Methods of treatment with anthracycline derivatives
AssigneePro-Neuron, Inc.
InventorsDavid Farquhar, Abdallah Cherif
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Abstract
The present invention is a compound having the structure where: anthracycline is doxorubicin, daunorubicin or a derivative thereof; N is the 3′ nitrogen of daunosamine; Ra is H or alkyl; X is, O, S, CRc2 or NRc where Rc is H or alkyl; Rb is alkyl or aryl; n is 1 to 6; and m is 0 to 6. Ra and Rc are preferably H, methyl, ethyl, propyl or butyl, although other alkyl substituents are usable. Rb is alkyl or aryl. The compound of the present invention as described above is activatable in vivo by esterases and spontaneous dehydration to form an aldehyde. The aldehyde may couple to nucleophiles of intracellular macromolecules. The compounds of the present invention are cytotoxically effective in the inhibition of human myeloma cells.
Claims21
A method of treating human T-lymphoblastic or myleoma cells sensitive to doxorubician or daunorubicin the method comprising treating said cells with a therapeutically effective amount of a compound having the formula
- where:
- anthracycline is doxorubicin or daunorubicin;
- N is the 3′ nitrogen of daunosamine;
- Ra is H, methyl, ethyl, propyl or butyl;
- X is O, S, CRc2 or NRc, where Rc is H, methyl, ethyl, propyl or butyl;
- Rb is methyl, ethyl, propyl or butyl;
- n is 1 to 6;
- and
- m is 0 to 6.
Dependencies are inferred from the claim text.