IP Library Granted Patent US 8,802,682
Granted Patent B2
US 8,802,682 · App. 13/459,055 · Granted Aug 12, 2014

Compound useful for the treatment of degenerative and inflammatory diseases

Inventors: Christel Jeanne Marie Menet (Mechelen, BE); Alastair James Hodges (Saffron Walden, GB); Huw David Vater (Saffron Walden, GB)
Assignee: Galapagos NV
C07D471/04A61K31/496
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Quick Facts
Patent No.
US 8,802,682
App. No.
13/459,055
Granted
Aug 12, 2014
Kind
B2
Abstract

A pyrazolopyridine compound according to Formula I, able to inhibit JAK is disclosed, as well as pharmaceutically acceptable salts, a solvate thereof, solvates of the pharmaceutically acceptable salts and biologically active metabolites thereof. The compound may be prepared as a pharmaceutical composition, and may be used for the treatment or prophylaxis of a variety of conditions in mammals including humans, and particularly, such conditions as may be associated with aberrant JAK activity, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL 6 .

Claims (12)

1. The compound according to Formula I:

or a pharmaceutically acceptable salt, or a biologically active metabolite thereof.

2. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of the compound or pharmaceutically acceptable salt thereof, according to claim 1 .

3. The pharmaceutical composition of claim 2 , wherein the carrier is selected from a parenteral carrier, an oral carrier and a topical carrier.

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

5. The pharmaceutical composition according to claim 4 , wherein the further therapeutic agent is an agent selected from analgesics, NSAIDS (non-steroidal anti-inflammatory drugs), and DMARDS (disease-modifying anti-rheumatic drugs).

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

7. The method according to claim 6 , wherein said compound is administered in combination with more than one further therapeutic agents selected from arthritis treatment agents.

8. The method according to claim 6 , wherein said compound is administered in combination with one further therapeutic agent selected from arthritis treatment agents.

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

10. The method according to claim 7 , wherein the further therapeutic agents are selected from analgesics, NSAIDS (non-steroidal anti-inflammatory drugs), and DMARDS (disease-modifying anti-rheumatic drugs).

11. The method according to claim 8 , 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 (3)
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 May 31, 2012
From: MENET, CHRISTEL JEANNE MARIE; HODGES, ALASTAIR JAMES; VATER, HUW DAVID; BIOFOCUS DPI LTD.
To: GALAPAGOS NV
Reel/Frame 028293/0508 →
Continuity (2)
Provisional Application 61479956 · Apr 28, 2011
Related Publication 20120277247A1 · Nov 1, 2012