申请人:——
公开号:US20010051722A1
公开(公告)日:2001-12-13
The present invention provides for aminoaryl oxazolidinone N-oxide compounds of Formula I
1
wherein the variables are as defined herein. These compounds are exceedingly water soluble which is useful in preparing pharmaceutical formulations of these compounds. They are also rapidly converted back to the parent amines in vivo, making them useful as prodrugs of the parent amines. They are effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp., and in organisms such as Mycoplasma spp.
本发明提供了一种式为I1的氨基芳基噁唑啉酮N-氧化物化合物,其中变量的定义如本文所述。这些化合物在水中极易溶解,这对于制备这些化合物的药物配方非常有用。它们在体内也能迅速转化回母体胺,因此可作为母体胺的前药物使用。它们对许多人类和兽医病原体具有有效作用,包括革兰氏阳性的需氧菌,如多重耐药葡萄球菌、链球菌和肠球菌,以及厌氧菌,如Bacteroides spp.和Clostridia spp.菌种,以及抗酸菌,如结核分枝杆菌、埃及分枝杆菌和分枝杆菌属,以及支原体属等生物。