Analogs of ghrelin substituted at the n-terminal

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 14/575 (2006.01) A61K 38/16 (2006.01) A61K 38/22 (2006.01) C07K 14/61 (2006.01) C07K 14/72 (2006.01)

Patent

CA 2664558

The invention comprises peptidyl analogs of ghrelin having greater stability which are active at the GHS receptor according to formulae depicted below: (R2)-A1-A2-A3-A4-A5-A6-A7-A8-A9-A10-A11-A12-A13-A14-A15-A16-A17-A18-A19-A20-A21-A22- A23-A24-A25-A26-A27-A28-R1 wherein the definitions of A1 to A28, R1 and R2 are provided for in the specification, with the exception that the N-terminal amino acid must be selected from the group consisting of Inp, 1-Apc and 4-Apc, the pharmaceutically acceptable salts thereof and pharmaceutical compositions comprising an effective amount of said compound together with therapeutic and non-therapeutic uses thereof.

La présente invention concerne des analogues peptidyl de ghréline de plus grande stabilité qui sont actifs au niveau du récepteur GHS, lesquels analogues sont représentés par la formule : (R2)-A1-A2-A3-A4-A5-A6-A7-A8-A9-A10-A11-A12-A13-A14-A15-A16-A17-A18-A19-A20-A21-A22- A23-A24-A25-A26-A27-A28-R1, A1 à A28 de même que R1 et R2 étant tels que définis dans la spécification, étant entendu que l'acide aminé N-terminal doit être sélectionné dans le groupe comprenant Inp, 1-Apc et 4-Apc, et concerne également les sels pharmaceutiquement acceptables de ceux-ci, des compositions pharmaceutiques contenant une quantité efficace de ces composés, ainsi que des utilisations thérapeutiques et non thérapeutiques de ceux-ci.

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