Superpotent calcitonin analogs having greatly increased hypocalcemic action in vivo

US6617423B1 · kind B1 · utility

Assignee

• Max-Planck-Gesellschaft zur Föderung der Wissenschaften e.V. · US

Inventors

• Afroditi Kapurniotu · Aachen, DE
• Jurgen Bernhagen · Tübingen, DE
• Herwig Brunner · Stuttgart, DE

Key dates

• Filing date: Dec 20, 2000
• Grant date: Sep 9, 2003
• Expiry date: Mar 21, 2021

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K38/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Calcitonins and calcitonin derivatives such as are employed for therapy for, for example, osteoporosis. Paget's disease or hypercalcemia. The calcitonins and calcitonin derivatives are distinguished by a bridging of the amino acids present in the positions 17 and 21. In this case, by means of a suitable choice of the amino acids present in these positions an 18- or 19-membered ring is produced. This ring leads to an increased conformational stability and to an increased activity of the modified calcitonin. A particularly suitable hCt (human Ct) analog is the cyclo17,21-[Asp17, Orn21]-hCt according to the invention having a 19-membered ring structure between the lactam-bridged Asp17 and Orn21.