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    Anorexigenic 4-[(3,4-dialkoxyphenyl)alkyl]-2-imidazolidinone derivatives
    5.
    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。

    N-acyl-2,3-benzodiazepine derivatives for treating acute and chronic neurodegenerative disorders
    6.
    发明授权
    N-acyl-2,3-benzodiazepine derivatives for treating acute and chronic neurodegenerative disorders 失效
    用于治疗急性和慢性神经变性疾病的N-酰基-2,3-苯并二氮杂衍生物

    公开(公告)号：US5639751A

    公开(公告)日：1997-06-17

    申请号：US477801

    申请日：1995-06-07

    申请人： Ferenc Andrasi ,  Pal Berzsenyi ,  Peter Botka ,  Sandor Farkas ,  Katalin Goldschmidt ,  Tamas Hamori ,  Jeno Korosi ,  Imre Moravcsik ,  Istvan Tarnawa

    发明人： Ferenc Andrasi ,  Pal Berzsenyi ,  Peter Botka ,  Sandor Farkas ,  Katalin Goldschmidt ,  Tamas Hamori ,  Jeno Korosi ,  Imre Moravcsik ,  Istvan Tarnawa

    IPC分类号： C07D491/04 ,  A61K31/55 ,  A61K31/44

    CPC分类号： C07D491/04

    摘要： The invention relates to novel N-acyl-2,3-benzodiezapine derivatives of the general formula (I), their stereoisomers and acid-addition salts, pharmaceutical compositions containing them and a process for their preparation. In the general formula (I)R stands for a C.sub.1-6 alkanoyl group optionally substituted by a methoxy, cyano, carboxyl, amino, C.sub.1-4 alkylamino, di(C.sub.1-4 alkyl)amino, pyrrolidino, phthalimido or phenyl group, or by one or more halogen(s); or R is a benzoyl, cyclopropanecarbonyl, C.sub.1-5 alkylcarbamoyl or phenylcarbamoyl group; or R is absent when a double bond exists between the N(3) and C(4) atoms;R.sup.1 means hydrogen; or R.sup.1 is absent when a double bond exists between the N(3) and C(4) atoms;R.sup.2 means a C.sub.1-3 alkyl group; orR.sup.1 and R.sup.2 together stand for a methylene group and no double bond is present between the N(3) and C(4) atoms;R.sup.3 means hydrogen or a C.sub.1-4 alkanoyl group;R.sup.4 represents hydrogen; a C.sub.1-6 alkanoyl group optionally substituted by a methoxy, cyano, carboxyl, amino, C.sub.1-4 alkylamino, di(C.sub.1-4 alkyl)amino, pyrrolidino, phthalimido or phenyl group or by one or more halogen(s); as well as a benzoyl, palmitoyl, cyclopropanecarbonyl, C.sub.1-5 alkylcarbamoyl or phenylcarbamoyl group; andthe dotted lines represent valence bonds optionally being present, with the proviso that no double bond exists between the N(3) and C(4) atoms when both R.sup.3 and R.sup.4 stand for hydrogen.The compounds of the general formula (I) possess valuable central nervous system effects, particularly muscle-relaxant, anticonvulsive and neuroprotective action. Thus, they may be useful for the treatment of various diseases of central nervous system origin.

    摘要翻译： 本发明涉及通式（I）的新型N-酰基-2,3-苯并二氮杂萘衍生物，其立体异构体和酸加成盐，含有它们的药物组合物及其制备方法。 在通式（I）中，R代表任选被甲氧基，氰基，羧基，氨基，C 1-4烷基氨基，二（C 1-4烷基）氨基，吡咯烷子基，邻苯二甲酰亚胺基或苯基取代的C 1-6烷酰基，或 通过一个或多个卤素; 或R是苯甲酰基，环丙烷羰基，C 1-5烷基氨基甲酰基或苯基氨基甲酰基; 或者当N（3）和C（4）原子之间存在双键时，R不存在; R1表示氢; 当N（3）和C（4）原子之间存在双键时，R1不存在; R2表示C1-3烷基; 或者R 1和R 2一起代表亚甲基，N（3）和C（4）原子之间不存在双键; R3表示氢或C1-4烷酰基; R4代表氢; 任选被甲氧基，氰基，羧基，氨基，C1-4烷基氨基，二（C1-4烷基）氨基，吡咯烷子基，苯二甲酰亚氨基或苯基或一个或多个卤素取代的C 1-6烷酰基; 以及苯甲酰基，棕榈酰基，环丙烷羰基，C 1-5烷基氨基甲酰基或苯基氨基甲酰基; 并且虚线表示任选存在的价键，条件是当R3和R4均代表氢时，N（3）和C（4）原子之间不存在双键。 通式（I）的化合物具有有价值的中枢神经系统作用，特别是肌肉松弛剂，抗惊厥和神经保护作用。 因此，它们可用于治疗中枢神经系统起源的各种疾病。

    N-acyl-2,3-benzodiazepine derivatives pharmaceutical compositions containing them and process for preparing same
    7.
    发明授权
    N-acyl-2,3-benzodiazepine derivatives pharmaceutical compositions containing them and process for preparing same 失效
    N-酰基-2,3-苯并二氮杂衍生物含有它们的药物组合物及其制备方法

