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    CYCLIC HYDRAZINE DERIVATIVES AS TNF-ALPHA INHIBITORS
    82.
    发明授权
    CYCLIC HYDRAZINE DERIVATIVES AS TNF-ALPHA INHIBITORS 有权
    骑行肼TNF-α抑制剂

    公开(公告)号：EP1137640B1

    公开(公告)日：2005-09-21

    申请号：EP99965432.0

    申请日：1999-12-02

    申请人： F. HOFFMANN-LA ROCHE AG

    发明人： BROADHURST, Michael John ,  JOHNSON, William Henry ,  WALTER, Daryl Simon

    IPC分类号： C07D233/80 ,  A61K31/395 ,  C07D239/54 ,  C07D285/18 ,  C07D495/04 ,  C07D233/34 ,  C07D251/34 ,  C07D249/12 ,  C07D241/08 ,  C07D235/02 ,  C07D233/84 ,  C07D471/10 ,  C07D239/96 ,  C07D401/06 ,  C07D233/96 ,  C07D285/10 ,  C07D487/04

    CPC分类号： C07D235/02 ,  C07D233/34 ,  C07D233/80 ,  C07D233/84 ,  C07D233/96 ,  C07D239/54 ,  C07D239/96 ,  C07D241/08 ,  C07D249/12 ,  C07D251/34 ,  C07D285/10 ,  C07D285/18 ,  C07D401/06 ,  C07D471/10 ,  C07D487/04 ,  C07D495/04

    摘要： Hydrazine derivatives of formula (I) wherein W represents O, S, CO, NR?5, (CR3R4)¿m, or CR11; X represents CO, NR6, (CH2)n, CR?12 or CHR13¿; Y represents CO, NR7, (CH2)p, or CHR14; Z represents CO, CS, SO¿2?, or CH2; m stands for 0 or 1; n and p each individually stand for 0, 1, or 2; R?1¿ represents lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl or aryl-lower alkyl; R2 represents lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl or a group of the formula V-aryl, V-heterocyclyl or -(CH¿2?)q-CH=CR?8R9; R3, R4, R5, R6 and R7¿ each independently represent hydrogen, optionally substituted lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl, aryl-lower alkyl, heterocyclyl or heterocyclyl-lower alkyl; or R?3 and R4¿ together with the carbon atom to which they are attached form a 3- to 8-membered ring; or R?5 and R6 or R5 and R7¿ together with the nitrogen atoms to which they are attached form a 3- to 8-membered ring; or R?11 and R12¿ together with the sp2 carbon atoms to which they are attached form a fused lower cycloalkenyl, aryl or heteroaryl ring; or R5 with either R?13 or R14¿ together represent lower alkylene in which a CH¿2? group is optionally replaced by a heteroatom; or either R?6 or R7¿ with either R3 or R4 together represent lower alkylene in which a CH¿2? group is optionally replaced by a heteroatom; or R?3 and R4¿ together represent lower alkylene in which a CH¿2? group is optionally replaced by a heteroatom; V represents a spacer group; R?8 and R9¿ together represent lower alkylene in which a CH¿2? group is optionally replaced by a heteroatom; and q stands for 1 or 2; with the provisos that (i) at least one of W, X and Y represents one of the heteroatoms previously indicated for these substituents or CO, (ii) Z represents CO or SO2 or CS when W represents O; (iii) W, X, Y and Z are not all CO and (iv) W, X and Y are not all NR?5, NR6 and NR7¿, respectively; and pharmaceutically acceptable salts thereof inhibit the release of tumour necrosis factor alpha (TNF-α) from cells. They can be used as medicaments, especially in the treatment of inflammatory and autoimmune diseases, osteoarthritis, respiratory diseases, tumours, cachexia, cardiovascular diseases, fever, haemorrhage and sepsis.