IP Library Granted Patent US 10,336,773
Granted Patent B2
US 10,336,773 · App. 15/806,680 · Granted Jul 2, 2019

Neprilysin inhibitors

Inventors: Roland Gendron (El Verano, CA); Adam D. Hughes (Half Moon Bay, CA)
Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
C07D498/08A61K31/42A61K31/422A61K31/5377A61K45/06C07D207/34C07D213/79C07D213/80C07D213/81C07D231/14C07D233/26C07D233/90C07D237/04C07D237/24C07D239/34C07D239/36C07D241/24C07D249/04C07D249/08C07D249/10C07D249/12C07D249/18C07D257/04C07D261/12C07D261/18C07D261/20C07D263/34C07D263/56C07D271/06C07D277/46C07D277/56C07D307/68C07D333/40C07D333/70C07D401/04C07D401/06C07D403/04C07D403/06C07D405/12C07D409/06C07D413/04C07D413/06C07D413/12C07D471/04C07D498/04
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Quick Facts
Patent No.
US 10,336,773
App. No.
15/806,680
Granted
Jul 2, 2019
Kind
B2
Abstract

In one aspect, the invention relates to compounds having the formula: where R 1 -R 6 , a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

Claims (6)

1. (2R,4R)-5-Biphenyl-4-yl-4-[(5-carboxymethyl-1H-pyrazole-3-carbonyl)amino]-2-hydroxy-pentanoic acid or a pharmaceutically acceptable salt thereof.

2. (2R,4R)-5-Biphenyl-4-yl-2-hydroxy-4-[(5-hydroxymethyl-1H-pyrazole-3-carbonyl)-amino]-pentanoic acid or a pharmaceutically acceptable salt thereof.

3. (2R,4R)-5-Biphenyl-4-yl-2-hydroxy-4-[(5-methoxymethyl-1H-pyrazole-3-carbonyl)-amino]-pentanoic acid or a pharmaceutically acceptable salt thereof.

4. A pharmaceutical composition comprising the compound of any one of claims 1 - 3 and a pharmaceutically acceptable carrier.

5. The pharmaceutical composition of claim 4 , further comprising an AT 1 receptor antagonist.

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

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 (7)
Continuation 15599769 · May 19, 2017
Continuation 15173870 · Jun 6, 2016
Division 14800966 · Jul 16, 2015
Continuation 14050733 · Oct 10, 2013
Division 13325425 · Dec 14, 2011
Provisional Application 61423180 · Dec 15, 2010
Related Publication 20180194776A1 · Jul 12, 2018