New stilbenes with vascular damaging activity

C - Chemistry – Metallurgy – 07 – C

Patent

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Details

C07C 43/23 (2006.01) A61K 31/09 (2006.01) A61K 47/48 (2006.01) A61P 35/00 (2006.01) C07F 9/12 (2006.01)

Patent

CA 2379544

A group of novel cis-stilbenes as disclosed of formula (1) wherein: R1, R2 and R3 are each independently alkyl, R4 is alkyl, haloalkyl, alkenyl, alkynyl, alkylthio, alkylsulphinyl, alkylsulphonyl or halo, R5 is hydrogen, alkoxy, alkyl, alkylthio, hydroxy or halo, or a pharmaceutically acceptable salt thereof or a prodrug such as a phosphate ester. These compounds have vascular damaging activity and are therefore potentially of value in treatment of diseases where reversal of neovascularisation may have therapeutic benefit.

L'invention concerne un nouveau groupe de cis-stilbènes représentés par la formule (1), ou un sel pharmaceutiquement acceptable de ceux-ci, ou un promédicament tel qu'un ester de phosphate. Dans cette formule, R?1¿, R?2¿, et R?3¿ représentent chacun indépendamment alkyle; R?4¿ représente alkyle, haloalkyle, alcényle, alcynyle, alkylthio, alkylsulphinyle, alkylsulphonyle ou halo; R?5¿ représente hydrogène, alcoxy, alkle, alkylthio, hydroxy ou halo. Ces composés possèdent une activité de dégradation vasculaire. et sont cependant potentiellement utiles pour traiter des maladies dans lesquelles le renversement de la néovascularisation peut présenter un bénéfice thérapeutique.

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