IP Library Granted Patent US 8,242,274
Granted Patent B2
US 8,242,274 · App. 12/508,950 · Granted Aug 14, 2012

Triazolopyridine kinase inhibitors useful for the treatment of degenerative and inflammatory diseases

Assignee: Galapagos NV
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Quick Facts
Patent No.
US 8,242,274
App. No.
12/508,950
Granted
Aug 14, 2012
Kind
B2
Abstract

A novel [1,2,4]triazolo[1,5-a]pyridine compound is disclosed that has a formula represented by the following: This compound may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, diseases involving cartilage degradation, bone and/or joint degradation, for example osteoarthritis; and/or conditions involving inflammation or immune responses, such as Crohn's disease, rheumatoid arthritis, psoriasis, allergic airways disease (e.g. asthma, rhinitis), juvenile idiopathic arthritis, colitis, inflammatory bowel diseases, endotoxin-driven disease states (e.g. complications after bypass surgery or chronic endotoxin states contributing to e.g. chronic cardiac failure), diseases involving impairment of cartilage turnover (e.g. diseases involving the anabolic stimulation of chondrocytes), congenital cartilage malformations, diseases associated with hypersecretion of IL6 and transplantation rejection (e.g. organ transplant rejection) and proliferative diseases.

Claims (19)

1. A compound according to Formula VIa:

or a pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of a compound according to claim 1 .

3. The pharmaceutical composition of claim 2 , wherein the carrier is a parenteral carrier.

4. The pharmaceutical composition of claim 2 , wherein the carrier is an oral carrier.

5. The pharmaceutical composition of claim 2 , wherein the carrier is a topical carrier.

6. The pharmaceutical composition according to claim 2 comprising a further therapeutic agent selected from arthritis treatment agents.

7. The pharmaceutical composition according to claim 6 , wherein the further therapeutic agent is an agent selected from analgesics, NSAIDS (non-steroidal anti-inflammatory drugs), and DMARDS (disease-modifying anti-rheumatic drugs).

8. A method for the treatment of rheumatoid arthritis, comprising administering an amount of a compound of claim 1 , sufficient to effect said treatment.

9. The method according to claim 8 , wherein the compound according to claim 1 is administered in combination with one or more further therapeutic agents selected from arthritis treatment agents.

10. The method according to claim 8 , wherein the compound according to claim 1 is administered in combination with one further therapeutic agent selected from arthritis treatment agents.

11. A method for the treatment of rheumatoid arthritis, comprising administering an amount of a pharmaceutical composition of claim 2 , sufficient to effect said treatment.

12. A method for the treatment of rheumatoid arthritis, comprising administering an amount of a pharmaceutical composition of claim 6 , sufficient to effect said treatment.

13. The method according to claim 11 , wherein said pharmaceutical composition is administered in combination with a further therapeutic agent selected from arthritis treatment agents.

14. The method according to claim 12 , wherein said pharmaceutical composition is administered in combination with a further therapeutic agent selected from arthritis treatment agents.

15. The method according to claim 9 , wherein the further therapeutic agent is an agent selected from analgesics, NSAIDS (non-steroidal anti-inflammatory drugs), and DMARDS (disease-modifying anti-rheumatic drugs).

16. The method according to claim 10 , wherein the further therapeutic agent is an agent selected from analgesics, NSAIDS (non-steroidal anti-inflammatory drugs), and DMARDS (disease-modifying anti-rheumatic drugs).

17. The method according to claim 13 , wherein the further therapeutic agent is an agent selected from analgesics, NSAIDS (non-steroidal anti-inflammatory drugs), and DMARDS (disease-modifying anti-rheumatic drugs).

18. The method according to claim 14 , wherein the further therapeutic agent is an agent selected from analgesics, NSAIDS (non-steroidal anti-inflammatory drugs), and DMARDS (disease-modifying anti-rheumatic drugs).

Assignments (4)
CHANGE OF NAME Recorded Jun 4, 2026
From: GALAPAGOS
To: LAKEFRONT BIOTHERAPEUTICS
Reel/Frame 074845/0068 →
SECURITY INTEREST Recorded Aug 23, 2019
From: GALAPAGOS NV
To: GILEAD SCIENCES, INC.
Reel/Frame 050149/0161 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 12, 2012
From: MENET, CHRISTEL JEANNE MARIE; BLANC, JAVIER
To: GALAPAGOS NV
Reel/Frame 028615/0672 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 15, 2009
From: MENET, CHRISTEL JEANNE MARIE; BLANC, JAVIER
To: GALAPAGOS NV
Reel/Frame 023383/0179 →
Continuity (3)
Provisional Application 61135920 · Jul 25, 2008
Provisional Application 61220685 · Jun 26, 2009
Related Publication 20100029709A1 · Feb 4, 2010