Macrolide synthesis process and solid-state forms

US8263753B2 · kind B2 · utility

Assignee

• INTERVET INTERNATIONAL B.V · NL

Inventors

• Monika Brink · Ingelheim am Rhein, DE
• Hans Peter Niedermann · Bubenheim, DE
• Tanja Schweisel · Arbach, DE
• Stephan Veit · Budenheim, DE
• Kerstin Fleischhauer · Wiesbaden, DE
• Ralf Warrass · Alzey, DE
• Heinz-Jorg Wennesheimer · Bingen, DE

Key dates

• Filing date: Jul 30, 2010
• Grant date: Sep 11, 2012
• Expiry date: Jul 30, 2030

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P31/04
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

This invention relates to a method for making macrolides, and, in particular, a method for making optionally substituted 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide and derivatives thereof, as well as uses of macrolides to make medicaments, methods of treatment using macrolides, and methods for making intermediates that, inter alia, may be used to make macrolides. This invention also relates to solvated and non-solvated crystalline forms of 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide, as well as methods for making such crystalline forms, medicaments comprising (or derived from) such crystalline forms, methods for making medicaments comprising (or derived from) such crystalline forms, methods of treatment using such crystalline forms, and kits comprising such crystalline forms.