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    Anorexigenic 4-[(3,4-dialkoxyphenyl)alkyl]-2-imidazolidinone derivatives
    1.
    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。

    3-(1-Pyrazolyl)-pyridazine derivatives
    2.
    发明授权
    3-(1-Pyrazolyl)-pyridazine derivatives 失效
    3-（1-吡唑基） - 哒嗪衍生物

    公开(公告)号：US4251658A

    公开(公告)日：1981-02-17

    申请号：US914084

    申请日：1978-06-09

    申请人： Geza Szilagyi ,  Endre Kasztreiner ,  Laszlo Tardos ,  Edit Kosa ,  Laszlo Jaszlits ,  Gyorgy Cseh ,  Andras Divald ,  Pal Tolnay ,  Sandor Elek ,  Istvan Elekes ,  Istvan Polgari

    发明人： Geza Szilagyi ,  Endre Kasztreiner ,  Laszlo Tardos ,  Edit Kosa ,  Laszlo Jaszlits ,  Gyorgy Cseh ,  Andras Divald ,  Pal Tolnay ,  Sandor Elek ,  Istvan Elekes ,  Istvan Polgari

    IPC分类号： C07D401/14 ,  A61K31/50 ,  A61K31/501 ,  A61P9/12 ,  A61P43/00 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14

    CPC分类号： C07D403/04

    摘要： 3-(1-Pyrazolyl)-pyridazine derivatives of the formula I, or pharmaceutically acceptable acid addition salts thereof, which decrease high blood pressure and inhibit catabolism or prostaglandins, ##STR1## wherein R.sup.1 is hydrogen or C.sub.1-4 alkyl,R.sup.2 is hydrogen, cyano, carboxyl, carbamoyl, carbaxoyl or C.sub.1-4 alkoxycarbonyl,R.sup.3 is hydrogen or chlorine or --NR.sup.4 NHR.sup.5 or NR.sup.6 R.sup.7, wherein R.sup.4 and R.sup.5 are each hydrogen or C.sub.1-4 alkyl, wherein R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-5 alkyl, C.sub.1-5 hydroxyalkyl, C.sub.3-7 cycloalkyl, phenyl or benzyl, or benzyl or phenylethyl substituted with one or two chlorine atoms or methoxy groups, or a furylmethyl, pyridylmethyl, pyrrolidine or piperazine ring, or when R.sup.7 is hydrogen, R.sup.6 is --(CH.sub.2).sub.n --NR.sup.4 R.sup.5 wherein n is an integer from 1 to 3.

    摘要翻译： 降低高血压并抑制分解代谢或前列腺素的式I的3-（1-吡唑基） - 哒嗪衍生物或其药学上可接受的酸加成盐，其中R 1是氢或C 1-4烷基， R2是氢，氰基，羧基，氨基甲酰基，碳酰基或C1-4烷氧基羰基，R3是氢或氯或-NR4NHR5或NR6R7，其中R4和R5分别是氢或C1-4烷基，其中R6和R7各自是氢或C1 或烷基，C 1-5羟基烷基，C 3-7环烷基，苯基或苄基，或被一个或两个氯原子或甲氧基取代的苄基或苯乙基，或呋喃基甲基，吡啶基甲基，吡咯烷或哌嗪环，或者当R7为氢时， R 6为 - （CH 2）n -NR 4 R 5，其中n为1至3的整数。

    2-Oxazoline derivatives
    7.
    发明授权
    2-Oxazoline derivatives 失效
    2-恶唑啉衍生物

    公开(公告)号：US3979405A

    公开(公告)日：1976-09-07

    申请号：US406784

    申请日：1973-10-16

    申请人： Istvan Tibor Toth ,  Pal Bite ,  Gyorgy Magyar ,  Eszter Diszler ,  Jozsef Borsy ,  Andrea Maderspach ,  Istvan Polgari ,  Sandor Elek ,  Istvan Elekes

    发明人： Istvan Tibor Toth ,  Pal Bite ,  Gyorgy Magyar ,  Eszter Diszler ,  Jozsef Borsy ,  Andrea Maderspach ,  Istvan Polgari ,  Sandor Elek ,  Istvan Elekes

    IPC分类号： C07D263/10 ,  A61K31/42 ,  A61K31/421 ,  C07D263/08 ,  C07D263/14

    CPC分类号： A61K31/42 ,  C07D263/14

    摘要： This invention relates to compounds of the formula ##SPC1##WhereinR.sup.1 is hydrogen or an alkyl group having 1-4 carbon atoms;R.sup.2 but R.sup.3 are hydrogen and if both R.sup.4 and R.sup.5 are hydrogen, R.sup.2 and R.sup.3 are alkyl groups having 1-4 carbon atoms or hydroxymethyl groups;R.sup.4 and R.sup.5 are hydrogen but where both R.sup.2 and R.sup.3 are hydrogen, R.sup.4 but R.sup.5 stand for alkyl groups having 1-4 carbon atoms, are amino groups, which may be mono or di-substituted by alkyl groups having 1-4 carbon atoms, or are allyloxymethyl groups;X is an oxygen or sulphur atom or an NH group;Y stands for a halogen atom or a halogeno-substituted phenyl group. The disclosure also concerns a process for the preparation of such compounds.

    摘要翻译： 本发明涉及下式的化合物：其中R1是氢或具有1-4个碳原子的烷基; R2但R 3为氢，如果R 4和R 5均为氢，则R 2和R 3为具有1-4个碳原子的烷基或羟甲基; R 4和R 5是氢，但其中R 2和R 3均为氢，R 4，但R 5代表具有1-4个碳原子的烷基，可以是可以被具有1-4个碳原子的烷基单取代或二取代的氨基， 或是烯丙氧基甲基; X是氧或硫原子或NH基; Y代表卤素原子或卤素取代的苯基。 本公开还涉及制备这些化合物的方法。