# US 9,750,784 B2 · Intraarticular application of pepstatin in the case of arthrosis

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- Number: US 9,750,784 B2
- Document ID: US9750784B2
- Status: Granted
- Kind: B2
- Application number: 14/910,317
- Filed: 2014-07-07
- Published: 2016-06-23
- Granted: 2017-09-05
- Earliest claimed: 2013-08-06
- Assignees: Merck Patent GmbH
- Applicants: Merck Patent GmbH
- Inventors: Markus Klein; Ralf Wodopia; Hans Guehring; Sven Lindemann
- Web page: https://patentgrep.com/patent/US9750784B2

## CPC

- A61K 38/08: Peptides having 5 to 11 amino acids {(A61K38/043 - A61K38/046 take precedence)}
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 25/02: for peripheral neuropathies
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- 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

## Abstract

The present invention relates to pharmaceutical preparations and medicaments for intraarticular administration, comprising pepstatin, and to the preparation and use thereof, in particular in the treatment and/or prophylaxis of arthrosis, traumatic cartilage injuries, arthritis, pain, allodynia or hyperalgesia, particularly preferably in arthrosis.

## Claims

### Claim 1

A method for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, selected from the group consisting of arthrosis, traumatic cartilage injuries, arthritis, pain, allodynia and hyperalgesia, comprising intraarticular administration to a patient in need of said treatment of a pharmaceutical preparation
comprising pepstatin and/or one of its physiologically acceptable salts, solvates, prodrugs and stereoisomers, including mixtures thereof in all ratios, and one or more excipients and/or adjuvants, said preparation formulated for intraarticular administration for the treatment and/or prophylaxis of said physiological and/or pathophysiological conditions,
wherein the pharmaceutical preparation is formulated for administration weekly to yearly, and
wherein the pharmaceutical preparation is administered weekly to yearly.

### Claim 2 (depends on 1)

The method of claim 1, for the treatment and/or prophylaxis of arthrosis.

### Claim 3

A method for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, selected from the group consisting of arthrosis, traumatic cartilage injuries, arthritis, pain, allodynia and hyperalgesia, comprising intraarticularly administering to a patient in need thereof pepstatin and/or one of its physiologically acceptable salts, solvates, prodrugs and stereoisomers, including mixtures thereof in all ratios,
wherein the pepstatin and/or one of its physiologically acceptable salts, solvates, prodrugs and stereoisomers is administered weekly to yearly.

### Claim 4

A method for the treatment and/or prophylaxis of arthrosis, comprising intraarticularly administering to a patient in need thereof pepstatin and/or one of its physiologically acceptable salts, solvates, prodrugs and stereoisomers, including mixtures thereof in all ratios,
wherein the pepstatin and/or one of its physiologically acceptable salts, solvates, prodrugs and stereoisomers, including mixtures thereof in all ratios, is administered weekly to yearly.

### Claim 5 (depends on 1)

The method of claim 1, wherein the preparation is administered fortnightly to half-yearly.

### Claim 6 (depends on 1)

The method of claim 1, wherein the preparation is administered monthly to quarterly.

### Claim 7 (depends on 2)

The method of claim 2, wherein the preparation is administered fortnightly to half-yearly.

### Claim 8 (depends on 2)

The method of claim 2, wherein the preparation is administered monthly to quarterly.

### Claim 9 (depends on 3)

The method of claim 3, wherein the pepstatin and/or one of its physiologically acceptable salts, solvates, prodrugs and stereoisomers, including mixtures thereof in all ratios, is administered fortnightly to half-yearly.

### Claim 10 (depends on 3)

The method of claim 3, wherein the pepstatin and/or one of its physiologically acceptable salts, solvates, prodrugs and stereoisomers, including mixtures thereof in all ratios, is administered monthly to quarterly.

### Claim 11 (depends on 4)

The method of claim 4, wherein the pepstatin and/or one of its physiologically acceptable salts, solvates, prodrugs and stereoisomers, including mixtures thereof in all ratios, is administered fortnightly to half-yearly.

### Claim 12 (depends on 4)

The method of claim 4, wherein the pepstatin and/or one of its physiologically acceptable salts, solvates, prodrugs and stereoisomers, including mixtures thereof in all ratios, is administered monthly to quarterly.