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25 条记录 (耗时 0.085 秒)

    2,3-benzodiazepine derivatives and their use as AMPA-receptor inhibitors
    6.
    发明授权
    2,3-benzodiazepine derivatives and their use as AMPA-receptor inhibitors 失效
    2,3-苯并二氮杂衍生物及其作为AMPA受体抑制剂的用途

    公开(公告)号：US06200970B1

    公开(公告)日：2001-03-13

    申请号：US09125008

    申请日：1998-11-05

    申请人： István Ling ,  Gizella Ábrahám ,  Sándor Sólyom ,  Tamás Hámori ,  István Tarnawa ,  Pál Berzsenyi ,  Ferenc Andrási ,  Emese Csuzdi ,  Márta Szöllósy ,  Antal Simay ,  István Lagi ,  Katalin Horváth

    发明人： István Ling ,  Gizella Ábrahám ,  Sándor Sólyom ,  Tamás Hámori ,  István Tarnawa ,  Pál Berzsenyi ,  Ferenc Andrási ,  Emese Csuzdi ,  Márta Szöllósy ,  Antal Simay ,  István Lagi ,  Katalin Horváth

    IPC分类号： A61K31551

    CPC分类号： C07D243/02

    摘要： A compound of formula I in which X means hydrogen or halogen, Y means —NR3— or —N═, R1 and R2 are the same or different and mean hydrogen, C1-C6 alkyl, nitro, halogen, the group —NR8R9, —O—C1-4 alkyl, —CF3, OH or C1-6 alkanoyloxy, R3 means hydrogen, the group —CO—R10, C1-6 alkyl or C3-7 cycloalkyl, R4 means optionally substituted C1-C6 alkyl, R5 means hydrogen or R4 and R5 together mean oxygen, R6 means C1-4 alkyl, R8 and R9 are the same or different and mean hydrogen, C1-C6 alkyl or —CO—C1-6 alkyl, R10 means hydrogen, optionally substituted C1-C6 alkyl, optionally substituted C6-10 aryl, the group —NR11R12, —O—C1-6 alkyl, C3-7 cycloalkyl, C2-6 alkenyl or —O—C3-7 cycloalkyl, R11 and R12 are the same or different and mean hydrogen, optionally substituted C1-C6 alkyl or optionally substituted C6-10 aryl and —C...C... means a double bond or single bonds or an isomer or physiologically compatible salt thereof with the proviso that the compound is not 1-(3-chlorophenyl)-4-methyl-8-methoxy, 5H-2,3-benzodiazepine.

    摘要翻译： 式Iin化合物，其中X表示氢或卤素，Y表示-NR3-或-N =，R1和R2相同或不同，表示氢，C1-C6烷基，硝基，卤素，-NR8R9基，-O- C 1-4烷基，-CF 3，OH或C 1-6烷酰氧基，R 3表示氢，-CO-R 10，C 1-6烷基或C 3-7环烷基，R 4表示任选取代的C 1 -C 6烷基，R 5表示氢或R 4， R5一起表示氧，R6表示C1-4烷基，R8和R9相同或不同，表示氢，C1-C6烷基或-CO-C1-6烷基，R10表示氢，任选取代的C 1 -C 6烷基，任选取代 C6-10芳基，基团-NR11R12，-O-C1-6烷基，C3-7环烷基，C2-6烯基或-O-C3-7环烷基，R11和R12相同或不同，表示氢，任选取代 C 1 -C 6烷基或任选取代的C 6-10芳基和C 1 -C 6表示双键或单键，其是异构体或其生理上相容的盐，条件是所述化合物不是1-（3-氯苯基） -4-甲基-8-甲氧基，5H-2,3-苯并二苯基 氮杂

    Process for preparing substituted urea derivatives
    8.
    发明授权
    Process for preparing substituted urea derivatives 失效
    制备取代脲衍生物的方法

    公开(公告)号：US4435567A

    公开(公告)日：1984-03-06

    申请号：US334470

    申请日：1981-12-28

    申请人： Gyorgy Lugosi ,  Antal Simay ,  Janos Bodnar ,  Laszlo Simandi ,  Eva Somfai

    发明人： Gyorgy Lugosi ,  Antal Simay ,  Janos Bodnar ,  Laszlo Simandi ,  Eva Somfai

    IPC分类号： C07D295/20 ,  C07C67/00 ,  C07C239/00 ,  C07C273/18 ,  C07C275/02 ,  C07C275/06 ,  C07C275/26 ,  C07C275/28 ,  C07C275/30 ,  C07C275/34 ,  C07D213/75 ,  C07D217/06 ,  C07D235/32 ,  C07D275/06 ,  C07D277/82 ,  C07D285/12 ,  C07D285/135 ,  C07D295/215 ,  C07C127/00 ,  C07C127/15 ,  C07C127/17 ,  C07C127/19

