# US 10,766,964 B2 · Compositions and methods for treating and preventing inflammation

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- Number: US 10,766,964 B2
- Document ID: US10766964B2
- Status: Granted
- Kind: B2
- Application number: 16/422,273
- Filed: 2019-05-24
- Published: 2019-11-28
- Granted: 2020-09-08
- Earliest claimed: 2014-09-05
- Assignees: Rsem, Limited Partnership
- Applicants: Rsem, Limited Partnership
- Inventors: Przemyslaw Sapieha; Normand Beaulieu
- Web page: https://patentgrep.com/patent/US10766964B2

## CPC

- C07K 16/2863: {against receptors for growth factors, growth regulators}
- A61K 31/7105: Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
- A61K 31/713: Double-stranded nucleic acids or oligonucleotides
- A61K 39/395: Antibodies (agglutinins A61K38/36 {; as drug carriers A61K47/50}); Immunoglobulins; Immune serum, e.g. antilymphocytic serum
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 17/00: Drugs for dermatological disorders
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A61P 27/02: Ophthalmic agents
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 31/04: Antibacterial agents
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07K 14/71: for growth factors; for growth regulators
- C07K 16/22: against growth factors {; against growth regulators}
- C12N 15/113: Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; {Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing (when used in plants C12N15/8218)}
- 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)
- A61K 2039/505: {comprising antibodies}
- C07K 2319/30: Non-immunoglobulin-derived peptide or protein having an immunoglobulin constant or Fc region, or a fragment thereof, attached thereto
- C12N 2310/14: interfering nucleic acids [NA]
- 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)
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)

## Abstract

The present invention provides novel compounds compositions and methods for (i) treating or preventing inflammation; and (ii) preventing or reducing hyperactivation of innate immune response, by inhibiting NRP1-dependent cell-signaling. Also provided are compounds, composition, and methods of specifically inhibiting SEMA3A-mediated cell signaling.

## Claims

### Claim 1

A fusion polypeptide comprising a neuropilin-1 (NRP1) polypeptide consisting of an amino acid sequence having at least 90% identity with residues 22-424 of SEQ ID NO: 107, wherein said fusion polypeptide does not comprise the b2 and c domains of native human NRP1 and has a purification tag linked to said NRP1 polypeptide.

### Claim 2 (depends on 1)

The fusion polypeptide of claim 1, wherein said NRP1 polypeptide consists of an amino acid sequence having at least 95% identity with residues 22-424 of SEQ ID NO: 107.

### Claim 3 (depends on 1)

The fusion polypeptide of claim 1, wherein said NRP1 polypeptide consists of residues 22-424 of SEQ ID NO: 107.

### Claim 4 (depends on 3)

The fusion polypeptide of claim 3, further comprising a polypeptide linker between the NRP1 polypeptide and the purification tag.

### Claim 5 (depends on 3)

The fusion polypeptide of claim 3, wherein the purification tag comprises a polyhistidine (His) tag.

### Claim 6 (depends on 1)

The fusion polypeptide of claim 1, wherein said purification tag is carboxy-terminal relative to the NRP1 polypeptide in the fusion polypeptide.

### Claim 7 (depends on 1)

The fusion polypeptide of claim 1, further comprising a polypeptide linker between the NRP1 polypeptide and the purification tag .

### Claim 8 (depends on 7)

The fusion polypeptide of claim 7, wherein the purification tag comprises a polyhistidine (His) tag.

### Claim 9 (depends on 7)

The fusion polypeptide of claim 7, wherein the polypeptide linker comprises a protease cleavage site.

### Claim 10 (depends on 9)

The fusion polypeptide of claim 9, wherein the protease cleavage site comprises the sequence set forth in SEQ ID NO: 76.

### Claim 11 (depends on 1)

The fusion polypeptide of claim 1, wherein the purification tag comprises a fragment crystallizable (Fc) domain.

### Claim 12 (depends on 11)

The fusion polypeptide of claim 11, wherein said Fc domain comprises the amino acid sequence of SEQ ID NO: 37.

### Claim 13 (depends on 1)

The fusion polypeptide of claim 1, wherein the purification tag comprises a polyhistidine (His) tag.

### Claim 14 (depends on 1)

A pharmaceutical composition comprising the fusion polypeptide of claim 1 and at least one pharmaceutically acceptable excipient.

### Claim 15 (depends on 14)

The pharmaceutical composition of claim 14, wherein said composition is an ophthalmic or ocular composition.

### Claim 16 (depends on 14)

The pharmaceutical composition of claim 14, wherein said ophthalmic or ocular composition is an eye drop or injectable composition.

### Claim 17 (depends on 3)

A pharmaceutical composition comprising the fusion polypeptide of claim 3 and at least one pharmaceutically acceptable excipient.

### Claim 18 (depends on 17)

The pharmaceutical composition of claim 17, wherein said composition is an ophthalmic or ocular composition.

### Claim 19 (depends on 18)

The pharmaceutical composition of claim 18, wherein said composition ophthalmic or ocular composition is an eye drop or injectable composition.