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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:
Jorge Alsina-Fernandez,Lili Guo,John Lee
申请号:
US15648542
公开号:
US20180016318A1
申请日:
2017.07.13
申请国别(地区):
US
年份:
2018
代理人:
摘要:
The present invention provides a compound or a pharmaceutically acceptable salt of the Formula:X1IVX2SLDVPIGLLQILX3EQEKQEKEKQQAK*TNAX4ILAQV-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 —X5—X6, 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-Amino-ethoxy)-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-(γE)2-CO—(CH2)x—CO2H where x is 16 or 18.
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