利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

94 条记录 (耗时 0.031 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.

    Imidazo [1,5-a][1,5] benzodiazepines
    5.
    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。

    7-Azoxy substituted-1,4-benzodiazepin-2-ones
    6.
    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。

    Malonic acid derivatives, processes for their preparation their use and pharmaceutical compositions containing them
    9.
    发明授权
    Malonic acid derivatives, processes for their preparation their use and pharmaceutical compositions containing them 有权
    丙二酸衍生物，其制备方法，其用途和含有它们的药物组合物

    公开(公告)号：US06794365B2

    公开(公告)日：2004-09-21

    申请号：US09790641

    申请日：2001-02-23

    申请人： Fahad A. Al-Obeidi ,  Armin Walser ,  Peter Wildgoose

    发明人： Fahad A. Al-Obeidi ,  Armin Walser ,  Peter Wildgoose

    IPC分类号： C07K506

    CPC分类号： C07D213/56 ,  A61K38/00 ,  C07C257/18 ,  C07C279/14 ,  C07C2601/14 ,  C07K5/0202 ,  C07K5/06026 ,  C07K5/06034

    摘要： The present invention relates to new malonic acid derivatives of the formula I, wherein R(1), R(2), R(3), R(4), R(5), and R(6) have the meanings indicated in the claims. The compounds of formula I are inhibitors of the blood clotting enzyme factor Xa. The invention also relates to processes for the preparation of the compounds of formula I, to methods of inhibiting factor Xa activity and of inhibiting blood clotting, to the use of the compounds of formula I in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and to the use of the compounds of formula I in the preparation of medicaments to be applied in such diseases. The invention further relates to compositions containing a compound of formula I in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula I together with pharmaceutically acceptable carrier substances and auxiliary substances.

    摘要翻译： 本发明涉及式I的新型丙二酸衍生物，其中R（1），R（2），R（3），R（4），R（5）和R（6） 索赔。 式I化合物是凝血酶因子Xa的抑制剂。 本发明还涉及制备式I化合物的方法，抑制因子Xa活性和抑制血液凝固的方法，使用式I化合物治疗和预防可治疗的疾病 或通过抑制诸如血栓栓塞性疾病的因子Xa活性来防止，以及式I化合物在制备用于这些疾病的药物中的用途。 本发明还涉及含有式I化合物的组合物，其与惰性载体混合或以其它方式结合，特别是含有式I化合物与药学上可接受的载体物质和辅助物质的药物组合物。

    Malonic acid derivatives, processes for their preparation, for their use and pharmaceutical compositions containing them
    10.
    发明授权
    Malonic acid derivatives, processes for their preparation, for their use and pharmaceutical compositions containing them 有权
    丙二酸衍生物，其制备方法，用途及含有它们的药物组合物

    公开(公告)号：US06395737B1

    公开(公告)日：2002-05-28

    申请号：US09473053

    申请日：1999-12-28

    申请人： Elisabeth Defossa ,  Uwe Heinelt ,  Otmar Klingler ,  Gerhard Zoller ,  Hans Matter ,  Fahad A. Al-Obeidi ,  Armin Walser ,  Peter Wildgoose

    发明人： Elisabeth Defossa ,  Uwe Heinelt ,  Otmar Klingler ,  Gerhard Zoller ,  Hans Matter ,  Fahad A. Al-Obeidi ,  Armin Walser ,  Peter Wildgoose

    IPC分类号： A61K31165

    CPC分类号： C07C257/18 ,  C07C279/14

    摘要： New compounds for the inhibition of blood clotting proteins, and more particularly, to malonic acid derivatives of the formula I, wherein R(1), R(2), R(3), R(4), R(5), and R(6) have the meanings indicated in the claims. The compounds of formula I are inhibitors of the blood clotting enzyme factor Xa. Processes for the preparation of the compounds of formula I, methods of inhibiting factor Xa activity and of inhibiting blood clotting, use of the compounds of formula I in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and use of the compounds of formula I in the preparation of medicaments to be applied in such diseases. Compositions containing a compound of formula I in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula I together with pharmaceutically acceptable carrier substances and auxiliary substances.

    摘要翻译： 用于抑制血液凝固蛋白质的新化合物，更具体地，涉及式I的丙二酸衍生物，其中R（1），R（2），R（3），R（4），R（5）和 R（6）具有权利要求中所示的含义。 式I化合物是凝血酶因子Xa的抑制剂。 用于制备式I化合物的方法，抑制因子Xa活性和抑制血液凝固的方法，式I化合物在治疗和预防疾病中的用途，其可以通过抑制因子Xa来治疗或预防 活性如血栓栓塞性疾病，以及式I化合物在制备用于这些疾病的药物中的应用。 含有式I化合物的组合物与惰性载体混合或以其它方式结合，特别是含有式I化合物的药物组合物以及药学上可接受的载体物质和辅助物质。