IP Library › Granted Patent US 9,283,183
Granted Patent B2
US 9,283,183 · App. 14/539,550 · Granted Mar 15, 2016

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
A61K9/124A61K31/4545A61K45/06C07D211/62C07D401/12
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Quick Facts
Patent No.
US 9,283,183
App. No.
14/539,550
Granted
Mar 15, 2016
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 (17)

1. A pharmaceutical composition comprising a pharmaceutically acceptable propellant 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.

2. The pharmaceutical composition of claim 1 , wherein the composition further comprises an agent selected from β 2 adrenergic receptor agonists, steroidal anti-inflammatory agents, phosphodiesterase-4 inhibitors, and combinations thereof.

3. The pharmaceutical composition of claim 2 , wherein the composition comprises a β 2 adrenergic receptor agonist and a steroidal anti-inflammatory agent.

4. The pharmaceutical composition of claim 1 , wherein said biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]-methylamino}ethyl)piperidin-4-yl ester or pharmaceutically acceptable salt thereof is in solution.

5. The pharmaceutical composition of claim 1 , wherein said biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]-methylamino}ethyl)piperidin-4-yl ester or pharmaceutically acceptable salt thereof is in a suspension.

6. The pharmaceutical composition of claim 1 , wherein the propellant is a hydrofluoroalkane.

7. The pharmaceutical composition of claim 6 , wherein the hydrofluoroalkane is 1,1,1,2-tetrafluoroethane.

8. The pharmaceutical composition of claim 6 , wherein the hydrofluoroalkane is 1,1,1,2,3,3,3-heptafluoro-n-propane.

9. The pharmaceutical composition of claim 1 , wherein the composition further comprises a co-solvent selected from ethanol and pentane.

10. The pharmaceutical composition of claim 1 , wherein the composition further comprises a surfactant selected from the sorbitan trioleate, oleic acid, lecithin, and glycerin.

11. The pharmaceutical composition of claim 1 , comprising from about 0.01% to about 5% by weight of said biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester or pharmaceutically acceptable salt thereof; from about 0% to about 20% by weight ethanol; and from about 0% to about 5% by weight surfactant; with the remainder being a hydrofluoroalkane propellant.

12. The pharmaceutical composition of claim 1 , wherein said biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]-methylamino}ethyl)piperidin-4-yl ester or pharmaceutically acceptable salt thereof is micronized.

13. A pharmaceutical composition comprising 1,1,1,2-tetrafluoroethane 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.

14. A pharmaceutical composition comprising 1,1,1,2,3,3,3-heptafluoro-n-propane 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.

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

16. The pharmaceutical composition of claim 15 , wherein the β 2 adrenergic receptor agonist is formoterol or a pharmaceutically acceptable salt thereof.

17. The pharmaceutical composition of claim 2 , wherein the composition further comprises a steroidal anti-inflammatory agent.

Continuity (9)
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 20150164795A1 · Jun 18, 2015