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US 12,622,948 B2Granted
GLP-1/GIP dual agonists
AssigneeSun Pharmaceutical Industries Limited
InventorsRajamannar Thennati, Vinod Sampatrao Burade, Muthukumaran Natarajan, Dhiren Rameshchandra Joshi, Manish Harendraprasad Gandhi, Chandulal Thakarshibhai Jivani, Abhishek Tiwari, Krunal Harishbhai Soni
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Abstract
The present invention relates to long acting glucagon-like peptide-1 and human glucose-dependent insulinotropic polypeptide (GIP) dual agonist polypeptide which may be useful for treating type 2 diabetes mellitus (T2D), diabetes with obesity, obesity and hyperlipidemia.
Claims24
A polypeptide comprising the amino acid sequence:
- (SEQ ID NO:
- 3)
- Y-X1-E-G-T-F-T-S-D-Y-S-I-X2-L-D-K-I-A-Q-X3-A-F-V-
- Q-W-L-X4-A-G-G-P-S-S-G-A-P-P-P-S,
- or a pharmaceutically acceptable salt thereof,
- wherein:
- X1 is Aib or (L)-norvaline;
- X2 is Leu or (L)-norvaline;
- X3 is Lys, wherein the side chain amino (ε-amino) group of the Lys is acylated with a moiety having the formula:
- wherein:
- U is —C(O)—CH2—O—(CH2)2—O—(CH2)2—NH—}, wherein} is point of attachment to W;
- W is —C(O)—C(CH3)2—NH—], wherein] is point of attachment to Y;
- Y is —C(O)—(CH2)2—CH(COOH)NH—, wherein — is point of attachment to Z;
- and
- Z is —C(O)—(CH2)n—COOH or —C(O)—(CH2)n—CH3, wherein n is an integer from 14 to 20;
- X4 is Ile;
- and
- the acid group of the C-terminal amino acid is a free carboxylic acid group or is amidated as a C-terminal primary amide.
15 more elements
A polypeptide selected from the group consisting of:
- or a pharmaceutically acceptable salt thereof;
- wherein:
Dependencies are inferred from the claim text.