基本信息:
- 专利标题: NITROHETEROARYL-CONTAINING RIFAMYCIN DERIVATIVES
- 专利标题(中):含有硝基的含有RIFAMYCIN衍生物
- 申请号:PCT/US2007015970 申请日:2007-07-12
- 公开(公告)号:WO2008008480A3 公开(公告)日:2008-03-13
- 发明人: DING CHARLES Z , KIM IN HO , WANG JIANCHENG , MA ZHENKUN , JIN YAFEI , COMBRINK KEITH D , LU GENLIANG , LYNCH A SIMON
- 申请人: CUMBRE PHARMACEUTICALS INC , DING CHARLES Z , KIM IN HO , WANG JIANCHENG , MA ZHENKUN , JIN YAFEI , COMBRINK KEITH D , LU GENLIANG , LYNCH A SIMON
- 专利权人: CUMBRE PHARMACEUTICALS INC,DING CHARLES Z,KIM IN HO,WANG JIANCHENG,MA ZHENKUN,JIN YAFEI,COMBRINK KEITH D,LU GENLIANG,LYNCH A SIMON
- 当前专利权人: CUMBRE PHARMACEUTICALS INC,DING CHARLES Z,KIM IN HO,WANG JIANCHENG,MA ZHENKUN,JIN YAFEI,COMBRINK KEITH D,LU GENLIANG,LYNCH A SIMON
- 优先权: US83024506 2006-07-12
- 主分类号: C07D498/08
- IPC分类号: C07D498/08 ; A61K31/395 ; C07D498/18 ; C07D498/22 ; C07D519/00
摘要:
Substituted rifamycin derivatives of formula I uses thereof and pharmaceutical compositions containing the rifamycin derivatives are disclosed. Methods of synthesizing these substituted rifamycin derivatives are also disclosed. The rifamycin derivatives possess antibacterial activity, and are effective against a number of human and veterinary pathogens in the treatment of bacterial diseases.or their pharmaceutically acceptable salt thereof, wherein R 1 is a hydrogen or acetyl group, G is a structure of formula (II, III, IV or V): wherein, in formula (II, III, IV or V), Q is N- or CR 2 . which is bonded to a linkage, group "L", which in turn is bonded to a structure A-NO 2 ,and R 2 is a group selected from hydrogen, substituted or unsubstituted (C 1 -C 6 )alkyl, aryl, heteroaryl, or heterocycloalkyl group; The structure A-NO 2 is a structural formula (VI1 VII, VIII or IX): wherein Y is a bond which is bonded to linkage group "L", defined as above; and Z is a carbon (-CR 7 R 8 -), carbonyl (-C(O)-), amide (-C(O)N-), sulfonamide (-S(O 2 )N-), or a heteroatom selected from N, O, S, SO or SO 2 ; wherein R 5 , R 6 , R 7 , and R 8 are independently a group selected from hydrogen, substituted or unsubstituted (C 1 -C 6 )alkyl, aryl. heteroaryl. or heterocycloalkyl group; R 5 and R 6 R 7 and R 8 can join together to form a five to seven-member ring system optionally containing one to three heteroatoms.
摘要(中):
公开了其取代的利福霉素衍生物的用途,并且公开了含有利福霉素衍生物的药物组合物。 还公开了合成这些取代的利福霉素衍生物的方法。 利福霉素衍生物具有抗细菌活性,并且在治疗细菌性疾病中对许多人和兽医病原体有效。或其药学上可接受的盐,其中R 1是氢或乙酰基,G 是式(II,III,IV或V)的结构:其中,在式(II,III,IV或V)中,Q是N-或CR 2。 其键合到键,组“L”,其又结合于结构A-NO 2,并且R 2是选自氢,取代的基团 或未取代的(C 1 -C 6 -C 6)烷基,芳基,杂芳基或杂环烷基; 结构A-NO 2结构式(VI1 VII,VIII或IX):其中Y是与上述定义的连接基团“L”键合的键; (C(O) - ),酰胺(-C(O)N-),磺酰胺(C(O) (-S(O)2 - )N-)或选自N,O,S,SO或SO 2的杂原子; 其中R 5,R 6,R 7和R 8独立地是选自氢,取代的 或未取代的(C 1 -C 6 -C 6)烷基,芳基。 杂。 或杂环烷基; R 5和R 6 R 7和R 8可以连接在一起以形成五至七元环 系统任选地含有一至三个杂原子。
IPC结构图谱:
C | 化学;冶金 |
--C07 | 有机化学 |
----C07D | 杂环化合物 |
------C07D498/00 | 杂环化合物,在稠环系中至少有1个杂环具有氮和氧原子作为仅有的杂环原子 |
--------C07D498/02 | .在稠环系中含有两个杂环 |
----------C07D498/08 | ..桥系 |