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US 10,053,417 B2Granted
Neprilysin inhibitors
AssigneeTheravance Biopharma R&D IP, LLC
InventorsErik Fenster, Melissa Fleury, Adam D. Hughes
Life of this patent
Estimating the term…
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:
- R1 is selected from the group consisting of H;
- C1-8alkyl optionally substituted with one or more fluoro atoms;
- C1-3alkylene-C6-10aryl;
- C1-3alkylene-C1-9heteroaryl;
- C3-7cycloalkyl;
- C2-3alkylene-OH;
- —[(CH2)2O]1-3CH3;
- C1-6alkylene-OC(O)R20;
- C1-6alkylene-NR21R22;
- —CH2CH(NH2)—COOCH3;
- C1-6alkylene-C(O)R23;
- C0-6alkylenemorpholine;
- C1-6alkylene-SO2—C1-6alkyl;
- R2 is —CH2OH and R3 is —CH3;
- R4 and R5 are independently selected from the group consisting of hydrogen, halo, —OH, —CH3, —OCH3, —CN, and —CF3;
- or a pharmaceutically-acceptable salt thereof.
14 more elements
(2S,4R)-5-(3′-chlorobiphenyl-4-yl)-4-formylamino-2-hydroxymethyl-2-methyl-pentanoic acid or a pharmaceutically-acceptable salt thereof.
Dependencies are inferred from the claim text.