利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

16 条记录 (耗时 0.022 秒)

    1,2,3,5-Tetrahydro-4H-1,5-benzodiazepine-4-ones
    2.
    发明授权
    1,2,3,5-Tetrahydro-4H-1,5-benzodiazepine-4-ones 失效
    1,2,3,5-四氢-4H- 1,5-BENZODIAZEPINE-4-ONES

    公开(公告)号：US4111931A

    公开(公告)日：1978-09-05

    申请号：US874074

    申请日：1978-02-01

    申请人： Armin Walser ,  Rodney Ian Fryer

    发明人： Armin Walser ,  Rodney Ian Fryer

    IPC分类号： A61K31/55 ,  A61P21/02 ,  A61P25/20 ,  C07D243/12 ,  C07D487/04

    CPC分类号： C07D487/04 ,  C07D243/12 ,  Y10S514/906

    摘要： The present invention concerns compounds of the formula ##STR1## wherein X is hydrogen or halogen; R.sub.1 is hydrogen, halogen or trifluoromethyl; R.sub.2 is hydrogen or lower alkyl; and R.sub.3 is hydrogen, --COO lower alkyl or CON(R.sub.4).sub.2 wherein R.sub.2 is lower alkyl or hydrogen and may be differentand the pharmaceutically acceptable salts thereof.Also provided are methods for the preparation of these compounds as well as pharmaceutical formulations which contain the active compounds of this invention. The compounds of the formula illustrated above are useful as anxiolytics, anticonvulsants, muscle relaxants and sedative agents.

    7-Azoxy substituted-1,4-benzodiazepin-2-ones
    3.
    发明授权
    7-Azoxy substituted-1,4-benzodiazepin-2-ones 失效
    7-氮氧基取代的-1,4-苯并二氮杂-2-酮

    公开(公告)号：US3989681A

    公开(公告)日：1976-11-02

    申请号：US419582

    申请日：1973-11-28

    申请人： Rodney Ian Fryer ,  Armin Walser

    发明人： Rodney Ian Fryer ,  Armin Walser

    IPC分类号： C07D243/26 ,  C07C107/04

    CPC分类号： Y10S514/906

    摘要： Novel 1,4-benzodiazepin-2-ones of the formula ##SPC1##WhereinR.sub.1 is selected from the group consisting of hydrogen, lower alkyl, cycloalkyl-lower alkyl, hydroxylower alkyl, lower alkoxy-lower alkyl and di-lower alkylamino-lower alkyl;R.sub.2 signifies hydrogen or lower alkyl; R.sub.3 signifies hydrogen or halogen; R.sub.4 signifies lower alkylAnd the pharmaceutically acceptable acid addition salts thereof, are disclosed together with processes for preparing these compounds and novel intermediates used in these processes. These 7-azoxy substituted-1,4-benzodiazepin-2-ones are useful as muscle relaxant, anti-convulsant and sedative agents.

    摘要翻译： 新颖的1,4-苯并二氮杂-2-酮，式WHEREIN R1选自氢，低级烷基，环烷基 - 低级烷基，羟基低级烷基，低级烷氧基 - 低级烷基和二 - 低级烷基氨基 - 低级烷基; R2表示氢或低级烷基; R3表示氢或卤素; R4表示低级烷基和其药学上可接受的酸的添加剂，与制备这些化合物和在这些方法中使用的新型中间体的方法无关。 这些7-氧杂取代的1,4-苯并二氮杂-2-酮可用作肌肉松弛剂，抗惊厥剂和镇静剂。

    Imidazo [1,5-a][1,5] benzodiazepines
    6.
    发明授权
    Imidazo [1,5-a][1,5] benzodiazepines 失效
    咪唑并[8,1-a {9 {8,5 {9 {苯并二氮杂

    公开(公告)号：US4080323A

    公开(公告)日：1978-03-21

    申请号：US775347

    申请日：1977-03-07

    申请人： Armin Walser ,  Rodney Ian Fryer

    发明人： Armin Walser ,  Rodney Ian Fryer

    IPC分类号： A61K31/55 ,  A61P21/02 ,  A61P25/20 ,  C07D243/12 ,  C07D487/04

    CPC分类号： C07D487/04 ,  C07D243/12 ,  Y10S514/906

    摘要： The present invention concerns compounds of the formula ##STR1## wherein X is hydrogen or halogen; R.sub.1 is hydrogen, halogen or trifluoromethyl; R.sub.2 is hydrogen or lower alkyl; and R.sub.3 is hydrogen, --COO lower alkyl or CON(R.sub.4).sub.2 wherein R.sub.4 is lower alkyl or hydrogen and may be differentAnd the pharmaceutically acceptable salts thereof.Also provided are methods for the preparation of these compounds as well as pharmaceutical formulations which contain the active compounds of this invention. The compounds of the formula illustrated above are useful as anxiolytics, anticonvulsants, muscle relaxants and sedative agents.

