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    Lipophillically-substituted piperidine oxadiazolyl compounds and their use in stimulating cognitive functions
    4.
    发明授权
    Lipophillically-substituted piperidine oxadiazolyl compounds and their use in stimulating cognitive functions 失效
    亲油取代的哌啶恶二唑基化合物及其在刺激认知功能中的用途

    公开(公告)号：US4837241A

    公开(公告)日：1989-06-06

    申请号：US89747

    申请日：1987-08-26

    申请人： Leif H. Jensen ,  Per Sauerberg ,  Frank Watjen ,  Jens W. Kindtler

    发明人： Leif H. Jensen ,  Per Sauerberg ,  Frank Watjen ,  Jens W. Kindtler

    IPC分类号： A61K31/445 ,  A61K31/44 ,  A61P25/02 ,  A61P25/28 ,  C07D413/04 ,  C07D413/14 ,  G01N21/90

    CPC分类号： C07D413/04 ,  C07D413/14

    摘要： New piperidine compounds having the formula ##STR1## wherein at least one of R.sup.3, R.sup.4, and R.sup.5 are ##STR2## and the other independently are H, C.sub.1-6 -alkyl, wherein R' is H, C.sub.1-8 -alkyl, phenyl, thienyl, cyclopropyl, or C.sub.1-3 -alkoxymethyl; and R.sup.1 and R.sup.6 independently are H or C.sub.1-6 -alkyl, and wherein ##STR3## and salts thereof with pharmaceutically-acceptable acids. The new compounds are useful in improving the cognitive functions of the forebrain and hippocampus of mammals, and are therefore useful in the treatment of Alzheimer's disease.

    摘要翻译： 具有式“IMAGE”的新的哌啶化合物，其中R 3，R 4和R 5中的至少一个是H，并且另外独立地是H，C 1-6 - 烷基，其中R'是H，C 1-8 - 烷基，苯基 ，噻吩基，环丙基或C 1-3 - 烷氧基甲基; 并且R 1和R 6独立地为H或C 1-6 - 烷基，并且其中其与药学上可接受的酸形成。 新化合物可用于改善哺乳动物前脑和海马的认知功能，因此可用于治疗阿尔茨海默氏病。

    Benzimidazole derivatives and pharmaceutical compositions comprising these compounds
    5.
    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。

    AMPA antagonists and a method of treatment
    6.
    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
    7.
    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）

    Isatinoxime derivatives, their preparation and use
    9.
    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
    10.
    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.