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2. 发明公开

EP2030982A1 GLYCOPEPTIDE ANTIBIOTIC DERIVATIVE 审中-公开
标题翻译：抗生素治疗糖尿病
公开(公告)号：EP2030982A1
公开(公告)日：2009-03-04
申请号：EP07744107.9
申请日：2007-05-25
申请人： SHIONOGI & CO., LTD.
发明人： NISHITANI, Yasuhiro , YOSHIDA, Osamu , IWAKI, Tsutomu , KATO, Issei
IPC分类号： C07K9/00 , A61K38/00 , A61P31/04 , C07K7/06 , C07K14/36
CPC分类号： C07K9/008 , A61K38/00 , A61K38/04
摘要： The present invention provides a novel glycopeptide antibiotic derivative.
These derivatives are represented by the formula (I)

or a pharmaceutically acceptable salt or solvate thereof,
wherein
R A is

-X 1 -Ar 1 -X 2 -Y-X 3 -Ar 2

wherein
X 1 , X 2 and X 3 are single bond; heteroatom-containing group selected from the group consisting of -N=, =N-, - NR 1 - (R 1 is hydrogen or lower alkyl), -O-, -S-, -SO- and -SO 2 -, or a linkage thereof; or alkylene or alkenylene optionally substituted and optionally interrupted by one or more of said heteroatom-containing group;
Y is -NR 2 CO-, -CONR 2 - (R 2 is hydrogen or lower alkyl), or a group of the formula (II) wherein R 3 is alkylene;
Ar 1 and Ar 2 are a carbocycle or a heterocycle which is optionally substituted and may have an unsaturated bond;
R B is

-NHNR X R Y or -NR Z OR W

wherein
R X is hydrogen or lower alkyl;
R Y is hydrogen, optionally substituted lower alkyl, C(=NH)NH 2 , CSNH 2 , COCONH 2 , CN, optionally substituted heterocyclic group, and optionally substituted carbamoyl;
R Z is hydrogen or lower alkyl;
R W is hydrogen, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted heterocyclic group, optionally substituted heterocyclic carbonyl or optionally substituted carbamoyl;
R C is hydrogen or optionally substituted alkyl, wherein said alkyl may be interrupted by a heteroatom-containing group selected from N=, =N-, -NR 1 - (R 1 is hydrogen or lower alkyl), -O-, -S-, -SO- and -SO 2 -; and
R is optionally substituted alkyl.
摘要翻译：本发明提供了一种新型糖肽抗生素衍生物。这些衍生物由式（I）表示或其药学上可接受的盐或溶剂化物，其中RA为€ƒ€ƒ€ƒ€ƒ€ƒ-X 1 -Ar 1 -X 2 -YX 3 -Ar 2其中X 1，X 2和X 3为单键; 选自-N =，= N - ， - NR 1 - （R 1为氢或低级烷基）， - O - ， - S - ， - SO-和-SO 2 - 的含杂原子的基团，或其联系; 或任选被取代并任选被一个或多个所述含杂原子基团中断的亚烷基或亚烯基; Y是-NR 2 CO-，-CONR 2 - （R 2是氢或低级烷基）或式（II）的基团，其中R 3是亚烷基; Ar 1和Ar 2是任选被取代并可具有不饱和键的碳环或杂环; R B是€ƒ€ƒ€ƒ€ƒ€ƒ-NHNR X R Y或-NR Z OR W其中R X是氢或低级烷基; R Y是氢，任选取代的低级烷基，C（= NH）NH 2，CSNH 2，COCONH 2，CN，任选取代的杂环基和任选取代的氨基甲酰基; R Z是氢或低级烷基; R W是氢，任选取代的低级烷基，任选取代的低级烯基，任选取代的杂环基，任选取代的杂环羰基或任选取代的氨基甲酰基; RC是氢或任选取代的烷基，其中所述烷基可以被选自N =，N-，-NR 1 - （R 1是氢或低级烷基），-O-，-S- ，-SO-和-SO 2 - ; 和R是任选取代的烷基。

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