申请人:Liu Li
公开号:US20110184158A1
公开(公告)日:2011-07-28
The present invention relates to a macrolide derivative as well as preparation and use thereof. The macrolide derivative of the present invention, i.e., a hydrate of erythromycin salts, has a molecular formula of C
37
H
67
NO
13
.A.nH
2
O, n=1.0-11.0, in which A is an organic acid or an organic acids, selected from lactobionic acid, thiocyanic acid, maleic acid, fumaric acid, thiocyanic acid, acetic acid, methanesulfonic acid, benzenesulfonic acid, nicotinic acid, lactic acid, citric acid, tartaric acid, aspartic acid, glutamic acid and phosphoric acid, the hydrate has good water solubility and better storage stability, which is suitable for the manufacture of a medicament for the treatment and prophylaxis of infectious diseases in human or animal caused by Gram-positive or negative bacteria.
本发明涉及一种大环内酯衍生物及其制备和使用。本发明的大环内酯衍生物是红霉素盐的水合物,其分子式为C37H67NO13.A.nH2O,其中n=1.0-11.0,A是有机酸或有机酸的混合物,包括乳糖酸、硫氰酸、马来酸、富马酸、乙酸、甲磺酸、苯磺酸、烟酸、乳酸、柠檬酸、酒石酸、天冬氨酸、谷氨酸和磷酸。该水合物具有良好的水溶性和更好的储存稳定性,适用于制造用于治疗和预防由革兰氏阳性或阴性细菌引起的人或动物感染性疾病的药物。