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US 9,428,457 B2Granted
Neprilysin inhibitors
AssigneeTheravance Biopharma R&D IP, LLC
InventorsErik Fenster, Melissa Fleury, Adam D. Hughes
Life of this patent
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Abstract
In one aspect, the invention relates to compounds having the formula: where R1-R5 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.
Claims4
A compound selected from:
- (a) (2R,4R)-5-(3′-Chlorobiphenyl-4-yl)-2-hydroxy-4-(2-hydroxyacetylamino)-pentanoic acid;
- (b) (2R,4R)-5-(3′-Chlorobiphenyl-4-yl)-2-hydroxy-4-(2-methoxyacetylamino)-pentanoic acid;
- (c) (2R,4R)-5-(3′-Chlorobiphenyl-4-yl)-4-(2-ethoxyacetylamino)-2-hydroxy-pentanoic acid;
- (d) (2R,4R)-5-(3′-Chlorobiphenyl-4-yl)-2-hydroxy-4-(2-isopropoxyacetylamino pentanoic acid
- (e) (2R,4R)-5-(3′-Chlorobiphenyl-4-yl)-2-hydroxy-4-[2-(pyridin-3-yloxy)-acetylamino]-pentanoic acid;
- (f) (2R,4R)-4-(2-Benzyloxy-acetylamino)-5-(3′-chlorobiphenyl-4-yl)-2-hydroxy-pentanoic acid;
- (g) (2R,4R)-5-(3′-Chlorobiphenyl-4-yl)-2-hydroxy-4-(2-phenoxyacetylamino)-pentanoic acid;
- (h) (2R,4R)-5-(3′-Chlorobiphenyl-4-yl)-2-hydroxy-4-[2-(4-hydroxyphenoxy)-acetylamino]-pentanoic acid;
- (i) (2S,4R)-5-(3′-Chlorobiphenyl-4-yl)-2-hydroxy-4-[2-(3-methoxyphenoxy)-acetylamino]-pentanoic acid;
- (j) (2S,4R)-5-(3′-Chlorobiphenyl-4-yl)-2-hydroxymethyl-4-(2-methoxy-acetylamino)-2-methylpentanoic acid;
- (k) (2S,4R)-4-(2-Benzyloxyacetylamino)-5-(3′-chlorobiphenyl-4-yl)-2-hydroxymethyl-2-methyl-pentanoic acid;
- or
- a pharmaceutically acceptable salt thereof.
10 more elements
Dependencies are inferred from the claim text.