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    Substituted phenyl ketones
    2.
    发明授权
    Substituted phenyl ketones 失效
    取代苯基酮

    公开(公告)号：US4069229A

    公开(公告)日：1978-01-17

    申请号：US740701

    申请日：1976-11-11

    申请人： Cedric Herbert Hassall ,  William Henry Johnson ,  Antonin Krohn ,  Carey Ernest Smithen ,  William Anthony Thomas

    发明人： Cedric Herbert Hassall ,  William Henry Johnson ,  Antonin Krohn ,  Carey Ernest Smithen ,  William Anthony Thomas

    IPC分类号： A61K38/00 ,  C07D213/50 ,  C07D243/24 ,  C07D249/08 ,  C07K5/06 ,  C07K5/065 ,  C07K5/068 ,  C07K5/072 ,  C07K5/078

    CPC分类号： C07K5/06191 ,  C07D213/50 ,  C07D243/24 ,  C07D249/08 ,  C07K5/06026 ,  C07K5/06034 ,  C07K5/06043 ,  C07K5/06078 ,  C07K5/06086 ,  C07K5/06095 ,  C07K5/06104 ,  C07K5/06165 ,  A61K38/00 ,  Y10S514/906

    摘要： This invention is directed toward pharmacologically active compounds of the formula ##STR1## wherein A represents a nitrogen atom which may be substituted by a methyl, cyclopropylmethyl, di(C.sub.1-4 alkyl)aminoethyl, methoxymethyl or hydroxyethyl group and B represents a carbonyl group or A and B together represent a grouping of the formula ##STR2## in which R.sup.a represents a hydrogen atom or a lower alkyl or hydroxymethyl group and X represents a nitrogen atom or C-R.sup.b wherein R.sup.b represents a hydrogen atom or a lower alkyl or hydroxymethyl group; R represents a halogen atom or a nitro or trifluoromethyl group; R.sup.1 represents a hydrogen atom or a lower alkyl group; R.sup.2 represents an acyl group derived from a naturally occurring amino acid (all such groups which contain an asymmetric carbon atom having the L- or D,L-configuration) and R.sup.3 represents a phenyl, halophenyl or 2-pyridyl groupAnd acid addition salts thereof.Also provided are methods for their preparation and intermediates thereof. These compounds exhibit activity as anticonvulsants, muscle relaxants and sedatives.

    摘要翻译： 本发明涉及下式的药理学活性化合物，其中A代表可被甲基，环丙基甲基，二（C 1-4烷基）氨基乙基，甲氧基甲基或羟乙基取代的氮原子，B代表羰基或 A和B一起表示式为“IMAGE”的分组，其中Ra表示氢原子或低级烷基或羟甲基，X表示氮原子或C-Rb，其中Rb表示氢原子或低级烷基或羟甲基 ; R表示卤素原子或硝基或三氟甲基; R1表示氢原子或低级烷基; R 2表示衍生自天然存在的氨基酸的酰基（所有这些基团含有具有L或D，L构型的不对称碳原子），R 3表示苯基，卤代苯基或2-吡啶基。其酸加成盐 。

    Substituted phenyl ketones
    6.
    发明授权
    Substituted phenyl ketones 失效
    取代苯基酮

    公开(公告)号：US4105852A

    公开(公告)日：1978-08-08

    申请号：US741001

    申请日：1976-11-11

    申请人： Cedric H. Hassall ,  William H. Johnson ,  Antonin Krohn ,  Carey E. Smithen ,  William A. Thomas

    发明人： Cedric H. Hassall ,  William H. Johnson ,  Antonin Krohn ,  Carey E. Smithen ,  William A. Thomas

    IPC分类号： A61K38/00 ,  C07D213/50 ,  C07D243/24 ,  C07D249/08 ,  C07K5/06 ,  C07K5/065 ,  C07K5/068 ,  C07K5/072 ,  C07K5/078 ,  C07D233/64

    CPC分类号： C07K5/06191 ,  C07D213/50 ,  C07D243/24 ,  C07D249/08 ,  C07K5/06026 ,  C07K5/06034 ,  C07K5/06043 ,  C07K5/06078 ,  C07K5/06086 ,  C07K5/06095 ,  C07K5/06104 ,  C07K5/06165 ,  A61K38/00 ,  Y10S514/906

    摘要： This invention is directed toward pharmacologically active compounds of the formula ##STR1## wherein A represents a nitrogen atom which may be substituted by a methyl, cyclopropylmethyl, di(C.sub.1-4 alkyl)aminoethyl, methoxymethyl or hydroxyethyl group and B represents a carbonyl group or A and B together represent a grouping of the formula ##STR2## in which R.sup.a represents a hydrogen atom or a lower alkyl or hydroxymethyl group and X represents a nitrogen atom or C--R.sup.b wherein R.sup.b represents a hydrogen atom or a lower alkyl or hydroxymethyl group; R represents a halogen atom or a nitro or trifluoromethyl group; R.sup.1 represents a hydrogen atom or a lower alkyl group; R.sup.2 represents an acyl group derived from a naturally occurring amino acid (all such groups which contain an asymmetric carbon atom having the L- or D,L-configuration) and R.sup.3 represents a phenyl, halophenyl or 2-pyridyl group and acid addition salts thereof.Also provided are methods for their preparation and intermediates thereof. These compounds exhibit activity as anticonvulsants, muscle relaxants and sedative.

    摘要翻译： 本发明涉及下式的药理学活性化合物，其中A表示可被甲基，环丙基甲基，二（C 1-4烷基）氨基乙基，甲氧基甲基或羟乙基取代的氮原子，B表示羰基或A 和B一起表示其中R a表示氢原子或低级烷基或羟甲基并且X表示氮原子的式“IMAGE”或其中R b表示氢原子或低级烷基或羟甲基的C-R b的基团; R表示卤素原子或硝基或三氟甲基; R1表示氢原子或低级烷基; R2表示衍生自天然存在的氨基酸的酰基（所有这些基团含有具有L或D的不对称碳原子，L构型），R 3表示苯基，卤代苯基或2-吡啶基，其酸加成盐 。