Thiophenes
    1.
    发明授权
    Thiophenes 失效
    噻吩类

    公开(公告)号:US3880849A

    公开(公告)日:1975-04-29

    申请号:US39062773

    申请日:1973-08-22

    申请人: HOFFMANN LA ROCHE

    CPC分类号: C07D333/42 C07D333/44

    摘要: IN WHICH R4 and R5 each represent hydrogen or lower alkyl or R4 and R5 together with the nitrogen atom to which they are attached represent a 3-, 5-, 6- or 7-membered saturated heterocyclic ring which, in the case of a 5-, 6- or 7-membered ring, may contain a further nitrogen atom or an oxygen or sulphur atom and may be substituted by lower alkyl or hydroxy lower alkyl and n stands for 1, 2, 3 or 4, R2 represents hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower alkoxy lower alkyl or hydroxy lower alkyl or R1 and R2 together with the nitrogen atom to which they are attached represent a 3-, 5-, 6- or 7-membered saturated heterocyclic ring which, in the case of a 5-, 6- or 7-membered ring, may contain a further nitorgen atom or an oxygen or sulphur atom and may be substituted by lower alkyl or hydroxy lower alkyl and R3 represents hydrogen or halogen or lower alkyl, provided that when R1 represents lower alkyl and R2 and R3 each represent hydrogen and the variable nitro group is present in the 5position, then R1 represents lower alkyl containing 2 to 7 carbon atoms, AND PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS OF THOSE COMPOUNDS DESCRIBED HEREIN WHICH ARE BASIC AND THUS AMENABLE TO FORMING ACID ADDITION SALTS HAVING PROTOZOACIDAL, BACTERICIDAL, ANTHELMINTIC AND SCHISTOSOMICIDAL ACTIVITY ARE DISCLOSED.

    WHEREIN R1 represents lower alkyl, lower alkenyl, lower alkynyl, halo lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl, lower alkylthio lower alkyl, lower alkylcarbonyl, halo lower alkylcarbonyl, lower alkanoyloxy lower alkyl, lower aroyloxy lower alkyl, pyridylcarbonyloxy lower alkyl, lower alkylaminocarbonyloxy lower alkyl or

    Compound represented by the formula

    摘要翻译: 由式WH表示的化合物R1表示低级烷基,低级烯基,低级炔基,卤代低级烷基,羟基低级烷基,低级烷氧基低级烷基,低级烷硫基低级烷基,低级烷基羰基,卤代低级烷基羰基,低级烷酰氧基低级烷基,低级芳酰氧基低级 烷基,吡啶基羰基氧基低级烷基,低级烷基氨基羰氧基低级烷基或其中R4和R5各自表示氢或低级烷基或R4和R5与它们所连接的氮原子一起代表3-,5-,6-或7-元 饱和杂环,其在5-,6-或7-元环的情况下可以含有另外的氮原子或氧或硫原子,并且可以被低级烷基或羟基低级烷基取代,n代表1, 2,3或4中,R 2表示氢,低级烷基,低级烯基,低级炔基,低级烷氧基低级烷基或羟基低级烷基,或者R 1和R 2与它们所连接的氮原子一起代表3-,5-, - 或7成员 饱和杂环,其在5-,6-或7-元环的情况下可以含有另外的Nitorgen原子或氧或硫原子,并且可以被低级烷基或羟基低级烷基取代,并且R 3表示氢或 卤素或低级烷基,条件是当R 1表示低级烷基且R 2和R 3各自表示氢并且可变硝基存在于5-位时,则R 1表示含有2-7个碳原子的低级烷基,并且药学上可接受的酸添加物 本文所描述的这些化合物可以用于形成具有抗真菌药,杀菌剂,抗炎药和抗病毒药物活性的酸加药盐。

    (2-Aminobenzophenone) acetonitriles
    5.
    发明授权
    (2-Aminobenzophenone) acetonitriles 失效
    (2-氨基二苯甲酮)乙腈

    公开(公告)号:US3906025A

    公开(公告)日:1975-09-16

    申请号:US51302474

    申请日:1974-10-08

    申请人: HOFFMANN LA ROCHE

    CPC分类号: C07D243/16 C07C255/00

    摘要: A process for preparing 1,4-benzodiazepines via the catalytic hydrogenation of the corresponding Alpha -(2aminobenzophenone)acetonitrile. The products obtainable by this process are known compounds and are useful as sedatives, anticonvulsants and muscle relaxants.

    摘要翻译: 通过相应的α-(2-氨基二苯甲酮)乙腈的催化氢化制备1,4-苯并二氮杂的方法。 通过该方法可获得的产物是已知的化合物,并且可用作镇静剂,抗惊厥药和肌肉松弛剂。

    1-Hydroxymethyl-amino-2-alkyl-or allyl-2-(3{40 -methoxy-phenyl)-chclohexanes
    10.
    发明授权
    1-Hydroxymethyl-amino-2-alkyl-or allyl-2-(3{40 -methoxy-phenyl)-chclohexanes 失效
    1-羟甲基 - 氨基-2-烷基 - 或烯丙基-2-(3(40-甲氧基 - 苯基) - 环己烷

    公开(公告)号:US3862986A

    公开(公告)日:1975-01-28

    申请号:US28595072

    申请日:1972-09-01

    申请人: HOFFMANN LA ROCHE

    发明人: HELLERBACH JOSEPH

    IPC分类号: C07D221/12 C07C91/16

    摘要: 1,2,3,4,4a,10b-Hexahydro- and 1,2,3,4,4a,5,6,10boctahydrophenanthridines, substituted in the 9-postion with hydroxy, lower alkoxy, hydroxy-substituted lower alkoxy or lower alkoxy-substituted lower alkoxy and whose 10b-carbon atom is quaternized with lower alkyl, lower cycloalkyl-alkyl or lower alkenyl, are described. The end products are useful as analgesic agents.

    摘要翻译: 在9-位上用羟基,低级烷氧基,羟基取代的低级烷氧基取代的1,2,3,4,4a,10b-六氢 - 和1,2,3,4,4a,5,6,10b-八氢吩芬宁 或低级烷氧基取代的低级烷氧基,并且其10b-碳原子被低级烷基,低级环烷基 - 烷基或低级烯基季铵化。 最终产品可用作止痛剂。