IP Library Granted Patent US 10,315,984
Granted Patent B2
US 10,315,984 · App. 15/843,427 · Granted Jun 11, 2019

Neprilysin inhibitors

Inventors: Melissa Fleury (Brisbane, CA); Adam D. Hughes (Half Moon Bay, 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 10,315,984
App. No.
15/843,427
Granted
Jun 11, 2019
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 (9)

1. A compound of:

(a) (2R,4R)-5-(3′-chlorobiphenyl-4-yl)-4-{[3-(2-fluorophenyl)isoxazole-5-carbonyl]amino}-2-hydroxypentanoic acid;

(b) (2R,4R)-5-(3′-chlorobiphenyl-4-yl)-4-{[3-(2-fluorophenyl)isoxazole-5-carbonyl]amino}-2-hydroxypentanoic acid ethoxycarbonyloxymethyl ester;

(c) (2R,4R)-5-(3′-chlorobiphenyl-4-yl)-4-{[3-(2-fluorophenyl)isoxazole-5-carbonyl]amino}-2-hydroxypentanoic acid isopropoxycarbonyloxymethyl ester;

(d) (2R,4R)-5-(3′-chlorobiphenyl-4-yl)-4-{[3-(2-fluorophenyl)isoxazole-5-carbonyl]amino}-2-hydroxypentanoic acid acetoxymethyl ester;

(e) (2R,4R)-5-(3′-chlorobiphenyl-4-yl)-4-{[3-(2-fluorophenyl)isoxazole-5-carbonyl]amino}-2-hydroxypentanoic acid (S)-2-methoxycarbonylamino-3-methylbutyryloxymethyl ester; or

a pharmaceutically-acceptable salt thereof.

2. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and the compound of claim 1 .

3. A method for treating hypertension, heart failure, or renal disease, comprising administering to a patient a therapeutically effective amount of the compound of claim 1 .

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 28, 2026
From: THERAVANCE BIOPHARMA R&D IP, LLC
To: EONHF, INC.
Reel/Frame 075494/0756 →
Continuity (6)
Continuation 15581327 · Apr 28, 2017
Continuation 14792810 · Jul 7, 2015
Continuation 13911819 · Jun 6, 2013
Provisional Application 61773969 · Mar 7, 2013
Provisional Application 61657229 · Jun 8, 2012
Related Publication 20180327350A1 · Nov 15, 2018