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    CYCLIC HYDRAZINE DERIVATIVES AS TNF-ALPHA INHIBITORS
    7.
    发明申请
    CYCLIC HYDRAZINE DERIVATIVES AS TNF-ALPHA INHIBITORS 审中-公开
    循环盐酸衍生物作为TNF-ALPHA抑制剂

    公开(公告)号：WO00035885A1

    公开(公告)日：2000-06-22

    申请号：PCT/EP1999/009423

    申请日：1999-12-02

    IPC: A61K31/4166 ,  A61K31/4184 ,  A61K31/433 ,  A61K31/438 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/513 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  A61K31/549 ,  A61P7/00 ,  A61P7/04 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P19/02 ,  A61P29/00 ,  A61P31/04 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  C07D233/34 ,  C07D233/38 ,  C07D233/80 ,  C07D233/84 ,  C07D233/86 ,  C07D233/96 ,  C07D235/02 ,  C07D239/22 ,  C07D239/54 ,  C07D239/96 ,  C07D241/08 ,  C07D249/12 ,  C07D251/34 ,  C07D253/06 ,  C07D285/10 ,  C07D285/18 ,  C07D401/06 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D495/04 ,  A61K31/395

    CPC classification number: 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

    Abstract: Hydrazine derivatives of formula (I) wherein W represents O, S, CO, NR , (CR R )m, or CR ; X represents CO, NR , (CH2)n, CR or CHR ; Y represents CO, NR , (CH2)p, or CHR ; Z represents CO, CS, SO2, or CH2; m stands for 0 or 1; n and p each individually stand for 0, 1, or 2; R represents lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl or aryl-lower alkyl; R represents lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl or a group of the formula V-aryl, V-heterocyclyl or -(CH2)q-CH=CR R ; R , R , R , R and R 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 and R together with the carbon atom to which they are attached form a 3- to 8-membered ring; or R and R or R and R together with the nitrogen atoms to which they are attached form a 3- to 8-membered ring; or R and R together with the sp carbon atoms to which they are attached form a fused lower cycloalkenyl, aryl or heteroaryl ring; or R with either R or R together represent lower alkylene in which a CH2 group is optionally replaced by a heteroatom; or either R or R with either R or R together represent lower alkylene in which a CH2 group is optionally replaced by a heteroatom; or R and R together represent lower alkylene in which a CH2 group is optionally replaced by a heteroatom; V represents a spacer group; R and R together represent lower alkylene in which a CH2 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 , NR and NR , respectively; and pharmaceutically acceptable salts thereof inhibit the release of tumour necrosis factor alpha (TNF- alpha ) 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.

    Abstract translation: 式（I）的肼衍生物，其中W表示O，S，CO，NR 5，（CR 3 R 4）m或CR 11; X表示CO，NR 6，（CH 2）n，CR 12或CHR 13; Y表示CO，NR 7，（CH 2）p或CHR 14; Z表示CO，CS，SO2或CH2; m代表0或1; n和p各自分别代表0,1或2; R 1表示低级烷基，低级烯基，低级环烷基，低级环烷基 - 低级烷基，芳基或芳基 - 低级烷基; R 2表示低级烷基，低级烯基，低级环烷基，低级环烷基 - 低级烷基或式V-芳基，V-杂环基或 - （CH 2）q -CH = CR 8 R 9的基团。 R 3，R 4，R 5，R 6和R 7各自独立地表示氢，任选取代的低级烷基，低级烯基，低级环烷基，低级环烷基 - 低级烷基，芳基，芳基 - 低级烷基，杂环基或杂环基 - 低级烷基; 或R 3和R 4与它们所连接的碳原子一起形成3至8元环; 或R 5和R 6或R 5和R 7与它们所连接的氮原子一起形成3-至8-元环; 或R 11和R 12与它们所连接的sp 2碳原子一起形成稠合的低级环烯基，芳基或杂芳基环; 或R 5与R 13或R 14一起代表低级亚烷基，其中CH2基团任选被杂原子取代; 或R 6或R 7与R 3或R 4一起代表低级亚烷基，其中CH2基团任选被杂原子取代; 或R 3和R 4一起代表其中CH2基团任选被杂原子取代的低级亚烷基; V表示间隔基; R 8和R 9一起代表其中CH2基团任选被杂原子取代的低级亚烷基; q代表1或2; 条件是（i）W，X和Y中的至少一个表示先前对这些取代基或CO表示的杂原子之一，（ii）当W表示O时，Z表示CO或SO 2或CS; （iii）W，X，Y和Z不都是CO，（iv）W，X和Y不分别是NR 5，NR 6和NR 7; 和其药学上可接受的盐抑制肿瘤坏死因子α（TNF-α）从细胞的释放。 它们可以用作药物，特别是用于治疗炎性和自身免疫疾病，骨关节炎，呼吸系统疾病，肿瘤，恶病质，心血管疾病，发热，出血和败血症。

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