IP Library Granted Patent US 9,333,197
Granted Patent B2
US 9,333,197 · App. 14/254,359 · Granted May 10, 2016

Apoptosis signal-regulating kinase inhibitor

Inventor: Gregory Notte (Foster City, CA)
Assignee: Gilead Sciences, Inc.
A61K31/4439C07D213/56C07D233/56C07D401/04C07D401/14
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Quick Facts
Patent No.
US 9,333,197
App. No.
14/254,359
Granted
May 10, 2016
Kind
B2
Abstract

The present invention relates to a compound of formula (I): The compound has apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and is thus useful in the treatment of diseases such as kidney disease, diabetic nephropathy and kidney fibrosis.

Claims (23)

1. A method of treating a inhibiting kidney disease fibrosis comprising administering to a patient in need thereof a therapeutically effective amount of a compound of formula (I)

or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 , wherein the kidney-disease fibrosis is associated with diabetic kidney disease.

3. The method of claim 1 , wherein the pharmaceutically acceptable salt is the hydrochloride salt.

4. The method of claim 1 , wherein the therapeutic amount ranges from 1 mg to 250 mg.

5. The method of claim 1 , wherein the compound of formula (I) or a pharmaceutically acceptable salt thereof is administered orally.

6. The method of claim 1 , wherein the compound of formula (I) or a pharmaceutically acceptable salt thereof is administered in a single or multiple doses.

7. The method of claim 1 , wherein the compound of formula (I) or a pharmaceutically acceptable salt thereof is administered in combination with other therapeutic agents.

8. The method of claim 7 , wherein the one or more therapeutic agents is selected from the group consisting of angiotensin converting enzyme inhibitors, angiotensin II receptor blockers, antihypertensive agents, antibiotic agents, analgesic agents, antidepressant agents, or antianxiety agents.

9. The method of claim 7 , wherein the pharmaceutical composition and the one or more therapeutic agents are administered simultaneously.

10. The method of claim 7 , wherein the pharmaceutical composition and the one or more therapeutic agents are administered one after the other within intervals.

11. A method of treating fibrosis in a kidney comprising administering to a patient in need thereof a pharmaceutical composition comprising a compound of formula (I)

or a pharmaceutically acceptable salt thereof.

12. The method of claim 11 , wherein the pharmaceutically acceptable salt is the hydrochloride salt.

13. The method of claim 11 , wherein the pharmaceutical composition further comprises one or more pharmaceutically acceptable carriers.

14. The method of claim 11 , wherein the pharmaceutical composition is prepared for delivery as solid tablets.

15. The method of claim 11 , wherein the pharmaceutical composition is administered in a single or multiple doses.

16. The method of claim 15 , wherein the dose comprises 1 mg to 250 mg of the compound of formula (I).

17. The method of claim 11 , wherein the pharmaceutical composition is administered orally.

18. The method of claim 11 , wherein the pharmaceutical composition is administered in combination with one or more therapeutic agents.

19. The method of claim 18 , wherein the one or more therapeutic agents is selected from the group consisting of angiotensin converting enzyme inhibitors, angiotensin II receptor blockers, antihypertensive agents, antibiotic agents, analgesic agents, antidepressant agents, or antianxiety agents.

20. The method of claim 18 , wherein the pharmaceutical composition and the one or more therapeutic agents are administered simultaneously.

21. The method of claim 18 , wherein the pharmaceutical composition and the one or more therapeutic agents are administered one after the other within intervals.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 16, 2014
From: NOTTE, GREGORY
To: GILEAD SCIENCES, INC.
Reel/Frame 032689/0274 →
Continuity (3)
Division 13748901 · Jan 24, 2013
Provisional Application 61591710 · Jan 27, 2012
Related Publication 20140228412A1 · Aug 14, 2014