Eurotinones, and derivatives thereof, processes for...

C - Chemistry – Metallurgy – 07 – D

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C07D 313/12 (2006.01) A61K 31/00 (2006.01) A61P 35/00 (2006.01) C12N 1/14 (2006.01)

Patent

CA 2451230

The invention relates to novel compounds of general formula (I), wherein R(1), R(2), R(3), R(4) independently represent hydrogen or an alkyl radical. The compounds of formula (I) are inhibitors of KDR-kinase, having an anti- angiogenetic effect, and are suited for the prevention and/or treatment of malignant illnesses. The compounds of formula (I) can be obtained by fermenting the microorganism Eurotium echinalutum Delacroix (DSM 13872) or by means of chemical derivatization of the compounds obtained after fermenting said microorganism. The invention also relates to a method for producing compounds of Formula (I), the use of said compounds for producing a drug for treating malignant illnesses and illnesses which can be treated by inhibiting KDR-Kinase, and for pharmaceutical preparations containing at least one compound of formula (I).

La présente invention concerne de nouveaux composés de formule générale (I) dans laquelle R(1), R(2), R(3), R(4) représentent indépendamment hydrogène ou un radical alkyle. Les composés de formule (I) sont des inhibiteurs de la KDR-kinase et conviennent à la prévention et/ou au traitement de maladies de type malignes, en raison de leur effet anti-angiogène. Les composés de formule (I) peuvent être obtenus par fermentation du micro-organisme Eurotium echinulatum Delacroix (DSM 13872) ou par dérivatisation chimique des composés obtenus après la fermentation dudit micro-organisme. L'invention a également pour objet un procédé destiné à la préparation des composés de formule (I), l'utilisation des composés de formule (I) pour préparer un produit pharmaceutique destiné au traitement de maladies de type malignes et de maladies qui peuvent être traitées par inhibition de la KDR-kinase, ainsi que des préparations pharmaceutiques contenant au moins un composé de formule (I).

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