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NOVEL FATTY ACID MODIFIED UROCORTIN-2 ANALOGS FOR THE TREATMENT OF DIABETES AND CHRONIC KIDNEY DISEASE
专利权人:
ELI LILLY AND COMPANY
发明人:
ALSINA-FERNANDEZ,Jorge,GUO, Lili,LEE, John
申请号:
PH12019500074
公开号:
PH12019500074A1
申请日:
2019.01.11
申请国别(地区):
PH
年份:
2019
代理人:
摘要:
The present invention provides a compound or a pharmaceutically acceptable salt of the Formula : X1 I V X2 S L D V P I G L L Q I L X3 E Q E K Q E K E K Q Q A K* T N A X4 I L A Q V-NH2 wherein the X1 denotes that the I residue is modified by either acetylation or methylation at the N-terminus; wherein X2 is L or T; wherein X3 is L or I; wherein X4 is Q or E; and wherein a modified K residue ("K*") at position 29 is modified through conjugation to the epsilon-amino group of the K-side chain with a group of the formula -X-5X6, wherein X5 is selected from the group consisting of one to four amino acids; one to four ([2-(2-Amino-ethoxy)-ethoxy]-acetyl) moieties; and combinations of one to four amino acids and one to four ([2-(2-Aminoethoxy)- ethoxy]-acetyl) moieties; and X6 is a C14-C24 fatty acid. In some embodiments, the group of the formula -X5 -X6 is ([2- (2-Amino-ethoxy)-ethoxy]-acetyl)2-(#E)2-CO-(CH2)x-CO2H where x is 16 or 18.
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