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292 条记录 (耗时 0.034 秒)

    Peptoid compounds
    125.
    发明公开
    Peptoid compounds 有权
    拟肽连接

    公开(公告)号：EP2343285A3

    公开(公告)日：2011-08-10

    申请号：EP11158209.4

    申请日：2002-06-28

    申请人： UNIVERSITY OF WOLLONGONG

    发明人： Bremner, John ,  Pyne, Stephen ,  Keller, Paul ,  Coghlan, Dan ,  Garas, Adel ,  Witchard, Helen ,  Boyle, Tim ,  Coates, Jonathan

    IPC分类号： C07D245/04 ,  C07D255/04 ,  C07D273/08 ,  C07D273/02 ,  C07D487/02 ,  C07D209/18 ,  C07D209/88 ,  C07C233/31 ,  C07K5/06 ,  C07K5/08 ,  C07K5/10 ,  A61K38/12 ,  A61K38/06 ,  A61P31/04 ,  C07D209/86 ,  C07D487/04 ,  C07C229/36 ,  C07C233/47 ,  C07C237/22 ,  C07C251/24

    CPC分类号： C07C229/36 ,  A61K38/00 ,  C07C233/47 ,  C07C237/22 ,  C07C251/24 ,  C07C279/14 ,  C07D209/86 ,  C07D245/04 ,  C07D255/04 ,  C07D273/02 ,  C07D487/04 ,  C07K5/06086 ,  C07K5/06095 ,  C07K5/0812 ,  C07K5/1016

    摘要： A compound of the formula (I):

    wherein
    A is an aromatic or heteroaromatic ring system or partially or fully reduced derivatives thereof;
    Q is hydrogen, C 1 -C 12 straight chain, branched or cyclic alkyl substituted with one or more hydroxy groups, or a mono- or di-saccharide moiety;
    Z is -CR 10 R 11 -, -NR 12 -, -C(O)O-, -C(O)NR 12 - or -O-, where R 10 and R 11 are independently selected from hydrogen, hydroxy, C 1 -C 6 alkyl, C 6 -C 10 aryl, C 1 -C 6 alkoxy and -N(R 13 ) 2 and where each R 13 is independently selected from hydrogen and C 1 -C 6 alkyl, and where R 12 is selected from hydrogen and C 1 -C 6 alkyl; R 1 is selected from hydrogen, hydroxy, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, -NR(R 13 ) 2 and -N(R 12 )-COR 14 ; where R 12 and R 13 are as defined above, and where R 14 is selected from hydrogen, hydroxy, C 1 -C 6 alkyl, C 1 -C 6 alkoxy and -NR 12 ;
    R 2 is selected from hydrogen, hydroxy, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, -N(R 13 ) 2 and -N(R 12 )-COCHR 2a R 2b ; where R 2a and R 2b are selected from hydrogen, hydroxy, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, -N(R 13 ) 2 and -N(R 12 )-COR 14 ; where R 12 , R 13 and R 14 are as defined above;
    R 3 , R 4 and R 5 are independently selected from hydrogen, C 1 -C 6 alkyl and α side chains of α-amino acids or their enantiomers or their derivatives;
    R 6 is -CO 2 R 15 , -CONHR 16 , -CONHOR 16 , -CONHNHR 16 , -SO 2 N(R 16 ) 2 , -SO 2 R 17 or -P(O)(OR 18 )(OR 18 ) where each R 15 , R 16 , R 17 and R 18 is independently selected from hydrogen, C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl, C 6 -C 10 aryl and C 7 -C 10 arylalkyl;
    B is an α-amino acid residue, a β-amino acid residue or an α,α-disubstituted amino acid residue, such residue forming amide linkages with the adjacent molecules;
    W is -O- or CR 10 R 11 where R 10 and R 11 are as defined above;
    Y is an optionally substituted amino group, a moiety containing an optionally substituted amino group or a salt thereof:
    ------ is a single or double bond;
    R 7 and R 8a are hydrogen or are absent if ------ is a double bond; and
    R 8b and R 9 are hydrogen, and X is selected from (CR 10 R 11 ) u , -(CR 10 R 11 ) u -CH=CH-, -NR 12 (CR 10 R 11 ) u -, -(CR 10 R 11 ) u NR 12 -, -O(CR 10 R 11 ) u -, -(CR 10 R 11 ) u O- or -O(CR 10 R 11 )CH=CH- where R 10 , R 11 and R 12 are as defined above; or
    R 8b and R 9 together form a covalent bond between X and the carbon to which R 8b is attached, and X is selected from (CR 10 R 11 ) x , -NR 12 (CR 10 R 11 ) x -, -(CR 10 R 11 ) x NR 12 -, -O(CR 10 R 11 ) x - or -(CR 10 R 11 ) x O-, where R 10 , R 11 and R 12 are as defined above;
    n, m, r and t are independently selected from 0 or 1;
    s is an integer selected from 0 to 3;
    p is an integer selected from 0 to 6, provided that when W is -O-, p is at least 1; and u, x and q are independently selected from 0 to 4;
    and salts and pharmaceutically acceptable derivatives thereof.
    The compound of formula (I) are useful in the treatment of bacterial infections.