏头痛，局部缺血和癫痫。

9. 发明授权

US5017585A Method of treating calcium overload 失效
标题翻译：治疗钙超载的方法
公开(公告)号：US5017585A
公开(公告)日：1991-05-21
申请号：US337301
申请日：1989-04-13
申请人： Palle Jakobsen , Jorgen Drejer
发明人： Palle Jakobsen , Jorgen Drejer
IPC分类号： C07D211/20 , C07D211/22 , C07D405/12 , C07D405/14 , C07D417/14
CPC分类号： C07D405/12 , C07D211/20 , C07D211/22 , C07D405/14 , C07D417/14
摘要： Novel piperidine compounds having the formula ##STR1## wherein R.sup.3 is 3,4-methylenedioxyphenyl, aryl or heteroaryl which are optionally substituted with one or more halogen, C.sub.1-6 -alkoxy, optionally substituted aryloxy or aryl-C.sub.1-6 -alkoxy, cyano, mono or poly halogenated C.sub.1-6 -alkyl, C.sub.1-6 -alkenyl, C.sub.1-6 -alkyl, C.sub.3-5 -alkylene or trifluoromethyl groups,R.sup.1 is straight or branched C.sub.1-8 -alkyl unsubstituted or substituted with one or more cyano, ester, dialkylamino, hydroxy, amido, halogeno, substituted or unsubstituted piperidino, morpholino, thiomorpholino, dioxolanyl, tetrahydrofuranyl, C.sub.1-8 -alkoxy or C.sub.3-8 cycloalkyl groups,X is hydrogen, halogen, trifluoromethyl, hydroxy cyano or C.sub.1-8 -alkoxy,Y is O or S;provided that R.sup.1 is not unsubstituted C.sub.1-8 -alkyl, when R.sup.3 is 3,4-methylenedioxyphenyl, aryl or heteroaryl optionally subsituted with one or more C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, C.sub.3-5 -alkylene, C.sub.3-8 -cycloalkyl or aralkoxy, and at the same time X is hydrogen or halogenand a salt thereof with a pharmaceutically acceptible acid.The novel compounds are useful in the treatment of anoxia, migraine, ischemia and epilepsy.
摘要翻译：具有式（I）的新颖的哌啶化合物，其中R 3为3,4-亚甲二氧基苯基，芳基或杂芳基，其任选被一个或多个卤素，C 1-6 - 烷氧基，任选取代的芳氧基或芳基-C 1-6 - 烷氧基，氰基，单或多卤代C 1-6 - 烷基，C 1-6 - 烯基，C 1-6 - 烷基，C 3-5 - 亚烷基或三氟甲基，R 1是未取代或被一个或更多氰基，酯，二烷基氨基，羟基，酰氨基，卤代，取代或未取代的哌啶子基，吗啉代，硫代吗啉代，二氧戊环基，四氢呋喃基，C 1-8 - 烷氧基或C 3-8环烷基，X是氢，卤素，三氟甲基，羟基氰基或 C 1-8 - 烷氧基，Y是O或S; 条件是当R 3为3,4-亚甲二氧基苯基时，R 1不是未取代的C 1-8 - 烷基，任选被一个或多个C 1-6 - 烷基，C 1-6 - 烷氧基，C 3-5 - 亚烷基， 8-环烷基或芳烷氧基，同时X是氢或卤素及其与药学上可接受的酸的盐。新型化合物可用于治疗缺氧，偏头痛，局部缺血和癫痫。

10. 发明授权

US06239128B1 Indole-2,3-dione-3-oxime derivatives for therapeutic use 失效
标题翻译：用于治疗用途的吲哚-2,3-二酮-3-肟衍生物
公开(公告)号：US06239128B1
公开(公告)日：2001-05-29
申请号：US09675214
申请日：2000-09-29
申请人： Frank Watjen , Jorgen Drejer
发明人： Frank Watjen , Jorgen Drejer
IPC分类号： A61K3155
CPC分类号： C07D471/04
摘要： The present invention relates to the use of indole-2,3-dione-3-oxime derivatives in a method of combating diseases and disorders associated with or mediated by the release of excitatory amino acids.
摘要翻译：本发明涉及吲哚-2,3-二酮-3-肟衍生物在抗兴奋性氨基酸释放相关疾病和病症的方法中的应用。

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