# US 10,946,021 B2 · Methods of treating or alleviating joint diseases by administering an inhibitor of discoidin domain receptor 1 (DDR1)

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 10,946,021 B2
- Document ID: US10946021B2
- Status: Granted
- Kind: B2
- Application number: 16/496,666
- Filed: 2018-03-23
- Published: 2020-01-30
- Granted: 2021-03-16
- Earliest claimed: 2017-03-23
- Assignees: Kaohsiung Medical University
- Applicants: Kaohsiung Medical University
- Inventors: Chau-Zen Wang; Chung-Hwan Chen; Liang-Yin Chou; Yu Chou; Mei-Ling Ho; Yi-Hsiung Lin
- Web page: https://patentgrep.com/patent/US10946021B2

## CPC

- A61K 31/519: ortho- or peri-condensed with heterocyclic rings
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 19/04: for non-specific disorders of the connective tissue
- C07K 16/2851: {against the lectin superfamily, e.g. CD23, CD72}
- C12N 15/1138: {against receptors or cell surface proteins}
- C07K 2317/76: Antagonist effect on antigen, e.g. neutralization or inhibition of binding
- C12N 2310/11: Antisense
- C12N 2310/14: interfering nucleic acids [NA]
- 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)
- 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 relates to a use of Discoidin Domain Receptor 1 (DDR1) inhibitor in preparing a medicament for preventing or treating a joint disease. The present invention further relates to a use of DDR1 activator in preparing a medicament for preventing or treating abnormalities of endochondral ossification-related conditions.

## Claims

### Claim 1

A method for treating or alleviating a joint symptom associated with degenerative arthritis in a subject, comprising:
identifying the subject having the degenerative arthritis; and
administering to the subject an effective amount of a composition including a Discoidin Domain Receptor 1 (DDR1) inhibitor,
wherein the DDR1 inhibitor is

### Claim 2 (depends on 1)

The method as claimed in claim 1, wherein the joint symptom is a joint disease.

### Claim 3 (depends on 2)

The method as claimed in claim 2, wherein the joint disease is a degenerative joint disease.

### Claim 4 (depends on 3)

The method as claimed in claim 3, wherein the degenerative joint disease is osteoarthritis.

### Claim 5 (depends on 3)

The method as claimed in claim 3, wherein the degenerative joint disease is caused by a joint injury, an anterior cruciate ligament injury, or aging.

### Claim 6 (depends on 5)

The method as claimed in claim 5, wherein the joint injury is at least one of a traumatic injury and a post-operative injury.

### Claim 7 (depends on 1)

The method as claimed in claim 1, wherein the subject is a human subject.

### Claim 8 (depends on 1)

The method as claimed in claim 1, wherein the DDR1 inhibitor is

### Claim 9 (depends on 1)

The method as claimed in claim 1, wherein the subject has a condition associated with increased levels of mammalian target of rapamycin (mTOR) and collagen type X.

### Claim 10 (depends on 9)

The method as claimed in claim 9, wherein the condition associated with the increased levels of mTOR and collagen type X increases a potential development of at least one of a cartilage degradation and a chondrocyte death in the subject, and the administration of the composition inhibits, mitigates or alleviates the condition.

### Claim 11

A method for treating or alleviating a degenerative joint disease in a subject, comprising:
administering to the subject an effective amount of a composition including a Discoidin Domain Receptor 1 (DDR1) inhibitor for treating or alleviating the degenerative joint disease in the subject,
wherein the DDR1 inhibitor is

### Claim 12 (depends on 11)

The method as claimed in claim 11, wherein the subject has an articular cartilage damage.

### Claim 13 (depends on 11)

The method as claimed in claim 11, wherein the degenerative joint disease is osteoarthritis.

### Claim 14

A method for reducing, inhibiting, mitigating or alleviating at least one of a cartilage degradation and a chondrocyte death in a subject suffering therefrom, comprising:
administering to the subject an effective amount of a Discoidin Domain Receptor 1 (DDR1) inhibitor, thereby reducing, inhibiting, mitigating or alleviating the at least one of the cartilage degradation and the chondrocyte death in the subject,
wherein the DDR1 inhibitor is

### Claim 15 (depends on 14)

The method as claimed in claim 14, wherein the subject has a traumatic injury to cartilage tissues.

### Claim 16 (depends on 14)

The method as claimed in claim 14, wherein the DDR1 inhibitor specifically or preferentially inhibits DDR1 activity.
