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US 5,492,924 AGranted
Phorbine derivatives and their use in the diagnosis and therapy of cancer
AssigneesFox Chase Cancer Center, The French National Institute of Health and Medical Research (Inserm), Yissum Research Development Company of the Hebrew University of Jerusalem
InventorsShimon Gatt, Arie Dagan, Rene Santus, Jean-Claude Maziere, J. Donald Chapman, Edward L. Engelhardt
Life of this patent
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Abstract
Phorbine derivatives having high potency and light absorptivity in the 650 to 780 nanometer range are useful in cancer diagnosis and therapy, especially photodynamic therapy.
Claims13
A phorbine derivative of the formula ##STR9## wherein X represents C.dbd.O or C--OH;
- R.sub.1 represents --CH.dbd.CH.sub.2 or --COCH.sub.3 ;
- R.sub.2 represents -lower alkyl of C.sub.1 -C.sub.6 carbon atoms, --CH.sub.2 --OH, or CHO (formyl);
- R.sub.3 and R.sub.4 may be the same or different and represent --H, --OH, --COOH or CO.sub.2 -- lower alkyl of C.sub.1 -C.sub.6 ;
- and
- R.sub.5 represents --(CH.sub.2).sub.2 --CO--NH--(CH.sub.2).sub.m --Z,
- Z being selected from the group consisting of OH, O-lower alkyl of C.sub.1 -C.sub.6, CH.sub.3, SH, S-lower alkyl of C.sub.1 -C.sub.6, SO.sub.3.sup.-, or PO.sub.3.sup.-- and m is an integer from 1 to 12.
3 more elements
Dependencies are inferred from the claim text.