Bicyclic oligopeptides and their use as glucagon receptor...

Details Bicyclic oligopeptides and their use as glucagon receptor... Bicyclic oligopeptides and their use as glucagon receptor...

C - Chemistry, Metallurgy

07

K

C07K 7/56 (2006.01) A61K 38/12 (2006.01) C07K 14/36 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2489189

The invention relates to a bicyclic oligopeptide or ester thereof having the capability to inhibit the glucagon receptor, which essentially consists of(a) a first cyclic group, which comprises at least one cysteine group and is formed by an amide bonding of the N-terminal amino acid with the second carboxylate group of a diacid amino acid, and (b) a second cyclic group which is formed by an amide bonding of an amino acid with the -carboxylate group of said diacid amino acid, and by a disulfide bonding of the C-terminal cysteine and a cysteine group within the first cyclic group (a); andto the use of such bicyclic oligopeptides for the preparation of a medicament for the treatment or prevention of diseases, in which glucagon receptors are involved.

L'invention concerne un oligopeptide bicyclique ou un ester associé capable d'inhiber le récepteur du glucagon comprenant essentiellement (a) un premier groupe cyclique qui contient au moins un groupe de la cystéine et est formé par une liaison amide de l'acide aminé à terminal N avec le second groupe carboxylate d'un acide aminé de diacide, et (b) un second groupe cyclique qui est formé par une liaison amide d'un acide aminé avec le groupe .alpha.-carboxylate dudit acide aminé de diacide, et par une liaison de disulfure de la cystéine à terminal C et d'un groupe de la cystéine au sein du premier groupe cyclique (a). Cette invention a aussi pour objet l'utilisation de tels oligopeptides bicylciques dans la préparation d'un médicament destiné au traitement ou à la prévention de maladies, dans lesquelles les récepteurs du glucagon jouent un rôle.

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