IP Library › Granted Patent US 9,975,875
Granted Patent B2
US 9,975,875 · App. 15/680,323 · Granted May 22, 2018

Diamide compounds having muscarinic receptor antagonist and Beta2 adrenergic receptor agonist activity

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
C07D401/12
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Quick Facts
Patent No.
US 9,975,875
App. No.
15/680,323
Granted
May 22, 2018
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 (15)

1. A compound of the formula:

wherein:

G 2 is —NH 2 or —COOH;

Ar 1 is selected from phen-1,3-ylene and phen-1,4-ylene, wherein the phenylene group is unsubstituted or substituted with 1 to 3 substituents selected independently from C 1-3 alkyl, —O—(C 1-3 alkyl) and halo;

R 1 is selected independently from C 1-3 alkyl, —O—(C 1-3 alkyl), hydroxyl and halo;

R 2 is selected independently from C 1-3 alkyl, —O—(C 1-3 alkyl) and halo;

R 3 is selected independently from C 1-3 alkyl; or two R 3 groups are joined to form C 1-3 alkylene, C 2-3 alkenylene or oxiran-2,3-diyl;

a is 0, 1, 2 or 3;

b is 0, 1, 2 or 3;

c is 0, 1, 2, 3 or 4;

n is 0 or 1;

p is 0, 1, 2, 3, 4, 5 or 6; provided that when n is 0, p is 1, 2, 3, 4, 5 or 6; and

R a is selected from C 1-6 alkyl.

2. The compound according to claim 1 , wherein G 2 is —NH 2 .

3. The compound according to claim 1 , wherein G 2 is —COOH.

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 (10)
Continuation 15497446 · Apr 26, 2017
Continuation 15379673 · Dec 15, 2016
Continuation 15180165 · Jun 13, 2016
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 20170362200A1 · Dec 21, 2017