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Acylated glucagon analogs
专利权人:
ZEALAND PHARMA A/S
发明人:
RIBER, DITTE,MEIER, EDDI,DAUGAARD, JENS,SKOVGAARD, MARIE,TOLBORG, JAKOB,KAMPEN, GITA,BÆK, CAMILLA
申请号:
ES10737252
公开号:
ES2537287T3
申请日:
2010.06.24
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
A compound having the formula R1-Z-R2 in which R1 is H, C1-4 alkyl, acetyl, formyl, benzoyl or trifluoroacetyl; R2 is OH or NH2; and Z is a peptide having the formula I: His-X2-Gln-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-X12-Tyr-Leu-Asp-X16-X17-Ala-Ala-X20 - X21-Phe-Val-X24-Trp-Leu-X27-X28-Ala-X30; (I) in which X2 is selected from Aib or Ser; X12 is selected from Lys, Arg and Leu; X16 is selected from Arg and X; X17 is selected from Arg and X; X20 is selected from Arg, His and X; X21 is selected from Asp and Glu; X24 is selected from Ala and X; X27 is selected from Leu and X; X28 is selected from Arg and X; X30 is X or is absent; wherein at least one of X16, X17, X20, X24, X27, X28 and X30 is X; and wherein each residue X is independently selected from the group consisting of Glu, Lys, Ser, Cys, Dbu, Dpr and Orn; wherein the side chain of at least one residue X is conjugated to a lipophilic substituent having the formula: (i) Z1, wherein Z1 is a lipophilic residue conjugated directly to the side chain of X; or (ii) Z1Z2, where Z1 is a lipophilic residue, Z2 is a spacer and Z1 is conjugated to the side chain of X by Z2; with the proviso that Z is not HSQGTFTSDYSKYLDS-K (Hexadecanoil-g-Glu) -AAHDFVEWLLRA.Un compuesto que tiene la fórmula R1-Z-R2 en la que R1 es H, alquilo C1-4, acetilo, formilo, benzoílo o trifluoroacetilo; R2 es OH o NH2; y Z es un péptido que tiene la fórmula I: His-X2-Gln-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-X12-Tyr-Leu-Asp-X16-X17-Ala-Ala-X20- X21-Phe-Val-X24-Trp-Leu-X27-X28-Ala-X30; (I) en la que X2 se selecciona de Aib o Ser; X12 se selecciona de Lys, Arg y Leu; X16 se selecciona de Arg y X; X17 se selecciona de Arg y X; X20 se selecciona de Arg, His y X; X21 se selecciona de Asp y Glu; X24 se selecciona de Ala y X; X27 se selecciona de Leu y X; X28 se selecciona de Arg y X; X30 es X o está ausente; en la que al menos uno de X16, X17, X20, X24, X27, X28 y X30 es X; y en donde cada resto X se selecciona independientemente del grupo que consiste en Glu, Lys, S
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来源网址:
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