Neprilysin inhibitors
AssigneeTheravance Biopharma R&D IP, LLC
InventorsMelissa Fleury, Adam D. Hughes
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Abstract
In one aspect, the invention relates to compounds having the formula: where X, Ra, Rb, R2, and R7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds 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.
Claims20
A method of treating a cardiovascular disease in a subject in need thereof, comprising administering to the subject an effective amount of a compound of formula V:
- or a pharmaceutically acceptable salt thereof, wherein:
- Ra is selected from Cl and F and Rb is H;
- or Ra is H and Rb is selected from Cl, F, —CH3, and —CN;
- or Ra is F and Rb is Cl;
- R2 is selected from H, —C1-6 alkyl, —(CH2)2-3ORe, and —(CH2)2-3NReRe;
- R3 is selected from —OH, —OCH3, —OCH2CH3, and —C1-4alkyl;
- R7 is selected from H, —C1-6alkyl, —[(CH2)2O]1-3CH3, —CHRcOC(O)—C1-4alkyl, —CH2OC(O)CHRd—NH2, —CH2OC(O)CHRd—NHC(O)O—C1-6alkyl, —CHRcOC(O)O—C2-4alkyl, —CHRcOC(O)O-cyclohexyl, —CH2CH(NH2)C(O)OCH3, —C2-4alkylene-N(CH3)2, —C0-6 alkylenemorpholinyl, and
- Rc is selected from H and —C1-3 alkyl;
- Rd is selected from H, —CH3, —CH(CH3)2, phenyl, and benzyl;
- and
- each Re is independently selected from H and —CH3.
Dependencies are inferred from the claim text.