    公开(公告)号：US5536832A

    公开(公告)日：1996-07-16

    申请号：US423153

    申请日：1995-04-17

    申请人： Ferenc Andrasi ,  Pal Berzsenyi ,  Peter Botka ,  Sandor Farkas ,  Katalin Goldschmidt ,  Tamas Hamori ,  Jeno Korosi ,  Imre Moravcsik ,  Istvan Tarnawa

    发明人： Ferenc Andrasi ,  Pal Berzsenyi ,  Peter Botka ,  Sandor Farkas ,  Katalin Goldschmidt ,  Tamas Hamori ,  Jeno Korosi ,  Imre Moravcsik ,  Istvan Tarnawa

    IPC分类号： A61K31/55 ,  A61K20060101 ,  A61K31/00 ,  A61K31/335 ,  A61K31/395 ,  A61K31/551 ,  A61P9/08 ,  A61P9/10 ,  A61P21/02 ,  A61P25/00 ,  A61P25/08 ,  A61P25/28 ,  C07D20060101 ,  C07D243/00 ,  C07D243/02 ,  C07D247/00 ,  C07D317/00 ,  C07D317/08 ,  C07D317/44 ,  C07D491/00 ,  C07D491/04 ,  C07D491/056 ,  C07D493/04

    CPC分类号： C07D491/04

    摘要： The invention relates to novel N-acyl-2,3-benzodiezapine derivatives of the general formula (I), their stereoisomers and acid-addition salts, pharmaceutical compositions containing them and a process for their preparation. In the general formula (I)R stands for a C.sub.1-6 alkanoyl group optionally substituted by a methoxy, cyano, carboxyl, amino, C.sub.1-4 alkylamino, di(C.sub.1-4 alkyl)amino, pyrrolidino, phthalimido or phenyl group, or by one or more halogen(s); or R is a benzoyl, cyclopropanecarbonyl, C.sub.1-5 alkylcarbamoyl or phenylcarbamoyl group; or R is absent when a double bond exists between the N(3) and C(4) atoms;R.sup.1 means hydrogen; or R.sup.1 is absent when a double bond exists between the N(3) and C(4) atoms;R.sup.2 means a C.sub.1-3 alkyl group; orR.sup.1 and R.sup.2 together stand for a methylene group and no double bond is present between the N(3) and C(4) atoms;R.sup.3 means hydrogen or a C.sub.1-4 alkanoyl group;R.sup.4 represents hydrogen; a C.sub.1-6 alkanoyl group optionally substituted by a methoxy, cyano, carboxyl, amino, C.sub.1-4 alkylamino, di(C.sub.1-4 alkyl)amino, pyrrolidino, phthalimido or phenyl group or by one or more halogen(s); as well as a benzoyl, palmitoyl, cyclopropane-carbonyl, C.sub.1-5 alkylcarbamoyl or phenylcarbamoyl group; andthe dotted lines represent valence bonds optionally being present, with the proviso that no double bond exists between the N(3) and C(4) atoms when both R.sup.3 and R.sup.4 stand for hydrogen.The compounds of the general formula (I) possess valuable central nervous system effects, particularly muscle-relaxant, anticonvulsive and neuroprotective action. Thus, they may be useful for the treatment of various diseases of central nervous system origin.

    摘要翻译： 本发明涉及通式（I）的新型N-酰基-2,3-苯并二氮杂萘衍生物，其立体异构体和酸加成盐，含有它们的药物组合物及其制备方法。 在通式（I）中，R代表任选被甲氧基，氰基，羧基，氨基，C 1-4烷基氨基，二（C 1-4烷基）氨基，吡咯烷子基，邻苯二甲酰亚胺基或苯基取代的C 1-6烷酰基，或 通过一个或多个卤素; 或R是苯甲酰基，环丙烷羰基，C 1-5烷基氨基甲酰基或苯基氨基甲酰基; 或者当N（3）和C（4）原子之间存在双键时，R不存在; R1means氢; 当N（3）和C（4）原子之间存在双键时，R1不存在; R2表示C1-3烷基; 或者R 1和R 2一起代表亚甲基，N（3）和C（4）原子之间不存在双键; R3表示氢或C1-4烷酰基; R4表示氢; 任选被甲氧基，氰基，羧基，氨基，C 1-4烷基氨基，二（C 1-4烷基）氨基，吡咯烷子基，苯二甲酰亚氨基或苯基或被一个或多个卤素取代的C 1-6烷酰基; 以及苯甲酰基，棕榈酰基，环丙烷 - 羰基，C 1-5烷基氨基甲酰基或苯基氨基甲酰基; 并且虚线表示任选存在的价键，条件是当R3和R4均代表氢时，N（3）和C（4）原子之间不存在双键。 通式（I）的化合物具有有价值的中枢神经系统作用，特别是肌肉松弛剂，抗惊厥和神经保护作用。 因此，它们可用于治疗中枢神经系统起源的各种疾病。

    Spiro derivatives of the pyrazolo [1,5-d] [1,2,4] triazine ring system and a process for the preparation thereof
    9.
    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。