Back to results
US 2012/0258181 A1Published application
Anticancer combination of artemisinin-based drugs and other chemotherapeutic agents
AssigneeSigma-Tau Industrie Farmaceutiche Riunite S.p.A.
InventorsClaudio Pisano, Loredana Vesci
Life of this patent
Estimating the term…
Abstract
The present invention relates to combinations between artemisinin-based potent anti-malarial agents, selected from the group consisting of ART, DHA and ARM, and a further chemotherapeutic drug selected from the group consisting of a camptothecin derivative, or a PARP-1 inhibitor, or an intercalating DNA agent, or an alkylating agent. Such combinations, showed medium to strong synergism in various models of cancer, in particular in NSCL.
Claims19
A chemotherapeutic combination consisting of:
- a pharmaceutical agent (a) selected from the group consisting of ART, DHA and ARM;
- and a chemotherapeutic agent (b) selected from the group consisting of camptothecin derivatives which are themselves selected from the group consisting of 7-methoxyiminomethylcamptothecin, 7-methoxyiminomethyl-10-hydroxycamptothecin, 7-(ter-butoxycarbonyl-2-propoxy)-iminomethylcamptothecin, 7-ethoxyiminomethylcamptothecin, 7-isopropoxy-iminomethylcamptothecin, 7-(2-methylbutoxy)-iminomethylcamptothecin, 7-t-butoxyiminomethylcamptothecin, 7-t-butoxyiminomethyl-10-hydroxycamptothecin, 7-t-butoxyiminomethyl-10-methoxycamptothecin, 7-(4-hydroxybutoxy)-iminomethylcamptothecin, 7-triphenyl-methoxyiminomethylcamptothecin, 7-carboxymethoxyiminomethyl-camptothecin, 7-(2-amino)-ethoxyiminomethyl-camptothecin, 7-(2-N,N-dimethylamino)-ethoxyiminomethylcamptothecin, 7-allyloxyiminomethyl-camptothecin, 7-cyclohexyloxyiminomethylcamptothecin, 7-cyclohexylmethoxyiminomethylcamptothecin, 7-cyclooctyloxyiminomethyl-camptothecin, 7-cyclooctylmethoxyiminomethyl-camptothecin, 7-benzyloxy-iminomethylcamptothecin, 7-[(1-benzyloxyimino)-2-phenylethyl]camptothecin, 7-(lbenzyloxyimino)-ethylcamptothecin, 7-phenoxy-iminomethyleamptothecin, 7-(1-t-butoxyimino)-ethylcamptothecin, 7-p-nitrobenzyloxyiminomethylcamptothecin, 7-p-methylbenzyloxyiminomethylcamptothecin, 7-pentafluorobenzyloxyiminomethyl-camptothecin, 7-p-phenylbenzyloxyiminomethyl-camptothecin, 7-[2-(2,4-difluorophenyl)-ethoxyliminomethylcamptothecin, 7-(4-t-butylbenzyloxy)-iminomethylcamptothecin, 7-(1-adamantyloxy)-iminomethyl-camptothecin, 7-(1-adamantylmethoxy)-iminomethylcamptothecin, 7-(2-naphthyloxy)-iminomethyl-camptothecin, 7-(9-anthrylmethoxy)-iminomethylcamptothecin, 7-oxiranylmethoxyiminomethyl-camptothecin, 7-(6-uracyl)-methoxy-iminomethylcamptothecin, 7-[2-(1-uracyl)-ethoxy]-iminomethylcamptothecin, 7-(4-pyridyl)-methoxyiminomethyl-camptothecin, 7-(2-thienyl)-methoxyiminomethyl-camptothecin, 7-[(N-methyl)-4-piperidinyl]-methoxyiminomethylcamptothecin, 7-[2-(4-morpholininyl]-ethoxy]-iminomethylcamptothecin, 7-(benzoyloxyiminomethyl)-camptothecin, 7-[(1-hydroxyimino)-2-phenylethyl)-camptothecin, 7-ter-butyloxy-iminomethyl-camptothecin N-oxide, 7-methoxyiminomethylcamptothecin N-oxide, irinotecan and its active metabolite SN-38;
- PARD-1 inhibitors, intercalating DNA agents and alkylating agents;
- within said combination, each ingredient (a) and (b) are formulated from each other or are formulated in a single dosage form.
