Novel acylguanidine derivatives as inhibitors of bone...

C - Chemistry – Metallurgy – 07 – D

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C07D 239/16 (2006.01) A61K 31/505 (2006.01) C07C 279/20 (2006.01)

Patent

CA 2312712

The present invention relates to acylguanidine derivatives of formula (I) in which R1, R2, R4, R5, R6, A, m and n have the meanings indicated in the patent claims, their physiologically tolerable salts and their prodrugs. The compounds of formula (I) are valuable pharmaceutical active ingredients. They are vitronectin receptor antagonists and inhibitors of bone resorption by osteoclasts and are suitable, for example, for the therapy or prophylaxis of diseases which are caused at least partially by an undesired extend of bone resorption, for example of osteoporosis. The invention furthermore relates to processes for the preparation of compounds of formula (I), their use, in particular as pharmaceutical active ingredients, and pharmaceutical preparations comprising them.

L'invention concerne des dérivés d'acylguanidine représentés par la formule (I) dans laquelle R?1¿, R?2¿, R?4¿, R?5¿, R?6¿, A, m et n possèdent les significations énoncées dans les revendications, leurs sels tolérables sur le plan physiologique et leurs promédicaments. Ces composés constituent des ingrédients pharmaceutiquement actifs de valeur. Ils constituent des antagonistes du récepteur de vitronectine et des inhibiteurs de la résorption osseuse provoquée par des ostéoclastes et sont appropriés, par exemple, à la thérapie et à la prophylaxie de maladies provoquées au moins partiellement par une extension indésirable de la résorption osseuse, par exemple, de l'ostéoporose. Elle concerne, de plus, des procédés servant à préparer des composés de formule (I), leur utilisation, en particulier, en tant qu'ingrédients pharmaceutiques actifs, et des préparations pharmaceutiques les contenant.

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