Hgh-rh(1-29)nh2 analogues having antagonistic activity

Details Hgh-rh(1-29)nh2 analogues having antagonistic activity Hgh-rh(1-29)nh2 analogues having antagonistic activity

C - Chemistry, Metallurgy

07

K

C07K 14/60 (2006.01) A61K 38/25 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2253663

There A peptide selected from the group having the formulae: .alpha.) X-R1-R2- R3-R4-R5-R6-Thr-R8-R9-R10-R11-R12-Val-Leu-R15-Gln-Leu-Ser-R19-R20-R21-Leu-Leu- Gln-Asp-Ile-R27-R28-R29, wherein X is H, Ac, Aqc, IAc, BrProp, For, Ibu, Nac, 2-Nac, 1- or 2-Npt, 1- or 2-Npr, PhAc, Fpr, or any other aromatic or nonpolar acyl group, R1 is Tyr, His or Phe(Y), in which Y=H, F, Cl, Br, NO2, NH2, CH3 or OCH3, R2 is D-Arg, D-Cit, D-Har, D-Lys,D-Tic or D-Orn, R3 is Asp, D-Asp, Ala, D-Ala or Gly, R4 is Ala, Abu or Gly, R5 is Ile, Ala or Gly, R6 is Phe, Tic, Ala, Pro, Tpi, Nal or Phe(Y), in which Y=H, F, Cl, Br, NO2, NH2, CH3 or OCH3, R8 is Asn, Gln, Ser, Thr, Val, Leu, Ile, Ala, D-Ala, D-Asn, D-Gln, D- Thr, D-Leu, Abu, D-Abu, Nle, or Aib, R9 is Ser, R10 is Tyr or Phe(Y), in which Y=H, F, Cl, Br, NO2, CH3 or OCH3, R11 is Arg, D-Arg, or Cit, R12 is Lys, D- Lys, Cit, D-Cit, Orn, D-Orn, Nle or Ala, R15 is Gly, Ala, Abu or Gln, R19 is Ala or Abu, R20 is Arg, D-Arg or Cit, R21 is Lys, D-Lys, Orn or Cit, R27 is Met, Nle or Abu, R28 is Ser, Asn, Asp, Ala or Abu, R29 is Agm, Arg-NH2, Arg- OH, Cit-NH2, Cit-OH, Har-NH2 or Har-OH, and .beta.) X-A1-B2-A3-R4-R5-R6-Thr-A8- Ser-R10-R11-B12-Val-Leu-R15-A16-A17-Ser-R19-B20-B21-Leu-Leu-Gln-A25-Ile-R27- R28-B29, wherein a lactam bridge is formed between any one of the pairs of positions 1,2; 2,3; 8,12; 16,20; 17-21; 21,25; 25,29 or both 8,12 and 21,25 positions, and X is H, Ac, Aqc, IAc, BrProp, For, Ibu, Nac, 2-Nac, 1- or 2- Npt, 1- or 2-Npr, PhAc, Fpr, or any other aromatic or nonpolar acyl group, A is Glu, D-Glu, Gln, Asp, D-Asp, Asn, Abu, Leu, Tyr, His, Phe(Y), in which Y=H, F, Cl, Br, NO2, NH2, CH3 or OCH3, Ser, Thr, Val, Ile, Ala, D-Ala, D-Asn, D- Gln, D-Thr, D-Leu, Abu, D-Abu, Nle, or Aib, B is Lys, D-Lys, Arg, D-Arg, Orn, D-Orn, or Agm; R4 is Ala, Abu or Gly, R5 is Ile, Ala or Gly, R6 is Phe, Tic, Tpi, Nal or Phe(Y), in which Y=H, F, Cl, Br, NO2, NH2, CH3 or OCH3, R10 is Tyr or Phe(Y), in which Y=H, F, Cl, Br, NO2, NH2, CH3 or OCH3, R15 is Gly, Ala, Abu or Gln, R27 is Met, Nle or Abu, R28 is Ser, Asn, Asp, Ala or Abu, and pharmaceutically acceptable salts thereof.

