US 10,501,514 B2Granted

Cyclic galanin-analogs and uses thereof

AssigneeLanthioPep B.V.

InventorAnneke Kuipers

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Abstract

The invention generally relates to the field of medicine and pharmacology. More particularly, it relates to novel analogs of galanin, and the use thereof in therapy. Provided is a cyclic peptide analog of galanin, wherein the galanin analog comprises a (methyl)Lanthionine bridge and wherein the analog has the general formula “X1-X2-X3-X4-X5-X6-X7-X8-X9-X10-X11-X12-X13-X14-X15-X16-X17-X18-X19-X20-X21-X22-”, or a truncated variant thereof lacking X1 and/or up to 11 of the C-terminal residues, wherein two residues selected from the group consisting of X3, X4, X6, X7, X10 and X13-X19 together form a Lanthionine bridge of the structure Ala-S-Ala, or a methyl Lanthionine bridge of the structure Abu-S-Ala or Ala-S-Abu.

Galanin analog selected from the group consisting of:

GWNmelanNAmelanGYLLGPHAVGNHR,
(SEQ ID NO:
6)
GWNmelanNAmelanGYLLGPHAVGNH,
(SEQ ID NO:
7)
GWNLNAAmelanYLmelanGPHAVGNHR,
(SEQ ID NO:
8)
GWNLNAAmelanYLmelanGPHAVGNH,
(SEQ ID NO:
9)
GWNLNAAlanYLLlanGPHAVGNHR,
(SEQ ID NO:
10)
GWNLNAAlanYLLlanGPHAVGNH,
(SEQ ID NO:
11)
GWNLNAAGYLLGAmelanAVmelanNHR,
(SEQ ID NO:
12)
GWNLNAAGYLLGAmelanAVmelanNH,
(SEQ ID NO:
13)
GWNLNAAGYLLGAlanAVlan,
(SEQ ID NO:
14)
GWNLNAAGYLLGAlanAVlanNHR,
(SEQ ID NO:
15)
GWNLNAAGYLLGAlanAVlanNH,
(SEQ ID NO:
16)
GWNLNAAGYLLGAmelanAVGmelanHR,
(SEQ ID NO:
17)
GWNLNAAGYLLGAlanAVGlan,
(SEQ ID NO:
18)
GWNLNAAGYLLGAlanAVGlanHR,
(SEQ ID NO:
19)
GWNLNAAGYLLGAlanAVGNlanR,
(SEQ ID NO:
20)
GWNLNAAGYLLGAlanAVGNlan,
(SEQ ID NO:
21)
GWNLNAAGYLLGAlanAVGNHlan,
(SEQ ID NO:
22)
GWNLNAAGYLLGPHmelanVGmelanHR,
(SEQ ID NO:
23)
GWNLNAAGYLLGPHlanVGlan,
(SEQ ID NO:
24)
GWNLNAAGYLLGPHAmelanGNmelanR,
(SEQ ID NO:
25)
GWNLNAAGYLLGPHAlanGNlan,
(SEQ ID NO:
26)
GWNLNAAGYLLGASlanVGNHlan,
(SEQ ID NO:
27)
pEWNLNAAGYLLGAmelanAVmelanNHR,
(SEQ ID NO:
28)
pEWNLNAAGYLLGAmelanAVGmelanHR,
(SEQ ID NO:
29)
pEWNLNAAGYLLGAmelanAVmelanNH,
(SEQ ID NO:
30)
pEWNLNAAGYLLGAlanAVlan,
(SEQ ID NO:
31)
pEWNLNAAlanYLLlan,
(SEQ ID NO:
32)
pEWNLNAAGYLLGPHmelanVGmelanHR,
(SEQ ID NO:
33)
GWNLNAAGYLLGmelanHAmelanG,
(SEQ ID NO:
34)
GWNLNAAGYLLGPmelanAVmelan,
(SEQ ID NO:
35)
GWNLNAAGYLLAmelanHAmelanG,
(SEQ ID NO:
36)
GWNLNAAGYLLGAmelanAVmelan,
(SEQ ID NO:
37)
pEWNLNAAGYLLAmelanHAmelanG,
(SEQ ID NO:
38)
pEWNLNAAGYLLGAmelanAVmelan,
(SEQ ID NO:
39)
pEWNLNAAGYLLAlanHAlanG,
(SEQ ID NO:
40)
pEWNLNAAGYLLAmelanHAmelanGNHR,
(SEQ ID NO:
41)
GWNLNAAmelanYLmelanGPHAVGNHR,
(SEQ ID NO:
8)
pEWNLNAAGYLLGPHAmelanGNmelanR,
(SEQ ID NO:
42)
GWNLNAAGYLLAmelanHAmelanG,
(SEQ ID NO:
36)
pEWNLNAAGYLLAmelanHAmelanG,
(SEQ ID NO:
38)
GWNLNAAGYLLGAmelanAVmelan,
(SEQ ID NO:
37)
pEWNLNAAGYLLGAmelanAVmelan,
(SEQ ID NO:
39)
GWNVNAAGYLLGAmelanAVmelanNHR,
(SEQ ID NO:
43)
GWNDNAAGYLLGAmelanAVmelanNHR,
(SEQ ID NO:
44)
GWNNNAAGYLLGAmelanAVmelanNHR,
(SEQ ID NO:
45)
GWNLVAAGYLLGAmelanAVmelanNHR,
(SEQ ID NO:
46)
GWNLKAAGYLLGAmelanAVmelanNHR,
(SEQ ID NO:
47)
GWNLDAAGYLLGAmelanAVmelanNHR,
(SEQ ID NO:
48)
GWNLQAAGYLLGAmelanAVmelanNHR,
(SEQ ID NO:
49)
pEWNLNAAGYLLGPlanAVlan,
(SEQ ID NO:
50)
pEWTLNAAlanYLLlan,
(SEQ ID NO:
51)
pEWNLNAAGYLLGPmelanAVmelan,
(SEQ ID NO:
52)
or
pEWTLNAAmelanYLLmelan.
(SEQ ID NO:
53)

157 more elements

Facts

Application

15/557,273Filed 11 Mar 2016

Priority

EP 1515910213 Mar 2015

Published

US 2018/0057556 A11 Mar 2018

Granted

10 Dec 2019

Term ends

Not estimatedThe source records don’t support an estimate.

Classification17 codes

C07K 14/575
From animals; from humans: hormones
A61K 38/22
From animals; from humans: hormones
A61K 47/549
The modifying agent being an organic compound: sugars, nucleosides, nucleotides or nucleic acids
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…

Abstract

Claims5