US 10,092,648 B2Granted

Selective glucagon-like-peptide-2 (GLP-2) analogues

AssigneeZealand Pharma A/S

InventorsBjarne Due Larsen, Yvette Miata Petersen

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Abstract

GLP-2 analogs are disclosed which comprise one of more substitutions as compared to h[Gly2]GLP-2 and which may have the property of an increased small intestine/colon and stomach/colon selectivity. More particularly, preferred GLP-2 analogs disclosed herein comprise substitutions at one or more of positions 11, 16, 20, 24 and/or 28 of the wild-type GLP-2 sequence, optionally in combination with further substitutions at position 2 and one or more of positions 3, 5, 7, and 10, and/or a deletion of one or more of amino acids 31 to 33 and/or the addition of a N-terminal or C-terminal stabilizing peptide sequence. The analogs are particularly useful for the prophylaxis or treatment of stomach and bowel-related disorders and for ameliorating side effects of chemotherapy.

Claims17

Dependent claims

A glucagon-like peptide 2 (GLP-2) analogue represented by general Formula II:

R1—Z1-His-X2-X3-Gly-X5-X6-X7-X8-X9-X10-X11-X12-X13-X14-X15-X16-X17-Ala-X19-X20-X21-Phe-Ile-X24-Trp-Leu-Ile-X28-Thr-Lys-X31-X32-X33-Z2—R2 (SEQ ID NO:
4)
wherein:
R1 is hydrogen, C1-4 alkyl, methyl, acetyl, formyl, benzoyl or trifluoroacetyl;
X2 is Gly;
X3 is Glu or Asp;
X5 is Ser or Thr;
X6 is Phe;
X7 is Ser or Thr;
X8 is Asp;
X9 is Glu;
X10 is Leu;
X11 is Asn, Ala, Glu, or Ser;
X12 is Thr;
X13 is lie;
X14 is Leu;
X15 is Asp or Glu;
X16 is Ala, Glu, or Ser;
X17 is Leu;
X19 is Ala;
X20 is Ala, Glu, or Ser;
X21 is Asp;
X24 is Ala or Ser;
X28 is Ala, Glu, or Ser;
X31 is lie;
X32 is Thr;
X33 is Asp;
R2 is NH2 or OH;
Z1 and Z2 are independently absent or a peptide sequence of 1-10 amino acid units selected from the group consisting of Ala, Leu, Ser, Thr, Tyr, Asn, Gln, Asp, Glu, Lys, Arg, His, Met and Orn;
or a pharmaceutically acceptable salt thereof.

27 more elements

Dependencies are inferred from the claim text.

Facts

Application: 14/172,680Filed 4 Feb 2014 · continuation
Priority: DK 2006 014568 Nov 2006
Published: US 2014/0154214 A15 Jun 2014
Granted: 9 Oct 2018
Term ends: Not estimatedThe source records don’t support an estimate.

Classification14 codes

A61K 45/06
Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00: mixtures of active ingredients without…
A61K 38/26
Hormones: glucagons
A61P 1/00
Drugs for disorders of the alimentary tract or the digestive system
A61P 1/04
Drugs for disorders of the alimentary tract or the digestive system: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of…

Family

Application60/859,313Us provisional application · filed 15 Nov 2006
PCT/GB2007/004273Parent of this continuation · filed 8 Nov 2007
US 2014/0154214 A1Pre-grant publication · published 5 Jun 2014
Application12/514,042Parent of this continuation
US 8,642,727 B2Parent of this continuation
US 2012/0004392 A1Published application
US 10,092,648 B2This patent

From the US filing history. Foreign family members aren’t listed.