Crystalline (2S,4R)-5-(5'-chloro-2'-fluoro-[1,1'-biphenyl]-4-yl)-2-(ethoxymethyl)-4-(3-hydroxyisoxazole-5-carboxamido)-2-methylpentanoic acid and uses thereof
AssigneeTheravance Biopharma R&D IP, LLC
InventorsAdam D. Hughes, Melissa Fleury, Miroslav Rapta, Venkat R. Thalladi, R. Michael Baldwin, David L. Bourdet
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Abstract
In one aspect, the invention relates to a crystalline form of the structure: or a pharmaceutically acceptable salt thereof, having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising this crystalline form; methods of using this crystalline form and its soluble form (I); and processes for preparing soluble (I) and crystalline (I′) forms.
Claims63
A method of inhibiting neprilysin activity in a renally-impaired patient in need thereof, the method comprising administering to the renally-impaired patient Compound I having the structure:
- or a pharmaceutically acceptable salt thereof, wherein Compound I is administered orally once-daily at a dose of 10 mg to 600 mg.
A method of inhibiting neprilysin activity in a renally-impaired patient in need thereof, the method comprising administering to the renally-impaired patient a crystalline free acid form of a compound having the structure:
A method of treating heart failure in a renally-impaired patient, the method comprising administering a therapeutically effective amount of Compound I having the structure:
- or a pharmaceutically acceptable salt thereof, to the renally-impaired patient once-daily.
A method of treating heart failure in a renally-impaired patient, the method comprising administering a therapeutically effective amount of a crystalline free acid form of a compound having the structure:
- to the renally-impaired patient once-daily.
Dependencies are inferred from the claim text.