IP Library › Granted Patent US 8,173,815
Granted Patent B2
US 8,173,815 · App. 13/226,677 · Granted May 8, 2012

Biphenyl compounds useful as muscarinic receptor antagonists

Assignee: Theravance, Inc.
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Quick Facts
Patent No.
US 8,173,815
App. No.
13/226,677
Granted
May 8, 2012
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 (16)

1. A process for preparing biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, the process comprising:

reacting a compound of formula IX:

with a compound of formula VII:

in the presence of a reducing agent;

wherein a, b and c each represent 0; W represents O; m is 0; R 4 is methyl; s is 0; t is 1; Ar 1 represents phen-1,4-ylene; d is 0; n is 2; p is 0; the —CONR 7 R 8 group is in the para position; R 7 is hydrogen; and R 8 is hydrogen.

2. The process of claim 1 , where the reducing agent is hydrogen in the presence of a Group VIII metal catalyst.

3. The process of claim 1 , where the reducing agent is a metal hydride reducing agent.

4. The process of claim 3 , where the metal hydride reducing agent is sodium triacetoxyborohydride.

5. The process of claim 1 , where the reducing agent is used in combination with a titanium tetraalkoxide.

6. The process of claim 1 , where the reaction is conducted in a solvent selected from alcohols and halogenated hydrocarbons.

7. The process of claim 1 , where the reaction is performed at a temperature in the range of from 0° C. to 100° C.

8. The process of claim 7 , where the reaction is performed at a temperature in the range of from 0° C. to 10° C.

9. The process of claim 1 , where the compound of formula IX is prepared by reacting a compound of formula IV:

with a compound of formula XVII:

in the presence of a carboxylic acid/amine coupling agent.

10. The process of claim 9 , where the carboxylic acid/amine coupling agent is 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide and 1-hydroxybenzotriazole hydrate.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 3, 2014
From: THERAVANCE, INC.
To: THERAVANCE BIOPHARMA R&D IP, LLC
Reel/Frame 033118/0499 →
Continuity (5)
Continuation 12814629 · Jun 14, 2010
Continuation 11879835 · Jul 19, 2007
Continuation 11077433 · Mar 10, 2005
Provisional Application 60552443 · Mar 11, 2004
Related Publication 20110319625A1 · Dec 29, 2011