Fatty acid modified urocortin-2 analogs for the treatment of diabetes and chronic kidney disease

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United States of America Patent

PATENT NO 10894817
APP PUB NO 20180016318A1
SERIAL NO

15648542

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Abstract

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The present invention provides a compound or a pharmaceutically acceptable salt of the Formula:

description='In-line Formulae' end='lead'X1IVX2SLDVPIGLLQILX3EQEKQEKEKQQAK*TNAX4ILAQV-NH2 description='In-line Formulae' end='tail'

    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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Patent Owner(s)

  • ELI LILLY AND COMPANY

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Alsina-Fernandez, Jorge Indianapolis, US 34 231
Guo, Lili Carmel, US 25 69
Lee, John Carmel, US 257 5850

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