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US 2018/0105503 A1Published application
Neprilysin inhibitors
AssigneeTheravance Biopharma R&D IP, LLC
InventorsMelissa Fleury, Roland Gendron, Adam D. Hughes, Jane Schmidt
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Abstract
In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, X, R4, R5, and R6 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 process and intermediates for preparing such compounds.
Claims5
1-22. (canceled)
23:
- A compound of:
- (a) (2R,3R)-3-{[3-(6-bromo-pyridin-3-ylmethyl)-7-methyl-2-propyl-3H-benzoimidazole-5-carbonyl]-amino}-2-hydroxy-4-phenyl-butyric acid;
- (b) (2R,3R)-2-hydroxy-3-[(7-methyl-2-propyl-3-pyridin-3-ylmethyl-3H-benzoimidazole-5-carbonyl)-amino]-4-phenyl-butyric acid;
- (c) (2R,3R)-2-hydroxy-3-[(7-methyl-2-propyl-3-pyridin-3-ylmethyl-3H-benzoimidazole-5-carbonyl)-amino]-4-phenyl-butyric acid ethyl ester;
- (d) (2R,3R)-3-[(3-carboxymethyl-7-methyl-2-propyl-3H-benzoimidazole-5-carbonyl)-amino]-2-hydroxy-4-phenyl-butyric acid;
- (e) (2R,3R)-2-hydroxy-3-{[3-(2-methoxy-benzyl)-7-methyl-2-propyl-3H-benzoimidazole-5-carbonyl]-amino}-4-phenyl-butyric acid;
- (f) (2R,3R)-2-hydroxy-3-{[3-(4-methoxy-benzyl)-7-methyl-2-propyl-3H-benzoimidazole-5-carbonyl]-amino}-4-phenyl-butyric acid;
- (g) (2R,3R)-3-[(3-carbamoylmethyl-7-methyl-2-propyl-3H-benzoimidazole-5-carbonyl)-amino]-2-hydroxy-4-phenyl-butyric acid;
- (h) (2R,3R)-3-[(7-chloro-2-ethyl-3H-benzoimidazole-5-carbonyl)-amino]-2-hydroxy-4-phenyl-butyric acid;
- (i) (2R,3R)-3-[(7-chloro-2-ethyl-1H-benzoimidazole-5-carbonyl)-amino]-2-hydroxy-4-phenyl-butyric acid ethyl ester;
- (j) (2R,3R)-3-[(3H-benzotriazole-5-carbonyl)-amino]-2-hydroxy-4-phenyl-butyric acid;
- (k) (2R,3R)-3-[(3H-benzotriazole-5-carbonyl)-amino]-2-hydroxy-4-phenyl-butyric acid ethyl ester;
- (l) (2R,3R)-3-[(7-chloro-3H-benzotriazole-5-carbonyl)-amino]-2-hydroxy-4-phenyl-butyric acid;
- (m) (2R,3R)-3-[(7-chloro-3H-benzotriazole-5-carbonyl)-amino]-2-hydroxy-4-phenyl-butyric acid ethyl ester;
- (n) (2R,3R)-2-hydroxy-3-[(7-methyl-3H-benzotriazole-5-carbonyl)-amino]-4-phenyl-butyric acid;
- (o) (2R,3R)-3-[(7-fluoro-1H-benzotriazole-5-carbonyl)-amino]-2-hydroxy-4-phenyl-butyric acid;
- or
- a pharmaceutically acceptable salt thereof.
15 more elements
24:
- A pharmaceutical composition comprising the compound of claim 23 and a pharmaceutically acceptable carrier.
25:
- The pharmaceutical composition of claim 24, further comprising an AT1 receptor antagonist.
26:
- A method for treating hypertension, heart failure, or renal disease, comprising administering to a patient a therapeutically effective amount of the compound of claim 23.