公开(公告)号：US07632918B2

公开(公告)日：2009-12-15

申请号：US11361852

申请日：2006-02-24

申请人： Daniel Chu ,  Maria N. Preobrazhenskaya ,  Svetlana S. Printsevskaya ,  Eugenia N. Olsufyeva

发明人： Daniel Chu ,  Maria N. Preobrazhenskaya ,  Svetlana S. Printsevskaya ,  Eugenia N. Olsufyeva

IPC分类号： A61K38/14

CPC分类号： A61K38/14 ,  C07K9/008

摘要： Semi-synthetic glycopeptides having antibacterial activity are based on modifications of the eremomycin, A82846B, vancomycin, teicoplanin, and A-40,926 scaffolds, in particular, acylation of the sugar moieties on these scaffolds with certain acyl groups; and/or conversion of an acid moiety on the macrocyclic ring of these scaffolds to certain substituted amides; or having a combination of an alkylation modification of the amino substituent on the amino-substituted sugar moiety on these scaffolds with certain alkyl groups or acylation modification of the amino substituent on the amino-substituted sugar moiety on this scaffold with certain alkyl groups, and conversion of the acid moiety on the macrocyclic ring of this scaffolds to certain substituted amides. Also provided are methods for the synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.

摘要翻译： 具有抗菌活性的半合成糖肽基于依依霉素，A82846B，万古霉素，替考拉宁和A-40,926支架的修饰，特别是在具有某些酰基的这些支架上糖部分的酰化; 和/或将这些支架的大环上的酸部分转化为某些取代的酰胺; 或具有这些支架上的氨基取代的糖部分上的氨基取代基的烷基化修饰与某些烷基的组合或在该支架上的某些烷基上的氨基取代的糖部分上的氨基取代基的酰化修饰和转化 的该支架的大环上的酸部分与某些取代的酰胺。 还提供了合成化合物的方法，含有该化合物的药物组合物，以及该化合物用于治疗和/或预防疾病，特别是细菌感染的方法。