Heterocyclic silicon compounds and their use in the...

C - Chemistry – Metallurgy – 07 – F

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C07F 7/08 (2006.01) A61K 31/695 (2006.01)

Patent

CA 2507532

A compound of formula (I) wherein one of X and Y is silicon, and the other is carbon or silicon; Z is oxygen, sulphur or -N(R)-, wherein R is hydrogen or alkyl; R1 is hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy or cycloalkyl; and R2 is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, -alkyl-cycloalkyl, -alkyl-heterocycloalkyl, -alkyl-aryl or -alkyl- heteroaryl; or a pharmaceutically acceptable salt thereof. The compounds are used in the manufacture of a medicament for the treatment or prevention of a disease or condition associated with GnRH (gonadotropin-releasing hormone), e.g. for the treatment or prevention of progression of cancer (e.g. leukaemia therapy), of a fertility disorder, of HIV infection or AIDS, of Alzheimer~s disease of fibrosis, of endometriosis, of uterine fibroids or of uterine leiomyoma.

L'invention concerne un composé de formule (I) dans laquelle un élément parmi X et Y désigne un silicium et l'autre représente un carbone ou un silicium; Z représente un oxygène, un soufre ou -N(R)-, où R représente un hydrogène ou un alkyle; R?1¿ désigne un hydrogène, un halogène, un alkyle, un alcényle, un alkynyle, un alcoxy ou un cycloalkyle; et R?2¿ représente un alkyle, un alcényle, un alkynyle, un cycloalkyle, un hétérocycloalkyle, un aryle, un hétéroaryle, un -alkyl-cycloalkyle, un -alkyl-hétérocycloalkyle, un -alkyl-aryle ou un -alkyl-hétéroaryle; ou un sel acceptable sur le plan pharmaceutique de ceux-ci. Les composés sont utiles dans la fabrication d'un médicament destiné au traitement ou à la prévention d'une maladie ou d'un état associé à GnRH (hormone de libération de la gonadotropine), <i>par exemple</i> pour le traitement ou la prévention de la progression du cancer (<i>e.g.</i> la thérapie de la leucémie), d'un trouble de la fertilité, d'une infection au VIH ou du SIDA, de la maladie d'Alzheimer, de la fibrose, de l'endométriose, des fibromes utérins ou du fibromyome.

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