Guanidine derivatives as inhibitors of cell adhesion

US6340679B1 · kind B1 · utility

Assignees

• Aventis Pharma Deutschland GmbH · DE
• Genentech, Inc. · US

Inventors

• Anuschirwan Peyman · Kelkheim, DE
• Jochen Knolle · Kriftel, DE
• Karl-Heinz Scheunemann · Liederbach, DE
• David William Will · Schwalbach, DE
• Denis Carniato · Marcoussis, FR
• Jean-Francois Gourvest · Claye-Souilly, FR
• Thomas Gadek · Oakland, US
• Sarah C. Bodary · San Francisco, US

Key dates

• Filing date: Feb 11, 2000
• Grant date: Jan 22, 2002
• Expiry date: Feb 11, 2020

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D239/16
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to acylguanidine derivatives of the 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 the 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 the formula I, their use, in particular as active ingredients in pharmaceutical preparations, and pharmaceutical preparations comprising them.