US 11,725,036 B2
Modified lipidated relaxin B chain peptides and their therapeutic use
Olivier Duclos, Paris (FR); Stéphane Illiano, Paris (FR); Sergio Mallart, Paris (FR); Claire Minoletti-Hochepied, Paris (FR); Elisabetta Bianchi, Pomezia (IT); Raffaele Ingenito, Pomezia (IT); Paola Magotti, Vanløse (DK); and Alessia Santoprete, Pomezia (IT)
Assigned to Sanofi, Paris (FR)
Filed by Sanofi, Paris (FR)
Filed on Oct. 30, 2020, as Appl. No. 17/86,183.
Application 17/086,183 is a continuation of application No. 16/264,643, filed on Jan. 31, 2019, granted, now 10,961,295.
Claims priority of application No. 18305094 (EP), filed on Jan. 31, 2018.
Prior Publication US 2021/0292387 A1, Sep. 23, 2021
This patent is subject to a terminal disclaimer.
Int. Cl. C07K 14/64 (2006.01); A61K 38/00 (2006.01); A61P 3/10 (2006.01); A61P 13/12 (2006.01); A61P 9/14 (2006.01); A61P 9/10 (2006.01)
CPC C07K 14/64 (2013.01) [A61P 3/10 (2018.01); A61P 9/10 (2018.01); A61P 9/14 (2018.01); A61P 13/12 (2018.01); A61K 38/00 (2013.01)] 3 Claims
 
1. A peptide having a formula:
Nter-Ac-L-E-G-R-E-K-V-R-A-X19-I-X21-X22-E-G-X25-S-T-F-S-X30-R-A-X33-NH2-Cter
wherein:
Nter represents the N-terminal end of the peptide;
Cter represents the C-terminal end of the peptide;
Ac represents acetyl group;
L represents leucine
E represents glutamic acid;
G represents glycine;
R represents arginine;
K represents lysine;
V represents valine;
A represents alanine;
X19 represents Nε-acetyl-lysine;
I represents isoleucine;
X21 represents 2-amino-isobutyric acid
X22 represents 2-amino-isobutyric acid;
X25 represents the following structure:

OG Complex Work Unit Chemistry
in which:
* represents a covalent bond with the glycine preceding X25 in the formula;
♦ represents a covalent bond with the serine following X25 in the formula; and
Z represents a group of:
-[(PEGxx)b(gE)cCd],
b represents 3;
c represents 3;
PEGxx represents a polyethylene glycol derivative TTDS;
gE represents gamma-glutamic acid; and
Cd represents a linear saturated C16 (Palmitoyl) acyl group;
S represents serine;
T represents threonine;
F represents phenylalanine;
X30 represents α-methyl-lysine;
and
X33 represents Nε-acetyl-lysine;
or a salt or solvate thereof.