Klainetin and derivatives thereof, method for their...

C - Chemistry – Metallurgy – 07 – D

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C07D 311/32 (2006.01) A61K 31/12 (2006.01) A61K 31/353 (2006.01) A61P 25/00 (2006.01) C07C 45/78 (2006.01) C07C 49/835 (2006.01) C07C 49/84 (2006.01)

Patent

CA 2430466

The invention relates to compounds of general formula (I): and formula (II): wherein R1, R2, R3, R4, R5, X1, X2, X3, X4, X5 and Y are defined as per the description. The compounds of formula (I) and (II) inhibit cyclin-dependent kinases (CDKs) and additional kinases (KDR), have cytostatic properties and are particularly suitable for treating tumours. The compounds of formulas (I) and (II) can be obtained by extraction of the plant Uvaria klaineri, PLA 100484, by cell cultures of the plant Uvaria klaineri or by chemical synthesis. The invention also relates to a method for producing the compounds of formulas (I) and (II), to the use of said compounds for producing a medicament for treating malignant diseases and diseases that can be treated by inhibiting CDKs and KDR.

L'invention concerne des composés de formules générales (I) et (II), dans lesquelles R¿1?, R¿2?, R¿3?, R¿4?, R¿5? et X¿1?, X¿2?, X¿3?, X¿4?, X¿5?, ainsi que Y ont les significations indiquées dans la description. Les composés de formules (I) et (II) inhibent les kinases dépendantes des cyclines [cyclin-dependent kinases (CDK)] et d'autres kinases (KDR), ils possèdent des effets cytostatiques et sont particulièrement adaptés pour traiter des tumeurs. Ces composés peuvent être obtenus par extraction de la plante Uvaria klaineri, PLA 100484, par culture cellulaire de cette plante ou par synthèse chimique. L'invention concerne également un procédé permettant de produire les composés des formules (I) et (II), ainsi que l'utilisation de ces composés pour préparer un médicament servant à traiter des affections malignes et des maladies pouvant être traitées par inhibition des CDK et des KDR.

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