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65 条记录 (耗时 0.021 秒)

    Indole-2,3-dione-3-oxime derivatives
    41.
    再颁专利
    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：USRE38200E1

    公开(公告)日：2003-07-22

    申请号：US09956892

    申请日：2001-09-21

    申请人： Frank Watjen ,  Jorgen Drejer

    发明人： Frank Watjen ,  Jorgen Drejer

    IPC分类号： A61K315375

    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 R3 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 R31, R32, and R33 independendy represents hydrogen, alkyl, or hydroxyalkyl, and at least one of R31, R32, and R33 independently represents (CH2)nR34; wherein R34 represents hydroxy, carboxy, alkoxycarbonyl, alkenyloxycarbonyl, alkynyloxycarbonyl, cycloalkoxycarbonyl, cycloalkylalkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, CONR35R36, or “Het”; wherein n is 0, 1, 2, or 3; and R5 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-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-CH2—NR6—CH2—CH2—CH2-b; a-CH2—CH2—NR6—CH2—CH2-b; a-CH2—CH2—CH2—NR6—CH2-b; or a-CH2—CH2—CH2—CH2—NR6-b; wherein R6 represents hydrogen alkyl or CH2CH2OH; or a pharmaceutically acceptable salt thereof.

    摘要翻译： 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＆mdas

    Imidazoquinoxaline compounds and their use
    44.
    发明授权
    Imidazoquinoxaline compounds and their use 失效
    咪唑啉酮化合物及其用途

    公开(公告)号：US5102885A

    公开(公告)日：1992-04-07

    申请号：US616136

    申请日：1990-11-20

    申请人： Frank Watjen ,  Holger C. Hansen

    发明人： Frank Watjen ,  Holger C. Hansen

    IPC分类号： A61K31/495 ,  A61P25/00 ,  A61P25/08 ,  A61P25/20 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： New imidazoquinoxaline compounds having the general formula I ##STR1## wherein R.sup.1 and R.sup.2 independently are hydrogen, straight or branched C.sub.1-6 -alkyl, or C.sub.3-7 -cycloalkyl; R.sup.3 is hydrogen, straight or branched C.sub.1-6 -alkyl, straight or branched C.sub.2-6 -alkenyl, or aralkyl or aroylalkyl which may optionally be substituted with halogen or C.sub.1-6 -alkoxy; R.sup.4 and R.sup.5 independently are hydrogen, halogen, C.sub.1-6 -alkyl or trifluoromethyl.The compounds are useful in psychopharmaceutical preparations as anticonvolusants, anxiolytics, hypnotics and in improving the cognitive function of the brain of mammals.

    摘要翻译： 具有通式I（I）的新的咪唑并喹喔啉化合物，其中R 1和R 2独立地是氢，直链或支链C 1-6 - 烷基或C 3-7 - 环烷基; R 3是氢，可以任选被卤素或C 1-6 - 烷氧基取代的直链或支链C 1-6 - 烷基，直链或支链C 2-6 - 烯基或芳烷基或芳酰基烷基; R4和R5独立地是氢，卤素，C1-6烷基或三氟甲基。 这些化合物可用于精神药物制剂，如抗肿瘤剂，抗焦虑药，催眠药和改善哺乳动物脑部认知功能。

    Lipophillically-substituted piperidine oxadiazolyl compounds and their use in stimulating cognitive functions
    46.
    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。

    Oxadiazolyl intermediates
    50.
    发明授权
    Oxadiazolyl intermediates 失效
    恶二唑基中间体

    公开(公告)号：US4727153A

    公开(公告)日：1988-02-23

    申请号：US942200

    申请日：1986-12-16

    申请人： Frank Watjen ,  Mogens Engelstoft

    发明人： Frank Watjen ,  Mogens Engelstoft

    IPC分类号： C07D20060101 ,  C07D271/06 ,  C07D487/04 ,  C07D487/14

    CPC分类号： C07D271/06 ,  C07D487/04 ,  C07D487/14

    摘要： New oxadiazolyl imidazobenzodiazepine derivatives having the formula ##STR1## wherein R.sup.3 has the formula ##STR2## wherein R" is hydrogen, C.sub.1-6 alkyl C.sub.1-6 alkoxymethyl or C.sub.3-6 -cycloalkyl;R.sup.4 is hydrogen;R.sup.5 is C.sub.1-6 alkyl or R.sup.4 and R.sup.5 together form a 2-4 membered alkylene bridge; and R.sup.A is C.sub.1-6 alkyl, C.sub.1-6 alkoxy, or C.sub.1-3 trifluoroalkyl, pharmaceutical compositions thereof, and method of treating therewith, are disclosed.The compounds and pharmaceutical compositions are useful in the amelioration, mitigation, or elimination of central nervous system disorders related to benzodiazepine receptors and especially as anticonvulsants, anxiolytics, hypnotics, and nootropics.