2H-(1) benzoxepino (5,4-b)-1,4 oxazine derivatives
    4.
    发明公开
    2H-(1) benzoxepino (5,4-b)-1,4 oxazine derivatives 失效
    2H-(1)苯并氧杂(5,4-b)的-1,4- oxazinderivate。

    公开(公告)号:EP0116372A1

    公开(公告)日:1984-08-22

    申请号:EP84101519.1

    申请日:1984-02-14

    发明人: Freedman, Jules

    IPC分类号: C07D498/04 A61K31/535

    CPC分类号: C07D313/08

    摘要: Derivatives of 2H-[1]benzoxepino[5,4-b]-1,4-oxazine, such as (4a,11b)-3,4,4a,5,6,11b-hexahydro-2H-[1]benzoxepino[5,4-b]-1,4-oxazine, are prepared by acylating a 4-amino-2,3,4,5-tetrahydro-1-benzoxepin-5-ol, cyclizing the resulting chloroacetamido alcohol, reducing the 1,4-oxazine-3(4H)-one so obtained, acylating the resulting 2H-[1]benzoxepino[5,4-b]-1,4-oxazine, and reducing the N-acyl-2H-[1]benzoxepino[5,4-b]-1,4-oxazine so obtained. The novel compounds disclosed herein possess useful muscle relaxant and analgesic properties.

    摘要翻译: 2H- [1]苯并氧杂ino [5,4-b] -1,4-恶嗪衍生物,如(4a,11b)-3,4,4a,5,6,11b-六氢-2H- [1]苯并氧杂ino [5,4-b] -1,4-恶嗪通过酰化4-氨基-2,3,4,5-四氢-1-苯并氧杂七环-5-醇制备,环化所得氯乙酰胺醇,还原1 ,4-恶嗪-3(4H) - 酮,酰化所得的2H- [1]苯并氧杂环[5,4-b] -1,4-恶嗪,还原N-酰基-2H- [1]苯并氧杂ino [5,4-b] -1,4-恶嗪。 本文公开的新颖化合物具有有用的肌肉松弛剂和镇痛特性。

    2H-(1) benzoxepino(5,4-b)-1,4-oxazine derivatives
    7.
    发明公开
    2H-(1) benzoxepino(5,4-b)-1,4-oxazine derivatives 失效
    2H-(1)苯并氧杂庚因(5,4-b)-1,4-恶嗪衍生物

    公开(公告)号:EP0116373A1

    公开(公告)日:1984-08-22

    申请号:EP84101520.9

    申请日:1984-02-14

    CPC分类号: C07D313/08

    摘要: Derivates of 2H-[1]benzoxepino[5,4-b]-1,4-oxazine, such as trans-(4a, 11b)-3,4,4a,5,6,11b-hexahydro-10-methoxy-2H [1]benzoxepino[5,4-b]-1,4-oxazine, are prepared by acylating a trans-4-amino-2,3,4,5-tetrahydro-1-benzoxepin-5-ol, cyclizing the resulting chloroacetamido alcohol, reducing the 1,4-oxazine-3(4H)-one so obtained, acylating the resulting 2H-[1]benzoxepino[5,4-b]-1,4-oxazine, and reducing the N-acyl-2H-[1]benzoxepino[5,4,-b]-1,4-oxazine so obtained. The novel compounds disclosed herein possess useful antihypertensive properties.

    摘要翻译: 2H- [1]苯并氧杂庚英并[5,4-b] -1,4-恶嗪的衍生物,如反式 - (4a,11b)-3,4,4a,5,6,11b-六氢-10-甲氧基 - 2H [1]苯并氧杂庚英并[5,4-b] -1,4-恶嗪,通过酰化反式-4-氨基-2,3,4,5-四氢-1-苯并氧杂七环-5-醇, 得到氯乙酰胺醇,还原如此得到的1,4-恶嗪-3(4H) - 酮,酰化得到的2H- [1]苯并氧杂庚英并[5,4-b] -1,4-恶嗪,还原N-酰基 -2H- [1]苯并氧杂庚英并[5,4-b] -1,4-恶嗪。 本文公开的新化合物具有有用的抗高血压性质。

    Phenoxy-heterocyclic compounds
    10.
    发明公开
    Phenoxy-heterocyclic compounds 失效
    苯氧基 - 杂环化合物

    公开(公告)号:EP0423802A1

    公开(公告)日:1991-04-24

    申请号:EP90120052.7

    申请日:1990-10-19

    摘要: The present invention is directed to a class of phenoxy-heterocyclic compounds of the formula I:
    in which R₁ is represented by hydrogen, halogen, alkyl, alkoxy, OH, CF₃, CN, methylenedioxy, ethylenedioxy, methylene, 2,3-benzo, 3,4-benzo, alkylthio, alkylsulfonyl, alkylsulfinyl, cycloalkyl, cycloalkoxy or cycloalkylthio; R₂ is represented by halogen, alkyl, alkoxy, OH, CF₃, CN, alkylthio, alkylsulfinyl, cycloalkyl, cycloalkoxy or cycloalkylthio; R₃ is represented by hydrogen, halogen, alkyl, alkoxy, OH, CF₃, CN, methylenedioxy, ethylenedioxy, methylene, 2,3-benzo, 3,4-benzo, 4,5-benzo, 5,6-benzo, alkylthio, alkylsulfonyl, alkylsulfinyl, cycloalkyl, cycloalkoxy or cycloalkylthio; m is represented by the integer 1 or 2; p is represented by an integer from 0-4; and the pharmaceutically acceptable addition salts thereof, and to their use as anti-­depressants, anxiolytics and anti-hypertensive agents.

    摘要翻译: 本发明涉及一类式I的苯氧基 - 杂环化合物:其中R 1由氢,卤素,烷基,烷氧基,OH,CF 3,CN,亚甲二氧基,亚乙二氧基,亚甲基,2,3-苯并三唑, 烷基硫基,烷基磺酰基,烷基亚磺酰基,环烷基,环烷氧基或环烷硫基; R 2由卤素,烷基,烷氧基,OH,CF 3,CN,烷硫基,烷基亚磺酰基,环烷基,环烷氧基或环烷硫基表示; R 3由氢,卤素,烷基,烷氧基,OH,CF 3,CN,亚甲二氧基,亚乙二氧基,亚甲基,2,3-苯并,3,4-苯并,4,5-苯并,5,6-苯并,烷硫基, 烷基磺酰基,烷基亚磺酰基,环烷基,环烷氧基或环烷硫基; m由整数1或2表示; p由0-4的整数表示; 及其药学上可接受的加成盐,以及它们作为抗抑郁药,抗焦虑药和抗高血压药的用途。