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    • 8. 发明申请
    • ANTIMICROBIAL AGENTS
    • 抗菌药物
    • WO2004073709A1
    • 2004-09-02
    • PCT/GB2004/000621
    • 2004-02-17
    • PROLYSIS LIMITEDCZAPLEWSKI, LloydERRINGTON, JeffreyBAYSTON, DanBOYD, AndrewBROOKFIELD, FrederickHATCHER, Stuart
    • CZAPLEWSKI, LloydERRINGTON, JeffreyBAYSTON, DanBOYD, AndrewBROOKFIELD, FrederickHATCHER, Stuart
    • A61K31/415
    • C07D213/61A61K31/13A61K31/135A61K31/415A61K31/4164A61K31/425C07C211/29C07C217/58C07C257/16C07C257/18C07C275/70C07C279/12C07C279/18C07C279/28C07C2601/14C07D209/08C07D209/14C07D209/86C07D213/38C07D215/12C07D231/06C07D231/12C07D231/16C07D233/48C07D233/64C07D239/26C07D249/08C07D277/10C07D277/28C07D277/64C07D307/52C07D307/81C07D311/14C07D317/58C07D333/20C07D333/58C07D409/12
    • Compounds of formula (I) are antibacterial agents: wherein B represents R 2 R 3 N-, R 2 NH-C(=NR 3 )-, or R 2 NH-C(=NR 3 )-NR 4 - wherein each of R 2 , R 3 and R 4 represents hydrogen or a C 1 -C 6 alkyl, phenyl, phenyl(C 1 -C 6 alkyl)-, monocyclic heteroaryl, monocyclic heteroaryl (C 1 -C 6 alkyl)-, or cyano group, or R 2 and R 3 form a ring together with the nitrogen atoms to which they are attached; L represents a divalent radical of formula (II): -(Alk 1 ) m -(CYC 1 )p (Alk 2 ) n -[(Alk 3 ) r (CyC 2 ) s -(Alk 4 ) t ] w -, wherein Alk 1 , Alk 2 , Alk 3 and Alk 4 each independently represent (i) an optionally substituted divalent C 1 -C 3 alkylene radical which may optionally contain an ether (-0-), thioether (-S-) or amino (-NR A- ) link wherein R A is hydrogen or C 1 -C 3 alkyl, (ii) an optionally substituted -CH=CH- radical, or (iii) a -C=C- radical; Cyc 1 and Cyc 2 each independently represent an optionally substituted divalent monocyclic carbocyclic or heterocyclic radical having from 5 to 8 ring atoms; m, n, p, r, s, t and w each independently represent 0 or 1, provided that at least one of m, n and p is 1; R represents an optionally substituted C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, or Cyc-, (Cyc)-(C 1 -C 6 alkyl)-, (Cyc)-(C 2 -C 6 alkenyl)-, or (Cyc)-(C 2 -C 6 alkynyl)- radical wherein Cyc represents a monocyclic carbocyclic or heterocyclic radical having from 5 to 8 ring atoms; and R 1 represents an optionally substituted (aryl)-(C 1 -C 6 alkyl)-, (aryl)-(C 2 -C 6 alkenyl)-(aryl)-(C 2 -C 6 alkynyl)-, (heteroaryl)-(C 1 -C 6 alkyl)-, (heteroaryl)-(C 2 -C 6 alkenyl)- or (heteroaryl)-(C 2 -C 6 alkynyl)- radical.
    • 式(I)化合物是抗菌剂:其中B表示R2R3N-,R2NH-C(= NR3) - 或R2NH-C(= NR3)-NR4-,其中R2,R3和R4各自表示氢或C1- C6烷基,苯基,苯基(C1-C6烷基) - ,单环杂芳基,单环杂芳基(C1-C6烷基) - 或氰基,或R2和R3与它们所连接的氮原子一起形成环; L表示式(II)的二价基团: - (Alk 1)m-(CYC 1)p(Alk 2)n - [(Alk 3)r(CyC 2)] - (Alk 4)t] w-,其中Alk 1,Alk 2,Alk 3和Alk 4各自独立地表示(i)任选取代的二价C 1 -C 3亚烷基,其可任选地 含有醚(-O-),硫醚(-S-)或氨基(-NR A - )连接,其中R aA是氢或C 1 -C 3烷基,(ii)任选取代的-CH = CH- 或(iii)-C = C-基团; Cyc 1和Cyc 2各自独立地表示具有5至8个环原子的任选取代的二价单环碳环或杂环基; m,n,p,r,s,t和w各自独立地表示0或1,条件是m,n和p中的至少一个为1; R代表任选取代的C 1 -C 6烷基,C 2 -C 6烯基,C 2 -C 6炔基或环 - ,(环) - (C 1 -C 6烷基) - ,(Cyc) - (C 2 -C 6烯基) Cyc) - (C 2 -C 6炔基) - 基,其中Cyc表示具有5至8个环原子的单环碳环或杂环基; 并且R 1表示任选取代的(芳基) - (C 1 -C 6烷基) - ,(芳基) - (C 2 -C 6烯基) - (芳基) - (C 2 -C 6炔基) - ,(杂芳基) ) - ,(杂芳基) - (C 2 -C 6烯基) - 或(杂芳基) - (C 2 -C 6炔基) - 基。