Process for the preparation of dibenzothiepin derivative
    13.
    发明授权
    Process for the preparation of dibenzothiepin derivative 失效
    二苯并噻吩衍生物的制备方法

    公开(公告)号:US4891433A

    公开(公告)日:1990-01-02

    申请号:US102981

    申请日:1987-09-30

    IPC分类号: C07C323/62 C07D337/14

    CPC分类号: C07C323/62 C07D337/14

    摘要: A novel process for the preparation of 2-(10,11-dihydro-10-oxodibenzo[b, f]thiepin-2-yl)propionic acid which shows high anti-inflammatory and analgetic action is disclosed. The process starts from a propiophenone derivative having the formula (II): ##STR1## wherein R.sup.1 is hydrogen or a lower alkyl group, which is once converted into a haloacetal compound via a halo-ketone compound, and then converted into the desired dibenzothiepin derivative through a combination of rearrangement, hydrolysis and ring closure in variable sequences.

    摘要翻译: 公开了一种制备显示出高抗炎和止痛作用的2-(10,11-二氢-10-氧代二苯并[b,f]硫杂-2-基)丙酸的新方法。 该方法从具有式(II)的苯丙酮衍生物开始:其中R1是氢或低级烷基,其通过卤代酮化合物一度转化为卤代缩醛化合物,然后转化为 通过可变序列的重排,水解和闭环的组合,所需的二苯并噻吩衍生物。

    Amino-alcohol derivatives and processes for their preparation
    15.
    发明授权
    Amino-alcohol derivatives and processes for their preparation 失效
    氨基醇衍生物及其制备方法

    公开(公告)号:US5250546A

    公开(公告)日:1993-10-05

    申请号:US551037

    申请日:1990-07-11

    IPC分类号: C07D295/13 A61K31/445

    CPC分类号: C07D295/13

    摘要: Amino-alcohol derivatives of the formula, ##STR1## where R.sub.1 is a straight or branched alkyl group having 3 to 8 carbon atoms, R.sub.2 and R.sub.3 are each a lower alkyl group, or R.sub.2 and R.sub.3 form a 5- to 7-membered ring together with the adjacent nitrogen atom which may have an oxygen atom attached thereto, R.sub.4 is a hydrogen atom or a lower alkyl group, R.sub.5 is a hydrogen atom or a lower alkyl group, X is a hydrogen or halogen atom or a lower alkyl or lower alkoxy group, and n is an integer of 2 or 3, and acid addition salts thereof, are effectively useful as medicines and agricultural chemicals. Processes are also disclosed for preparing such compounds.

    摘要翻译: 其中R1是具有3至8个碳原子的直链或支链烷基,R2和R3各自为低级烷基,或R2和R3形成5-至7-元环的下式的氨基醇衍生物, 与可能具有氧原子的相邻氮原子一起,R4是氢原子或低级烷基,R5是氢原子或低级烷基,X是氢或卤素原子或低级烷基或低级烷基 烷氧基,n为2或3的整数,其酸加成盐可有效用作药物和农药。 还公开了制备这些化合物的方法。

    Glycerol derivative and anti-hypertensive agent
    16.
    发明授权
    Glycerol derivative and anti-hypertensive agent 失效
    甘油衍生物和抗高血压药

    公开(公告)号:US5183811A

    公开(公告)日:1993-02-02

    申请号:US554343

    申请日:1990-07-19

    摘要: A novel glycerol derivative which is effective to reduce blood pressure has the formula: ##STR1## wherein R.sup.1 is an alkyl group having 10-22 carbon atoms, R.sup.2 is lower acyl, benzoyl, aryl, mono-, di- or triarylalkyl, alkyl, cycloalkyl, or cycloalkylalkyl; Q is substituted or unsubstituted alkylene containing 1-4 carbon atoms, l is 0 or 1; Y is a nitrogen-containing heterocyclic group or a nitrogen-containing bridged heterocyclic group (--(Q).sub.l -- is attached to a carbon atom contained in a hetero-ring of the heterocyclic group) in which Y is the bridged heterocyclic group where l is 0; and each of R.sup.5, R.sup.6 and R.sup.7 is hydrogen, lower alkyl, aryl or aralkyl.

    摘要翻译: 有效降低血压的新型甘油衍生物具有下式:其中R1是具有10-22个碳原子的烷基,R2是低级酰基,苯甲酰基,芳基,单 - ,三 - 芳基烷基,烷基, 环烷基或环烷基烷基; Q是取代或未取代的含有1-4个碳原子的亚烷基,l是0或1; Y是含氮杂环基或含氮桥接杂环基( - (Q)1-连接到杂环基杂环中含有的杂原子上的碳原子),其中Y是桥连杂环基,其中l 是0; R 5,R 6和R 7各自为氢,低级烷基,芳基或芳烷基。

    Process for protection of brain cells
    18.
    发明授权
    Process for protection of brain cells 失效
    保护脑细胞的过程

    公开(公告)号:US4835155A

    公开(公告)日:1989-05-30

    申请号:US87408

    申请日:1987-08-20

    CPC分类号: A61K31/495

    摘要: A process for protection of brain cells comprises orally or parenterally administering into a man suffering from ischemia or being susceptable to ischemia a piperazine derivative having the formula: ##STR1## wherein R.sup.1 is hydrogen or a lower alkyl group, R.sup.2 is hydroxyl, an aralkyloxy group, a lower alkoxy group having 1-5 carbon atoms or a lower alkenyloxy group having 3-5 carbon atoms, R.sup.3 is hydrogen, an aralkyloxy group, a lower alkoxy group having 1-5 carbon atoms or a lower alkenyloxy group having 3-5 carbon atoms and R.sup.4 is hydrogen or a lower alkoxy group having 1-5 carbon atoms.

    摘要翻译: 保护脑细胞的方法包括口服或肠胃外给予患有缺血或易于缺血的人具有下式的哌嗪衍生物:其中R 1是氢或低级烷基,R 2是羟基,芳烷氧基 ,具有1-5个碳原子的低级烷氧基或具有3-5个碳原子的低级烯氧基,R3是氢,芳烷氧基,具有1-5个碳原子的低级烷氧基或具有3-5个碳原子的低级烯氧基 碳原子,R 4是氢或具有1-5个碳原子的低级烷氧基。