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

US10472335B2 · 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
• R. Michael Baldwin · San Mateo, US
• David L. Bourdet · Millbrae, US

Key dates

• Filing date: Sep 10, 2018
• Grant date: Nov 12, 2019
• Expiry date: Sep 10, 2038

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.