# US 9,518,265 B2 · C5a binding nucleic acids

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- Number: US 9,518,265 B2
- Document ID: US9518265B2
- Status: Granted
- Kind: B2
- Application number: 14/371,006
- Filed: 2013-01-10
- Published: 2014-12-11
- Granted: 2016-12-13
- Earliest claimed: 2012-01-10
- Assignees: NOXXON Pharma AG
- Applicants: NOXXON Pharma AG
- Inventors: Kai Hohlig; Axel Vater; Klaus Buchner; Christian Maasch; Sven Klussmann
- Web page: https://patentgrep.com/patent/US9518265B2

## CPC

- C12N 15/115: Aptamers, i.e. nucleic acids binding a target molecule specifically and with high affinity without hybridising therewith {; Nucleic acids binding to non-nucleic acids, e.g. aptamers}
- A61K 31/7088: Compounds having three or more nucleosides or nucleotides
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 7/00: Drugs for disorders of the blood or the extracellular fluid
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 17/02: for treating wounds, ulcers, burns, scars, keloids, or the like
- A61P 25/00: Drugs for disorders of the nervous system
- 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 31/00: Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P 31/04: Antibacterial agents
- A61P 35/00: Antineoplastic 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 14/472: {Complement proteins, e.g. anaphylatoxin, C3a, C5a}
- C12N 2310/16: Aptamers
- C12N 2310/344: Position-specific modifications, e.g. on every purine, at the 3'-end
- G01N 2333/4716: Complement proteins, e.g. anaphylatoxin, C3a, C5a
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)
- 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
- 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)
- 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)

## Abstract

The present invention is related to a nucleic acid molecule capable of binding to human C5a, wherein the nucleic acid molecule comprises a central stretch of nucleotides, wherein the central stretch of nucleotides comprises a nucleotide sequence of 5′ AUGn1GGUGKUn2n3RGGGHUGUKGGGn4Gn5CGACGCA 3′ [SEQ ID NO: 61], wherein n1 is U or dU, n2 is G or dG, n3 is A or dA, n4 is U or dU, n5 is U or dU and G, A, U, C, H, K, and R are ribonucleotides, and dU, dG and dA are 2′-deoxyribonucleotides.

## Claims

### Claim 1

An L-nucleic acid that binds to human C5a or to mouse C5a, or a homolog of said L-nucleic acid, wherein said L-nucleic acid comprises the nucleic acid selected from the group consisting of SEQ ID NO:37 and SEQ ID NO:59, and the homolog has at least 85% homology to SEQ ID NO:37 or to SEQ ID NO:59.

### Claim 2 (depends on 1)

The L-nucleic acid according to claim 1, wherein the L-nucleic acid is an antagonist of an activity mediated by human or mouse C5a.

### Claim 3 (depends on 1)

The L-nucleic acid according to claim 1, wherein the L-nucleic acid comprises a modification group.

### Claim 4 (depends on 3)

The L-nucleic acid according to claim 3, wherein the modification group is selected from the group consisting of polyethylene glycol, linear polyethylene glycol, branched polyethylene glycol, hydroxyethyl starch, a peptide, a protein, a polysaccharide, a sterol, polyoxypropylene, polyoxyamidate and poly (2-hydroxyethyl)-L-glutamine.

### Claim 5 (depends on 4)

The L-nucleic acid according to claim 4, wherein the linear polyethylene glycol or branched polyethylene glycol comprises a molecular weight of from about 20,000 to about 120,000 Da.

### Claim 6 (depends on 4)

The L-nucleic acid according to claim 4, wherein the hydroxyethyl starch comprises a molecular weight of from about 100 to about 700 kDa.

### Claim 7 (depends on 3)

The L-nucleic acid according to claim 3, wherein the modification group is coupled to the L-nucleic acid by a linker.

### Claim 8 (depends on 3)

The L-nucleic acid according to claim 3, wherein the modification group is at a terminus of the L-nucleic acid.

### Claim 9 (depends on 8)

The L-nucleic acid according to claim 8, wherein the modification group is at the 5′ terminus of the L-nucleic acid.

### Claim 10 (depends on 1)

A pharmaceutical composition comprising an L-nucleic acid according to claim 1 and a pharmaceutically acceptable excipient, a pharmaceutically acceptable carrier, a pharmaceutically active agent or a combination thereof.

### Claim 11 (depends on 1)

A complex comprising the L-nucleic acid according to claim 1 and C5a.

### Claim 12 (depends on 1)

A method for the detection of the L-nucleic acid of claim 1 in a sample, wherein the method comprises the steps of:
a) providing a capture probe specific for the L-nucleic acid of claim 1, wherein the capture probe is at least partially complementary to a first part of the L-nucleic acid according to claim 1, and a detection probe specific for the L-nucleic acid of claim 1, wherein the detection probe is at least partially complementary to a second part of the L-nucleic acid according to claim 1, or, alternatively, the capture probe is at least partially complementary to a second part of the L-nucleic acid according to claim 1 and the detection probe is at least partially complementary to a first part of the L-nucleic acid according to claim 1;
b) adding the capture probe and the detection probe separately or combined to a sample containing the L-nucleic acid according to claim 1 or presumed to contain the L-nucleic acid according to claim 1;
c) allowing the capture probe and the detection probe to react either simultaneously or in any order sequentially with the L-nucleic acid according to claim 1 or part thereof;
d) optionally detecting whether or not the capture probe is hybridized to the L-nucleic acid according to claim 1; and
e) detecting a complex formed in step c) consisting of the L-nucleic acid according to claim 1, the capture probe and the detection probe.