Novel guanidine derivatives as inhibitors of cell adhesion

C - Chemistry – Metallurgy – 07 – D

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C07D 239/16 (2006.01) A61K 31/505 (2006.01) C07D 409/12 (2006.01)

Patent

CA 2371789

The present invention relates to acylguanidine derivatives of formula (I) in which R1, R2, R4, Ar, X and n have the meanings indicated in the claims, their physiologically tolerable salts and their prodrugs. The compounds of formula (I) are valuable pharmacologically active compounds. They are vitronectin receptor antagonists and inhibitors of cell adhesion. They inhibit, for example, bone resorption by osteoclasts and are suitable for the therapy and prophylaxis of diseases which are caused at least partially by an undesired extent of bone resorption, for example osteoporosis. The invention furthermore relates to processes for the preparation of compounds of formula (I), their use, in particular as active ingredients in pharmaceutical preparations, and pharmaceutical preparations comprising them.

La présente invention se rapporte à des dérivés d'acylguanidine représentés par la formule (I) dans laquelle R<1>, R<2>, R<4>, Ar, X et n sont définis dans les revendications, ainsi qu'à leurs sels pharmaceutiquement acceptables et à leurs promédicaments. Les composés représentés par la formule (I) sont des composés pharmacologiquement actifs particulièrement intéressants. Ce sont des antagonistes des récepteurs de la vitronectine et des inhibiteurs d'adhésion cellulaire. Ils inhibent, par exemple, la résorption osseuse par les ostéoclastes et sont adaptés au traitement thérapeutique et prophylactique des maladies qui sont au moins partiellement dues à un développement indésirable de résorption osseuse, par exemple l'ostéoporose. L'invention se rapporte en outre à des processus de préparation des composés de formule (I), à leur utilisation, notamment en tant qu'ingrédients actifs dans des préparations pharmaceutiques et à des préparations pharmaceutiques contenant de tels composés.

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