C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 14/585 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2245379
Superpotent calcitonin analogs (Ct) having greatly increased hypocalcemic action in vivo. The invention relates to calcitonins and calcitonin derivatives such as are employed for the therapy, for example, of osteoporosis, of Paget's disease or of hypercalcemia. The calcitonins and calcitonin derivatives according to the invention are distinguished by a bridging of the amino acids present in the positions 17 and 21. In this case, 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 Ct) analog is the type cyclo17.21- [Asp17,Om21]-hCt according to the invention having a 19-membered ring structure between the lactam--bridged Asp17 and Om21.
L'invention porte sur des calcitonines et des dérivés de calcitonines, comme ceux utilisés pour le traitement, par exemple, de l'ostéoporose, de la maladie de Paget ou de l'hypercalcémie. Les calcitonines et dérivés de calcitonines de l'invention sont caractérisés par un pontage des acides aminés présents en positions 17 et 21. Dans ce cas, grâce à un choix approprié des acides aminés présents à ces positions, il est possible d'obtenir un cycle de 18 ou 19 chaînons. Ce cycle permet d'obtenir une calcitonine modifiée présentant une meilleure stabilité de configuration et une plus grande activité. Un analogue de hCt (Ct humaine) particulièrement approprié, selon l'invention, est la cyclo-17,21-[Asp17,Om21]-hCt, possédant un cycle de 19 chaînons entre l'Asp17 l'Om21 ainsi pontés.
Bernhagen Jurgen
Brunner Herwig
Kapurniotu Afroditi
Fraunhofer-Gesellschaft Zur Forderung Der Angewandten Forschung
Mcfadden Fincham
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