申请人:——
公开号:US20020019543A1
公开(公告)日:2002-02-14
Ar is optionally substituted with 1 to 3 R
X
groups, and where n is 0, 1, 2 or 3; and a group of formula III:
1
herein:
R
4
is selected from hydrogen; and straight or branched alkyl;
R
5
is selected from hydrogen; straight, branched, unsaturated or alicyclic alkyl, optionally substituted with 1 to 3 R
X
groups, where the alkyl group is optionally interrupted by X, where X is selected from O, S, NH and N(COCH
3
); allyloxy and 9-fluorenylmethyloxy; and (CH
2
)
n
Ar, where Ar is selected from phenyl, furanyl, thienyl, pyridyl, naphthyl, biphenyl, dibenzofuranyl, dibenzothienyl, fluorenyl and fluorenonyl, where n is 0, 1, 2 or 3, and where Ar is optionally substituted with 1 to 3 R
X
groups; and
R
X
is selected from OR, CN, C(O)NH
2
, C(O)NHR, C(O)N(R)
2
, OC(O)NH
2
, OC(O)R, CHO, SO
2
NH
2
, SOR, CF
3
, C(O)R, COOR, F, Cl, Br, I, OCH
2
Ph, NHR, N(R)
2
,, NHCOR, NHCO
2
t-Bu, NHCO
2
allyl, NH
2
, and R, where R is hydrogen, C
1
to C
15
alkyl, or aryl.
The invention is further directed to a pharmaceutical composition containing the compound, as well as a method for treating bacterial infections in animals or humans, wherein the composition can be administered in combination with a &bgr;-lactam antibiotic.
Ar 可以用 1 至 3 个 RX 群取代,其中 n 为 0、1、2 或 3;以及公式 III:1 中的一组,其中:R4 选自氢;直链或支链烷基;R5 选自氢、直链、支链、不饱和或脂环烷基,可选地取代 1 至 3 个 RX 群,其中烷基可以被 X 所打断,X 选自 O、S、NH 和 N(COCH3);烯丙氧基和 9-
芴甲氧基;以及 (
CH2)nAr,其中 Ar 选自苯基、
呋喃基、
噻吩基、
吡啶基、
萘基、
联苯基、
二苯并呋喃基、
二苯并噻吩基、
芴基和
芴烯基,其中 n 为 0、1、2 或 3,且 Ar 可选地取代 1 至 3 个 RX 群;而 RX 选自 OR、CN、C(O)NH2、C(O)NHR、C(O)N(R)2、OC(O)NH2、OC(O)R、CHO、SO2NH2、SOR、
CF3、C(O)R、COOR、F、Cl、Br、I、O Ph、NHR、N(R)2、NHCOR、NHCO2t-Bu、NHCO2allyl、NH2 和 R,其中 R 是氢、C1 至 C15 烷基或芳基。本发明还涉及一种含有该化合物的药物组合物,以及一种用于治疗动物或人体细菌感染的方法,其中该组合物可以与β-内酰胺类抗生素联合使用。