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    Heterocyclic derivatives
    5.
    发明公开
    Heterocyclic derivatives 失效
    杂环衍生物

    公开(公告)号：EP0071434A2

    公开(公告)日：1983-02-09

    申请号：EP82303911.0

    申请日：1982-07-23

    申请人： GLAXO GROUP LIMITED

    发明人： Hayes, Roger ,  Bays, David Edmund ,  Mackinnon, John Wilson Macfarlane ,  Carey, Linda ,  Blatcher, Philip

    IPC分类号： C07C129/14 ,  C07D401/06 ,  C07D249/14 ,  C07D239/46 ,  C07D471/04 ,  C07D257/06 ,  C07C93/14 ,  C07C93/187

    CPC分类号： C07D239/47 ,  C07C279/28 ,  C07D249/14 ,  C07D257/06 ,  C07D295/096 ,  C07D401/06 ,  C07D471/04

    摘要： The invention relates to compounds of the general formula (I)
    and physiologically acceptable salts, hydrates and bioprecursors thereof, in which

    R 1 represents hydrogen, C 1-14 alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, trifluoroalkyl, heteroaralkyl or alkyl substituted by cycloalkyl, hydroxy, alkoxy, amino, alkylamino or dialkylamino; and
    R 2 represents hydrogen or C 1-4 alkyl group;
    or R 1 and R 2 together with the nitrogen atom to which they are attached form a 5 to 10 membered ring which may be saturated or may contain at least one double bond, may be unsubstituted or may be substituted by one or more C 1-3 alkyl groups or a hydroxy group and/or may contain another heteroatom selected from oxygen or sulphur:
    Alk represents a straight or branched alkylene chain of 1 to 3 carbon atoms;
    Q represents a benzene ring in which incorporation into the rest of the molecule is through bonds at the 1- and 3- or 1-and 4- positions:
    R 5 represents hydrogen or acyl;
    n and m, which may be the same or different, are each 1 or 2; Z represents one of the groups
    where X represents NCN, NS0 2 Methyl, NS0 2 Phenyl or CHNO 2 ;
    R 8 represents alkyl;
    A represents N and B represents CR 7 ; or
    A represents CR 7 and B represents N; or
    A and B both represent N;
    R 3 represents hydrogen, alkyl, alkenyl, aralkyl, hydroxy C 2-6 alkyl, alkoxy C 2-6 alkyl or C 1-4 alkanoyloxy C 2-6 alkyl;
    R 7 represents hydrogen, alkyl, alkenyl, aralkyl, acyloxyalkyl, alkylthioalkyl, arylthioalkyl, aryloxyalkyl, aralkyloxyalkyl, or the group (CH 2 ) q R 8 where q is zero, 1, 2, 3, 4, or 6 and the alkylene chain (CH 2 ) q may be straight or branched, and
    R 6 is hydroxy, alkoxy, nitro, heteroaryl, tetrahydropyranyloxy or CH 2 NHC(=X)NHR 9 where X is as defined above, and R 9 is alkyl;
    or R 6 is the group NR 10 R 11 , where R 10 is hydrogen or alkyl; and R 11 is hydrogen, alkyl, alkenyl, aryl, aralkyl, or heteroaralkyl, or R 11 is the group SO 2 R 12 where R 12 is alkyl or aryl; or R 11 is the group COR 13 where R, 3 is hydrogen, alkyl, aryl, aralkyl, alkoxy, halomethyl, heteroaryl, heteroaralkyl or the group NHR 14 where R 14 is hydrogen, alkyl, cycloalkyl, aryl or aralkyl; or R 10 and R 11 together represent the group =CR 15 R 16 where R 15 represents aryl or heteroaryl and R 16 represents hydrogen or alkyl;
    or R 6 is the group SO 2 R 17 in which R 17 is hydroxy, alkyl, aryl or the group NR 18 R 19 where R, s and R 19 , which may be the same or different, each represent hydrogen or alkyl;
    or R 6 is the group COR20 where R 20 is hydrogen, hydroxy, alkoxy, aryloxy, aralkyloxy, alkyl, aryl, aralkyl or the group NRZ 21 R 22 where R 21 is hydrogen or alkyl optionally substituted by a hydroxy or alkoxy group; and R 22 is hydrogen, alkyl (optionally substituted by a hydroxy or alkoxy group), alkenyl, aryl, aralkyl or cycloalkyl, or NR 21 R 22 forms a 5 to 8 membered ring which may contain another heteroatom, e.g. oxygen, or a double bond and/or may be substituted by hydroxy or one or two C 1-3 alkyl groups; or R 6 is the group CR 23 =NR 24 where R23 is hydrogen, alkyl, aryl or aralkyl and R 24 is hydroxy, alkoxy, aralkyloxy or -NHC(=Y)NH 2 where Y is oxygen or sulphur;
    or when A represents CR 7 and B represents N, the groups R 3 and R 7 taken together represent (̵ CH=CH )̵ 2 or - (CH 2 ) 4 ;
    with the proviso that when the group R 6 contains a carbon atom through which it is linked to the alkylene group (CH 2 )q then the total number of carbon atoms in the resulting chain is not greater than 6 (i.e. q is not greater than 5);
    R 4 represents phenyt, phenoxy or pyridinyl which may optionally be substituted by one or more halogen, alkyl, alkoxyalkyl or alkoxy groups or by a methylenedioxy group;
    p represents an integer which is 1, 2 or 3;
    The compounds show pharmacological activity as selective histamine H 2 -antagonists.

    摘要翻译： 本发明涉及通式（I）的化合物及其生理学上可接受的盐，水合物和生物前体，其中R 1表示氢，C 1-4烷基，环烷基，烯基，炔基，芳烷基，三氟烷基，杂芳烷基或烷基取代的 羟基，烷氧基，氨基，烷基氨基或二烷基氨基; 并且R 2表示氢或C 1-4烷基; 或R 1和R 2与它们所连接的氮原子一起形成5至10元环，其可以是饱和的或可以含有至少一个双键，可以是未取代的或可以被一个或多个C 1-3烷基取代 或羟基和/或可以含有选自氧或硫的其它杂原子：Alk表示1至3个碳原子的直链或支链亚烷基链; Q表示苯环，其中分子的其余部分通过1-和3-或1-和4-位上的键连接：R5表示氢或酰基; n和m可以相同或不同，各自为1或2; Z表示之一，其中X表示NCN，NSO 2甲基，NSO 2苯基或CHNO 2; R8代表烷基; A表示N，B表示CR7; 或A表示CR7，B表示N; 或A和B均表示N; R3表示氢，烷基，烯基，芳烷基，羟基C2-6烷基，烷氧基C2-6烷基或C1-4烷酰氧基C2-6烷基;