1 more element
A medicament comprising a chemotherapeutic combination consisting of:
- a pharmaceutical agent (a) selected from the group consisting of ART, DHA and ARM;
- and a chemotherapeutic agent (b) selected from the group consisting of camptothecin derivatives selected from the group consisting of 7-methoxyiminomethylcamptothecin, 7-methoxyiminomethyl-10-hydroxycamptothecin, 7-(ter-butoxycarbonyl-2-propoxy)-iminomethylcamptothecin, 7-ethoxyiminomethylcamptothecin, 7-isopropoxy-iminomethylcamptothecin, 7-(2-methylbutoxy)-iminomethylcamptothecin, 7-t-butoxyiminomethylcamptothecin, 7-t-butoxyiminomethyl-10-hydroxycamptothecin, 7-t-butoxyiminomethyl-10-methoxycamptothecin, 7-(4-hydroxybutoxy)-iminomethylcamptothecin, 7-triphenyl-methoxyiminomethylcamptothecin, 7-carboxymethoxyiminomethyl-camptothecin, 7-(2-amino)-ethoxyiminomethyl-camptothecin, 7-(2-N,N-dimethylamino)-ethoxyiminomethylcamptothecin, 7-allyloxyiminomethyl-camptothecin, 7-cyclohexyloxyiminomethylcamptothecin, 7-cyclohexylmethoxyiminomethylcamptothecin, 7-cyclooctyloxyiminomethyl-camptothecin, 7-cyclooctylmethoxyiminomethyl-camptothecin, 7-benzyloxy-iminomethylcamptothecin, 7-[1-benzyloxyimino)-2-phenylethyl]camptothecin, 7-(lbenzyloxyimino)-ethylcamptothecin, 7-phenoxyiminomethyleamptothecin, 7-(1-t-butoxyimino)-ethylcamptothecin, 7-p-nitrobenzyl-oxyiminomethylcamptothecin, 7-p-methylbenzyloxyiminomethylcamptothecin, 7-pentafluorobenzyloxyiminomethyl-camptothecin, 7-p-phenylbenzyloxyiminomethyl-camptothecin, 7-[2-(2,4-difluorophenyl)-ethoxy]iminomethylcamptothecin, 7-(4-t-butylbenzyloxy)-iminomethylcamptothecin, 7-(1-adamantyloxy)-iminomethyl-camptothecin, 7-(1-adamantylmethoxy)-iminomethylcamptothecin, 7-(2-naphthyloxy)-iminomethyl-camptothecin, 7-(9-anthrylmethoxy)-iminomethylcamptothecin, 7-oxiranylmethoxyiminomethyl-camptothecin, 7-(6-uracyl)-methoxy-iminomethylcamptothecin, 7-[2-(1-uracyl)-ethoxy]-iminomethylcamptothecin, 7-(4-pyridyl)-methoxyiminomethyl-camptothecin, 7-(2-thienyl)-methoxyiminomethyl-camptothecin, 7-[(N-methyl)-4-piperidinyl]-methoxyiminomethylcamptothecin, 7-[2-(4-morpholininyl]-ethoxy]-iminomethylcamptothecin, 7-(benzoyloxyiminomethyl)-camptothecin, 7-[(1-hydroxyimino)-2-phenylethyl)-camptothecin, 7-ter-butyloxy-iminomethyl-camptothecin N-oxide, 7-methoxyiminomethylcamptothecin N-oxide, irinotecan and its active metabolite SN-38, PARP-1 inhibitors, intercalating DNA agents and alkylating agents, as medicament.
Dependencies are inferred from the claim text.