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23 条记录 (耗时 0.037 秒)

    Spiro derivatives of the pyrazolo [1,5-d] [1,2,4] triazine ring system and a process for the preparation thereof
    14.
    发明授权
    Spiro derivatives of the pyrazolo [1,5-d] [1,2,4] triazine ring system and a process for the preparation thereof 失效
    吡唑并[1,5-d] [1,2,4]三嗪环系的螺衍生物及其制备方法

    公开(公告)号：US4469692A

    公开(公告)日：1984-09-04

    申请号：US442451

    申请日：1982-11-17

    申请人： Endre Tihanyi ,  Ferenc Andrasi ,  Melinda Gal ,  Eleonora Sineger

    发明人： Endre Tihanyi ,  Ferenc Andrasi ,  Melinda Gal ,  Eleonora Sineger

    IPC分类号： C07D487/04 ,  A61K31/4162 ,  A61K31/4196 ,  A61K31/53 ,  A61P25/20 ,  A61P41/00 ,  C07D487/10 ,  A61K31/415

    CPC分类号： C07D487/10

    摘要： A spiro derivative of the pyrazolo [1,5-d] [1,2,4] triazine ring system of the formula I ##STR1## wherein R.sub.1 and R.sub.2 represent, independently from each other, a hydrogen atom or a C.sub.1-4 alkyl group,R.sub.3 stands for a hydrogen atom, an unbranched or branched C.sub.1-4 alkyl, C.sub.2-5 alkenyl or benzyl group,R.sub.4 represents a hydrogen atom, an unbranched or branched C.sub.1-4 alkyl, C.sub.4-6 cycloalkyl, an unsubstituted or mono-halo or polyhalo benzyl group, andn is a whole number from 4 to 8,wherein R stands for an unbranched or branched C.sub.1-4 alkyl, or C.sub.4-6 cycloalkyl, C.sub.2-5 alkenyl, an unsubstituted or a monohalogeno or polyhalogenobenzyl group, and X represents a halogen or a 4-methyl-phenylsulfonyloxy group. Compounds of the formula I exhibit valuable CNS activities.

    摘要翻译： 式I的吡唑并[1,5-d] [1,2,4]三嗪环系的螺衍生物其中R 1和R 2彼此独立地表示氢原子或C 1-4 烷基，R3表示氢原子，无支链或支链C 1-4烷基，C 2-5烯基或苄基，R 4表示氢原子，无支链或支链C 1-4烷基，C 4-6环烷基，未取代或未取代的 单卤素或多卤代苄基，n为4至8的整数，其中R代表无支链或支链C 1-4烷基或C 4-6环烷基，C 2-5链烯基，未取代或单卤素或多卤代苄基 基团，X表示卤素或4-甲基 - 苯基磺酰氧基。 式I的化合物显示出有价值的CNS活性。

    Anorexigenic 4-[(3,4-dialkoxyphenyl)alkyl]-2-imidazolidinone derivatives
    19.
    发明授权
    Anorexigenic 4-[(3,4-dialkoxyphenyl)alkyl]-2-imidazolidinone derivatives 失效
    厌氧性4 - [（3,4-二烷氧基苯基）烷基] -2-咪唑烷酮衍生物

    公开(公告)号：US4308278A

    公开(公告)日：1981-12-29

    申请号：US90450

    申请日：1979-11-01

    申请人： Geza Schneider ,  Ferenc Andrasi ,  Pal Berzsenyi ,  Arpad Lazar ,  Sandor Elek ,  Istvan Elekes ,  Istvan Polgari

    发明人： Geza Schneider ,  Ferenc Andrasi ,  Pal Berzsenyi ,  Arpad Lazar ,  Sandor Elek ,  Istvan Elekes ,  Istvan Polgari

    IPC分类号： A61K31/415 ,  A61K31/4166 ,  A61P1/00 ,  A61P3/04 ,  C07C45/71 ,  C07D233/32 ,  C07D233/34 ,  C07D233/38 ,  C07D233/78

    CPC分类号： C07C255/00 ,  C07C45/71 ,  C07D233/32 ,  C07D233/38 ,  C07D233/78 ,  Y10S514/91

    摘要： 4-[(3,4-Dialkoxyphenyl)alkyl]-2-imidazolidinone derivatives having the formula I ##STR1## wherein R.sup.1 stands for a cycloalkyl group containing from 3 to 6 carbon atoms or benzyl group;R.sup.2 stands for hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms;R.sup.3 stands for hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms;R.sup.4 stands for hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms or an alkoxycarbonyl group containing from 1 to 4 carbon atoms; andR.sup.5 stands for hydrogen atom or an alkoxycarbonyl group containing from 1 to 4 carbon atoms,are prepared by(a) reducing a hydantoin derivative having the general formula II, wherein R.sup.1 and R.sup.2 are as defined above, with lithium aluminum hydride in a neutral organic solvent, or(b) hydrogenating catalytically an 1,3-dihydro-2H-imidazol-2-one derivative having the general formula III, wherein R.sup.1 and R.sup.3 are as defined above, while the meaning of R.sup.4 is hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms, or(c) reacting a carbamate derivative having the general formula IV, wherein R.sup.1 is as defined above, while R.sup.6 stands for an alkyl group containing from 1 to 4 carbon atoms, with an organic or inorganic base.The compounds having the formula I possess valuable therapeutical properties, mainly anorexigenic activity.

    摘要翻译： 4 - [（3,4-二烷氧基苯基）烷基] -2-咪唑啉酮衍生物，其具有式I其中R1代表含有3至6个碳原子的环烷基或苄基; R2代表氢原子或含有1至4个碳原子的烷基; R3代表氢原子或含有1至4个碳原子的烷基; R4表示氢原子或含有1至4个碳原子的烷基或含有1至4个碳原子的烷氧基羰基; 并且R5代表氢原子或含有1至4个碳原子的烷氧基羰基，是通过以下步骤制备的：（a）将具有通式II的乙内酰脲衍生物（其中R 1和R 2如上定义）与中性的氢化铝锂 有机溶剂，或（b）催化氢化具有通式III的1,3-二氢-2H-咪唑-2-酮衍生物，其中R 1和R 3如上所定义，而R 4的含义是氢原子或烷基 含有1至4个碳原子的基团，或（c）使具有通式IV的氨基甲酸酯衍生物与其中R 1如上定义，而R6代表含有1至4个碳原子的烷基，与有机或无机 基础。 具有式I的化合物具有有价值的治疗性质，主要是厌食症活性。