BIOLOGICALLY ACTIVE MACROLIDES, COMPOSITIONS, AND USES THEREOF

摘要

The present invention provides a compound of the formula (I) or (II), wherein R<1> is H, alkyl, alkenyl or aryl, R<2> is H, alkyl or aryl, R<3> is H, a alkyl, alkenyl or aryl, R<4> and R<4>-R<8> are independently R<10>, C(O)R<10> or SO2R<10>, wherein R<10> is H, alkyl, alkenyl or aryl, and R<9> is R<9a>, C(O)R<9a> or SO2R<9a>, wherein R<9a> is H, alkyl, alkenyl or aryl. R<9a> can be unsubstituted or substituted with one or more oxo(=O), OR<9b>, OC(O)R<9b>, OSO2R<9b>, NHR<9b>, NHC(O)R<9b> and NHSO2R<9b> groups. R<9b> is H, alkyl, alkenyl, or aryl. R<9b> can be unsubstituted or substituted with one or more groups such as oxo(=O), OR<9c>, CO2R<9c>, CO2R<9c> and OC(O)R<9c>. R<9c> is H, or a unsubstituted or substituted alkyl, alkenyl or aryl. The present invention further provides a composition comprising at least one compound of the present invention and a pharmaceutically acceptable carrier, alone or in combination with at least one additional active agent. The present invention further provides a method of treating a condition treatable by the inhibition of vacuolar-type (H+)-ATPase and a method of treating cancer.