SOLID FORMS OF DOLUTEGRAVIR SALTS AND A METHOD OF THEIR PREPARATION

The invention relates to solid forms of salts of dolutegravir of formula I, (4R,12aS)-N-(2,4-difluorobenzyl)-7-hydroxy-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxamide, a method of their preparation and their use in a dosage form. Fo...

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Bibliographic Details
Main Authors KREJCIK, Lukas, OBADALOVA, Iva, DAMMER, Ondrej, HAVLICEK, Jaroslav, SVOBODOVA, Jaroslava
Format Patent
LanguageEnglish
French
German
Published 20.12.2017
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:The invention relates to solid forms of salts of dolutegravir of formula I, (4R,12aS)-N-(2,4-difluorobenzyl)-7-hydroxy-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxamide, a method of their preparation and their use in a dosage form. For example, solid forms of dolutegravir with amines (e.g.diethylamine, N,N'-dibenzylethylenediamine, meglumine, ethanolamine, diethanolamine, tromethamine, tert-butylamine), potassium, magnesium and calcium are well usable. These salts can be conveniently used to increase purity of dolutegravir and its stabilization in terms of chemical as well as polymorphic purity.
Bibliography:Application Number: EP20160712715