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29 条记录 (耗时 0.023 秒)

    Isatineoxime derivatives and their use
    11.
    发明授权
    Isatineoxime derivatives and their use 失效
    伊马替尼肟衍生物及其用途

    公开(公告)号：US5223527A

    公开(公告)日：1993-06-29

    申请号：US899620

    申请日：1992-06-16

    申请人： Frank Watjen ,  Jorgen Drejer ,  Leif H. Jensen

    发明人： Frank Watjen ,  Jorgen Drejer ,  Leif H. Jensen

    IPC分类号： C07D209/60

    CPC分类号： C07D209/60

    摘要： A compound having the formula ##STR1## wherein R.sup.1 is C.sub.1-6 -alkyl which may be branched or cyclic;R.sup.2 is C.sub.1-6 -alkyl which may be branched or cyclic; or wherein R.sup.1 and R.sup.2 together represent --(CH.sub.2).sub.n --, wherein n is 3, 4, 5.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R 1是可以是支链或环状的C 1-6 - 烷基; R2是可以是支链或环状的C 1-6 - 烷基; 或其中R 1和R 2一起表示 - （CH 2）n - ，其中n为3,4,5。以及治疗对谷氨酸和天冬氨酸受体的封闭反应的哺乳动物（包括人）的病症的方法，其中 相同。

    Isatine derivatives, their preparation and use
    12.
    发明授权
    Isatine derivatives, their preparation and use 失效
    伊马替尼衍生物，其制备和用途

    公开(公告)号：US5198461A

    公开(公告)日：1993-03-30

    申请号：US710790

    申请日：1991-06-05

    申请人： Frank Watjen ,  Jorgen Drejer ,  Leif H. Jensen

    发明人： Frank Watjen ,  Jorgen Drejer ,  Leif H. Jensen

    IPC分类号： C07D209/40

    CPC分类号： C07D209/40

    摘要： A method of treatment with compounds having the formula ##STR1## R.sup.1 is hydrogen, C.sub.1-6 -alkyl which may be branched, C.sub.3-7 -cycloalkyl, benzyl, phenyl which may be substituted, acyl, hydroxy, C.sub.1-6 -alkoxy, CH.sub.2 CO.sub.2 R' wherein R' is hydrogen or C.sub.1-6 -alkyl which may be branched, CH.sub.2 CN, CH.sub.2 CONR.sup.IV R.sup.V wherein R.sup.IV and R.sup.V independently are hydrogen or C.sub.1-6 -alkyl, or CH.sub.2 C(.dbd.NOH)NH.sub.2 ; R.sup.2 is hydrogen, benzyl, C.sub.1-6 -alkyl which may be branched, or C.sub.3-7 -cycloalkyl; R.sup.4, R.sup.5, R.sup.6, R.sup.7 independently are hydrogen, C.sub.1-6 -alkyl which may be branched, phenyl, halogen, C.sub.1-6 -alkoxy, NO.sub.2, CN, CF.sub.3, OCF.sub.3, or SO.sub.2 NR"R'" wherein R" and R'" independently are hydrogen, aralkoxy, aralkyl, or C.sub.1-6 -alkyl; or R.sup.6 and R.sup.7 together form an additional 4 to 7 membered ring which may be aromatic or partial saturated and which may be substituted with halogen, NO.sub.2, CF.sub.3, CN, OCF.sub.3, SO.sub.2 NR" R"' wherein R" and R"' independently are hydrogen, aralkoxy, aralkyl, or C.sub.1-6 -alkyl, and R.sup.4 and R.sup.5 have the meanings set forth above, are disclosed, as well as pharmaceutical compositions thereof. Certain of the compounds are novel.The compounds and pharmaceutical compositions containing the compounds are useful in the treatment of central nervous system disorders and especially conditions sensitive to excitatory amino acids.

    摘要翻译： 具有下式的化合物的方法是氢，可以是支链的C 1-6 - 烷基，C 3-7 - 环烷基，苄基，可被取代的苯基，酰基，羟基，C 1-6 - 烷氧基， CH2CO2R'其中R'是氢或可以是支链的C 1-6 - 烷基，CH 2 CN，CH 2 CONRIVRV其中RIV和RV独立地是氢或C 1-6 - 烷基或CH 2 C（= NOH）NH 2; R2是氢，苄基，可以是支链的C 1-6 - 烷基或C 3-7 - 环烷基; R4，R5，R6，R7独立地是氢，可以是支链的C1-6烷基，苯基，卤素，C1-6烷氧基，NO2，CN，CF3，OCF3或SO2NR''R“ '和R“独立地是氢，芳烷氧基，芳烷基或C 1-6 - 烷基; 或R6和R7一起形成另外的4至7元环，其可以是芳族或部分饱和的并且可以被卤素，NO 2，CF 3，CN，OCF 3，SO 2 NR“R”取代，其中R“和R' 独立地是氢，芳烷氧基，芳烷基或C 1-6 - 烷基，并且R 4和R 5具有上述含义，以及其药物组合物。 某些化合物是新颖的。 含有这些化合物的化合物和药物组合物可用于治疗中枢神经系统疾病，特别是对兴奋性氨基酸敏感的病症。

    Method of treating calcium overload
    14.
    发明授权
    Method of treating calcium overload 失效
    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。

    6,7-disubstituted-2,3-dihydroxyquinoxaline compounds, pharmaceutical compositions thereof, and their use as neuroleptics
    15.
    发明授权
    6,7-disubstituted-2,3-dihydroxyquinoxaline compounds, pharmaceutical compositions thereof, and their use as neuroleptics 失效
    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。

    Piperidine compounds and their preparation and use
    16.
    发明授权
    Piperidine compounds and their preparation and use 失效

    公开(公告)号：US5019582A

    公开(公告)日：1991-05-28

    申请号：US407237

    申请日：1989-09-14

    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 Sor 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.

