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    • 1. 发明申请
    • AN ANTIMICROBIAL AGENT
    • 抗菌药物
    • WO2003070715A1
    • 2003-08-28
    • PCT/AU2003/000222
    • 2003-02-21
    • GRIFFITH UNIVERSITYMONASH UNIVERSITYVON ITZSTEIN, Laurence, MarkCOPPEL, Ross, LeonDAVIS, Christopher, BonnerTHOMSON, Robin, JoyOWEN, David, James
    • VON ITZSTEIN, Laurence, MarkCOPPEL, Ross, LeonDAVIS, Christopher, BonnerTHOMSON, Robin, JoyOWEN, David, James
    • C07D307/20
    • A61K31/341C07D307/20
    • A compound of general formula (I): wherein R1 and R2 may be the same or different and are selected from the group consisting of hydrogen, optionally substituted C4-30 alkyl and optionally substituted C4-30 alkenyl, provided that R1 and R2 may not both be hydrogen, or R1 and R2 together with the nitrogen atom from which they depend form a saturated or unsaturated, optionally substituted heterocyclic group which may include additional heteroatoms selected from the group consisting of O, N and S, or R1 and R2 together with the nitrogen atom from which they depend form an optionally substituted lactam moiety; X1 is selected from the group consisting of OR3, SR3, NR3R'3, hydrogen, halogen, CN, C(O)NR3R'3, C(O)OR3, OSO3R3, OPO3R3, NNR3R'3, SNR3R'3, NHSR3, SSR3 and substituted alkyl; X2 is selected from the group consisting of OR4, SR4, NR4R'4, hydrogen, halogen, CN, C(O)NR4R'4, C(O)OR4, OSO3R4, OPO3R4, NNR4R'4, SNR4R'4, NHSR4, SSR4 and substituted alkyl; X3 is selected from the group consisting of OR5, SR5, NR5R'5, hydrogen, halogen, CN, C(O)NR5R'5, C(O)OR5, OSO3R5, OPO3R5R'5, NNR5R'5, SNR5R'5, NHSR5, SSR5 and substituted alkyl; X4 is selected from the group consisting of OR6, SR6, NR6R'6, hydrogen, halogen, CN, C(O)NR6R'6, C(O)OR6, OSO3R6, OPO3R6R'6, NNR6R'6, SNR6R'6, NHSR6, SSR6 and substituted alkyl; R3, R'3, R4, R'4, R5, R'5, R6 and R'6 are the same or different and are selected from the group consisting of hydrogen, optionally substituted alkyl, optionally substituted aralkyl, optionally substituted aryl, optionally substituted acyl and a carbohydrate moiety; or a pharmaceutically acceptable salt thereof.
    • 通式I的化合物:其中R 1和R 2可以相同或不同,并且选自氢,任选取代的C 4-30烷基和任选取代的C 4-30烯基,条件是R 1和R 2不能均为 氢或R1和R2与它们所依赖的氮原子一起形成饱和或不饱和的任选取代的杂环基,其可以包括另外的选自O,N和S的杂原子,或者R 1和R 2与氮 它们所依赖的原子形成任选取代的内酰胺部分X1选自OR3,SR3,NR3R'3,氢,卤素,CN,CONR3R'3,COOR3,OSO3R3,OPO3R3,NNR3R'3,SNR3R'3 ,NHSR 3,SSR 3和取代的烷基X 2选自OR4,SR4,NR4R'4,氢,卤素,CN,CONR4R'4,COOR4,OSO3R4,OPO3R4,NNR4R4,SNR4R'4,NHSR4,SSR4 并且取代的烷基X 3选自OR 5,S R5,NR5R'5,氢,卤素,CN,CONR5R'5,COOR5,OSO3R5,OPO3R5R'5,NNR5R'5,SNR5R'5,NHSR5,SSR5和取代的烷基X4选自OR6,SR6, NR6R'6,氢,卤素,CN,CONR6R'6,COOR6,OSO3R6,OPO3R6R'6,NNR6R'6,SNR6R'6,NHSR6,SSR6和取代的烷基R3,R'3,R4,R'4,R5, R'5,R 6和R 6相同或不同,并且选自氢,任选取代的烷基,任选取代的芳烷基,任选取代的芳基,任选取代的酰基和碳水化合物部分或其药学上可接受的盐。