基本信息:
- 专利标题: ANTIBACTERIAL AGENTS
- 专利标题(中):抗菌剂
- 申请号:PCT/GB2002/005409 申请日:2002-12-02
- 公开(公告)号:WO2004033441A1 公开(公告)日:2004-04-22
- 发明人: BECKETT, Raymond, Paul , WIJKMANS, Jac , KRULLE, Thomas
- 申请人: BRITISH BIOTECH PHARMACEUTICALS LTD , BECKETT, Raymond, Paul , WIJKMANS, Jac , KRULLE, Thomas
- 申请人地址: Watlington Road, Oxford OX4 6LY GB
- 专利权人: BRITISH BIOTECH PHARMACEUTICALS LTD,BECKETT, Raymond, Paul,WIJKMANS, Jac,KRULLE, Thomas
- 当前专利权人: BRITISH BIOTECH PHARMACEUTICALS LTD,BECKETT, Raymond, Paul,WIJKMANS, Jac,KRULLE, Thomas
- 当前专利权人地址: Watlington Road, Oxford OX4 6LY GB
- 代理机构: WALLS, Alan, J.
- 优先权: GB0223532.3 20021009
- 主分类号: C07D295/185
- IPC分类号: C07D295/185
摘要:
Compounds of formula (II) have antibacterial activity: wherein: Q represents a radical of formula -N(OH)CH(=0) or formula -C(=O)NH(OH); R 1 represents hydrogen, methyl or trifluoromethyl or, except when Q is a radical of formula -N(OH)CH(=0), a hydroxy, halo or amino group; R 2 represents a group R 10 -(D) n -(ALK) m - wherein R 10 represents hydrogen or an optionally substituted C 1 -C 6 alkyl, C 2 -C 6 alkynyl, C 2 -C 6 alkynyl, cycloalkyl, aryl, or heterocyclyl group and ALK represents a straight or branched divalent C 1 -C 6 alkylene, C 2 -C 6 alkynylene, or C 2 -C 6 alkynylene radical, and may be interrupted by one or more non-adjacent -NH-, -O- or -Slinkages, D represents -NH-, -O- or -S-, and m and n are independently 0 or 1; R 4 represents the side chain of a natural or non-natural alpha amino acid; ring A represents an optionally substituted monocyclic heterocyclic ring containing from 5 to 7 ring atoms, one of which is the nitrogen atom shown, the remaining ring atoms being selected from compatible combinations of carbon, oxygen, sulfur and nitrogen; X is oxygen or sulfur; Y is oxygen, sulfur or -NH-; R is 0, 1, 2 or 3; and ring B represents an optionally substituted carbocyclic or heterocyclic ring system.
摘要(中):
式(II)的化合物具有抗菌活性:其中:Q表示式-N(OH)CH(= O)或式-C(= O)NH(OH)的基团; 除了当Q是式-N(OH)CH(= O)基团,羟基,卤素或氨基基团时,R 1表示氢,甲基或三氟甲基。 R 2表示基团R 10 - (D)n-(ALK)m - ,其中R 10表示氢或任选取代的C 1 -C 6烷基,C 2 -C 6炔基,C 2 -C 6炔基,环烷基,芳基或杂环基,并且ALK表示 直链或支链二价C 1 -C 6亚烷基,C 2 -C 6亚炔基或C 2 -C 6亚炔基,并且可被一个或多个不相邻的-NH-,-O-或-S-链接间隔,D表示-NH-, - O-或-S-,m和n独立地为0或1; R4表示天然或非天然α氨基酸的侧链; 环A表示含有5至7个环原子的任选取代的单环杂环,其中一个是所示的氮原子,剩余的环原子选自碳,氧,硫和氮的相容组合; X是氧或硫; Y是氧,硫或-NH-; R为0,1,2或3; 环B表示任选取代的碳环或杂环系。
IPC结构图谱:
C | 化学;冶金 |
--C07 | 有机化学 |
----C07D | 杂环化合物 |
------C07D295/00 | 杂环化合物,含多亚甲基亚胺环,最少有五元环,3-氮杂二环[3.2.2]-壬烷,哌嗪,吗啉或硫吗啉环,仅有氢原子直接连在环碳原子上 |
--------C07D295/02 | .除环杂元素外,仅含氢原子和碳原子 |
----------C07D295/18 | ..被羧酸或羧酸的硫或氮的类似物衍生的基 |
------------C07D295/182 | ...由羧酸衍生的基 |
--------------C07D295/185 | ....由脂肪羧酸 |