Neprilysin inhibitors
US-2017217959-A1 · Aug 3, 2017 · US
Neprilysin inhibitors
US9981999B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9981999-B2 |
| Application number | US-201715589289-A |
| Country | US |
| Kind code | B2 |
| Filing date | May 8, 2017 |
| Priority date | Jun 8, 2012 |
| Publication date | May 29, 2018 |
| Grant date | May 29, 2018 |
How to read this patent
A practical reading order for non-experts. Skip the full description unless you need deep technical detail.
- Title
What the patent document calls the invention.
- Abstract
A short plain-language summary of the technical disclosure.
- Assignees and inventors
Who owns or filed the patent and who is credited as inventor.
- Key dates
Filing, priority, publication, and grant dates set the timeline.
- First independent claim
The legal scope of protection — read this for what is actually claimed.
- CPC / IPC classifications
Technology tags used to group this patent with similar filings.
- Citations and related patents
Prior art links and similar publications in this corpus.
Abstract
Official abstract text for this publication.
In one aspect, the invention relates to compounds having the formula X: 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.
First claim
Opening claim text (preview).
What is claimed is: 1. A compound of: (a) (R)-3-[N-(5′-chloro-2′-fluorobiphenyl-4-ylmethyl)-N′-(3-mathoxyisoxazole-5-carbonyl)hydrazino]-2-hydroxypropionic Acid 5-methyl-2-oxo[1,3]dioxol-4-ylmethyl ester; (b) (R)-3-[N-(5′-chloro-2′-fluorobiphenyl-4-ylmethyl)-N′-(3-methoxyisoxazole-5-carbonyl)hydrazino]-2-hydroxypropionic acid 2,2,3,3,3-pentafluoropropyl ester; (c) (R)-3[N-(5′-chloro-2′-fluorobiphenyl-4-ylmethyl)-N′-(3-methoxyisoxazole-5-carbonyl)hydrazino]-2-hydroxypropionic acid acetoxymethyl ester; (d) (R)-3[N-(5′-chloro-2′-fluorobiphenyl-4-ylmethyl)-N′-(3-methoxyisoxazole-5-carbonyl)hydrazino]-2-hydroxypropionic acid 2-methoxy-ethyl ester; (e)butyric acid (R)-3[N-(5′-chloro-2′-fluorobiphenyl-4-ylmethyl)-N′-(3-methoxyisoxazole-5-carbonyl)hydrazino]-2-hydroxypropionyloxymethyl ester; (f) (R)-3[N-(5′-chloro-2′-fluorobiphenyl-4-ylmethyl)-N′-(3-methoxyisoxazole-5-carbonyl)hydrazino]-2-hydroxypropionic acid ethoxycarbonyloxymethyl ester; (g) (R)-3[N-(5′-chloro-2′-fluorobiphenyl-4-ylmethyl)-N′-(3-methoxyisoxazole-5-carbonyl)hydrazino]-2-hydroxypropionic acid 2-morpholin-4-ylethyl ester; (h) (S)-2-methoxycarbonylamino-3-methylbutyric acid (R)-3-[N-(5′-chloro-2′-fluorobiphenyl-4-ylmethyl)-N′-(3-methoxyisoxazole-5-carbonyl)hydrazino]-2-hydroxypropionyloxymethyl ester; (i) (R)-3[N-(5′-chloro-2′-fluorobiphenyl-4-ylmethyl)-N′-(3-methoxyisoxazole-5-carbonyl)hydrazino]-2-hydroxypropionic acid isopropoxycarbonyloxymethyl ester; (j) (R)-2-(2-aminoacetoxy)-3[N-(5′-chloro-2′-fluorobiphenyl-4-ylmethyl)-N′-(3-methoxyisoxazole-5-carbonyl)hydrazino]propionic acid ethyl ester; (k) (R)-3[N-(5′-chloro-2′-fluorobiphenyl-4-ylmethyl)-N′-(3-methoxyisoxazole-5-carbonyl)hydrazino]-2-propionyloxypropionic acid; (l) (S)-2-amino-3-methylbutyric acid (R)-3[N-(5′-chloro-2′-fluorobiphenyl-4-ylmethyl)-N′-(3-methoxyisoxazole-5-carbonyl)-hydrazino]-2-hydroxypropionyloxymethyl ester; (m) (S)-2-methoxycarbonylamino-3-methylbutyric acid (R)-1-carboxy-2[N-(5′-chloro-2′-fluorobiphenyl-4-ylmethyl)-N′-(3-methoxyisoxazole-5-carbonyl)hydrazino]ethyl ester; (n) (S)-2-aminopropionic acid (R)-1-carboxy-2-[N-(5′-chloro-2′-fluorobiphenyl-4-ylmethyl)-N′-(3-methoxyisoxazole-5-carbonyl)hydrazino]ethyl ester; (o) (S)-2-amino-3-methylbutyric acid (R)-1-carboxy-2-[N-(5′-chloro-2′-fluorobiphenyl-4-ylmethyl)-N′-(3-methoxyisoxazole-5-carbonyl)hydrazino]ethyl ester; (p) (R)-2-(2-aminoacetoxy)-3[N-(5′-chloro-2′-fluorobiphenyl-4-ylmethyl)-N′-(3-methoxyisoxazole-5-carbonyl)hydrazino]propionic acid; (q) (R)-3[N-(5′-chloro-2′-fluorobiphenyl-4-ylmethyl)-N′-(3-methoxyisoxazole-5-carbonyl)hydrazino]-2-hydroxypropionic acid 1-cyclohexyloxycarbonyloxyethyl ester; or a pharmaceutically-acceptable salt thereof.
Assignees
Inventors
Classifications
Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title
Antihypertensives · CPC title
Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure · CPC title
Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen · CPC title
linked by a chain containing hetero atoms as chain links · CPC title
Patent family
Related publications grouped by family.
External sources
Frequently asked questions
Answers are generated from the same data shown on this page.
- What does patent US9981999B2 cover?
- In one aspect, the invention relates to compounds having the formula X: 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…
- Who is the assignee on this patent?
- Theravance Biopharma R&D Ip Llc
- What technology area does this patent fall under?
- Primary CPC classification C07F9/653. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue May 29 2018 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
- What related patents are in patentsdb?
- We list 3 related publications on this page (citations in our corpus or others sharing the same primary CPC).