Insulin derivatives and synthesis thereof

Details Insulin derivatives and synthesis thereof Insulin derivatives and synthesis thereof

C - Chemistry, Metallurgy

07

K

C07K 14/62 (2006.01) A61K 38/28 (2006.01) A61P 3/10 (2006.01) C07K 1/00 (2006.01) C07K 1/107 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2415425

Derivatives of insulin are described which are conjugated to thyroid hormones. The thyroid hormone is, for instance, D-thyroxine (3,3',5,5'-tetraiodo-D- thyronine). Other analogues are described in which a spacer having a alkanediyl chain at least eleven carbon atoms long is included. Binding studies show useful binding characteristics to thyroid binding proteins. New synthetic methods in which racemisation of the thyroxin is minimised, are described.

L'invention concerne des dérivés d'insuline conjugués à des hormones thyroïdiennes, comme par exemple la D-thyroxine (3,3',5,5'-tétraiodo-D-thyronine), et d'autres analogues dans lesquels un séparateur présentant une chaîne alkanediyle longue d'au moins onze atomes de charbon est inclus. Des études en matière de liaison révèlent l'existence de protéines de liaison thyroïdiennes à propriétés de liaison utiles. L'invention concerne également de nouveaux procédés de synthèse selon lesquels la racémisation de la thyroxine est minimisée.

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