L'invention concerne un peptide A sélectionné dans le groupe ayant la formule: .alpha.) X-R?1¿-R?2¿-R?3¿-R?4¿-R?5¿-R?6¿-Thr-R?8¿-R?9¿-R?10¿-R?11¿-R?12¿-Val-Leu-R?15¿-Gln-Leu-Ser-R?19¿-R?20¿-R?21¿-Leu-Leu-Gln-Asp-Ile-R?27¿-R?28¿-R?29¿, dans lequel X est H, Ac, Aqc, IAc, BrProp, For, Ibu, Nac, 2-Nac, 1- ou 2-Npt, 1- ou 2-Npr, PhAc, Fpr, ou un autre groupe acyle aromatique ou non polaire, R?1¿ est Tyr, His ou Phe(Y), dans lequel Y=H, F, Cl, Br, NO¿2?, NH¿2?, CH¿3? ou OCH¿3?, R?2¿ est D-Arg, D-Cit, D-Har, D-Lys, D-Tic ou D-Orn, R?3¿ est Asp, D-Asp, Ala, D-Ala ou Gly, R?4¿ est Ala, Abu ou Gly, R?5¿ est Ile, Ala ou Gly, R?6¿ est Phe, Tic, Ala, Pro, Tpi, Nal ou Phe(Y), dans lequel Y=H, F, Cl, Br, NO¿2?, NH¿2?, CH¿3? or OCH¿3?, R?8¿ est Asn, Gln, Ser, Thr, Val, Leu, Ile, Ala, D-Ala, D-Asn, D-Gln, D-Thr, D-Leu, Abu, D-Abu, Nle, ou Aib, R?9¿ est Ser, R?10¿ est Tyr ou Phe(Y), dans lequel Y=H, F, Cl, Br, NO¿2?, CH¿3? ou OCH¿3?, R?11¿ est Arg, D-Arg, ou Cit, R?12¿ est Lys, D-Lys, Cit, D-Cit, Orn, D-Orn, Nle ou Ala, R?15¿, est Gly, Ala, Abu ou Gln, R?19¿ est Ala ou Abu, R?20¿ est Arg, D-Arg ou Cit, R?21¿ est Lys, D-Lys, Orn ou Cit, R?27¿ est Met, Nle ou Abu, R?28¿ est Ser, Asn, Asp, Ala ou Abu, R?29¿ est Agm, Arg-NH¿2?, Arg-OH, Cit-NH¿2?, Cit-OH, Har-NH¿2? ou Har-OH, et .beta.) X-A?1¿-B?2¿-A?3¿-R?4¿-R?5¿-R?6¿-Thr-A?8¿-Ser-R?10¿-R?11¿-B?12¿-Val-Leu-R?15¿-A?16¿-A?17¿-Ser-R?19¿-B?20¿-B?21¿-Leu-Leu-Gln-A?25¿-Ile-R?27¿-R?28¿-B?29¿, dans lequel un pont lactame est placé entre l'une quelconque des paires de positions (1,2; 2,3; 8,12; 16,20; 17-21; 21,25; 25,29 ou dans les deux paires de 8,12 et 21,25 positions et X est H, Ac, Aqc, IAc, BrProp, For, Ibu, Nac, 2-Nac, 1- ou 2-Npt, 1- ou 2-Npr, PhAc, Fpr, ou un autre groupe acyle aromatique ou non polaire, A est Glu, D-Glu, Gln, Asp, D-Asp, Asn, Abu, Leu, Tyr, His, Phe(Y), dans lequel Y=H, F, Cl, Br, NO¿2?, NH¿2?, CH¿3? ou OCH¿3?, Ser, Thr, Val, Ile, Ala, D-Ala, D-Asn, D-Gln, D-Thr, D-Leu, Abu, D-Abu, Nle, ou Aib, B est Lys, D-Lys, Arg, D-Arg, Orn, D-Orn, ou Agm; R?4¿ est Ala, Abu ou Gly, R?5¿ est Ile, Ala ou Gly, R?6¿ est Phe, Tic, Tpi, Nal ou Phe(Y), dans lequel Y=H, F, Cl, Br, NO¿2?, NH¿2?, CH¿3? ou OCH¿3?, R?10¿ est Tyr ou Phe(Y), dans lequel Y=H, F, Cl, Br, NO¿2?, NH¿2?, CH¿3? ou OCH¿3?, R?15¿ est Gly, Ala, Abu ou Gln, R?27¿ est Met, Nle ou Abu, R?28¿ est Ser, Asn, Asp, Ala ou Abu, et des sels pharmaceutiquement acceptables desdits groupes.

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