# US 8,540,997 B2 · Complement receptor 1 and 2 fusion proteins

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- Number: US 8,540,997 B2
- Document ID: US8540997B2
- Status: Granted
- Kind: B2
- Application number: 13/162,434
- Filed: 2011-06-16
- Published: 2012-01-19
- Granted: 2013-09-24
- Earliest claimed: 2002-11-15
- Assignees: MUSC Foundation for Research Development; The Regents of the University of Colorado, a body corporate
- Applicants: Stephen Tomlinson; V. Michael Holers
- Inventors: Stephen Tomlinson; V. Michael Holers
- Web page: https://patentgrep.com/patent/US8540997B2

## CPC

- C07K 14/70596: {Molecules with a "CD"-designation not provided for elsewhere}
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- 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 5/14: of the thyroid hormones, e.g. T3, T4
- A61P 7/00: Drugs for disorders of the blood or the extracellular fluid
- A61P 7/06: Antianaemics
- A61P 7/08: Plasma substitutes; Perfusion solutions; Dialytics or haemodialytics; Drugs for electrolytic or acid-base disorders, e.g. hypovolemic shock (artificial tears A61P27/04)
- 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 9/14: Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 11/06: Antiasthmatics
- A61P 13/12: of the kidneys
- A61P 15/08: for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/02: for treating wounds, ulcers, burns, scars, keloids, or the like
- A61P 19/00: Drugs for skeletal disorders
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 21/04: for myasthenia gravis
- 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 31/00: Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P 31/04: Antibacterial agents
- A61P 31/06: for tuberculosis
- A61P 31/10: Antimycotics
- A61P 31/12: Antivirals
- A61P 31/14: for RNA viruses
- A61P 31/16: for influenza or rhinoviruses
- A61P 31/18: for HIV
- A61P 31/20: for DNA viruses
- A61P 31/22: for herpes viruses
- A61P 33/00: Antiparasitic agents
- A61P 33/02: Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
- A61P 33/04: Amoebicides
- A61P 33/06: Antimalarials
- A61P 33/12: Schistosomicides
- A61P 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- A61P 37/00: Drugs for immunological or allergic disorders
- A61P 37/02: Immunomodulators
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07K 14/705: Receptors; Cell surface antigens; Cell surface determinants {(tumour specific antigens C07K14/4748)}
- C07K 16/2896: {against molecules with a "CD"-designation, not provided for elsewhere}
- 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 2319/00: Fusion polypeptide
- 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
- 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

Modulation of the complement system represents a therapeutic modality for numerous pathologic conditions associated with complement activation. In a strategy to prepare complement inhibitors that are targeted to sites of complement activation and disease, compositions comprising a complement inhibitor linked to complement receptor (CR) 2 are disclosed. The disclosed are compositions can be used in methods of treating pathogenic diseases and inflammatory conditions by modulating the complement system.

## Claims

### Claim 1

A composition comprising a construct, wherein the construct is a fusion protein consisting of:
(a) a complement receptor 2 (CR2) or a fragment thereof, wherein the fragment consists of at least the first two N-terminal short consensus repeat (SCR) domains of the CR2 protein;
(b) a modulator of complement activity, wherein the modulator consists of one or more active sites of CR1; and
(c) optionally, a linker linking (a) and (b).

### Claim 2 (depends on 1)

The composition of claim 1, wherein the sequence of the modulator consists of SEQ ID NO. 14.

### Claim 3 (depends on 1)

The composition of claim 1, wherein the modulator consists of murine CR1 or human CR1.

### Claim 4 (depends on 1)

The composition of claim 1, wherein the CR2 or fragment thereof is fused to the N-terminus of the modulator.

### Claim 5 (depends on 1)

The composition of claim 1, wherein the CR2 or fragment thereof is fused to the C-terminus of the modulator.

### Claim 6 (depends on 1)

The composition of claim 1, wherein the CR2 is a full-length CR2 protein.

### Claim 7 (depends on 1)

The composition of claim 1, wherein the CR2 or fragment thereof consists of the four N-terminal SCR domains of the CR2 protein.

### Claim 8 (depends on 1)

The composition of claim 1, wherein the modulator consists of the entire extracellular region of CR1.

### Claim 9 (depends on 1)

The composition of claim 1, wherein at least one of the one or more active sites of CR1 consists of a leader peptide, wherein the sequence of the leader peptide consists of amino acids 6-46 of SEQ ID NO:14.

### Claim 10 (depends on 1)

The composition of claim 1, wherein said modulator consists of SCR1-4 of CR1.

### Claim 11 (depends on 1)

The composition of claim 1, wherein said modulator consists of SCR8-11 of CR1.

### Claim 12 (depends on 1)

The composition of claim 1, wherein said modulator consists of SCR15-18 of CR1.

### Claim 13 (depends on 1)

The composition of claim 1, wherein at least one of the one or more active sites of CR1 consists of the C1q binding site of CR1.