IP Library › Granted Patent US 9,682,957
Granted Patent B2
US 9,682,957 · App. 15/379,673 · Granted Jun 20, 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
C07D401/12
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 9,682,957
App. No.
15/379,673
Granted
Jun 20, 2017
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 (22)

1. A compound of the formula:

wherein:

Y is a group of formula (a):

and Y is attached at the 3- or 4-position of the phenylene ring relative to the

group;

X is selected from —C(O)NH— and —NHC(O)—;

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;

R 4 is selected independently from C 1-3 alkyl, —O—(C 1-3 alkyl) and halo;

R a is selected from C 1-6 alkyl;

a is 0, 1, 2 or 3;

b is 0, 1, 2 or 3;

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

d is 0, 1, 2 or 3;

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;

q is 0, 1, 2, 3, 4, 5 or 6;

and

P 2a and P 2b are selected independently from C 1-6 alkyl, or P 2a and P 2b are joined to form C 2-6 alkylene.

2. The compound according to claim 1 , wherein P 2a and P 2b are joined to form C 2-4 alkylene.

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 (8)
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 20170096412A1 · Apr 6, 2017