    摘要翻译： 本发明涉及下式的化合物，其中X是氢或卤素; R1是氢，卤素或三氟甲基; R2是氢或低级烷基; 并且R 3是氢，-COO低级烷基或CON（R 4）2，其中R 4是低级烷基或氢，并且可以是不同的，并且其药学上可接受的盐。

    Intermediates for the production of tricyclic benzodiazepines
    7.
    发明授权
    Intermediates for the production of tricyclic benzodiazepines 失效
    用于生产三环苯并二氮杂类的中间体

    公开(公告)号：US4017532A

    公开(公告)日：1977-04-12

    申请号：US676092

    申请日：1976-04-12

    申请人： Michael Edward Derieg ,  James Valentine Earley ,  Rodney Ian Fryer ,  Leo Henryk Sternbach

    发明人： Michael Edward Derieg ,  James Valentine Earley ,  Rodney Ian Fryer ,  Leo Henryk Sternbach

    IPC分类号： C07D213/24 ,  C07D243/16 ,  C07C69/96

    CPC分类号： C07D243/16 ,  C07D213/24

    摘要： Tricyclic benzodiazepine derivatives ("A") bearing a hydroxylower alkyl substituent in the 1-position and a heterocyclic ring joined between positions 4 and 5 of the benzodiazepine moiety are described. The heterocyclic ring will contain the nitrogen atom appearing at position 4 of the benzodiazepine ring as well as the hetero atom, which may be either oxygen or nitrogen, attached to the carbon atom at the 5-position of the benzodiazepine ring. "A" bearing an oxygen atom in the new heterocyclic ring may be formed from the corresponding 4,5-unsaturated benzodiazepines by treatment with an epoxide compound in the presence of an acid catalyst. "A" bearing either a nitrogen or an oxygen atom in the new heterocyclic ring may be prepared by cyclization of the corresponding open compound. "A" are useful as sedative, muscle relaxant and anti-convulsant agents.

    摘要翻译： 描述了在1-位上带有羟基低级烷基取代基的三环苯并二氮杂衍生物（“A”）和苯并二氮杂部分位置4和5之间连接的杂环。 杂环将含有出现在苯并二氮杂环的第4位的氮原子以及与苯并二氮杂环的5-位的碳原子连接的可以是氧或氮的杂原子。 在新的杂环中带有氧原子的“A”可以通过在酸催化剂的存在下用环氧化合物处理由相应的4,5-不饱和的苯并二氮杂卟啉形成。 在新杂环中带有氮原子或氧原子的“A”可以通过相应的开放化合物的环化来制备。 “A”可用作镇静剂，肌肉松弛剂和抗惊厥剂。

    Intermediates for the production of tricyclic benzodiazepines
    8.
    发明授权
    Intermediates for the production of tricyclic benzodiazepines 失效
    用于生产三环苯并二氮杂类的中间体

    公开(公告)号：US4017531A

    公开(公告)日：1977-04-12

    申请号：US676077

    申请日：1976-04-12

    申请人： Michael Edward Derieg ,  James Valentine Earley ,  Rodney Ian Fryer ,  Leo Henryk Sternbach

    发明人： Michael Edward Derieg ,  James Valentine Earley ,  Rodney Ian Fryer ,  Leo Henryk Sternbach

    IPC分类号： C07D213/24 ,  C07D243/16 ,  C07C69/96

    CPC分类号： C07D243/16 ,  C07D213/24

    摘要： Tricyclic benzodiazepine derivatives ("A") bearing a hydroxylower alkyl substituent in the 1-position and a heterocyclic ring joined between positions 4 and 5 of the benzodiazepine moiety are described. The heterocyclic ring will contain the nitrogen atom appearing at position 4 of the benzodiazepine ring as well as the hetero atom, which may be either oxygen or nitrogen, attached to the carbon atom at the 5-position of the benzodiazepine ring. A bearing an oxygen atom in the new heterocyclic ring may be formed from the corresponding 4,5-unsaturated benzodiazepines by treatment with an epoxide compound in the presence of an acid catalyst. A bearing either a nitrogen or an oxygen atom in the new heterocyclic ring may be prepared by cyclization of the corresponding open compound. A are useful as sedative, muscle relaxant and anti-convulsant agents.

    摘要翻译： 描述了在1-位上带有羟基低级烷基取代基的三环苯并二氮杂衍生物（“A”）和苯并二氮杂部分位置4和5之间连接的杂环。 杂环将含有出现在苯并二氮杂环的第4位的氮原子以及与苯并二氮杂环的5-位的碳原子连接的可以是氧或氮的杂原子。 在新杂环中带有氧原子的A可以通过在酸催化剂存在下用环氧化合物处理由相应的4,5-不饱和苯并二氮杂卟啉形成。 在新杂环中带有氮原子或氧原子的化合物可以通过相应的开放化合物的环化来制备。 A可用作镇静剂，肌肉松弛剂和抗惊厥剂。

    Process for preparing o-nitrobenzylketones
    9.
    发明授权
    Process for preparing o-nitrobenzylketones 失效
    制备邻硝基苄基酮的方法

    公开(公告)号：US3931225A

    公开(公告)日：1976-01-06

    申请号：US435050

    申请日：1974-01-21

    申请人： Rodney Ian Fryer ,  Edward Ernest Garcia

    发明人： Rodney Ian Fryer ,  Edward Ernest Garcia

    IPC分类号： C07C49/76 ,  C07D209/08 ,  C07D209/10 ,  C07D209/48

    CPC分类号： C07D209/48 ,  C07C201/12 ,  C07D209/08 ,  C07D209/10

    摘要： o-nitrobenzylketones are prepared by reacting a trans-.beta.-substituted amino-2-nitrostyrene with a lower alkanoyl halide, halo-lower alkanoyl halide, phthalimido-lower alkanoyl halide, benzoyl halide or substituted benzoyl halide, and subsequently hydrolyzing the resulting product to yield the desired o-nitrobenzylketone.

    摘要翻译： 邻硝基苄基酮通过反式-β-取代的氨基-2-硝基苯乙烯与低级烷酰卤，卤代低级烷酰卤，苯二甲酰亚氨基 - 低级烷酰卤，苯甲酰卤或取代的苯甲酰卤反应制备，随后将所得产物水解成 得到所需的邻硝基苄基酮。