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65 条记录 (耗时 0.028 秒)

    Isatinoxime derivatives, their preparation and use
    12.
    发明授权
    Isatinoxime 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：US5242918A

    公开(公告)日：1993-09-07

    申请号：US936579

    申请日：1992-08-27

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

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

    IPC分类号： C07C205/45 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04

    CPC分类号： C07D471/04 ,  C07C205/45 ,  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 straight, C.sub.1-6 -alkyl which may be branched or cyclic,R.sup.2 is hydrogen or straight, 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 --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;Q is NOH or O;Z=O, S, N--R.sup.II, ##STR2## wherein R.sup.II, R.sup.III, R.sup.IV and R.sup.V independently are hydrogen, benzyl, 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 branched or cyclic;X is --(CH.sub.2).sub.o -- wherein o is 0, 1, 2, or 3;Y is --(CH.sub.2).sub.p -- wherein p is 0, 1, 2 or 3;.alpha. and .beta. indicate attachment points,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 4和R 5独立地是氢，卤素，CF 3，CN，NO 2或SO 2 NR 1 R 2，其中R 1是氢或直链，可以是支链或环状的C 1-6 - 烷基，R 2是氢或直链， 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）nA-（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; Q是NOH或O; Z = O，S，N-RII，其中RII，RIII，RIV和RV独立地是氢，苄基，C1-6羧酸 - 酰基，可以是支链或环状的C1-6 - 烷氧基或C1-6 可以是支链或环状的 - 烷基; X是 - （CH 2）o - ，其中o是0,1,2或3; Y是 - （CH 2）p - ，其中p是0,1,2或3; α和β表示连接点，以及一种治疗对谷氨酸和天冬氨酸受体的封闭有反应的哺乳动物（包括人）的病症的方法。

    Imidazoquinoxaline compounds and their preparation and use
    13.
    发明授权
    Imidazoquinoxaline compounds and their preparation and use 失效
    咪唑啉酮化合物及其制备和使用

    公开(公告)号：US5075304A

    公开(公告)日：1991-12-24

    申请号：US353793

    申请日：1989-05-18

    申请人： Holger C. Hansen ,  Frank Watjen

    发明人： Holger C. Hansen ,  Frank Watjen

    IPC分类号： A61K31/495 ,  A61P25/00 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： New imidazoquinoxaline compounds having the general formula ##STR1## wherein R.sup.3 is ##STR2## or CO.sub.2 R' wherein R' isC.sub.3-7 -cycloalkyl;R.sup.5 is methyl, which is substituted with hydrogen, alkoxycarbonyl, heteroaryl, morpholino, C.sub.3-7 -cycloalkyl, C.sub.1-6 -alkenyl, arylacyl, alkylacyl, alkoxyalkyl, alkoxy, phthalimidophenyl, aralkyl or aryl, all of which are substituted with hydrogen, halogen, C.sub.1-6 -alkyl, amino, azido, or C.sub.1-6 -alkoxy;and R.sup.6 is H, C.sub.1-6 -alkyl, halogen, or CF.sub.3.The compounds are useful in psychopharmaceutical preparations as anticonvulsants, anxiolytics, hypnotics, and in improving the cognitive function of the brain of mammals.

    Piperidine derivatives as neurotransmitter re-uptake inhibitors
    17.
    发明授权
    Piperidine derivatives as neurotransmitter re-uptake inhibitors 失效
    哌啶衍生物作为神经递质再摄取抑制剂

    公开(公告)号：US06376673B1

    公开(公告)日：2002-04-23

    申请号：US09415227

    申请日：1999-10-12

    申请人： Peter Moldt ,  Frank Watjen ,  Jorgen Scheel-Kruger

    发明人： Peter Moldt ,  Frank Watjen ,  Jorgen Scheel-Kruger

    IPC分类号： C07D21118

    CPC分类号： C07D211/28

    摘要： The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salt thereof; wherein R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl or 2-hydroxyethyl; R3 is —CR′═NOR″ wherein R′ and R″ each independently are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, cycloalkylalkenyl, alkynyl, cycloalkylalkynyl, aryl or benzyl; R4 is phenyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, amino, nitro, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, aryl and heteroaryl; 3,4-methylenedioxyphenyl; benzyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, amino, nitro, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, aryl and heteroaryl; heteroaryl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, amino, nitro, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, aryl and heteroaryl; or naphthyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, amino, nitro, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, aryl and heteroaryl. The compounds possess valuable pharmaceutical properties as monoamine neurotransmitter, i.e. dopamine, serotonin, noradrenaline, reuptake inhibitors.

    摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐; 其中R是氢，烷基，烯基，炔基，环烷基，环烷基烷基或2-羟乙基; R3是-CR'= NOR“，其中R'和R”各自独立地为氢，烷基，环烷基，环烷基烷基，烯基，环烷基烯基，炔基，环烷基炔基，芳基或苄基; R4是可以被选自卤素，CF 3，CN，氨基，硝基，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，芳基和杂芳基的取代基取代一次或多次的苯基; 3,4-亚甲二氧基苯基; 苄基，其可以被选自卤素，CF 3，CN，氨基，硝基，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，芳基和杂芳基的取代基取代一次或多次; 可以被选自卤素，CF 3，CN，氨基，硝基，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，芳基和杂芳基的取代基取代一次或多次的杂芳基; 或萘基，其可以被选自卤素，CF 3，CN，氨基，硝基，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，芳基和杂芳基的取代基取代一次或多次。 该化合物具有作为单胺神经递质（即多巴胺，5-羟色胺，去甲肾上腺素，再摄取抑制剂）的有价值的药物性质。

    Indole-2,3-dione-3-oxime derivatives
    18.
    发明授权
    Indole-2,3-dione-3-oxime derivatives 失效
    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。

    Isatineoxime derivatives, their preparation and use
    19.
    发明授权
    Isatineoxime derivatives, their preparation and use 失效
    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。

    Benzimidazole derivatives, their preparation and use
    20.
    发明授权
    Benzimidazole derivatives, their preparation and use 失效
    苯并咪唑衍生物，其制备和用途

    公开(公告)号：US5200422A

    公开(公告)日：1993-04-06

    申请号：US731412

    申请日：1991-07-17

    申请人： Soren-Peter Olesen ,  Frank Watjen

    发明人： Soren-Peter Olesen ,  Frank Watjen

    IPC分类号： C07D235/26 ,  C07D235/28 ,  C07D235/30

    CPC分类号： C07D235/28 ,  C07D235/26 ,  C07D235/30

    摘要： A compound having the formula ##STR1## wherein R.sup.1 is hydrogen, NH.sub.2 or C.sub.1-6 -alkyl which may be branched;X is O, S, NCN;Y is O, S;R.sup.4, R.sup.5, R.sup.6 and R.sup.7 independently of each other are hydrogen, halogen, CF.sub.3, NO.sub.2, NH.sub.2, OH, C.sub.1-6 -alkoxy, C(.dbd.O)-phenyl or SO.sub.2 NR.sup.I R.sup.II wherein R.sup.I and R.sup.II independently are hydrogen or C.sub.1-6 -alkyl;R.sup.11 is hydrogen, halogen, NO.sub.2 or SO.sub.2 NR'R" wherein R' and R" independently are hydrogen or C.sub.1-6 -alkyl;R.sup.13 is hydrogen, halogen, phenyl, CF.sub.3, NO.sub.2 ;R.sup.12 is hydrogen or together with R.sup.13 forms a C.sub.4-7 -carbocyclic ring which may be aromatic or partially saturated;R.sup.14 is hydrogen or together with R.sup.13 forms a C.sub.4-7 -carbocyclic ring which may be aromatic or partially saturated;pharmaceutical compositions thereof,and a method of treating a disease in a mammal, including a human, responsive to opening of potassium channels, which comprises administering to a mammal in need thereof an effective amount of a compound as first above indicated, are disclosed.

    摘要翻译： 具有式“IMAGE”的化合物，其中R 1是氢，NH 2或可以是支链的C 1-6 - 烷基; X为O，S，NCN; Y是O，S; R4，R5，R6和R7彼此独立地是氢，卤素，CF3，NO2，NH2，OH，C1-6 - 烷氧基，C（= O） - 苯基或SO2NRIRII，其中RI和RII独立地是氢或C1-6 -烷基; R11是氢，卤素，NO2或SO2NR'R“，其中R'和R”独立地是氢或C1-6烷基; R 13是氢，卤素，苯基，CF 3，NO 2; R 12是氢或与R 13一起形成可以是芳族或部分饱和的C 4-7 - 碳环; R 14是氢或与R 13一起形成可以是芳族或部分饱和的C 4-7 - 碳环; 其药物组合物，以及治疗包括人的哺乳动物（包括人）在开放钾通道中的疾病的方法，该方法包括对有需要的哺乳动物施用有效量的如上所述的化合物。