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255 条记录 (耗时 0.042 秒)

    Pyrimido-2-benzazepines
    61.
    发明授权
    Pyrimido-2-benzazepines 失效
    嘧啶-2-苯并吖庚因

    公开(公告)号：US4481142A

    公开(公告)日：1984-11-06

    申请号：US437047

    申请日：1982-10-27

    申请人： Rodney I. Fryer ,  Norman W. Gilman ,  Eugene J. Trybulski ,  Armin Walser

    发明人： Rodney I. Fryer ,  Norman W. Gilman ,  Eugene J. Trybulski ,  Armin Walser

    IPC分类号： C07C45/63 ,  C07C45/68 ,  C07C45/71 ,  C07C65/34 ,  C07C291/04 ,  C07C309/66 ,  C07D209/48 ,  C07D223/16 ,  C07D239/42 ,  C07D317/16 ,  C07D317/30 ,  C07D487/04

    CPC分类号： C07D209/48 ,  C07C291/04 ,  C07C309/66 ,  C07C45/63 ,  C07C45/68 ,  C07C45/71 ,  C07C65/34 ,  C07D223/16 ,  C07D239/42 ,  C07D317/16 ,  C07D317/30 ,  C07D487/04

    摘要： There is presented compounds of the formula ##STR1## wherein A is selected from the group consisting of ##STR2## R.sub.1 is selected from the group consisting of hydrogen, chlorine, bromine, lower alkyl, the group NR.sub.4 R.sub.5, the group --CH.sub.2 --CO--R.sub.7, the group--NH(CH.sub.2).sub.m NR.sub.8 R.sub.9, hydroxy, lower alkoxy, mercapto and lower alkyl mercapto; R.sub.2 is selected from the group consisting of hydrogen, amino and dilower alkyl amino; R.sub.3 is selected from the group consisting of hydrogen, lower acyloxy and hydroxy; X is selected from the group consisting of hydrogen, halogen, trifluoromethyl, ethyl, .alpha.-hydroxy ethyl and acetyl; Y is hydrogen or halogen; R.sub.4 and R.sub.5 are hydrogen or lower alkyl or together with their co-bonded nitrogen atom form a five to seven membered heterocyclic group; R.sub.7 is selected from the group consisting of hydroxy lower alkoxy and NR.sub.8 R.sub.9 ; R.sub.8 and R.sub.9 are hydrogen or lower alkyl; n is 0 or 1 and m is 1 to 7 with the limitations that (1) at least one of R.sub.1 and R.sub.2 are hydrogen, (2) when R.sub.3 is lower acyloxy or hydroxy, A is the group (a), X is hydrogen, halogen, trifluoromethyl, ethyl or acetyl and R.sub.1 is the group --NH(CH.sub.2).sub.m NR.sub.8 R.sub.9, then R.sub.8 and R.sub.9 are lower alkyl, (3) when A is group (d) and R.sub.1 is the group --NH(CH.sub.2).sub.m NR.sub.8 R.sub.9 then R.sub.8 and R.sub.9 are lower alkyl and (4) when n is 1, R.sub.1 is hydrogen, lower alkyl, lower alkoxy, chlorine, bromine or the group --CH.sub.2 --CO-- R.sub.7 with R.sub.7 as above then A is the group (a) or (b) and the pharmaceutically acceptable salts thereof.The compounds exhibit pharmacological activity as anxiolytics and sedatives.Also presented Are various novel intermediates and processes to produce the above end products.

    摘要翻译： 提供式IMA的化合物，其中A选自由下列组成的组：R 1选自氢，氯，溴，低级烷基，NR 4 R 5基团，基团 -CH 2 -CO-R 7，基团-NH（CH 2）m NR 8 R 9，羟基，低级烷氧基，巯基和低级烷基巯基; R2选自氢，氨基和二元烷基氨基; R3选自氢，低级酰氧基和羟基; X选自氢，卤素，三氟甲基，乙基，α-羟基乙基和乙酰基; Y是氢或卤素; R4和R5是氢或低级烷基，或与它们的共键键合的氮原子一起形成5至7元杂环基; R7选自羟基低级烷氧基和NR8R9; R8和R9是氢或低级烷基; n为0或1，m为1至7，限制为（1）R 1和R 2中的至少一个为氢，（2）当R3为酰氧基或羟基时，A为（a），X为氢 ，卤素，三氟甲基，乙基或乙酰基，R 1为基团-NH（CH 2）m NR 8 R 9，则R 8和R 9为低级烷基，（3）当A为基团（d）且R 1为基团-NH（CH 2）m NR 8 R 9时 R8和R9为低级烷基，（4）当n为1时，R1为氢，低级烷基，低级烷氧基，氯，溴或基团-CH2-CO- R7，R7为上述，则A为（a）或 （b）及其药学上可接受的盐。 该化合物显示出作为抗焦虑药和镇静剂的药理活性。 还提出了各种新型中间体和方法来生产上述最终产品。

    Aminosulfonylthiadiazolylureas
    67.
    发明授权
    Aminosulfonylthiadiazolylureas 失效
    氨基磺酰基噻二唑基脲

    公开(公告)号：US4255182A

    公开(公告)日：1981-03-10

    申请号：US128774

    申请日：1980-03-10

    申请人： John Krenzer

    发明人： John Krenzer

    IPC分类号： A01N47/36 ,  C07D285/12 ,  C07D285/135 ,  C07D317/12 ,  C07D317/16 ,  C07D317/28 ,  C07D319/06 ,  C07D339/06 ,  C07D405/12 ,  C07D405/14

    CPC分类号： C07D285/135 ,  A01N47/36 ,  C07D317/12 ,  C07D317/16 ,  C07D317/28 ,  C07D319/06 ,  C07D339/06

    摘要： Disclosed are compounds of the formula ##STR1## wherein R.sup.1 is alkyl, R.sup.2 is selected from the group consisting of hydrogen and alkyl; or R.sup.1 and R.sup.2 together with the nitrogen atom form a cyclic ring structure having 4 or 5 carbon atoms; m is the integer 0 or 1; when m is 1, R.sup.4 and R.sup.5 are each independently selected from the group consisting of hydrogen and alkyl or up to 3 carbon atoms; when m is 0, R.sup.4 is hydrogen and R.sup.5 is the same as defined above; R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.9 are each independently selected from the group consisting of hydrogen and alkyl; n is an integer from 0 to 2; and Z.sup.1 and Z.sup.2 are each independently selected from the group consisting of oxygen and sulfur. These compounds are useful as herbicides.

    摘要翻译： 公开了式IMA的化合物，其中R 1是烷基，R 2选自氢和烷基; 或者R1和R2与氮原子一起形成具有4或5个碳原子的环状结构; m是整数0或1; 当m为1时，R 4和R 5各自独立地选自氢和烷基或至多3个碳原子; 当m为0时，R 4为氢，R 5为上述定义。 R3，R6，R7，R8，R9各自独立地选自氢和烷基; n为0〜2的整数; Z 1和Z 2各自独立地选自氧和硫。 这些化合物可用作除草剂。