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21.
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.
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公开(公告)号:US4962122A
公开(公告)日:1990-10-09
申请号:US277561
申请日:1988-11-29
申请人: Palle Jakobsen , Jorgen Drejer
发明人: Palle Jakobsen , Jorgen Drejer
IPC分类号: A61K31/135 , A61K31/275 , A61K31/33 , A61K31/357 , A61K31/36 , A61P3/00 , A61P3/14 , A61P9/00 , A61P9/08 , A61P9/10 , A61P25/04 , A61P25/06 , A61P25/08 , C07C213/02 , C07C217/48 , C07C255/54 , C07D317/64 , C07D521/00
CPC分类号: C07D317/64 , C07C217/48 , C07C255/54 , C07C2101/02 , C07C2102/08 , C07C2102/10
摘要: Novel aryloxyphenylpropylamines having the formula ##STR1## wherein R.sup.1 is C.sub.3-7 -cycloalkyl, C.sub.3-10 -alkyl, or alkenyl which may be straight, branched or cyclic, unsubstituted or substituted with C.sub.1-4 -alkoxy, aryloxy or cycloalkyl or cycloalkylalkyl; andR.sup.2 is 3,4-methylenedioxyphenyl, aryl or heteroaryl, which are optionally substituted with one or more cyano, halogen, C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, C.sub.1-6 -alkenyl, trifluoromethyl, C.sub.3-5 -alkylene, aryloxy or aralkoxyand a salt thereof with a pharmaceutically acceptable acid.The novel compounds are useful in the treatment of anoxia, migraine, ischemia and epilepsy.
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公开(公告)号:US4877799A
公开(公告)日:1989-10-31
申请号:US106154
申请日:1987-10-08
申请人: Jorgen Drejer , Palle Jakobsen
发明人: Jorgen Drejer , Palle Jakobsen
IPC分类号: A61K31/443 , A61K31/445 , A61K31/451 , A61P3/00 , C07D211/20 , C07D211/22 , C07D405/12
CPC分类号: C07D405/12 , C07D211/20 , C07D211/22
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 C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, C.sub.3-8 -cycloalkyl, C.sub.3-5 -alkylene or aralkoxy,R.sup.1 is straight or branched C.sub.1-8 -alkyl, C.sub.4-8 -alkoxy-C.sub.4-8 -alkyl, C.sub.4-7 -cycloalkyl, aryloxy-C.sub.3-8 -alkyl, C.sub.4-8 -alkenyl, or C.sub.4-8 -cycloalkylalkyl, or R.sup.1 may also be hydrogen or C.sub.1-3 -alkyl, when R.sup.3 is aryl, which is substituted with two or more of C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, C.sub.3-8 -cycloalkyl, aralkoxy, or with C.sub.3-5 -alkylene.X is hydrogen or halogen, and whereinY is O or S or a salt thereof with a pharmaceutically-acceptable acid, pharmaceutical compositions thereof, method-of-treating therewith.The novel compounds are useful in the treatment of anoxia, migraine, ischemia and epilepsy.
摘要翻译: 具有式“IMAGE”的新型哌啶化合物,其中R 3是3,4-亚甲二氧基苯基,芳基或杂芳基,其任选被一个或多个C 1-6 - 烷基,C 1-6 - 烷氧基,C 3-8 - 环烷基,C 3-5 - 亚烷基或芳烷氧基,R 1是直链或支链C 1-8 - 烷基,C 4-8 - 烷氧基-C 4-8 - 烷基,C 4-7 - 环烷基,芳氧基-C 3-8 - 烷基,C 4-8烯基或C 4 -8-环烷基烷基或R 1也可以是氢或C 1-3 - 烷基,当R 3是被两个或多个C 1-6 - 烷基,C 1-6 - 烷氧基,C 3-8 - 环烷基,芳烷氧基 ,或与C 3-5 - 亚烷基。 X是氢或卤素,并且其中Y是O或S或其盐与药学上可接受的酸,其药物组合物,其处理方法。 新型化合物可用于治疗缺氧,偏头痛,局部缺血和癫痫。
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公开(公告)号:US5019592A
公开(公告)日:1991-05-28
申请号:US558810
申请日:1990-07-27
申请人: Palle Jakobsen , Jorgen Drejer
发明人: Palle Jakobsen , Jorgen Drejer
IPC分类号: A61K31/135 , A61K31/275 , A61K31/33 , A61K31/357 , A61K31/36 , A61P3/00 , A61P3/14 , A61P9/00 , A61P9/08 , A61P9/10 , A61P25/04 , A61P25/06 , A61P25/08 , C07C213/02 , C07C217/48 , C07C255/54 , C07D317/64 , C07D521/00
CPC分类号: C07D317/64 , C07C217/48 , C07C255/54 , C07C2101/02 , C07C2102/08 , C07C2102/10
摘要: Novel aryloxyphenylpropylamines having the formula ##STR1## wherein R.sup.1 is C.sub.3-7 -cycloalkyl, C.sub.3-10 -alkyl, or alkenyl which may be straight, branched or cyclic, unsubstituted or substituted with C.sub.1-4 -alkoxy, aryloxy or cycloalkyl or cycloalkylalkyl; andR.sup.2 is 3,4-methylenedioxyphenyl, aryl or heteroaryl, which are optionally substituted with one or more cyano, halogen, C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, C.sub.1-6 -alkenyl, trifluoromethyl, C.sub.3-5 -alkylene, aryloxy or aralkoxyand a salt thereof with a pharmaceutically acceptable acid.The novel compounds are useful in the treatment of anoxia, migraine, ischemia and epilepsy.
