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    N-acyl-2,3-benzodiazepine derivatives for treating acute and chronic neurodegenerative disorders
    7.
    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
    8.
    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。

    N-acyl-2,3-benzoidazepine derivatives, pharmaceutical compositions containing them and process for preparing same
    9.
    发明授权
    N-acyl-2,3-benzoidazepine derivatives, pharmaceutical compositions containing them and process for preparing same 失效
    N-酰基-2,3-苯并吖庚因衍生物，含有它们的药物组合物及其制备方法

    公开(公告)号：US5519019A

    公开(公告)日：1996-05-21

    申请号：US472454

    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 ,  C07D243/02

    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; 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。