Piperidine derivatives, and their application in therapy
    11.
    发明授权
    Piperidine derivatives, and their application in therapy 失效
    哌啶衍生物及其在治疗中的应用

    公开(公告)号:US4853387A

    公开(公告)日:1989-08-01

    申请号:US223076

    申请日:1988-07-22

    IPC分类号: C07D401/12

    CPC分类号: C07D401/12

    摘要: A compound which is a piperidine derivative of formula (I) ##STR1## in which: n is 1, 2, 3 or 4,R is hydrogen or a halogen,R', which is identical to R, is hydrogen or a halogen,either R.sub.1 is H or OH and R.sub.2 is H, or R.sub.1 and R.sub.2 together denote a bond,R.sub.3 is hydrogen or (C.sub.1-4) alkyl, andR.sub.4 is H or OH,including tautomeric forms thereof, or a pharmaceutically acceptable acid addition salt thereof.

    摘要翻译: 作为式(I)的哌啶衍生物的化合物其中:n为1,2,3或4,R为氢或卤素,与R相同的R'为氢或 卤素,R 1是H或OH,R 2是H,或者R 1和R 2一起表示键,R 3是氢或(C 1-4)烷基,R 4是H或OH,包括其互变异构形式或药学上可接受的 其酸加成盐。

    1-Phenylpiperazines
    18.
    发明授权
    1-Phenylpiperazines 失效
    1-苯基哌嗪

    公开(公告)号:US4267328A

    公开(公告)日:1981-05-12

    申请号:US61245

    申请日:1979-07-27

    摘要: Phenylpiperazine derivatives having the general formula (I) ##STR1## in which R.sub.1 represents a radical S(O).sub.m R.sub.3, S(O).sub.n CF.sub.3 or ##STR2## in which radicals m is 0, 1 or 2, n is 1 or 2, R.sub.3 is an alkyl radical having 1 to 10 carbon atoms and R.sub.4 and R.sub.5 independently represent a hydrogen atom or an alkyl radical having 1 to 4 carbon atoms, or the N atom, R.sub.4 and R.sub.5 together form a heterocyclic ring, which can contain another hetero-atom, and R.sub.2 represents a hydrogen atom, the radical CH.sub.2 --CH.sub.2 --OH or a radical of formula CH.sub.2 --CH.sub.2 --O--COR.sub.6, CH.sub.2 --CH.sub.2 --O--CONHR.sub.6 or CH.sub.2 --CH.sub.2 --O--R.sub.6 in which radicals R.sub.6 being an alkyl radical having 1 to 6 carbon atoms and their pharmaceutically acceptable acid addition salts are useful psychotropic agents and analgesics. Compounds in which R.sub.1 is --SCH.sub.3 and simultaneously R.sub.2 is H are not part of the invention. These derivatives can be prepared by reacting an aniline derivative of formula ##STR3## with a compound of formula ##STR4## in which X represents a halogen atom or OH, alkyl--SO.sub.3 or aryl--SO.sub.3 group or the two X symbols together represent a divalent oxygen atom, thereby completing a morpholine ring.

    摘要翻译: 具有通式(I)的化合物(I)其中R 1表示基团S(O)m R 3,S(O)n CF 3或者其中基团m为0,1或2的基团,n为1 或2,R3是具有1-10个碳原子的烷基,R4和R5独立地表示氢原子或具有1至4个碳原子的烷基,或者N原子,R4和R5一起形成杂环,其可以 含有另一个杂原子,R 2表示氢原子,基团CH 2 -CH 2 -OH或式CH 2 -CH 2 -O-COR 6,CH 2 -CH 2 -O-CONHR 6或CH 2 -CH 2 -O-R 6的基团,其中 基团R6是具有1至6个碳原子的烷基,其药学上可接受的酸加成盐是有用的精神药物和镇痛药。 其中R 1为-SCH 3且同时为R 2的化合物不是本发明的一部分。 这些衍生物可以通过使式(I)的苯胺衍生物与其中X表示卤素原子或OH,烷基-SO 3或芳基-SO 3基团的式(III)化合物或式 X符号一起表示二价氧原子,从而完成吗啉环。

    2-aminopyrimidine-4-carboxamide derivatives, their preparaton and their
application in therapy
    19.
    发明授权
    2-aminopyrimidine-4-carboxamide derivatives, their preparaton and their application in therapy 失效
    2-氨基嘧啶-4-羧酰胺衍生物及其制剂及其在治疗中的应用

    公开(公告)号:US5229392A

    公开(公告)日:1993-07-20

    申请号:US872028

    申请日:1992-04-23

    CPC分类号: C07D239/42

    摘要: A compound which is a 2-aminopyrimidine-4-carboxamide derivative represented by general formula (I) ##STR1## in which m represents 2 or 3,n represents 2 or 3,R.sub.1 represents hydrogen or methyl, andX represents a substituent selected from the group consisting of hydrogen, fluorine, chlorine, methoxy, ethoxy, methyl and 1-methylethyl, with the proviso that more than one substituent X may be present in which case each X may be the same or different, or a pharmaceutically acceptable acid addition salt thereof.

    摘要翻译: 作为通式(I)表示的2-氨基嘧啶-4-甲酰胺衍生物的化合物,其中m表示2或3,n表示2或3,R 1表示氢或甲基,X表示 选自氢,氟,氯,甲氧基,乙氧基,甲基和1-甲基乙基的取代基,条件是可以存在多于一个取代基X,在这种情况下,每个X可以相同或不同,或药学上 其可接受的酸加成盐。