Exendins and exendin agonists modified with polyamino acids
First Claim
Patent Images
1. A compound comprising an exendin-4 agonist analog which comprises the amino acid sequence of SEQ ID NO:
- 51 linked to a polylysine through the C-terminal amino acid residue.
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Accused Products
Abstract
Modified exendins and exendin agonists having an exendin or exendin agonist linked to one or more molecular weight increasing compounds, for example, polyamino acids, polyethylene glycol polymers, and related formulations and dosages and methods of administration thereof are provided. These modified exendins and exendin agonists, compositions comprising the modified exendin or the agonist thereof are useful in treating diabetes and conditions that would be benefited by lowering plasma glucose or delaying and/or slowing gastric emptying or inhibiting food intake.
76 Citations
20 Claims
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1. A compound comprising an exendin-4 agonist analog which comprises the amino acid sequence of SEQ ID NO:
- 51 linked to a polylysine through the C-terminal amino acid residue.
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2. A pharmaceutical composition comprising (A) a compound which comprises an exendin-4 agonist analog which comprises the amino acid sequence of SEQ ID NO:
- 51 linked to a polylysine through the C-terminal amino acid residue; and
(B) a pharmaceutically acceptable carrier. - View Dependent Claims (3)
- 51 linked to a polylysine through the C-terminal amino acid residue; and
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4. A pharmaceutical composition comprising (A) a compound which comprises an exendin-4 which comprises the amino acid sequence of SEQ ID NO:
- 2 or an exendin-4 agonist analog which comprises the amino acid sequence of SEQ ID NO;
51 linked to a polylysine through (i) the C-terminal amino acid residue, (ii) an internal lysine amino acid at position 12 or 27, (iii) an internal aspartic acid amino acid, (iv) an internal glutamic acid amino acid, or (v) the N-terminal amino acid residue; and
(B) a pharmaceutically acceptable carrier. - View Dependent Claims (5, 6, 7, 8, 9, 10)
- 2 or an exendin-4 agonist analog which comprises the amino acid sequence of SEQ ID NO;
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11. A pharmaceutical composition comprising (A) a compound which comprises exendin-4 which comprises the amino acid sequence of SEQ ID NO:
- 2 or an exendin-4 agonist analog which comprises the amino acid sequence of SEQ ID NO;
51 linked to a polyamino acid through the C-terminal amino acid residue; and
(B) a pharmaceutically acceptable carrier. - View Dependent Claims (12, 13, 14)
- 2 or an exendin-4 agonist analog which comprises the amino acid sequence of SEQ ID NO;
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15. A pharmaceutical composition comprising (A) a compound which comprises exendin-4 which comprises the amino acid sequence of SEQ ID NO:
- 2 or an exendin-4 agonist analog which comprises the amino acid sequence of SEQ ID NO;
51 linked to a polyamino acid through (i) the C-terminal amino acid residue, (ii) the internal lysine amino acid at position 12 or 27, (iii) the internal aspartic acid amino acid, (iv) the internal glutamic acid amino acid, or (v) the N-terminal amino acid residue; and
(B) a pharmaceutically acceptable carrier. - View Dependent Claims (16, 17, 18, 19, 20)
- 2 or an exendin-4 agonist analog which comprises the amino acid sequence of SEQ ID NO;
Specification