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Anti-inflammatory pharmaceutical products

A drug and inflammation technology, applied in the field of anti-inflammatory compounds, can solve problems such as increasing half-life

Active Publication Date: 2014-04-30
RESOTHER PHARMA APS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Like the Ac1-188 fragment (and the native protein), it has N-terminal acetylation to increase its stability and potentially increase its half-life

Method used

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  • Anti-inflammatory pharmaceutical products
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Experimental program
Comparison scheme
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Embodiment Construction

[0047] In the attached sequence listing:

[0048] SEQ ID NO: 1 is the first 50 amino acids of human annexin 1 .

[0049] SEQ ID NO: 2 is amino acid 11-48 of human annexin 1 modified by a variable, the change may be 11, 22 corresponding to 1, 12, 15 and 26 of SEQ ID NO: 2 , any natural amino acid at positions 25 and 36 (relative to human annexin 1).

[0050] SEQ ID NO: 3 is almost identical to SEQ ID NO: 2, the only difference is that SEQ ID NO: 3 lacks the first residue of SEQ ID NO: 2.

[0051] SEQ ID NO: 4 is one embodiment of the polypeptide of the present disclosure, UGP021. UGP021 is 50 amino acids in length. UGP021 is amino acid 2-50 of human annexin 1, wherein the 50th position of the polypeptide is glycine. In one embodiment, UGP021 is referred to as ANXA1(2-50)Gly51-OH.

[0052] SEQ ID NO: 5 is one embodiment of the polypeptide of the present disclosure, UGP022. UGP022 is 49 amino acids in length. UGP022 is amino acids 2-50 of human annexin 1, wherein the polyp...

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Abstract

Polypeptides having homology to regions of the N-terminal 50 residues of human Annexin 1 are provided for medical use as anti-inflammatory agents. Some of the polypeptides have homology to the N-terminal 48 residues of human Annexin 1, especially to residues 2-48 and 11-48 thereof. In some embodiments, properties of these compounds are improved by at least one modification at residues corresponding to residues 11, 22, 25 and / or 36 of human Annexin 1, and / or by C-terminal amidation of the polypeptide. Analogs of amino acids 2-26 of human Annexin 1, especially acetylated at the N-terminus and / or amidated at the C-terminus and having modifications at 11 and / or 22 are also disclosed for medical use as anti-inflammatory agents.

Description

[0001] related application [0002] This application claims priority to U.S. Provisional Application Serial No. 61 / 497,270, filed June 15, 2011, and U.S. Application Serial No. 13 / 524,381, filed June 15, 2012, the entire contents of which applications are hereby incorporated by reference for the teachings therein. into this article. technical field [0003] Embodiments disclosed herein relate to anti-inflammatory compounds having defined structural homology to human annexin 1, pharmaceutical compositions thereof, and the medical treatment and use of these compounds and compositions as anti-inflammatory agents. Background technique [0004] The annexin superfamily consists of 13 calcine-binding proteins with significant biological and structural homology. Annexin is structurally divided into a highly conserved core domain and a variable N-terminal domain. Annexin 1 (ANXA1, 37 kDa) is an anti-inflammatory protein that inhibits extravasation of blood-derived polymorphonuclear...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/00A61K38/00
CPCC07K14/4721A61K38/00A61K38/1709A61P29/00C07K14/4703
Inventor 安杰洛·P·孔萨尔沃诺泽·M·梅赫塔毛罗·佩雷蒂杰蒙德·达利
Owner RESOTHER PHARMA APS