Cyclic crf antagonist peptides

Details Cyclic crf antagonist peptides Cyclic crf antagonist peptides

C - Chemistry, Metallurgy

07

K

C07K 14/575 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2291856

Novel cyclic CRF antagonist peptides are created by shortening the N-terminus of a CRF family peptide by 8 residues and adding an acyl group. CML is present in what would be the 27-position of the native CRF sequence, and a cyclizing bond is created between the side chains of the residues in positions 30 and 33. The side chain of Lys, preferably, in position 33 is linked to the side chain of Glu in position 30 by a lactam bridge. Disclosed CRF antagonists include: (cyclo 30-33)[Ac-Asp9, D-Phe12, Nle21,38, CML27,40, Glu30, Lys33]r/hCRF(9-41); (cyclo 30-33) [Ac-Asp9, D-Phe12, CML18,27, Nle21,38, Glu30, Lys33]r-hCRF(9-41); (cyclo 30-33)[Ac-Asp9, D-Phe12, Nle21,38, CML27,37, Glu30, Lys33]r/hCRF(9-41); (cyclo 30-33)[Ac-Asp9, D-Phe12, CML14,27, Nle21,38, Glu30, Lys33]r/hCRF(9-41); (cyclo 30-33)[Ac-Asp9, D-Phe12, Nle21,38, CML27, Glu30, Lys33]r/hCRF(9-41); and (cyclo 30-33)[Ac-Asp9, D-Phe12, Nle21,38, CML27,40, Glu30, Aib32, Lys33]r/hCRF(9-41).

La présente invention concerne de nouveaux peptides cycliques antagonistes du CRF créés par réduction de huit résidus de l'extrémité terminale N d'un peptide de la famille du CRF et par adjonction d'un groupe acyle. CML est présent dans la position 27 de la séquence naturelle de CRF et une liaison de cyclisation est créée entre les chaînes latérales des résidus en position 30 et 33. La chaîne latérale de Lys, de préférence, en position 33, est liée à la chaîne latérale de Glu en position 30 par un pont de lactame. Les antagonistes du CFR décrits comprennent: (cyclo 30-33)[Ac-Asp?9¿, D-Phe?12¿, Nle?21'38¿, CML?27'40¿, Glu?30¿, Lys?33¿]r/hCRF(9-41); (cyclo 30-33)[Ac-Asp?9¿, D-Phe?12¿, CML?18'27¿, Nle?21'38¿, Glu?30¿, Lys?33¿]r/hCRF(9-41); (cyclo 30-33)[Ac- Asp?9¿, D-Phe?12¿, Nle?21'38¿, CML?27'37¿, Glu?30¿, Lys3?3¿]r/hCRF(9-41); (cyclo 30-33)[Ac-AsP?9¿, D-Phe?12¿, CML?14'27¿, Nle?21'38¿, Glu?30¿, Lys?33¿]r/hCRF(9-41); (cyclo 30-33)[Ac-Asp?9¿, D-Phe?12¿, Nle?21'38¿, CML?27¿, Glu?30¿, Lys?33¿]r/hCRF(9-41); et (cyclo 30-33)[Ac-Asp?9,¿ D-Phe?12¿, Nle?21'38¿, CML?27'40¿, Glu?30¿, Aib?32¿, Lys?33¿]r/hCRF(9-41).

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