# US 2013/0157964 A1 · Blockade Of Inflammatory Proteases With Cyclic Peptides

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- Number: US 2013/0157964 A1
- Document ID: US20130157964A1
- Status: Published application
- Kind: A1
- Application number: 13/486,548
- Filed: 2012-06-01
- Published: 2013-06-20
- Earliest claimed: 2011-06-02
- Assignees: The Regents of the University of California
- Inventors: Michael E. Selsted; Dat Q. Tran
- Web page: https://patentgrep.com/patent/US20130157964A1

## CPC

- A61K 38/1729: {Cationic antimicrobial peptides, e.g. defensins}
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 38/10: Peptides having 12 to 20 amino acids {(A61K38/043 - A61K38/046 take precedence)}
- A61K 38/12: Cyclic peptides {, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C (A61K38/043 - A61K38/046 take precedence)}
- A61K 38/55: Protease inhibitors
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- 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 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 35/00: Antineoplastic agents
- A61P 37/02: Immunomodulators
- 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 14/4723: {Cationic antimicrobial peptides, e.g. defensins}
- F01P 5/04: Pump-driving arrangements
- F24F 5/0007: {cooling apparatus specially adapted for use in air-conditioning (F24F5/0046 takes precedence)}
- F24F 6/16: using rotating elements
- B63J 2003/002: {by using electric power}
- F01P 2005/046: {with electrical pump drive}
- F24F 2203/1028: combined with a spraying device
- F24F 2203/1076: comprising three rotors
- 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)
- F01P: COOLING OF MACHINES OR ENGINES IN GENERAL; COOLING OF INTERNAL-COMBUSTION ENGINES (arrangements in connection with cooling of propulsion units in vehicles B60K11/00; heat-transfer, heat-exchange or heat-storage materials C09K5/00; {cooling of gas-turbine engines F02C7/12}; heat exchange in general, radiators F28)
- F24F: AIR-CONDITIONING; AIR-HUMIDIFICATION; VENTILATION; USE OF AIR CURRENTS FOR SCREENING (removing dirt or fumes from areas where they are produced B08B15/00; vertical ducts for carrying away waste gases from buildings E04F17/02; tops for chimneys or ventilating shafts, terminals for flues F23L17/02)
- B63J: AUXILIARIES ON VESSELS

## Abstract

Drug compositions for treatment of one or more inflammatory conditions can includes at least one of a θ-defensin, analog or derivative thereof. Inventive methods include researching θ-defensins, analogs or derivatives thereof for their efficacy with respect to anti-inflammatory effects, and providing such compositions to the marketplace for the purpose of treating inflammatory conditions. Of particular interest are drug compositions effective to produce clinically relevant inhibition of tumor necrosis factor alpha (TNF-α)-converting enzyme (TACE) or other proinflammatory proteases, and/or sheddases. it is contemplated that preferred compositions can be used to treat rheumatoid arthritis, inflammatory bowel disease, and other chronic inflammatory diseases, autoimmune diseases, cancer, and Alzheimer's, osteoarthritis, inflammation-related neurodegenerative and other inflammation-related diseases.

## Claims

### Claim 1

A method of marketing a drug composition, wherein the drug composition includes a θ-defensin, analog or derivative thereof, the method comprising:
determining efficacy of the drug composition with respect to an anti-inflammatory effect in a human; and
providing the drug composition to a marketplace to treat an inflammatory condition.

### Claim 2 (depends on 1)

The method of claim 1, wherein the drug composition is RTD-1-27.

### Claim 3 (depends on 1)

The method of claim 1, wherein the drug composition is RTD-1-28.

### Claim 4 (depends on 1)

The method of claim 1, wherein the drug composition is RTD-1-29.

### Claim 5 (depends on 1)

The method of claim 1, wherein the step of determining efficacy comprises sponsoring at least one of toxicity study, an efficacy study and a dose-response study with respect to the drug composition.

### Claim 6 (depends on 1)

The method of claim 1, wherein the step of determining efficacy comprises relying on data generated by another with respect to at least one of toxicity study, an efficacy study and a dose-response study with respect to the drug composition.

### Claim 7 (depends on 1)

The method of claim 1, wherein the anti-inflammatory effect comprises clinically relevant inhibition of a proinflammatory protease.

### Claim 8 (depends on 7)

The method of claim 7, wherein the proinflammatory protease is tumor necrosis factor alpha (TNF-α)-converting enzyme (TACE).

### Claim 9 (depends on 1)

The method of claim 1, wherein the anti-inflammatory effect comprises clinically relevant inhibition of a proinflammatory protease.

### Claim 10 (depends on 1)

The method of claim 1, wherein the anti-inflammatory effect comprises clinically relevant inhibition of a sheddase.

### Claim 11 (depends on 1)

The method of claim 1, wherein the anti-inflammatory effect comprises clinically relevant inhibition of Cathepsin-C.

### Claim 12 (depends on 1)

The method of claim 1, wherein the step of providing the drug composition to the marketplace comprises producing for sale at least one kilogram of the drug composition.

### Claim 13 (depends on 12)

The method of claim 12, wherein the step of producing comprises manufacturing the at least one kilogram of the drug composition.

### Claim 14 (depends on 1)

The method of claim 1, further comprising packaging the drug composition in an oral formulation.

### Claim 15 (depends on 1)

The method of claim 1, wherein the inflammatory condition comprises a chronic inflammatory disease.

### Claim 16 (depends on 1)

The method of claim 1, wherein the inflammatory condition comprises rheumatoid arthritis.

### Claim 17 (depends on 1)

The method of claim 1, wherein the inflammatory condition comprises an autoimmune disease.

### Claim 18 (depends on 1)

The method of claim 1, further comprising marketing the drug composition as a treatment for a cancer.

### Claim 19 (depends on 1)

The method of claim 1, further comprising marketing the drug composition as a treatment for a neurodegenerative disease.

### Claim 20 (depends on 1)

The method of claim 1, further comprising marketing the drug composition as a treatment for an inflammatory bowel disease.

### Claim 21 (depends on 1)

The method of claim 1, further comprising marketing the drug composition as a treatment for Alzheimer's disease.

### Claim 22 (depends on 1)

The method of claim 1, further comprising marketing the drug composition as a treatment for osteoarthritis.

### Claim 23 (depends on 1)

The method of claim 1, further comprising marketing the drug composition to treat persons who are non-responders to an anti-TNF-α treatment.

### Claim 24

A method of manufacturing a medicament for administration to an animal to treat an inflammatory condition, wherein the medicament includes at least one of a θ-defensin, analog or derivative thereof.

### Claim 25 (depends on 24)

The method of claim 24, wherein the medicament includes at least one of RTD-1-27, RTD-1-28 and RTD-1-29.

### Claim 26 (depends on 24)

The method of claim 24, wherein the medicament is effective to produce a clinically relevant inhibition of a proinflammatory protease.

### Claim 27 (depends on 26)

The method of claim 26, wherein the proinflammatory protease is tumor necrosis factor alpha (TNF-α)-converting enzyme (TACE).

### Claim 28 (depends on 24)

The method of claim 24, wherein the medicament is effective to produce a clinically relevant inhibition of a proinflammatory protease.

### Claim 29 (depends on 24)

The method of claim 24, wherein the medicament is effective to produce a clinically relevant inhibition of a sheddase.
