Thienylalanine derivatives as inhibitors of cell adhesion

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 409/12 (2006.01) A61K 31/505 (2006.01) A61P 19/08 (2006.01) A61P 19/10 (2006.01)

Patent

CA 2394767

The present invention relates to compounds of formula (I), in which A, B, X, Y, R1, R2, R3 and n have the meanings indicated in the claims. The compounds of formula (I) are valuable pharmacologically active compounds. They are vitronectin receptor antagonists and inhibitors of cell adhesion and are suitable for the therapy and prophylaxis of illnesses which are based on the interaction between vitronectin receptors and their ligands in cell-cell or cell-matrix interaction processes or which can be prevented, alleviated or cured by influencing such interactions. For example, they can be applied for inhibiting bone resorption by osteoclasts and thus for treating and preventing osteoporosis, or for inhibiting undesired angiogenesis or proliferation of cells of the vascular smooth musculature. The invention fruthermore relates to processes for the preparation of compounds of formula (I), their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.

La présente invention concerne des composés de formule (I) dans laquelle A, B, X, Y, R?1¿, R?2¿, R?3¿ et n possèdent les significations indiquées dans les revendications. Les composés de formule (I) sont des composés actifs valables sur le plan pharmaceutique. Ce sont des antagonistes du récepteur de la vitronectine et des inhibiteurs d'adhésion cellulaire et ils sont indiqués pour la thérapie et la prophylaxie de maladies basées sur l'interaction entre les récepteurs de vitronectine et leurs ligands dans des processus d'interaction cellule-cellule ou cellule-matrice, ou qui peuvent être prévenues, atténuées ou guéries en influençant de telles interactions. Ils peuvent être appliqués, par exemple, afin d'inhiber la résorption osseuse par les ostéoclastes et donc pour traiter et prévenir l'ostéoporose, ou afin d'inhiber une angiogénèse indésirable ou une prolifération cellulaire de la musculature lisse vasculaire. L'invention concerne aussi des procédés de préparation des composés de formule (I), leur utilisation, en particulier comme principes actifs de produits pharmaceutiques, ainsi que des compositions pharmaceutiques les contenant.

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