Product containing at least one phosphatase cdc25 inhibitor...

A - Human Necessities – 61 – K

Patent

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Details

A61K 31/425 (2006.01) A61K 31/42 (2006.01) A61P 35/00 (2006.01) C07D 263/56 (2006.01) C07D 277/64 (2006.01) C07D 277/66 (2006.01) C07D 413/04 (2006.01) C07D 413/12 (2006.01) C07D 417/04 (2006.01) C07D 417/12 (2006.01) C07D 519/00 (2006.01)

Patent

CA 2530668

The invention relates to a product containing at least one phosphatase Cdc25 inhibitor combined with at least one other anticancer agent for simultaneous, separate or staggered therapeutic use during treatment for cancer. According to the invention, the other anticancer agent is preferably selected from: DNA base analogs such as 5-fluorouracil; inhibitors of type I and/or type II topoisomerases, such as camptothecin and the analogs thereof, doxorubicin or amsacrine; compounds interacting with the cellular spindle, for example, paclitaxel (Taxol); compounds acting on the cytoskeleton, such as vinblastine; inhibitors of the transduction of the signal passing via the heterotrimeric G proteins; prenyltransferase inhibitors, and especially farnesyltransferase inhibitors; cyclin-dependent kinase (CDKs) inhibitors; alkylating agents such as cisplatin; folic acid antagonists such as methotrexate; and inhibitors of DNA synthesis and cellular division, such as mitomycin C. The invention also relates to (1R)-1-[({(2R)-2-amino--3-[(8S)-8-(cyclohexylmethyl)-2-phenyl-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl]--3-oxopropyl}dithio)methyl]-2-[(8S)-8-(cyclohexylmethyl)-2-phenyl--5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl]-2-oxoethylamine, or the pharmaceutically acceptable salts thereof, that can be used as anticancer agents.

L'invention a pour objet un produit comprenant au moins un inhibiteur de phosphatase Cdc25 en association avec au moins un autre agent anti-cancéreux pour une utilisation thérapeutique simultanée, séparée ou étalée dans le temps dans le traitement du cancer. Selon l'invention, l'autre agent anti-cancéreux est de préférence choisi parmi : des analogues de bases de l'ADN comme le 5- fluorouracyle ; des inhibiteurs de topoisomérases de type I et/ou II comme par exemple la camptothécine et ses analogues, la doxorubicine ou l'amsacrine ; des composés interagissant avec le fuseau cellulaire comme par exemple le paclitaxel (Taxol) ; des composés agissant sur le cytosquelette comme la vinblastine ; des inhibiteurs de la transduction du signal passant par les protéines G hétérotrimériques ; des inhibiteurs de prényltransférases, et en particulier les inhibiteurs de farnésyltransférases ; des inhibiteurs des kinases dépendantes des cyclines (CDKs) ; des agents alkylants comme le cisplatine ; des antagonistes de l'acide folique comme le méthotrexate ; et des inhibiteurs de la synthèse de l'ADN et de la division cellulaire comme la mitomycine C. L'invention a encore pour objet la (1R)-1-[({(2R)-2-amino-~3- [(8S)-8-(cyclohexylméthyl)-2-phényl-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)- yl]~-3-oxopropyl}dithio)méthyl]-2-[(8S)-8-(cyclohexylméthyl)-2-phényl~-5,6- dihydroimidazo[1,2-a]pyrazin-7(8H)-yl]-2-oxoéthylamine, ou ses sels pharmaceutiquement acceptables, utiles en tant qu'agents anti-cancéreux.

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