IP Library › Granted Patent US 8,551,978
Granted Patent B2
US 8,551,978 · App. 13/369,109 · Granted Oct 8, 2013

Diamide compounds having muscarinic receptor antagonist and β

Inventors: Adam D. Hughes (Belmont, CA); Yan Chen (Foster City, CA); John R. Jacobsen (San Mateo, CA); Eric L. Stangeland (Pacifica, CA); Rose Yen (San Francisco, CA)
Assignee: Theravance, Inc.
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Quick Facts
Patent No.
US 8,551,978
App. No.
13/369,109
Granted
Oct 8, 2013
Kind
B2
Abstract

This invention relates to a compound of formula I: or a pharmaceutically acceptable salt thereof. Such compounds possess both muscarinic receptor antagonist and β 2 adrenergic receptor agonist activities. The invention also relates to pharmaceutical compositions comprising such compounds, processes and intermediates for preparing such compounds, and methods of using such compounds as bronchodilating agents to treat pulmonary disorders.

Claims (12)

1. A method for treating a pulmonary disorder in a patient comprising administering to the patient biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-{[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethylamino]methyl}-phenylcarbamoyl)butyl]methylcarbamoyl}ethyl)piperidin-4-yl ester of formula:

or a pharmaceutically acceptable salt thereof.

2. A method for treating a pulmonary disorder in a patient comprising

(a) administering to the patient biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-{[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethylamino]methyl}-phenylcarbamoyl)butyl]methylcarbamoyl}ethyl)piperidin-4-yl ester of formula:

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.

3. The method of claim 1 or 2 , wherein the pulmonary disorder is chronic obstructive pulmonary disease.

4. The method of claim 1 or 2 , wherein the pulmonary disorder is asthma.

5. A method for producing bronchodilation in a mammal comprising administering to the mammal a bronchodilation-producing amount of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-{[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethylamino]methyl}-phenylcarbamoyl)butyl]methylcarbamoyl}ethyl)piperidin-4-yl ester of formula:

or a pharmaceutically acceptable salt thereof.

6. The method of claim 5 , wherein the mammal is a human.

Assignments (2)
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 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 10, 2014
From: THERAVANCE, INC.
To: THERAVANCE RESPIRATORY COMPANY, LLC
Reel/Frame 033175/0547 →
Continuity (3)
Division 12761532 · Apr 16, 2010
Provisional Application 61172039 · Apr 23, 2009
Related Publication 20130137665A1 · May 30, 2013