Novel counterparts of camptothecin, their application as...

C - Chemistry – Metallurgy – 07 – D

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C07D 491/22 (2006.01) A61K 31/475 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2275351

The invention concerns novel counterparts of camptothecin and particularly the products complying with the following formulae: -5-ethyl-9,10-difluoro-4,5-dihydro-5-hydroxy-12- (4-methyl piperidinomethyl) -1H-oxepino[3', 4':6,7]indolizino[1,2-b] quinolein-3,15(4H,13H)-dione; -5-ethyl-12-diethylaminomethyl-9-fluoro-4,5-dihydro-5-hydroxy-10-methyl-1H-oxepino [3',4':6,7] indolizino[1,2-b]quinolein-3,15(4H,13H)-dione; -5-ethyl-9-fluoro-4,5-dihydro-5-hydroxy-10-methyl-12- (4-methyl piperidinomethyl) -1H-oxepino[3',4':6,7]indolizino[1,2-b]quinolein-3,15(4H,13H)-dione. The invention also concerns their application as medicines, the pharmaceutical compositions containing them and their use in producing tumoricidal, antiviral or parasiticide medicines.

L'invention concerne de nouveaux analogues de la camptothécine et en particulier les produits répondant aux formules suivantes: -5-éthyl-9,l0-difluoro-4,5-dihydro-5-hydroxy-l2-(4-méthyl pipéridinométhyl) -1H-oxépino[3',4':6,7]indolizino[1,2-b] quinoléine-3,15(4H,13H)-dione; -5-éthyl-12-diéthylaminométhyl-9-fluoro-4,5- dihydro-5-hydroxy-10-méthyl-1H-oxépino [3',4':6,7] indolizino[1,2-b]quinoléine-3,15(4H,13H)-dione; -5-éthyl-9-fluoro-4,5-dihydro- 5-hydroxy-l0-méthyl-l2- (4-méthyl pipéridinométhyl) -1H-oxépino[3',4':6,7]indolizino[1,2-b] quinoléine-3,15(4H,13H)-dione; leur application comme médicaments, les compositions pharmaceutiques les renfermant et leur utilisation pour la réalisation de médicaments antitumoraux, antiviraux ou antiparasitaires.

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