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65 条记录 (耗时 0.026 秒)

    Benzimidazole derivatives and pharmaceutical compositions comprising these compounds
    23.
    发明授权
    Benzimidazole derivatives and pharmaceutical compositions comprising these compounds 失效
    苯并咪唑衍生物和包含这些化合物的药物组合物

    公开(公告)号：US06649609B2

    公开(公告)日：2003-11-18

    申请号：US10012490

    申请日：2001-12-12

    申请人： Lene Teuber ,  Frank Watjen

    发明人： Lene Teuber ,  Frank Watjen

    IPC分类号： C07D23506

    CPC分类号： C07D235/06 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/10 ,  C07D401/12 ,  C07D403/10 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14

    摘要： The present invention relates to novel 1-phenylbenzimidazole derivatives having particular alkoxycarbonyl substituents in the 5-position of the benz ring and having particular cyclic substituents in the meta-position of the phenyl ring, as well as to pharmaceutical compositions containing these compounds and to methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of GABAA receptor complex, and in particular for inducing and maintaining anaesthesia, sedation, and muscle relaxation, as well as for combating febrile convulsions in children. The compounds of the invention may also be used by veterinarians.

    摘要翻译： 本发明涉及在苯环的5-位上具有特定的烷氧基羰基取代基并且在苯环的间位具有特定的环状取代基的新的1-苯基苯并咪唑衍生物以及含有这些化合物的药物组合物和方法 的治疗。 本发明的化合物可用于治疗中枢神经系统疾病和病症，其对GABAα受体复合物的调节有反应，特别是诱导和维持麻醉，镇静和肌肉松弛以及对于 打击儿童发热性惊厥。 本发明的化合物也可以由兽医使用。

    Imidazoquinoxaline compounds and their preparation and use
    25.
    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
    27.
    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。

    Benzimidazole derivatives, their preparation and use
    30.
    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。