Analogues of camptothecin, their use as medicaments and the pharmaceutical compositions containing them
View Patent ↗Compositions for treating cancer comprising an amount of a camptothecin with a 7-ring β-hydroxy lactone ring of the formula wherein the substituents are defined as in the specification sufficient to treat cancer.
1. A pharmaceutical composition for treating colon and breast cancer in warm-blooded animals comprising an amount of an unsubstituted or pharmaceutically acceptable substituted camptothecin with a 7-ring member β-hydroxy lactone ring of the formula
wherein R 1 is selected from the group consisting of alkyl of 1 to 6 carbon atoms, alkenyl and alkynyl of 2 to 6 carbon atoms, haloalkyl of 1 to 6 carbon atoms, alkoxy alkyl of 2 to 12 carbon atoms and alkylthioalkyl of 2 to 12 carbon atoms, R p is hydrogen or an easily cleavable group, R 18 and R 19 are individually selected from the group consisting of hydrogen, halogen, OH and alkyl and alkoxy of 1 to 6 carbon atoms and its non-toxic, pharmaceutically acceptable salts sufficient to treat colon and breast cancer and a pharmaceutical carrier.
2. A pharmaceutical composition of claim 1 wherein R 1 is ethyl.
3. A pharmaceutical composition of claim 1 wherein R 18 and R 19 are hydrogen.
4. A pharmaceutical composition of claim 2 wherein R 18 and R 19 are hydrogen.
5. A pharmaceutical composition of claim 1 wherein R p is hydrogen.
6. A pharmaceutical composition of claim 2 wherein R p is hydrogen.
7. A composition of claim 1 wherein the camptothecin is (+)-5-ethyl-9,10-difluoro-5-hydroxy-4,5,13,15-tetrahydro-1H,3H-oxepino[3′,4′:6,7]indolizino[1,2-b]quinoline-3,15-dione or (+)-1-[9-chloro-5-ethyl-5-hydroxy-10-methyl-3,15-dioxo-4,5,13,15-tetrahydro-1H,3H-oxepino[3′,4′:6,7]indolizino[1,2-b]quinolin-12-yl methyl]-4-methyl-hexahydropyridium chloride.