Superpotent calcitonin analogs having greatly increased hypocalcemic action in vivo

US6265534A · kind A · 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: Aug 20, 1998
• Grant date: Jul 24, 2001
• Expiry date: Aug 20, 2018

Classification

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

Abstract

Superpotent calcitonin analogs have greatly increased hypocalcemic action in vivo. These calcitonins and calcitonin derivatives are employed for the therapy of, 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. By means of suitable choice of the amino acids present in these positions an 18-membered 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 calcitonin analog) is a cyclo.sup.17,21 -[Asp.sup.17, Orn.sup.21 ]-hCt having a 19-membered ring structure between the lactam-bridged Asp.sup.17 and Orn.sup.21.