IP Library Granted Patent US 9,670,140
Granted Patent B2
US 9,670,140 · App. 14/792,810 · Granted Jun 6, 2017

Neprilysin inhibitors

Inventor: Adam D. Hughes (Belmont, CA)
Assignee: Theravance Biopharma R&D IP, LLC
C07C229/22A61K31/41A61K31/415A61K31/4155A61K31/4192A61K31/4196A61K31/42A61K31/4439A61K31/675A61K45/06C07C271/22C07D207/26C07D231/14C07D231/18C07D231/20C07D249/04C07D249/12C07D249/18C07D253/08C07D257/04C07D261/18C07D263/38C07D401/04C07D405/12C07D405/14C07F9/65031
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Quick Facts
Patent No.
US 9,670,140
App. No.
14/792,810
Granted
Jun 6, 2017
Kind
B2
Abstract

In one aspect, the invention relates to compounds having the formula XII: where R a , R b , R 2 , R 7 , and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.

Claims (11)

1. A compound of:

(a) (2R,4R)-4-amino-5-(3′-chlorobiphenyl-4-yl)-2-hydroxypentanoic acid ethyl ester;

(b) (2R,4R)-4-amino-5-(3′-chlorobiphenyl-4-yl)-2-hydroxypentanoic acid 2,2,3,3,3-pentafluoropropyl ester;

(c) (2R,4R)-4-amino-5-(3′-chlorobiphenyl-4-yl)-2-hydroxypentanoic acid 5-methyl-2-oxo[1,3]dioxol-4-ylmethyl ester; or

(d) (2R,4R)-4-amino-5-(3′-chlorobiphenyl-4-yl)-2-hydroxypentanoic acid butyryloxymethyl ester.

2. A compound of:

(a) (2R,4R)-4-amino-5-(5′-chloro-2′-fluoro-biphenyl-4-yl)-2-hydroxypentanoic acid;

(b) (2R,4R)-4-amino-5-(5′-chloro-2′-fluorobiphenyl-4-yl)-2-hydroxypentanoic acid ethyl ester;

(c) (2R,4R)-4-amino-5-(5′-chloro-2′-fluorobiphenyl-4-yl)-2-hydroxypentanoic acid 5-methyl-2-oxo-[1,3]dioxol-4-ylmethyl ester;

(d) (2R,4R)-4-amino-5-(5′-chloro-2′-fluorobiphenyl-4-yl)-2-hydroxypentanoic acid 2,2,3,3,3-pentafluoropropyl ester; or

(e) (2R,4R)-4-amino-5-(5′-chloro-2′-fluorobiphenyl-4-yl)-2-hydroxypentanoic acid butyryloxymethyl ester.

Continuity (4)
Continuation 13911819 · Jun 6, 2013
Provisional Application 61773969 · Mar 7, 2013
Provisional Application 61657229 · Jun 8, 2012
Related Publication 20160002148A1 · Jan 7, 2016