会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 5. 发明公开
    • Peptoid compounds
    • Als Antibiotika geeignete peptoide Verbindungen
    • EP2343285A2
    • 2011-07-13
    • EP11158209.4
    • 2002-06-28
    • UNIVERSITY OF WOLLONGONG
    • Bremner, JohnPyne, StephenKeller, PaulCoghlan, DanGaras, AdelWitchard, HelenBoyle, TimCoates, Jonathan
    • C07D245/04C07D255/04C07D273/08C07D273/02C07D487/02C07D209/18C07D209/88C07C233/31C07K5/06C07K5/08C07K5/10A61K38/12A61K38/06A61P31/04
    • C07C229/36A61K38/00C07C233/47C07C237/22C07C251/24C07C279/14C07D209/86C07D245/04C07D255/04C07D273/02C07D487/04C07K5/06086C07K5/06095C07K5/0812C07K5/1016
    • 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.
    • 式(I)的化合物:其中A是芳族或杂芳族环系统或其部分或完全还原的衍生物; Q是氢,C 1 -C 12直链,被一个或多个羟基取代的支链或环状烷基,或单糖或二糖部分; Z是-CR 10 R 11 - , - NR 12 - , - C(O)O-,-C(O)NR 12 - 或-O-,其中R 10和R 11独立地选自氢,羟基,C 1 -C 6烷基,C 6 -C 10芳基,C 1 -C 6烷氧基和-N(R 13)2,并且其中每个R 13独立地选自氢和C 1 -C 6烷基,并且其中R 12是 选自氢和C 1 -C 6烷基; R 1选自氢,羟基,C 1 -C 6烷基,C 1 -C 6烷氧基,-NR(R 13)2和-N(R 12)-COR 14; 其中R 12和R 13如上定义,并且其中R 14选自氢,羟基,C 1 -C 6烷基,C 1 -C 6烷氧基和-NR 12; R 2选自氢,羟基,C 1 -C 6烷基,C 1 -C 6烷氧基,-N(R 13)2和-N(R 12)-COCHR 2a R 2b; 其中R 2a和R 2b选自氢,羟基,C 1 -C 6烷基,C 1 -C 6烷氧基,-N(R 13)2和-N(R 12)-COR 14; 其中R 12,R 13和R 14如上所定义; R 3,R 4和R 5独立地选自氢,C 1 -C 6烷基和± - 氨基酸的±侧链或其对映异构体或其衍生物; R 6是-CO 2 R 15,-CONHR 16,-CONHOR 16,-CONHNHR 16,-SO 2 N(R 16)2,-SO 2 R 17或-P(O)(OR 18)(OR 18) 其中每个R 15,R 16,R 17和R 18独立地选自氢,C 1 -C 6烷基,C 3 -C 7环烷基,C 6 -C 10芳基和C 7 -C 10芳基烷基; B是一个± - 氨基酸残基,一个2-氨基酸残基或一个±, - 二取代的氨基酸残基,这样的残基与相邻分子形成酰胺键; W是-O-或CR 10 R 11,其中R 10和R 11如上所定义; Y是任选取代的氨基,含有任选取代的氨基或其盐的部分: - 是单键或双键; 如果 - 是双键,R 7和R 8a是氢或不存在; 并且R 8b和R 9是氢,X选自(​​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-或-O(CR 10 R 11)CH = CH-,其中R 10,R 11 和R 12如上所定义; 或R 8b和R 9一起在X与连接有R 8b的碳之间形成共价键,X选自(​​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 - 或 - (CR 10 R 11)x O-,其中R 10,R 11和R 12如上所定义; n,m,r和t独立地选自0或1; s为0〜3的整数; p是选自0至6的整数,条件是当W为-O-,p为至少1; 并且u,x和q独立地选自0至4; 及其盐和药学上可接受的衍生物。 式(I)化合物可用于治疗细菌感染。