Boehringer Ingelheim International GmbH;Zealand Pharma A/S
发明人:
RIBER, Ditte,TOLBORG, Jakob Lind,HAMPRECHT, Dieter Wolfgang,RIST, Wolfgang
申请号：
ES14795564
公开号：
ES2688708T3
申请日:
2014.10.17
申请国别(地区):
ES
年份:
2018
代理人:
摘要：
A compound having the formula: R1-P1-P2-R2 in which R1 is H, C1-4 alkyl, acetyl, formyl, benzoyl or trifluoroacetyl； R2 is OH or NH2； P1 is a peptide that has the sequence: His-X2-X3-GTFTSDYSKYL-X15-X16-X17-X18-A-X20-DFI-X24-WLE-X28-A in which: X2 is selected from Aib, Ac3c, Ac4c and Ac5c； X3 is selected from Gln and His； X15 is selected from Asp and Glu； X16 is selected from Glu and ψ； X17 is selected from Arg and ψ； X18 is selected from Ala and Arg； X20 is selected from Lys and His； X24 is selected from Glu and ψ； X28 is selected from Ser and ψ； and P2 is absent or is a sequence of 1-20 amino acid units independently selected from the group consisting of Ala, Leu, Ser, Thr, Tyr, Cys, Glu, Lys, Arg, Dbu, Dpr and Orn； wherein the compound contains one and only one ψ and wherein said ψ is a residue of Lys, Arg, Orn or Cys in which the side chain is conjugated to a substituent having the formula -Z2Z1； -Z1 is a fatty chain having a polar group at one end of the chain and a connection to Z2, -X- at the end of the distal chain of the polar group, wherein the polar group comprises a carboxylic acid or a bioister of carboxylic acid, a phosphonic acid or a group of sulfonic acid； and -X- is a bond, -CO-, -SO- or -SO2-； -Z2- is a spacer of the formula: ** Formula ** in which: each Y is independently -NH, -NR, -S or -O, where R is alkyl, a protective group or forms a bond to another part of the Z2 spacer； each X is independently a link, CO-, SO- or SO2-； provided that when Y is -S, X is a link； each V is independently a bivalent organic moiety that links Y and X； and n is 1-10； a pharmaceutically acceptable salt or solvate thereof.Un compuesto que tiene la fórmula: R1-P1-P2-R2 en la que R1 es H, alquilo C1-4, acetilo, formilo, benzoílo o trifluoroacetilo； R2 es OH o NH2； P1 es un péptido que tiene la secuencia: His-X2-X3-GTFTSDYSKYL-X15-X16-X17-X18-A-X20-DFI-X24-WLE-X28-A en la que: X2 se selecciona entre Aib, Ac3c, Ac4c y Ac5c； X3 se selecciona entre Gln y His； X15 se selec