    CPC分类号： C07D213/75 ,  C07C273/1809 ,  C07D217/06 ,  C07D235/32 ,  C07D277/82 ,  C07D285/135 ,  C07D295/215

    摘要： A process for the preparation of substituted urea derivatives, and compositions and concentrates for the same purpose are disclosed. According to the process the substituted urea derivatives of formula (I) ##STR1## wherein R is hydrogen, alkyl, aryl, cycloalkyl or aralkyl, R.sup.1 and R.sup.2 are hydrogen, alkyl, alkenyl, alkinyl, alkoxy, oxyalkyl, cycloalkyl, aralkyl, alkoxycarbonylalkyl, aryl or heteroaryl, or R.sup.1 and R.sup.2 together with the adjacent nitrogen atom may form a saturated or unsaturated heterocycle, or a condensed and/or substituted ring system, and said heterocycle or said condensed and/or substituted ring system may contain also a sulfo group,can be manufactured by reacting an amine of formula (II) ##STR2## with an N-carbamoyl-benzoic acid sulfimide derivative of formula (III) ##STR3## The disclosed N-acylating composition comprises of from 3 to 60% by weight, preferably of from 5 to 50% by weight sulfimide derivative of formula (III), of from 97 to 40% by weight, preferably of from 95 to 50% by weight solvent, and if desired, an organic or inorganic base.The disclosed N-acylating concentrate comprises of from 60 to 95.5% by weight N-acylating agent of formula (III) and of from 4.5 to 40% by weight additives.

    摘要翻译： 公开了用于制备取代的脲衍生物的方法，以及用于相同目的的组合物和浓缩物。 根据该方法，式（I）的取代脲衍生物其中R是氢，烷基，芳基，环烷基或芳烷基，R1和R2是氢，烷基，烯基，炔基，烷氧基，烷氧基，环烷基，芳烷基，烷氧基羰基 ，芳基或杂芳基，或R 1和R 2与相邻的氮原子一起可以形成饱和或不饱和的杂环或稠合和/或取代的环系，并且所述杂环或所述缩合和/或取代的环系可以含有磺基 可以通过使式（II）的胺与式（III）的N-氨基甲酰基 - 苯甲酸硫酰亚胺衍生物反应来制备。所公开的N-酰化组合物包含3至60重量％ ，优选为5至50重量％的式（III）的亚磺酰亚胺衍生物，为97至40重量％，优选为95至50重量％的溶剂，如果需要，为有机或无机碱。 所公开的N-酰化浓缩物包含60至95.5重量％的式（III）的N-酰化剂和4.5至40重量％的添加剂。

    Psychostimulant agent
    10.
    发明授权
    Psychostimulant agent 失效
    精神刺激剂

    公开(公告)号：US5220068A

    公开(公告)日：1993-06-15

    申请号：US649239

    申请日：1991-01-29

    申请人： Jozsef Knoll ,  Antal Simay ,  Eva Szinnyei ,  Eva Somfai ,  Zoltan Torok ,  Karoly Mozsolits ,  Janos Bergmann

    发明人： Jozsef Knoll ,  Antal Simay ,  Eva Szinnyei ,  Eva Somfai ,  Zoltan Torok ,  Karoly Mozsolits ,  Janos Bergmann

    IPC分类号： A61K31/135

    CPC分类号： A61K31/135

    摘要： The present invention relates to a pharmaceutical composition comprising as active ingredient a compound of the Formula I ##STR1## wherein R.sup.1 stands for straight or branched chain alkyl comprising 1 to 8 carbon atoms; phenyl alkyl having 7 to 10 carbon atoms; phenyl; or cycloalkyl comprising 3 to 8 carbon atoms;R.sup.2 stands for straight or branched chain alkyl comprising 1 to 8 carbon atoms; alkyl comprising 1 to 8 carbon atoms substituted by halogen, hydroxy, alkoxy having 1 to 4 carbon atoms or by one or two phenyl groups; phenyl; or cycloalkyl having 3 to 8 carbon atoms,with the proviso that groups R.sup.1 and R.sup.2 together contain at least three carbon atoms. The invention also relates to a process for the preparation of compounds of the Formula I by methods known per se. The compounds of the Formula I are phychostimulants having a new spectrum of effect which can be used in therapy for increasing psychical activity (learning and retention) and for treating clinical patterns of depression and deficiencies of learning and retention like in Alzheimer's disease, and are void of side effects (e.g. due to catecholamine release) of known stimulants.

    摘要翻译： 本发明涉及包含作为活性成分的式I化合物（I）的药物组合物，其中R1代表包含1至8个碳原子的直链或支链烷基; 具有7至10个碳原子的苯基烷基; 苯基; 或包含3至8个碳原子的环烷基; R2代表包含1至8个碳原子的直链或支链烷基; 被卤素，羟基，具有1至4个碳原子的烷氧基或一个或两个苯基取代的碳原子数为1〜8的烷基; 苯基; 或具有3至8个碳原子的环烷基，条件是基团R 1和R 2一起含有至少3个碳原子。 本发明还涉及通过本身已知的方法制备式I化合物的方法。 式I的化合物是具有新的效应谱的phychostimulants，其可用于增加心理活动（学习和保留）的治疗和用于治疗抑郁症的临床模式和学习和保留的缺陷，如阿尔茨海默病，并且是无效的 的已知兴奋剂的副作用（例如由于儿茶酚胺释放）。