IP Library › Granted Patent US 9,572,802
Granted Patent B2
US 9,572,802 · App. 15/180,165 · Granted Feb 21, 2017

Diamide compounds having muscarinic receptor antagonist and β

Inventors: Adam D. Hughes (Belmont, CA); Daniel Byun (Alameda, CA); Yan Chen (Foster City, CA); Melissa Fleury (Brisbane, CA); John R. Jacobsen (San Mateo, CA); Eric L. Stangeland (Pacifica, CA); Richard D. Wilson (Orinda, CA); Rose Yen (San Francisco, CA)
Assignee: Theravance Respiratory Company LLC
A61K31/4709A61K45/06C07D401/12
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Quick Facts
Patent No.
US 9,572,802
App. No.
15/180,165
Granted
Feb 21, 2017
Kind
B2
Abstract

The invention provides diamide compounds having muscarinic receptor antagonist and β 2 adrenergic receptor agonist activity, pharmaceutical compositions thereof, and methods of treatment using the same.

Claims (57)

1. A compound of the formula:

or a pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition comprising

(a) a compound of claim 1 , or a pharmaceutically acceptable salt thereof; and

(b) a pharmaceutically acceptable carrier.

3. A pharmaceutical composition comprising

(a) a compound of claim 1 , or a pharmaceutically acceptable salt thereof;

(b) a steroidal anti-inflammatory agent or a pharmaceutically acceptable salt or solvate thereof; and

(c) a pharmaceutically acceptable carrier.

4. The pharmaceutical composition of claim 3 , wherein the steroidal anti-inflammatory agent is a corticosteroid or a pharmaceutically acceptable salt or solvate thereof.

5. A method for treating a pulmonary disorder in a patient comprising administering to the patient a compound of claim 1 or a pharmaceutically acceptable salt thereof.

6. A method for treating a pulmonary disorder in a patient comprising:

(a) administering to the patient a compound of claim 1 , or a pharmaceutically acceptable salt thereof; and

(b) administering to the patient a steroidal anti-inflammatory agent, or a pharmaceutically acceptable salt or solvate thereof;

wherein step (a) and (b) are conducted simultaneously or sequentially in any order.

7. The method of claim 5 , wherein the pulmonary disorder is chronic obstructive pulmonary disease.

8. The method of claim 5 , wherein the pulmonary disorder is asthma.

9. A method for producing bronchodilation in a mammal comprising administering to the mammal a bronchodilation-producing amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof.

10. The method of claim 9 , wherein the mammal is a human.

11. A compound of the formula:

or a pharmaceutically acceptable salt thereof.

12. A pharmaceutical composition comprising

(a) a compound of claim 11 , or a pharmaceutically acceptable salt thereof; and

(b) a pharmaceutically acceptable carrier.

13. A pharmaceutical composition comprising

(a) a compound of claim 11 , or a pharmaceutically acceptable salt thereof;

(b) a steroidal anti-inflammatory agent or a pharmaceutically acceptable salt or solvate thereof; and

(c) a pharmaceutically acceptable carrier.

14. The pharmaceutical composition of claim 13 , wherein the steroidal anti-inflammatory agent is a corticosteroid or a pharmaceutically acceptable salt or solvate thereof.

15. A method for treating a pulmonary disorder in a patient comprising administering to the patient a compound of claim 11 or a pharmaceutically acceptable salt thereof.

16. A method for treating a pulmonary disorder in a patient comprising:

(a) administering to the patient a compound of claim 11 , or a pharmaceutically acceptable salt thereof; and

(b) administering to the patient a steroidal anti-inflammatory agent, or a pharmaceutically acceptable salt or solvate thereof;

wherein step (a) and (b) are conducted simultaneously or sequentially in any order.

17. The method of claim 15 , wherein the pulmonary disorder is chronic obstructive pulmonary disease.

18. The method of claim 15 , wherein the pulmonary disorder is asthma.

19. A method for producing bronchodilation in a mammal comprising administering to the mammal a bronchodilation-producing amount of a compound of claim 11 , or a pharmaceutically acceptable salt thereof.

20. The method of claim 19 , wherein the mammal is a human.

21. A compound of the formula:

or a pharmaceutically acceptable salt thereof.

22. A pharmaceutical composition comprising

(a) a compound of claim 21 , or a pharmaceutically acceptable salt thereof; and

(b) a pharmaceutically acceptable carrier.

23. A pharmaceutical composition comprising

(a) a compound of claim 21 , or a pharmaceutically acceptable salt thereof;

(b) a steroidal anti-inflammatory agent or a pharmaceutically acceptable salt or solvate thereof; and

(c) a pharmaceutically acceptable carrier.

24. The pharmaceutical composition of claim 23 , wherein the steroidal anti-inflammatory agent is a corticosteroid or a pharmaceutically acceptable salt or solvate thereof.

25. A method for treating a pulmonary disorder in a patient comprising administering to the patient a compound of claim 21 or a pharmaceutically acceptable salt thereof.

26. A method for treating a pulmonary disorder in a patient comprising:

(a) administering to the patient a compound of claim 21 , or a pharmaceutically acceptable salt thereof; and

(b) administering to the patient a steroidal anti-inflammatory agent, or a pharmaceutically acceptable salt or solvate thereof;

wherein step (a) and (b) are conducted simultaneously or sequentially in any order.

27. The method of claim 25 , wherein the pulmonary disorder is chronic obstructive pulmonary disease.

28. The method of claim 25 , wherein the pulmonary disorder is asthma.

29. A method for producing bronchodilation in a mammal comprising administering to the mammal a bronchodilation-producing amount of a compound of claim 21 , or a pharmaceutically acceptable salt thereof.

30. The method of claim 29 , wherein the mammal is a human.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 12, 2020
From: THERAVANCE RESPIRATORY COMPANY, LLC
To: THERAVANCE BIOPHARMA R&D IP, LLC
Reel/Frame 054393/0695 →
Continuity (7)
Continuation 14638171 · Mar 4, 2015
Continuation 14327853 · Jul 10, 2014
Division 13964484 · Aug 12, 2013
Continuation 13369109 · Feb 8, 2012
Division 12761532 · Apr 16, 2010
Provisional Application 61172039 · Apr 23, 2009
Related Publication 20160361304A1 · Dec 15, 2016