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US 8,895,504 B2Granted
Amylin derivatives
AssigneeNovo Nordisk A/S
InventorsLauge Schäffer, Thomas Kruse, Jesper Lau, Henning Thøgersen
Life of this patent
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Abstract
Amylin derivatives, pharmaceutical compositions containing such derivatives, as well as methods of treating diabetes and hyperglycaemia are disclosed.
Claims11
A derivative of amylin, which is a human amylin analogue, wherein the human amylin analogue comprises an amino acid sequence of formula 1:
- Xaa1-Cys- Xaa3-Thr-Ala-Thr-Cys-Ala-Thr-Gln-Arg-Leu-Ala- Xaa14-Phe-Leu- Xaa17-Xaa18-Ser-Ser-Xaa21-Asn- Phe- Xaa24- Xaa25- Xaa26-Leu-Xaa28-Xaa29-Thr- Xaa31-Val-Gly-Ser-Asn-Thr-Tyr Formula (1) (SEQ ID No:2)
- wherein
- Xaa1 is deleted or independently selected from Lys, Arg, His and Glu;
- Xaa3 is independently selected from Asn and Lys;
- Xaa14 is independently selected from Glu, Asn, Gln and Asp;
- Xaa17 is independently selected from His, Ser, Gly, Arg and Pro;
- Xaa18 is independently selected from His or Arg;
- Xaa21 is independently selected from Asp, Asn and Gln;
- Xaa24 is independently selected from Glu and Gly;
- Xaa25 is independently selected from Ala and Pro;
- Xaa26 is independently selected from Pro and Ile;
- Xaa28 is independently selected from Ser and Pro;
- Xaa29 is independently selected from Ser and Pro;
- Xaa31 is independently selected from Glu and Asn;
- the C-terminal may optionally be derivatized as an amide;
- wherein a substituent is connected to the amino acid residue Xaa1 or to Cys in position 2, which substituent comprises an albumin binding moiety.
13 more elements
The derivative according to 6, wherein the linker comprises —C(O)—(CH2)l—O—[CH2CH2—O]m—(CH2)p-[NHC(O)—(CH2)l—O—[(CH2)n—O]m—(CH2)p]q—NH— wherein l, m, n, and p independently are 1-7, and q is 0-5.
Dependencies are inferred from the claim text.