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New all trans platinum (IV) complexes, their preparation and their use as antitumor agentsCM Patents

Índice de la ficha

Updated at
24/07/2026
Numero publicacion
EP.2404925.A1
Fecha publicacion
11/01/2012
Numero solicitud
EP20100305768
Fecha presentacion
09/07/2010

En detalle

Resumen

The present invention relates to derivatives of formula (I) in which R1 and R2, identical or different, represent a hydrogen atom or a linear or branched C1-4 alkyl radical; provided that one of R1 and R2 is different from a hydrogen atom; R3 represents a bicyclic group of general formula (II): X represents O or -CH 2 - or -(CH 2 ) 2 -; in the form of a free base, of an hydrate or of a solvate.

Reivindicaciones

1. A compound of general formula (I) : <img class="EMIRef" id="465012266-ib0018" /> in which: R1 and R2, identical or different, represent a hydrogen atom or a linear or branched C1-4 alkyl radical; provided that one of R1 and R2 is different from a hydrogen atom; R3 represents a bicyclic group of general formula (II): <img class="EMIRef" id="465012266-ib0019" /> X represents O or -CH<2> - or -(CH<2> )<2> -; in the form of a free base, of an hydrate or of a solvate. 2. A compound of formula (I) according to Claim 1, characterized in that R1 is H and R2 represents a linear or branched C1-4 alkyl radical; or R1 and R2 both are methyl. 3. A compound of formula (I) according to Claim 1 or 2, characterized in that R1 is H and R2 is an isopropyl group. 4. A compound of formula (I) according to Claim 1, characterized in that NH<2> -R3 is theexo- or theendo -norbornylamine; the compound of formula (I) being either in the form of a racemate or of its pure levogyre or dextrogyre enantiomer. 5. A compound according to Claim 1, where - R1 is H and R2 is isopropyl; - NH<2> -R3 is theexo- or theendo -norbornylamine; the compound of formula (I) being either in the form of a racemate or of its pure levogyre or dextrogyre enantiomer. 6. A compound according to Claim 1, where - R1 and R2 are methyl; - NH<2> -R3 is theexo -norbornylamine; the compound of formula (I) being either in the form of a racemate or of its pure levogyre or dextrogyre enantiomer. 7. A compound according to Claim 1, chosen among: -trans-trans-trans -{PtCl<2> (OH)<2> (isopropylamine)[(rac )-(exo )-norbornylamine]}; -trans-trans-trans -{PtCl<2> (OH)<2> (isopropylamine)[(rac )-(endo )-norbornylamine]}; and -trans-trans-trans -{PtCl<2> (OH)<2> (dimethylamine)[(exo)-2- norbornylamine]). 8. Process for the preparation of a compound of formula (I) as defined in claim 1, where the compound of formula (IV) <img class="EMIRef" id="465012266-ib0020" /> where R1, R2 and R3 are as defined in formula (I) according to claim 1, reacts with hydrogen peroxide in the darkness to give compound of formula (1). 9. Process for the preparation of a compound of formula (IV) as defined in claim 8, where the compound of formula (III) <img class="EMIRef" id="465012266-ib0021" /> where R1 and R2 are as defined in formula (I) according to claim 1, reacts with an amine of formula NH<2> R3, where R3 is as defined in formula (I) according to claim 1, followed by a treatment with water and hydrochloric acid to give compound of formula (IV). 10. Compound of formula (IV) <img class="EMIRef" id="465012266-ib0022" /> in which: R1 and R2, identical or different, represent a hydrogen atom or a linear or branched C1-4 alkyl radical R3 represents a bicyclic group of general formula (II): <img class="EMIRef" id="465012266-ib0023" /> X represents O or -CH<2> - or -(CH<2> )<2> - 11. Medicament, characterized in that it comprises a compound of formula (I) according to any one of Claims 1 to 7, a hydrate or a solvate of the compound of formula (I). 12. Pharmaceutical composition, characterized in that it comprises a compound of formula (I) according to any one of Claims 1 to 7, a hydrate or a solvate of this compound, and at least one pharmaceutically acceptable excipient. 13. A compound of formula (I) according to any one of Claims 1 to 7, for its use for the treatment of cancer.

Etiquetas

Inventores
Navarro Ranninger CarmenAlvarez-Valdes AmparoQuiroga Adoracion GomezVadillo Ana GonzalezLara Jose AlemanMailliet PatrickBourrie Bernard
Solicitantes
Universidad Autónoma de Madrid
Clasificacion ipc
A61P 35/ 00 A IC07F 15/ 00 A I
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