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

US11718591B2 · kind B2 · utility

Assignee

• Theravance Biopharma R&D IP, LLC · US

Inventors

• Adam D. Hughes · Rue de l'Église, US
• Melissa Fleury · San Mateo, US
• Miroslav Rapta · Redwood City, US
• Venkat R. Thalladi · Foster City, US
• Gene Timothy Fass · San Francisco, US
• Michael Simeone · San Francisco, US
• R. Michael Baldwin · San Mateo, US
• David L. Bourdet · Millbrae, US

Key dates

• Filing date: Dec 14, 2021
• Grant date: Aug 8, 2023
• Expiry date: Dec 14, 2041

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07B2200/13
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

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.