Crystalline(2S,4R)-5-(5′-chloro-2′-fluoro-[1,1′-bipheny]-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.
Claims15
A method for treating hypertension, heart failure, or renal disease in a patient in need thereof, the method comprising administering a crystalline free acid form of (2S,4R)-5-(5′-chloro-2′-fluoro-[1,1′-biphenyl]-4-yl)-2-(ethoxymethyl)-4-(3-hydroxyisoxazole-5-carboxamido)-2-methylpentanoic acid (Compound I′) to the patient.
A method of treating hypertension, heart failure, or renal disease in a renally-impaired patient, the method comprising administering a therapeutically effective amount of a crystalline free acid form of (2S,4R)-5-(5′-chloro-2′-fluoro-[1,1′-biphenyl ]-4-yl)-2-(ethoxymethyl)-4-(3-hydroxyisoxazole-5-carboxamido)-2-methylpentanoic acid (Compound I′) to the patient.
A method of increasing atrial natriuretic peptide (ANP) or cyclic guanosine monophosphate (cGMP) levels in a human for at least 24 hours, the method comprising administering to the human an ANP or cGMP-increasing amount of a crystalline free acid form of (2S,4R)-5-(5′-chloro-2′-fluoro-[1,1′-biphenyl]-4-yl)-2-(ethoxymethyl)-4-(3-hydroxyisoxazole-5-carboxamido)-2-methylpentanoic acid (Compound I′).
Dependencies are inferred from the claim text.