EP 3256477 A1 20171220 - SOLID FORMS OF DOLUTEGRAVIR SALTS AND A METHOD OF THEIR PREPARATION
Title (en)
SOLID FORMS OF DOLUTEGRAVIR SALTS AND A METHOD OF THEIR PREPARATION
Title (de)
FESTE FORMEN VON DOLUTEGRAVIRSALZEN UND VERFAHREN ZU DEREN HERSTELLUNG
Title (fr)
FORMES SOLIDES DES SELS DE DOLUTEGRAVIR ET PROCÉDÉ DE PRÉPARATION ASSOCIÉ
Publication
Application
Priority
- CZ 20150099 A 20150213
- CZ 2016000019 W 20160212
Abstract (en)
[origin: WO2016127965A1] 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.
IPC 8 full level
C07D 498/04 (2006.01); A61K 31/5365 (2006.01); A61P 31/18 (2006.01)
CPC (source: EP)
A61P 31/18 (2017.12); C07D 498/04 (2013.01); F02C 3/10 (2013.01); F02C 3/22 (2013.01); F02C 6/04 (2013.01)
Citation (search report)
See references of WO 2016127965A1
Designated contracting state (EPC)
AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
Designated extension state (EPC)
BA ME
DOCDB simple family (publication)
WO 2016127965 A1 20160818; CZ 201599 A3 20160824; EP 3256477 A1 20171220
DOCDB simple family (application)
CZ 2016000019 W 20160212; CZ 20150099 A 20150213; EP 16712715 A 20160212