Pro-drugs and counterparts of camptothecin, their...

C - Chemistry – Metallurgy – 07 – D

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Details

C07D 498/22 (2006.01) A61K 31/47 (2006.01) C07D 471/14 (2006.01) C07D 491/22 (2006.01)

Patent

CA 2275345

The invention concerns novel counterparts of camptothecin and in particular products complying with the following formulae: 8-ethyl-8,9-dihydro-8-hydroxy-1-benzyl-2H,10H,12H-[1,3]oxazino[5,6-f]oxepino[3',4':6,7]indolizino[1,2-b]quinolein-10,13(15H)-dione; 5-ethyl-9,10-difluoro-4,5-dihydro-5-(2-amino-1-oxoethoxy)-1H-oxepino[3',4':6,7]indolizino[1,2-b]quinolein-3,15(4H,13H)-dione; 5-ethyl-9,10-difluoro-4,5-dihydro-5-(2-amino-1-oxopropoxy)-1H-oxepino[3',4':6,7]indolizino[1,2-b]quinolein-3,15(4H,13H)-dione. The invention also concerns their method of preparation, their application as medicines, the pharmaceutical compositions containing them and their use in producing tumoricidal, antiviral and parasiticide medicines.

L'invention concerne de nouveaux analogues de la camptothécine et en particulier les produits répondant aux formules suivantes: 8-éthyl-8,9-dihydro-8-hydroxy-1-benzyl-2H, 10H, 12H-[1,3]oxazino[5,6- .function.]oxépino[3',4':6,7]indolizino[1,2-b]quinoléine-10,13(15H)-dione; 5-éthyl-9,10-difluoro-4,5-dihydro-5-(2-amino-1-oxoéthoxy)-1H- oxépino[3',4':6,7]indolizino[1,2-b]quinoléine-3,15(4H,13H)-dione; 5-éthyl- 9,10-difluoro-4,5-dihydro-5-(2-amino-1-oxopropoxy)-1H- oxépino[3',4':6,7]indolizino[1,2-b]quinoléine-3,15(4H,13H)-dione; leur procédé de préparation, 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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