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US 9,840,460 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.
Claims5
A compound of:
- where:
- R11 is —CH3;
- —CH2CH(CH3)2;
- pyridine;
- pyrimidine substituted with —OH;
- dihydroimidazole;
- and phenyl optionally substituted with one or two groups selected from Cl, F, Br, —CH3, —OCH3 or —NO2;
- or a pharmaceutically-acceptable salt thereof.
5 more elements
A compound selected from:
- (a) (2R,4R)-5-(3′-chlorobiphenyl-4-yl)-4-{[N′-(2,4-dinitrophenyl)-hydrazinooxalyl]-amino}-2-hydroxypentanoic acid;
- (b) (2R,4R)-5-(3′-chlorobiphenyl-4-yl)-2-hydroxy-4-[(N′-methylhydrazinooxalyl)-amino]pentanoic acid;
- (c) (2R,4R)-5-(3′-chlorobiphenyl-4-yl)-2-hydroxy-4-[(N′-isobutylhydrazinooxalyl)-amino]pentanoic acid;
- (d) (2R,4R)-5-(3′-chlorobiphenyl-4-yl)-2-hydroxy-4-[(N′-pyridin-4-yl-hydrazino-oxalyl)-amino]pentanoic acid;
- (e) (2R,4R)-5-(3′-chlorobiphenyl-4-yl)-2-hydroxy-4-[(N′-pyridin-3-yl-hydrazino-oxalyl)-amino]pentanoic acid;
- (f) (2R,4R)-5-(3′-chlorobiphenyl-4-yl)-2-hydroxy-4-{[N′-(6-hydroxy-pyrimidin-4-yl)-hydrazinooxalyl]amino}-pentanoic acid;
- (g) (2R,4R)-5-(3′-chlorobiphenyl-4-yl)-4-{[N′-(4,5-dihydro-1H-imidazol-2-yl)-hydrazinooxalyl]-amino}-2-hydroxypentanoic acid;
- (h) (2R,4R)-5-(3′-chlorobiphenyl-4-yl)-4-{[N′-(2-chloro-phenyl)-hydrazinooxalyl]-amino}-2-hydroxypentanoic acid;
- (i) (2R,4R)-5-(3′-chlorobiphenyl-4-yl)-4-{[N′-(2-fluoro-phenyl)-hydrazinooxalyl]-amino}-2-hydroxypentanoic acid;
- (j) (2R,4R)-5-(3′-chlorobiphenyl-4-yl)-4-{[N′-(3-chloro-phenyl)-hydrazinooxalyl]-amino}-2-hydroxypentanoic acid;
- (j) (2R,4R)-5-(3′-chlorobiphenyl-4-yl)-2-hydroxy-4-[(N′-o-tolyl-hydrazinooxalyl)-amino]-pentanoic acid;
- (k) (2R,4R)-5-(3′-chlorobiphenyl-4-yl)-2-hydroxy-4-[(N′-p-tolyl-hydrazinooxalyl)-amino]-pentanoic acid;
- (l) (2R,4R)-5-(3′-chlorobiphenyl-4-yl)-4-{[N′-(4-fluoro-phenyl)-hydrazinooxalyl]-amino}-2-hydroxypentanoic acid;
- (m) (2R,4R)-5-(3′-chlorobiphenyl-4-yl)-4-{[N′-(4-chloro-phenyl)-hydrazinooxalyl]-amino}-2-hydroxypentanoic acid;
- (n) (2R,4R)-4-{[N′-(4-bromophenyl)-hydrazinooxalyl]-amino}-5-(3′-chlorobiphenyl-4-yl)-2-hydroxypentanoic acid;
- (o) (2R,4R)-5-(3′-chlorobiphenyl-4-yl)-2-hydroxy-4-{[N′-(4-methoxyphenyl)-hydrazinooxalyl]amino}pentanoic acid;
- (p) (2R,4R)-5-(3′-chlorobiphenyl-4-yl)-2-hydroxy-4-[(N′-m-tolylhydrazinooxalyl)-amino]pentanoic acid;
- (q) (2R,4R)-5-(3′-chlorobiphenyl-4-yl)-2-hydroxy-4-[(N′-phenylhydrazinooxalyl)-amino]pentanoic acid;
- or
- a pharmaceutically acceptable salt thereof.
17 more elements
Dependencies are inferred from the claim text.