National Institutes of Health, a Component of the US Dept. of Health & Human Services

Charles L Cantrell

Michael R Boyd

Kirk R Gustafson

The present invention provides a compound of the formula (I) or (II), wherein Ris H, alkyl, alkenyl or aryl, Ris H, alkyl or aryl, Ris H, a alkyl, alkenyl or aryl, Rand R-Rare independently R, C(O)Ror SOR, wherein Ris H, alkyl, alkenyl or aryl, and Ris R, C(O)Ror SOR, wherein Ris H, alkyl, alkenyl or aryl. Rcan be unsubstituted or substituted with one or more oxo(&#x2550;O), OR, OC(O)R, OSOR, NHR, NHC(O)Rand NHSORgroups. Ris H, alkyl, alkenyl, or aryl. Rcan be unsubstituted or substituted with one or more groups such as oxo(&#x2550;O), OR, COR, CORand OC(O)R. Ris 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. 

Biologically active macrolides, compositions, and uses thereof

The present invention provides a compound of the formula (I) or (II, wherein Ris H, alkyl, alkenyl or aryl, Ris H, alkyl or aryl, Ris H, a alkyl, alkenyl or aryl, Rand R-Rare independently R, C(O)Ror SOR, wherein Ris H, alkyl, alkenyl or aryl, and Ris R, C(O)Ror SOR, wherein Ris H, alkyl, alkenyl or aryl. Rcan be unsubstituted or substituted with one or more oxo(&#x2550;O), OR, OC(O)R, OSOR, NHR, NHC(O)Rand NHSORgroups. Ris H, alkyl, alkenyl, or aryl. Rcan be unsubstituted or substituted with one or more groups such as oxo(&#x2550;O), OR, COR, CORand OC(O)R. Ris 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. 

The present invention provides a compound of formula (II). 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.

The present invention provides a compound of the formula (I). 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.

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Longmont, CO, United States of America

Charles L Cantrell