Compound useful for the treatement of degenerative and inflammatory diseases

Patent metadata

Field	Value
Publication number	US-9987272-B2
Application number	US-201615005442-A
Country	US
Kind code	B2
Filing date	Jan 25, 2016
Priority date	Apr 28, 2011
Publication date	Jun 5, 2018
Grant date	Jun 5, 2018

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.

First claim

What is claimed is:

1. A method for the treatment of Crohn's Disease, 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 Crohn's Disease.

3. A method for the treatment of Crohn's Disease, 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 Crohn's Disease treatment agents.

5. The method according to claim 3 , wherein said compound is administered in combination with one further therapeutic agent selected from Crohn's Disease 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 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.

Assignees

• Menet Christel Jeanne Marie
• Hodges Alastair James
• Vater Huw David
• Galapagos Nv

Inventors

• Menet Christel Jeanne Marie
• Hodges Alastair James
• Vater Huw David

Classifications

• A61P37/02

  Immunomodulators · CPC title

• A61P37/06

  Immunosuppressants, e.g. drugs for graft rejection · CPC title

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title

• A61P37/08

  Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14) · CPC title