4-substituted quinoline derivatives, method and intermediates for their preparation and pharmaceutical compositions containing them
申请人:Aventis Pharma S.A.
公开号:US20040224946A1
公开(公告)日:2004-11-11
The invention relates to 4-substituted quinoline compounds of general formula:
1
which are active as antimicrobials, in which:
X
1
, X
2
, X
3
, X
4
and X
5
is C—R′
1
, to C—R′
5
respectively, or alternatively at most one represents N,
Y represents CHR, CO, CROH, CRNH
2
, CRF or CF
2
, R being a hydrogen or alkyl, m is 1, 2 or 3 and n is 0, 1 or 2, Z is CH
2
or Z is O, S, SO, SO
2
and, in this case, n is equal to 2, R
2
is —CO
2
R, —CH
2
CO
2
R, —CH
2
—CH
2
CO
2
R, —CH
2
OH or —CH
2
—CH
2
OH, wherein R is as defined above,
R
3
represents phenyl, heteroaryl or alk-R°
3
, where alk is alkyl and R°
3
represents various groups, where appropriate containing oxygen, sulfur or amine, in their enantiomeric or diastereoisomeric forms or their mixtures, and/or where appropriate in the syn or anti form or their mixtures, and their salts.
本发明涉及通式为:1的4-取代喹啉化合物,其作为抗微生物活性物质,其中:X1、X2、X3、X4和X5分别为C—R′1至C—R′5,或者至多一个表示N,Y表示CHR、CO、CROH、CRNH2、CRF或CF2,其中R为氢或烷基,m为1、2或3,n为0、1或2,Z为CH2或Z为O、S、SO、SO2,在这种情况下,n等于2,R2为—CO2R、—CH2CO2R、—CH2—CH2CO2R、—CH2OH或—CH2—CH2OH,其中R如上所定义,R3表示苯基、杂环芳基或者alk-R°3,其中alk为烷基,R°3表示各种基团,适当含有氧、硫或胺,以它们的对映异构体或二对映异构体形式或它们的混合物存在,或者适当以syn或anti形式或它们的混合物存在,以及它们的盐。