Intervet International B.v.

Wista Laboratories Ltd.

Microbial Chemistry Research Foundation

Timo Rager

Fritz Blatter

Rolf Hilfiker

Monika Brink

Ralf Warrass

Hans Peter Niedermann

Stephan Veit

Meinrad Brenner

Guixan Hu

Guixian Hu

Tanja Schweisel

Kerstin Fleischhauer

Heinz-Joerg Wennesheimer

Heinz-Jörg Wennesheimer

Substantially pure methylthioninium chloride pentahydrate form A is prepared from methylthioninium chloride by phase equilibration of suspensions, crystallization or solvent evaporation, whereby the water content of the solvent corresponds to a water activity of at least 0.4 at 25&#xb0; C., and controlled drying of said methylthioninium chloride pentahydrate form A within its stability ranges of humidity, pressure and temperature.

Process for the preparation of substantially pure methylthionium chloride pentahydrate form A

Three dihydrate forms B, C and D and a monohydrate form E of methylthioninium chloride are described. Forms B, C, D and E can be prepared under controlled humidity and temperature from methylthioninium chloride with higher water content or conversion of a hydrate. The hydrates can be incorporated in pharmaceutical compositions.

Crystalline methylthioninium chloride hydrates

Described are methods 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, among other uses, may be used to make macrolides. Also described are 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.

Macrolide synthesis process and solid-state forms

Described are methods 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. Also described are 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.

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Basel, Switzerland

Timo Rager