Thienyl substituted acylguanidines as inhibitors of bone resorption and vitronectin receptor antagonists

US6660728B2 · kind B2 · utility

Assignees

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

Inventors

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

Key dates

• Filing date: Nov 14, 2002
• Grant date: Dec 9, 2003
• Expiry date: Nov 14, 2022

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D409/14
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

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