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公开(公告)号:US5227379A
公开(公告)日:1993-07-13
申请号:US803200
申请日:1991-12-05
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: Piperidine compounds having the formula ##STR1## wherein R.sup.3 is 3,4-methylenedioxyphenyl, phenyl, or naphthyl which are optionally substituted with one or more halogen, C.sub.1-6 -alkoxy, or phenoxy, cyano, mono or poly halogenated C.sub.1-6 -alkyl, C.sub.2-6 -alkenyl, C.sub.1-6 -alkyl, or C.sub.3-5 -alkylene, R.sup.1 is straight or branched C.sub.1-8 -alkyl substituted with piperidinyl morpholinyl thiomorpholinyl dioxolanyl or tetrahydrofuranyl, which heterocyclic radical is unsubstituted or C.sub.1-6 -alkyl substituted,X is hydrogen, halogen, trifluoromethyl, hydroxy, cyano, or C.sub.1-8 -alkoxy,Y is O or S; and pharmaceutically-acceptable acid addition salts thereof.The compounds are useful in the treatment of anoxia, migraine, ischemia, and epilepsy.
摘要翻译: 具有式(1)的哌啶化合物,其中R 3是任选被一个或多个卤素,C 1-6 - 烷氧基或苯氧基,氰基,单或多卤代C1取代的3,4-亚甲二氧基苯基,苯基或萘基 C6-烷基,C2-6-烯基,C1-6 - 烷基或C3-5 - 亚烷基,R1是被哌啶基吗啉基硫代吗啉基二氧戊环基或四氢呋喃基取代的直链或支链C 1-8 - 烷基,该杂环基是未取代的或C1 6-烷基取代的,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; 及其药学上可接受的酸加成盐。 该化合物可用于治疗缺氧,偏头痛,局部缺血和癫痫。
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公开(公告)号:US5145870A
公开(公告)日:1992-09-08
申请号:US529004
申请日:1990-05-24
申请人: Palle Jakobsen , Jorgen Drejer
发明人: Palle Jakobsen , Jorgen Drejer
IPC分类号: A61K31/135 , A61K31/275 , A61K31/357 , A61K31/36 , A61P9/10 , A61P21/02 , A61P25/04 , A61P25/06 , A61P25/08 , C07C213/02 , C07C217/48 , C07C217/72 , C07C253/30 , C07C255/59 , C07D317/64 , C07D521/00
CPC分类号: C07C217/72 , C07C217/48 , C07C255/59 , C07D317/64 , C07C2101/02 , C07C2102/10
摘要: Novel aryloxyphenylpropylamines having the formula ##STR1## wherein X is H, cyano, halogen, halogenoalkyl, C.sub.1-6 -alkoxy, C.sub.1-6 -alkyl, C.sub.1-5 -alkanoyl, C.sub.3-5 -alkylene, aryloxy or aralkoxy, andR is 3,4-methylenedioxy, aryl or heteroaryl which are optionally substituted with one or more cyano, halogeno, C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, C.sub.1-6 -alkenyl, trifluoromethyl, C.sub.3-5 -alkylene, aryloxy or aralkoxy; andR.sup.1 and R.sup.2 independently is C.sub.1-10 -alkyl, C.sub.3-7 -cycloalkyl, C.sub.2-10 -alkenyl, C.sub.3-6 -cycloalkyl-C.sub.1-5 -alkyl, optionally substituted with C.sub.1-5 -alkoxy or cyano;R.sup.1 and R.sup.2 may together form a carbocyclic ring and a salt thereof with a pharmaceutically acceptable acid,provided however that R.sup.1 is not C.sub.3-7 -cycloalkyl, C.sub.1-10 -alkyl, or alkenyl which may be straight, branched or cyclic, unsubstituted or substituted with C.sub.1-4 -alkoxy, aryloxy or cycloalkyl or cycloalkylalkyl, when X is H and R.sup.2 is a methyl group.The novel compounds are useful in the treatment of anoxia, migraine, ischemia, epilepsy, traumatic injury and neurodegenerative diseases.
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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.
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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.
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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.
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