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    PIPERAZINE COMPOUNDS
    1.
    发明申请
    PIPERAZINE COMPOUNDS 审中-公开
    哌嗪化合物

    公开(公告)号：WO0125219A3

    公开(公告)日：2001-12-13

    申请号：PCT/EP0009722

    申请日：2000-10-05

    申请人： GLAXO GROUP LTD ,  ALVARO GIUSEPPE ,  FABIO ROMANO DI ,  GIOVANNINI RICCARDO ,  GUERCIO GIUSEPPE ,  ST DENIS YVES ,  URSINI ANTONELLA

    发明人： ALVARO GIUSEPPE ,  DI FABIO ROMANO ,  GIOVANNINI RICCARDO ,  GUERCIO GIUSEPPE ,  ST-DENIS YVES ,  URSINI ANTONELLA

    IPC分类号： A61K31/495 ,  A61K31/496 ,  A61P1/04 ,  A61P11/06 ,  A61P25/04 ,  A61P25/06 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P29/00 ,  C07D241/04 ,  C07D401/06 ,  C07D403/06

    CPC分类号： C07D401/06 ,  A61K31/135 ,  A61K31/196 ,  A61K31/495 ,  A61K31/496 ,  C07D241/04 ,  C07D403/06 ,  A61K2300/00

    摘要： The present invention relates to piperazine derivatives of formula (I) wherein R represents a halogen atom or a C1-4 alkyl group; R1 represents hydrogen or a C1-4 alkyl group; R2 represents hydrogen, a C1-4 alkyl, C2-6 alkenyl or a C3-7 cycloalkyl group; or R1 and R2 together with nitrogen and carbon atom to which they are attached respectively represent a 5-6 membered heterocyclic group; R3 represents a trifluoromethyl, a C1-4 alkyl, a C1-4 alkoxy, a trifluoromethoxy or a halogen group; R4 represents hydrogen, a (CH2)qR7 or a (CH2)rCO(CH2)pR7 group; R5 represents hydrogen, a C1-4 alkyl or a COR6 group; R6 represents hydrogen, hydroxy, amino, methylamino, dimethylamino a 5 membered heteroaryl group containing 1 to 3 heteroatoms selected from oxygen, sulphur and nitrogen or a 6 membered heteroaryl group containing 1 to 3 nitrogen atoms; R7 represents hydrogen, hydroxy or NR8R9 wherein R8 and R9 represent independently hydrogen or C1-4 alkyl optionally substituted by hydroxy, or by amino; R10 represents hydrogen, a C1-4 alkyl I group or R10 together with R2 represents a C3-7 cycloalkyl group; m is zero or an integer from 1 to 3; n is zero or an integer from 1 to 3; both p and r are independently zero or an integer from 1 to 4; q is an integer from 1 to 4; provided that, when R1 and R2 together with nitrogen and carbon atom to which they are attached respectively represent a 5 to 6 membered heterocyclic group, i) m is 1 or 2; ii) when m is 1, R is not fluorine and iii) when m is 2, the two substituents R are not both fluorine,and pharmaceutically acceptable salts and solvates thereof.

    摘要翻译： 本发明涉及式（I）的哌嗪衍生物，其中R表示卤素原子或C1-4烷基; R1表示氢或C1-4烷基; R 2表示氢，C 1-4烷基，C 2-6烯基或C 3-7环烷基; 或R 1和R 2与它们所连接的氮原子和碳原子分别表示5-6元杂环基; R3表示三氟甲基，C1-4烷基，C1-4烷氧基，三氟甲氧基或卤素基团; R4表示氢，（CH2）qR7或（CH2）rCO（CH2）pR7基团; R5代表氢，C1-4烷基或COR6基团; R 6表示氢，羟基，氨基，甲基氨基，二甲基氨基，含有1至3个选自氧，硫和氮的杂原子或含有1至3个氮原子的6元杂芳基的5元杂芳基; R 7表示氢，羟基或NR 8 R 9，其中R 8和R 9独立地表示氢或任选被羟基取代的C 1-4烷基或氨基; R 10表示氢，C 1-4烷基I基或R 10与R 2一起代表C 3-7环烷基; m为0或1〜3的整数; n为0或1〜3的整数; p和r分别独立为零或1至4的整数; q是1至4的整数; 条件是当R1和R2与它们所连接的氮原子和碳原子分别表示5至6元杂环基时，i）m为1或2; ii）当m为1时，R不为氟，iii）当m为2时，两个取代基R不同时为氟，其药学上可接受的盐和溶剂化物。