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    Benzimidazole derivatives and pharmaceutical compositions comprising these compounds
    1.
    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。

    1-phenyl-benzimidazole compounds and their use as GABA-a receptor modulators
    5.
    发明授权
    1-phenyl-benzimidazole compounds and their use as GABA-a receptor modulators 失效
    1-苯基 - 苯并咪唑化合物及其作为GABA-a受体调节剂的用途

    公开(公告)号：US06218547B1

    公开(公告)日：2001-04-17

    申请号：US09269643

    申请日：1999-03-31

    申请人： Lene Teuber ,  Frank Watjen

    发明人： Lene Teuber ,  Frank Watjen

    IPC分类号： C07D23502

    CPC分类号： C07D235/06 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D413/04

    摘要： The present invention relates to novel benzimidazole compounds, represented by general formula (I) in which o is 0, 1, 2 or 3; R1 represents an alkyl group, a phenyl group, or a monocyclic heterocyclic group, which groups may be substituted one or more times with substituents selected from alkyl, cycloalkyl, cycloalkyl-alkyl, alkoxy, halogen, trifluoromethyl, cyano, amino and nitro; or R1 represents a cyano group or a group of the formula -alkyl-CO2R2, alkenyl-CO2R2, —CO—R2, —CO2(CH2)mR2, or —C(R3)═N—OR2, R11 represents a group of formula —CO2—R9, or R11 represents a group of general formula (II) in which n is 0, 1, 2 or 3; or R11 may represent a group of general formula (III), in which n is 0, 1, 2 or 3; the novel compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, such as for example anxiety, sleep disorders, anaestesia, memory disorders, and epilepsia or other convulsive disorders.

    摘要翻译： 本发明涉及由通式（I）表示的新的苯并咪唑化合物，其中o为0,1,2或3; R1表示烷基，苯基或单环杂环基，该基团可以被选自烷基，环烷基，环烷基 - 烷基，烷氧基，卤素，三氟甲基，氰基，氨基和硝基的取代基取代一次或多次; 或R 1表示氰基或式 - 烷基-CO 2 R 2，烯基-CO 2 R 2，-CO-R 2，-CO 2（CH 2）m R 2或-C（R 3）= N-OR 2的基团，R 11表示式 -CO 2 -R 9或R 11表示其中n为0,1,2或3的通式（II）的基团; 或R 11可以表示通式（III）的基团，其中n为0,1,2或3; 本发明的新化合物可用于治疗对GABA A受体复合物调节有反应的中枢神经系统疾病和病症，例如焦虑症，睡眠障碍，麻醉，记忆障碍和癫痫或其它惊厥性疾病 。

    AMPA antagonists and a method of treatment
    9.
    发明授权
    AMPA antagonists and a method of treatment 失效
    AMPA拮抗剂和治疗方法

    公开(公告)号：US5843945A

    公开(公告)日：1998-12-01

    申请号：US951059

    申请日：1997-10-15

    申请人： Frank Watjen ,  Jorgen Drejer

    发明人： Frank Watjen ,  Jorgen Drejer

    IPC分类号： C07D471/04 ,  C07D487/04 ,  A61K31/55 ,  A61K31/495 ,  C07D487/00

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： The present patent application discloses compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein R.sup.1 is hydrogen, alkyl or benzyl; X is O or NOR.sup.2, wherein R.sup.2 is hydrogen, alkyl or benzyl; Y is N--R.sup.4 wherein R.sup.4 is hydrogen, OH or alkyl; n is 0 or 1; R.sup.6 is phenyl, naphthyl, thienyl, pyridyl, all of which may be substituted one or more times with substituents selected from the group consisting of halogen, CF.sub.3, NO.sub.2, amino, alkyl, alkoxy and phenyl; A is a ring of five to seven atoms fused with the benzo ring at the positions marked a and b. The compounds are useful in the treatment of cerebrovascular disorders. ##STR1##

    摘要翻译： 本专利申请公开了具有式（I）的化合物或其药学上可接受的盐，其中R 1是氢，烷基或苄基; X是O或NOR2，其中R2是氢，烷基或苄基; Y是N-R4，其中R4是氢，OH或烷基; n为0或1; R6是苯基，萘基，噻吩基，吡啶基，它们都可以被选自卤素，CF 3，NO 2，氨基，烷基，烷氧基和苯基的取代基取代一次或多次; A是在标记a和b的位置与苯环稠合的5至7个原子的环。 该化合物可用于治疗脑血管障碍。

    AMPA antagonists and method of treatment therewith
    10.
    发明授权
    AMPA antagonists and method of treatment therewith 失效
    AMPA拮抗剂及其治疗方法

    公开(公告)号：US5780493A

    公开(公告)日：1998-07-14

    申请号：US951821

    申请日：1997-10-16

    申请人： Frank Watjen ,  Jorgen Drejer

    发明人： Frank Watjen ,  Jorgen Drejer

    IPC分类号： C07D471/04 ,  C07D487/04 ,  A61K31/40 ,  A61K31/44 ,  C07D401/00 ,  C07D487/02

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： The present patent application discloses compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein R.sup.1 is hydrogen, alkyl or benzyl; X is O or NOR.sup.2, wherein R.sup.2 is hydrogen, alkyl or benzyl; Y is N--R.sup.4 wherein R.sup.4 is hydrogen, OH or alkyl; n is 0 or 1; R.sup.6 is phenyl, naphthyl, thienyl, pyridyl, all of which may be substituted one or more times with substituents selected from the group consisting of halogen; CF.sub.3, NO.sub.2, amino, alkyl, alkoxy and phenyl; A is a ring of five to seven atoms fused with the benzo ring at the positions marked a and b. The compounds are useful in the treatment of cerebrovascular disorders for example. ##STR1##

    摘要翻译： 本专利申请公开了具有式（I）的化合物或其药学上可接受的盐，其中R 1是氢，烷基或苄基; X是O或NOR2，其中R2是氢，烷基或苄基; Y是N-R4，其中R4是氢，OH或烷基; n为0或1; R6是苯基，萘基，噻吩基，吡啶基，它们都可以被选自卤素的取代基取代一次或多次; CF 3，NO 2，氨基，烷基，烷氧基和苯基; A是在标记a和b的位置与苯环稠合的5至7个原子的环。 该化合物可用于治疗例如脑血管障碍。 （一）