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    POLYMYXIN DERIVATIVES
    3.
    发明公开
    POLYMYXIN DERIVATIVES 审中-公开
    多金霉素衍生物

    公开(公告)号：EP2780357A1

    公开(公告)日：2014-09-24

    申请号：EP12797961.5

    申请日：2012-11-16

    申请人： Novacta Biosystems Limited ,  Cantab Anti-Infectives Limited

    发明人： SAADI, Mona ,  DUPERCHY, Esther ,  BROWN, Pamela ,  DAWSON, Michael John ,  WADMAN, Sjoerd Nicolaas

    IPC分类号： C07K7/62 ,  A61K38/12

    CPC分类号： C07K7/62 ,  A61K38/00

    摘要： Provided are compounds, the use of the said compounds in treatment, for example treatment of microbial infections, particularly by Gram negative bacteria. The compounds are polymyxin-based and are represented by the formula (I): and pharmaceutically acceptable salts thereof, where X is —NHC(O)—, —C(O)—, —OC(O)—, —CH2— or —SO2—; R5 represents C0-12 alkyl(C4-6 heterocyclyl), or C2-12 alkyl or C0-12 alkyl(C3-8 cycloalkylyl). and the alkyl or cycloalkylyl bears one, two or three hydroxyl groups, or a —NR6R7 group, or one —NR6R7 group and one or two hydroxyl groups; and R1 to R4 and R6 to R8 are as defined in the description.

    摘要翻译： 提供化合物，所述化合物在治疗中的用途，例如治疗微生物感染，特别是通过革兰氏阴性细菌。 所述化合物是基于多粘菌素的并且由式（I）表示：及其药学上可接受的盐，其中X是-NHC（O） - ，-C（O） - ，-OC（O） - ， 或-SO 2 - ; R 5表示C 10-12烷基（C 4-6杂环基）或C 2-12烷基或C 0-12烷基（C 3-8环烷基），并且烷基或环烷基带有一个，两个 或三个羟基，或-NF 6 R 7基团，或一个-NR 6 R 7基团和一个或两个羟基！ 组; 并且R 1至R 4和R 6至R 8如说明书中所定义。

    DEOXYACTAGARDINE DERIVATIVES
    4.
    发明公开
    DEOXYACTAGARDINE DERIVATIVES 有权
    脱氧心脏苷衍生物

    公开(公告)号：EP2387580A1

    公开(公告)日：2011-11-23

    申请号：EP10700336.0

    申请日：2010-01-12

    申请人： Novacta Biosystems Limited

    发明人： WADMAN, Sjoerd Nicolaas

    IPC分类号： C07K7/54 ,  A61K38/12

    CPC分类号： C07K7/54

    摘要： The present invention pertains generally to certain compounds of the deoxyactagardine A and B type. Such compounds are suitable for use in the treatment of microbial infections, for example
    Clostridium infection, such as C.
    perfringens , C.
    difficile , C.
    tetani, and/or C.
    botulinum , in particular C. difficile, especially infection of the colon and/or lower intestines and diarrhoea associated with the microbial infection.

    摘要翻译： 本发明通常涉及脱氧actagardine A和B型的某些化合物。 此类化合物适用于治疗微生物感染，例如梭菌感染，如产气荚膜梭菌，艰难梭菌，破伤风梭菌和/或肉毒梭菌，特别是艰难梭菌，特别是结肠感染 和/或与微生物感染相关的较低的肠和腹泻。

    LANTIBIOTIC-BASED COMPOUNDS HAVING ANTIMICROBIAL ACTIVITY
    6.
    发明公开
    LANTIBIOTIC-BASED COMPOUNDS HAVING ANTIMICROBIAL ACTIVITY 审中-公开
    链接将具有抗菌作用LANTIBIOTIKABASIS

    公开(公告)号：EP2167527A2

    公开(公告)日：2010-03-31

    申请号：EP08775990.8

    申请日：2008-07-18

    申请人： Novacta Biosystems Limited

    发明人： WADMAN, Sjoerd Nicolaas

    IPC分类号： C07K7/08 ,  C07K14/365 ,  A61K38/00 ,  A61P31/00

    CPC分类号： C07K7/08 ,  A61K38/00 ,  C07K14/365

    摘要： The present invention provides actagardine, actagradine B and deoxy actagardine B derivatives of formula (I), wherein: X1 denotes that the residue is Leu; Val; or Ile; X2 denotes that the residue is Leu; Val; or Ile; R1 represents an alkyl or heteroalkyl group, substituted by at least one hydroxyl substituent, and R2 represents hydrogen, or an alkyl or heteroalkyl group, optionally substituted by at least one hydroxyl substituent, or R1 and R2 taken together with the nitrogen atom represent a heterocyclic group having at least one hydroxyl substituent, wherein the heterocyclic group optionally further contains one or more heteroatoms; Z is an amino acid residue, -NR3R4, -NR5COR6, -NR5C(O)OR6; -NR5SOR6, NR5SO2 R6; -NR5C(S)NR6R7, -NR5C(NR8)NR6R7, or -N=R9, where R3, R4, R5, R6, R7, R8 and R9 are independently hydrogen, or a group, optionally substituted, selected from alkyl, heteroalkyl, aryl, heteroaryl, aralkyl and heteroaralkyl, with the proviso that R9 is not hydrogen; and Y is -S- or -S(O)-. The compounds find use in the treatment of microbial infections.