IP Library › Granted Patent US 10,343,995
Granted Patent B2
US 10,343,995 · App. 16/130,076 · Granted Jul 9, 2019

Biphenyl compounds useful as muscarinic receptor antagonists

Inventors: Mathai Mammen (Menlo Park, CA); YuHua Ji (Palo Alto, CA); YongQi Mu (Los Altos, CA); Craig Husfeld (Redwood City, CA); Li Li (Sunnyvale, CA)
Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
C07D211/62A61K9/124A61K9/1623A61K9/1652A61K31/4545A61K45/06C07D401/12
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Quick Facts
Patent No.
US 10,343,995
App. No.
16/130,076
Granted
Jul 9, 2019
Kind
B2
Abstract

This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, W, Ar 1 , R 1 , R 2 , R 3 , R 4 , R 6 , R 7 , and R 8 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.

Claims (23)

1. A method for producing bronchodilation in a mammal, the method comprising administering to the mammal a pharmaceutical composition comprising a pharmaceutically acceptable carrier and biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester or a pharmaceutically acceptable salt thereof; wherein the pharmaceutical composition is administered to the mammal in an amount sufficient to provide about 10 μg/day to about 200 μg/day of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]-methylamino}ethyl)piperidin-4-yl ester or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 , wherein the pharmaceutical composition is administered by inhalation.

3. The method of claim 1 , wherein the pharmaceutical composition is administered using a nebulizer inhaler.

4. The method of claim 1 , wherein the pharmaceutical composition is administered in a single daily dose.

5. The method of claim 1 , wherein the pharmaceutical composition comprises a pharmaceutically acceptable aqueous carrier.

6. The method of claim 5 , wherein the pharmaceutical composition has a pH in the range of from 3 to 8.

7. The method of claim 5 , wherein the pharmaceutical composition further comprises a buffer.

8. The method of claim 7 , wherein the buffer is a sodium chloride citric acid buffer.

9. The method of claim 5 , wherein the pharmaceutical composition is an isotonic aqueous solution.

10. The method of claim 9 , wherein the isotonic aqueous solution comprises about 0.05 μg/mL to about 10 mg/mL of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester or a pharmaceutically acceptable salt thereof.

11. The method of claim 1 , wherein the pharmaceutical composition further comprises a β 2 adrenergic receptor agonist.

12. The method of claim 1 , wherein the pharmaceutical composition further comprises a steroidal anti-inflammatory agent.

13. A method for producing bronchodilation in a human patient, the method comprising administering to the patient by inhalation a pharmaceutical composition comprising a pharmaceutically acceptable carrier and biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester or a pharmaceutically acceptable salt thereof; wherein the pharmaceutical composition is administered to the patient in an amount sufficient to provide about 10 μg/day to about 200 μg/day of biphenyl-2-ylcarbamic acid 1( 2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]-methylamino}ethyl)piperidin-4-yl ester or a pharmaceutically acceptable salt thereof.

14. The method of claim 13 , wherein the pharmaceutical composition is administered using a nebulizer inhaler.

15. The method of claim 13 , wherein the pharmaceutical composition is administered in a single daily dose.

16. The method of claim 13 , wherein the pharmaceutical composition comprises a pharmaceutically acceptable aqueous carrier.

17. The method of claim 16 , wherein the pharmaceutical composition has a pH in the range of from 3 to 8.

18. The method of claim 16 , wherein the pharmaceutical composition further comprises a buffer.

19. The method of claim 18 , wherein the buffer is a sodium chloride citric acid buffer.

20. The method of claim 16 , wherein the pharmaceutical composition is an isotonic aqueous solution.

21. The method of claim 20 , wherein the isotonic aqueous solution comprises about 0.05 μg/mL to about 10 mg/mL of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester or a pharmaceutically acceptable salt thereof.

22. The method of claim 13 , wherein the pharmaceutical composition further comprises a β 2 adrenergic receptor agonist.

23. The method of claim 13 , wherein the pharmaceutical composition further comprises a steroidal anti-inflammatory agent.

Continuity (13)
Continuation 15876525 · Jan 22, 2018
Continuation 15251144 · Aug 30, 2016
Continuation 15016528 · Feb 5, 2016
Continuation 14539550 · Nov 12, 2014
Continuation 14023794 · Sep 11, 2013
Continuation 13592713 · Aug 23, 2012
Continuation 13438105 · Apr 3, 2012
Continuation 13226677 · Sep 7, 2011
Continuation 12814629 · Jun 14, 2010
Continuation 11879835 · Jul 19, 2007
Continuation 11077433 · Mar 10, 2005
Provisional Application 60552443 · Mar 11, 2004
Related Publication 20190047957A1 · Feb 14, 2019
Cited By (2)
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