Methods of inhibiting the ghrelin/growth hormone...

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 7/08 (2006.01) A61K 31/445 (2006.01) A61K 38/22 (2006.01) A61P 3/04 (2006.01) C07K 7/06 (2006.01) C07K 14/575 (2006.01) C07K 14/60 (2006.01)

Patent

CA 2761901

The invention provides methods for treatment, prevention or management of obesity, obesity related disorders, diabetes mellitus, and metabolic syndrome in a subject by administering a ghrelin O-acyltransferase (GOAT) inhibitor and/or a ghrelin receptor antagonist to the subject. The invention also provides ghrelin receptor antagonists of formula (VII): A11-A12-A13-Gly-Ser-A14-Phe-Leu-A15-A16-A17-A18, wherein each of A11, A12, and A13 is independently absent, an amino acid, or an amino protecting group; each of A15-A16-A17, and A18 is independently absent or an amino acid; and A14 is a serine conjugated with a -C(O)C1-C20alky or a diaminopropionic acid conjugated with a -C(O)C1-C20alkyl group, provided that at least one of A11, A12, or A13 is present.

L'invention porte sur des procédés pour le traitement, la prévention ou la gestion de l'obésité, de troubles liés à l'obésité, du diabète sucré et du syndrome métabolique chez un sujet par l'administration d'un inhibiteur de la ghréline O-acyltransférase (GOAT) et/ou d'un antagoniste du récepteur de la ghréline au sujet. L'invention porte également sur des antagonistes du récepteur de la ghréline de formule (VII) : A11-A12-A13-Gly-Ser-A14-Phe-Leu-A15-A16-A17-A18, dans laquelle chacun parmi A11, A12 et A13 est indépendamment absent, un acide aminé ou un groupe protecteur amino, chacun parmi A15, A16, A17 et A18 est indépendamment absent ou un acide aminé ; et A14 est une sérine conjuguée à un alkyl-C(O)C1-C20 ou un acide diaminopropionique conjugué à un groupe alkyl-C(O)C1-C20, à la condition qu'au moins l'un parmi A11, A12 ou A13 soit présent.

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