IP Library Granted Patent US 9,241,931
Granted Patent B2
US 9,241,931 · App. 14/457,071 · Granted Jan 26, 2016

Compound useful for the treatment of degenerative and inflammatory diseases

Inventors: Christel Jeanne Marie Menet (Mechelen, BE); Alastair James Hodges (Essex, GB); Huw David Vater (Essex, GB)
Assignee: GALAPAGOS NV
A61K31/437A61K31/496A61K31/5377A61K31/541A61K45/06C07D471/04C07D491/107
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Quick Facts
Patent No.
US 9,241,931
App. No.
14/457,071
Granted
Jan 26, 2016
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 IL6.

Claims (13)

1. A method for the treatment of ulcerative colitis, comprising administering an amount of a compound according to Formula I:

or pharmaceutically acceptable salt thereof, sufficient to effect said treatment.

2. The method according to claim 1 , wherein the compound or pharmaceutically acceptable salt thereof, is administered in combination with a further therapeutic agent for the treatment of ulcerative colitis.

3. A method for the treatment of ulcerative colitis, comprising administering an amount of the pharmaceutical composition comprising a pharmaceutically acceptable carrier and an amount of a compound according to Formula I:

or a pharmaceutically acceptable salt thereof, sufficient to effect said treatment.

4. The method according to claim 3 , wherein said compound is administered in combination with one or more further therapeutic agents selected from ulcerative colitis treatment agents.

5. The method according to claim 3 , wherein said compound is administered in combination with one further therapeutic agent selected from ulcerative colitis treatment agents.

6. The method according to claim 2 , wherein the further therapeutic agent is an agent selected from glucocorticoids, synthetic disease modifying immunomodulatory agents, and biological disease modifying immunomodulatory agents.

7. The method according to claim 4 , wherein the further therapeutic agent is an agent selected from glucocorticoids, synthetic disease modifying immunomodulatory agents, and biological disease modifying immunomodulatory agents.

8. The method according to claim 5 , wherein the further therapeutic agent is an agent selected from glucocorticoids, synthetic disease modifying immunomodulatory agents, and biological disease modifying immunomodulatory agents.

9. The method according to claim 6 , wherein the further therapeutic agent is an agent selected from prednisone, budesonide, methotrexate, leflunomide, sulfasalazine, mesalazine, azathioprine, 6-mercaptopurine, cyclosporin, infliximab, adalimumab, rituximab, and abatacept.

10. The method according to claim 7 , wherein the further therapeutic agent is an agent selected from prednisone, budesonide, methotrexate, leflunomide, sulfasalazine, mesalazine, azathioprine, 6-mercaptopurine, cyclosporin, infliximab, adalimumab, rituximab, and abatacept.

11. The method according to claim 8 , wherein the further therapeutic agent is an agent selected from prednisone, budesonide, methotrexate, leflunomide, sulfasalazine, mesalazine, azathioprine, 6-mercaptopurine, cyclosporin, infliximab, adalimumab, rituximab, and abatacept.

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 Aug 18, 2014
From: MENET, CHRISTEL JEANNE MARIE; HODGES, ALASTAIR JAMES; VATER, HUW DAVID
To: GALAPAGOS NV
Reel/Frame 033551/0727 →
Continuity (3)
Continuation 13459055 · Apr 27, 2012
Provisional Application 61479956 · Apr 28, 2011
Related Publication 20150031706A1 · Jan 29, 2015