Growth hormone releasing peptides

Details Growth hormone releasing peptides Growth hormone releasing peptides

C - Chemistry, Metallurgy

07

K

C07K 7/06 (2006.01) A61K 38/07 (2006.01) A61K 38/08 (2006.01) A61P 5/06 (2006.01) C07K 5/10 (2006.01) C07K 5/117 (2006.01) A61K 38/25 (2006.01) C07K 14/60 (2006.01)

Patent

CA 2494300

Disclosed are peptide and peptidomimetic compounds generally according to formula (I), and pharmaceutically acceptable salts thereof, that are useful as GHRP analogs: R1-A2-A3-A4-A5-R2 (I) or a pharmaceutically acceptable salt thereof, wherein: A1 is Aib, Apc or Inp; A2 is D-Bal, D-Bip, D-Bpa, D-Dip, D- 1Nal, D-2Na1, D-Ser(Bzl), or D-Trp; A3 is D-Bal, D-Bip, D-Bpa, D-Dip, D-1Nal, D-2Nal, D-Ser(Bzl), or D-Trp; A4 is 2Fua, Orn, 2Pa1, 3Pal, 4Pa1, Pff, Phe, Pim, Taz, 2Thi, 3Thi, Thr(Bzl); A5 is Apc, Dab, Dap, Lys, Orn, or deleted; R1 is hydrogen, (C1-6)alkyl, (C5-14)aryl, (C1-6)alkyl(C5-14)aryl, (C3- 8)cycloakyl, or (C2-10)acyl; and R2 is OH or NH2; and pharmaceutical compositions and methods of use thereof.

L'invention concerne des peptides et des composés peptidomimétiques conformes, de façon générale, à la formule (I), et les sels pharmaceutiquement compatibles de ces composés, utilisés comme analogues de GHRP : R?1¿-A?2¿-A?3¿-A?4¿-A?5¿-R?2¿ (I) ou un sel pharmaceutiquement compatible de ce composé, formule dans laquelle A?1¿ désigne Aib, Apc ou Inp; A?2¿ désigne D-Bal, D-Bip, D-Bpa, D-Dip, D-1Nal, D-2Na1, D-Ser(Bzl), ou D-Trp; A?3¿ désigne D-Bal, D-Bip, D-Bpa, D-Dip, D-1Nal, D-2Nal, D-Ser(Bzl), ou D-Trp; A?4¿ désigne 2Fua, Orn, 2Pa1, 3Pal, 4Pa1, Pff, Phe, Pim, Taz, 2Thi, 3Thi, Thr(Bzl); A?5¿ désigne Apc, Dab, Dap, Lys, Orn, ou est supprimé; R?1¿ désigne l'hydrogène, (C1-6)alkyle, (C5-14)aryle, (C1-6)alkyle(C5-14)aryle, (C3-8)cycloalkyle, ou (C2-10)acyle; et R?2¿ désigne OH ou NH¿2?. L'invention concerne en outre des compositions pharmaceutiques et des procédés d'utilisation de celles-ci.

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