Neprilysin inhibitors

Patent metadata

Field	Value
Publication number	US-9873685-B2
Application number	US-201715497508-A
Country	US
Kind code	B2
Filing date	Apr 26, 2017
Priority date	Aug 8, 2012
Publication date	Jan 23, 2018
Grant date	Jan 23, 2018

Abstract

In one aspect, the invention relates to compounds having the formula:

where X, R a , R b , R 2 , and R 7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds 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.

First claim

What is claimed is:

1. A compound having the structure:

or a pharmaceutically acceptable salt thereof.

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

3. A pharmaceutical composition comprising a pharmaceutically acceptable carrier, a compound of claim 1 , and an AT 1 receptor antagonist.

4. The pharmaceutical composition comprising a pharmaceutically acceptable carrier, a compound of claim 1 , and a phosphodiesterase (PDE) inhibitor.

5. The pharmaceutical composition comprising a pharmaceutically acceptable carrier, a compound of claim 1 , and a renin inhibitor.

6. The pharmaceutical composition comprising a pharmaceutically acceptable carrier, a compound of claim 1 , and a diuretic.

7. 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 .

Assignees

• Theravance Biopharma R&D Ip Llc

Inventors

• Fleury Melissa
• Hughes Adam D

Classifications

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61P9/12

  Antihypertensives · CPC title

• A61P9/04

  Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure · CPC title

• A61P9/10

  for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis · CPC title

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title