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US 2002/0165148 A1Published application
Analogues and derivatives of gastrin releasing peptide (GRP)
OwnerPer Franklin Nielsen, Ulla Ribel-Madsen +1inventors
InventorsPer Franklin Nielsen, Ulla Ribel-Madsen, Peter Andreas Nicolai Reumert Wagtmann
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Abstract
The present invention relates to analogues and derivatives of GRP which have a protracted profile of action, as well as their use in treatment of e.g. Type 2 diabetes and obesity.
Claims49
An analogue or derivative of gastrin releasing protein (GRP) having Seq ID No. 2:
- 3 1 2 3 4 5 6 7 8 9 10 11 Xaa-Xaa-Leu-Xaa-Ala-Gly-Gly-Gly-Xaa-Val-Leu- 12 13 14 15 16 17 18 19 20 21 22 Thr-Lys-Xaa-Tyr-Pro-Arg-Gly-Xaa-His-Trp-Ala- 23 24 25 26 27 Val-Gly-His-Leu-Xaa
- wherein
- Xaa at position 1 is Val or pyroglutamic acid (Pyr),
- Xaa at position 2 is Pro, Gly, Val, Ile, or Thr,
- Xaa at position 4 is Pro, Gly, Val, lie, or Thr,
- Xaa at position 9 is Thr or Lys,
- Xaa at position 14 is Met or Leu,
- Xaa at position 19 is Asn or Lys,
- Xaa at position 27 is Met or Leu,
- wherein the ε-amino group of one or more Lys is optionally substituted with a lipophilic substituent optionally via a spacer,
- or
- (a) a C-1-6-ester thereof,
- (b) an amide, C-1-6-alkylamide, or C-1-6-dialkylamide thereof,
- (c) an Fmoc derivative thereof, and/or
- (d) a pharmaceutically acceptable salt thereof,
- except a peptide with the amino acid sequence having Seq. ID. No. 1 Val-Pro-Leu-Pro-Ala-Gly-Gly-Gly-Thr-Val-Leu-Thr-Lys-Met-Tyr-Pro-Arg-Gly-Asn-His-Trp-Ala-Val-Gly-His-Leu-Met
13 more elements
Dependencies are inferred from the claim text.