    Piperidine compounds and pharmaceutical compositions thereof
    17.
    发明授权
    Piperidine compounds and pharmaceutical compositions thereof 失效
    哌啶化合物及其药物组合物

    公开(公告)号：US4985446A

    公开(公告)日：1991-01-15

    申请号：US486252

    申请日：1990-02-28

    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 Sor 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.

    1-(4-piperidyl)-benzimidazoles having neurotrophic activity
    19.
    发明授权
    1-(4-piperidyl)-benzimidazoles having neurotrophic activity 失效
    具有神经营养活性的1-（4-哌啶基） - 苯并咪唑

    公开(公告)号：US06180649B2

    公开(公告)日：2001-01-30

    申请号：US09171530

    申请日：1998-11-19

    申请人： Peter Moldt ,  Bjarne Hugo Dahl ,  Jorgen Drejer ,  Oskar Axelsson

    发明人： Peter Moldt ,  Bjarne Hugo Dahl ,  Jorgen Drejer ,  Oskar Axelsson

    IPC分类号： A61K31445

    CPC分类号： C07D401/04

    摘要： The present invention discloses compounds of the formula wherein the dotted bonds are optional extra bonds allowing any tautomeric isomers compatible with substituents X and R3; R3 is non-existing, hydrogen, or alkyl; X is O, S, imino, alkoxy, alkylthio, or amino; R1 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, acyl, acylalkyl, alkoxyalkyl, dialkoxyalkyl, or phenylalkyl which may be substituted with alkyl, halogen, amino, nitro or cyano; and R4, R5, R6 and R7 independently of each other are hydrogen; halogen; amino; nitro; CN; CF3; COOH; COO-alkyl; alkyl; acyl; alkoxy; —(CH2)n,—OH wherein n is 0, 1, 2, or 3; —(CH2)m—O-alkyl wherein m is 0, 1,2, or 3; —(CH2)p—O-acyl wherein p is 0, 1,2, or 3; or a pharmaceutically acceptable addition salt thereof. The compounds are useful as pharmaceuticals, for example, in the treatment of traumatic lesions of peripheral nerves, the medulla, and/or the spinal cord, cerebral ischaemic neuronal damage, neuropathy and especially peripheral neuropathy, dementia, Alzheimer's disease, Huntington's disease, Parkinson's disease, amyotrophic lateral sclerosis, or any other neurodegenerative disease.

    摘要翻译： 本发明公开了以下结构的化合物：虚线键是任选的额外键，允许与取代基X和R 3相容的任何互变异构体; R3不存在，氢或烷基; X是O，S，亚氨基，烷氧基，烷硫基或 氨基; R 1是氢，烷基，烯基，炔基，环烷基，环烷基烷基，酰基，酰基烷基，烷氧基烷基，二烷氧基烷基或可被烷基，卤素，氨基，硝基或氰基取代的苯基烷基; 和R 4，R 5，R 6和R 7彼此独立地是氢; 卤素; 氨基; 硝基; CN; CF3; COOH; COO-烷基; 烷基; 酰基; 烷氧基 - （CH 2）n，-OH，其中n为0,1,2或3; - （CH 2）m -O-烷基，其中m为0,1,2或3; - （CH 2）p -O-酰基，其中p为0,1,2或3;或其药学上可接受的加成盐。 该化合物可用作药物，例如用于治疗周围神经，髓质和/或脊髓的创伤性损伤，脑缺血性神经元损伤，神经病变，特别是周围神经病变，痴呆，阿尔茨海默病，亨廷顿病，帕金森病 疾病，肌萎缩性侧索硬化或任何其他神经变性疾病。

    Aryloxyphenylpropylamines and their calcium overload blocking compositions and methods of use
    20.
    发明授权
    Aryloxyphenylpropylamines and their calcium overload blocking compositions and methods of use 失效
    丙烯酰氧基苯基丙胺及其钙超载阻断组合物及其使用方法

    公开(公告)号：US5310756A

    公开(公告)日：1994-05-10

    申请号：US898060

    申请日：1992-06-12

    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 ,  C07C255/50

    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- -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; orR.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 neurode-generative diseases.

    摘要翻译： 具有式（I）的新型芳氧基苯基丙胺其中X为H，氰基，卤素，卤代烷基，C 1-6 - 烷氧基，C 1 - 烷基，C 1-5 - 烷酰基，C 3-5 - 亚烷基，芳氧基或芳烷氧基， R 3为任选被一个或多个氰基，卤代C 1-6烷基，C 1-6 - 烷氧基，C 1-6 - 烯基，三氟甲基，C 3-5 - 亚烷基， 芳氧基或芳烷氧基; 且R 1和R 2独立地为C 1-10 - 烷基，C 3-7 - 环烷基，C 2-10 - 烯基，C 3-6 - 环烷基-C 1-5 - 烷基，任选被C 1-5 - 烷氧基或氰基取代; 或者R 1和R 2可以与药学上可接受的酸一起形成碳环和其盐，条件是R 1不是C 3-7 - 环烷基，可以是直链，支链或环状的C 1-10 - 烷基或链烯基，未取代的 或被C 1-4 - 烷氧基，芳氧基或环烷基或环烷基烷基取代，当X为H且R 2为甲基时。 新型化合物可用于治疗缺氧，偏头痛，局部缺血，癫痫，创伤性损伤和神经发生疾病。