# US 7,410,806 B2 · Compound for inhibiting the influx of polymorphonuclear leukocytes (PMNs) in a tissue, its selection, pharmaceutical compositions and use

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- Number: US 7,410,806 B2
- Document ID: US7410806B2
- Status: Granted
- Kind: B2
- Application number: 11/209,185
- Filed: 2005-08-22
- Published: 2006-03-02
- Granted: 2008-08-12
- Earliest claimed: 1999-04-06
- Assignees: Fornix Biosciences N.V.
- Inventors: Franciscus Petrus Nijkamp; Rosswell Robert Pfister; Jeffrey Lynn Haddox; James Edwin Blalock; Matteo Villain
- Web page: https://patentgrep.com/patent/US7410806B2

## CPC

- C07K 7/02: Linear peptides containing at least one abnormal peptide link
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- C07K 5/0823: {and Pro-amino acid; Derivatives thereof}
- G01N 33/5047: {Cells of the immune system}
- G01N 33/68: involving proteins, peptides or amino acids {(involving lipoproteins G01N33/92)}
- A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00)
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- G01N: INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES (measuring or testing apparatus or processes other than immunoassay, involving enzymes or microorganisms C12M, C12Q)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

The invention relates to a compound suitable for inhibiting the influx of polymorphonuclear leukocytes (PMNs) into a tissue involved in a chronic inflammatory disease. The compound according to the invention is capable of forming a complex with N-acetyl-Pro-Gly-Pro. The invention also relates to a method of selecting such a compound, a pharmaceutical composition and an application of the compound.

## Claims

### Claim 1

A method of screening a number of compounds with respect to their capability to inhibit the formation of a complex between 4RTR and N—AcPGP, screening occurring by means of an assay comprising a competition reaction between i) a compound A to be assayed and ii) a compound B comprising 4RTR and capable of binding N—AcPGP having an equilibrium constant K of 5·10−5 M−1 or lower, compound A and compound B being in competition for the binding to a Pro-Gly-Pro (PGP)—comprising compound C, with which the compound B is able to complex, having an equilibrium constant K of 5·10−5 M−1 or lower, and wherein a thus assayed compound A is selected having an equilibrium constant K for the reaction between compound A and the PGP-comprising compound C of 10−4 M−1 or lower.

### Claim 2 (depends on 1)

A method according to claim 1, characterized in that a compound A is selected having an equilibrium constant K of 10−5 M−1 or below.

### Claim 3 (depends on 1)

A method according to claim 1, characterized in that the compound C is N—R-Pro-Gly-Pro (“N—R-PGP”), wherein R is branched or linear alkyl- or acyl group having 1 to 6 carbon atoms.

### Claim 4 (depends on 1)

A method according to claim 1, characterized in that the assay is a homogenous assay.

### Claim 5 (depends on 1)

A method according to claim 1, characterized in that the assay is based on fluorescence (de)polarization or internal energy transfer.