Phenylpiperazine derivatives and their acid addition salts
    1.
    发明授权
    Phenylpiperazine derivatives and their acid addition salts 失效
    苯基哌嗪衍生物及其酸加成盐

    公开(公告)号:US4716161A

    公开(公告)日:1987-12-29

    申请号:US719456

    申请日:1985-04-03

    摘要: A phenylpiperazine derivative according to the present invention has the following general formula [I]: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen or alkoxy group having 1 to 3 carbon atoms, orR.sup.1 and R.sup.2 or R.sup.2 and R.sup.3 together with carbon atoms to which they are attached form --O(CH.sub.2).sub.m O-- wherein m is an integer of 1 to 3, oreither R.sup.1 or R.sup.2 is amine residue selected from the group consisting of --NH.sub.2 , --NHSO.sub.2 CH.sub.3, --NHCOCH.sub.3 and --NHCONH.sub.2 and the other is hydrogen or alkoxy group of 1 to 3 carbon atoms and R.sup.3 is hydrogen;R.sup.4 and R.sup.5 are independently hydrogen or alkyl group of 1 to 3 carbon atoms;Y is --CO-- or --SO.sub.2 -- provided that at least one of R.sup.1 and R.sup.2 is not hydrogen when Y is --CO--; andn is an integer of 2 to 4.An acid addition salt of the phenylpiperazine derivative having the general formula [I] is included in the present invention. The phenylpiperazine derivative as well as its acid addition salt according to the present invention have the ability to reduce the blood pressure.

    摘要翻译: 根据本发明的苯基哌嗪衍生物具有以下通式[I]:其中R 1,R 2和R 3独立地是氢或具有1至3个碳原子的烷氧基,或者R 1和R 2或R 2和R 3 与其连接的碳原子一起形成-O(CH 2)m O-,其中m是1至3的整数,或者R 1或R 2是选自-NH 2,-NHSO 2 CH 3,-NHCOCH 3和 -NHCONH 2,另一个是1或3个碳原子的氢或烷氧基,R 3是氢; R4和R5独立地是氢或1〜3个碳原子的烷基; Y是-CO-或-SO 2 - ,条件是当Y是-CO-时,R 1和R 2中的至少一个不是氢; n为2〜4的整数。本发明包括具有通式[I]的苯基哌嗪衍生物的酸加成盐。 根据本发明的苯基哌嗪衍生物及其酸加成盐具有降低血压的能力。

    Piperazine derivatives and their acid addition salts
    2.
    发明授权
    Piperazine derivatives and their acid addition salts 失效
    哌嗪衍生物及其酸加成盐

    公开(公告)号:US4613598A

    公开(公告)日:1986-09-23

    申请号:US708641

    申请日:1985-03-06

    摘要: A piperazine derivative according to the present invention has the following general formula [I]: ##STR1## wherein R.sup.1 is --OH, --OR.sup.3, --SR.sup.3, --SOR.sup.3 or --SO.sub.2 R.sup.3 wherein R.sup.3 is alkyl group having 1 to 3 carbon atoms;R.sup.2 is --SO.sub.2 NH.sub.2, --SO.sub.2 NHR.sup.4, --SO.sub.2 NR.sup.4 R.sup.5, --COOH, --COOR.sup.4, --CONH.sub.2, --CONHR.sup.4, --CONR.sup.4 R.sup.5, --NHCONH.sub.2, --NHCSNH.sub.2, --NHCONHR.sup.4, --NHCOR.sup.4 or --NHSO.sub.2 R.sup.4 wherein R.sup.4 and R.sup.5 are independently alkyl group having 1 to 3 carbon atoms; orR.sup.1 and R.sup.2 together with carbon atoms to which they are attached form ##STR2## Z is --CO-- or --CH(OH)--; Ar is pyridyl or substituted or unsubstituted phenyl; andn is an integer of 3 to 5.An acid addition salt of the piperazine derivative having the above formula [I] is included in the present invention. The piperazine derivative as well as its acid addition salt according to the present invention have the ability to reduce the blood pressure.

    摘要翻译: 根据本发明的哌嗪衍生物具有以下通式[I]:其中R 1是-OH,-OR 3,-SR 3,-SOR 3或-SO 2 R 3,其中R 3是具有1至3个碳原子的烷基 原子 R2是-SO2NH2,-SO2NHR4,-SO2NR4R5,-COOH,-COOR4,-CONH2,-CONHR4,-CONR4R5,-NHCONH2,-NHCSNH2,-NHCONHR4,-NHCOR4或-NHSO2R4,其中R4和R5独立地为具有1 至3个碳原子; 或R 1和R 2与它们所连接的碳原子一起形成Z是-CO-或-CH(OH) - ; Ar为吡啶基或取代或未取代的苯基; n为3〜5的整数。上述式[I]的哌嗪衍生物的酸加成盐包括在本发明中。 根据本发明的哌嗪衍生物及其酸加成盐具有降低血压的能力。