Solid forms of dolutegravir salts and process for preparing thereof
Řešení se týká pevných forem solí dolutegraviru vzorce I, (4R,12aS)-N-(2,4-difluorbenzyl)-7-hydroxy-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyridol[1´,2´:4,5]pyrazinol[2,1-b][1,3]oxazin-9-karboxamidu, způsobu jejich přípravy a použití do lékové formy. Dobře využitelné jsou například pevné for...
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| creator | Dammer Ondřej Obadalová Iva Krejčík Lukáš Svobodová Jaroslava Havlíček Jaroslav |
| description | Řešení se týká pevných forem solí dolutegraviru vzorce I, (4R,12aS)-N-(2,4-difluorbenzyl)-7-hydroxy-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyridol[1´,2´:4,5]pyrazinol[2,1-b][1,3]oxazin-9-karboxamidu, způsobu jejich přípravy a použití do lékové formy. Dobře využitelné jsou například pevné formy dolutegraviru s aminy (např. diethylaminem, N,N´-dibenzylethylendiaminem, megluminem, ethanolaminem, diethanolaminem, tromethaminem, terc-butylaminem), draslíkem, hořčíkem a vápníkem. Tyto soli mohou být s výhodou použity pro zvýšení čistoty dolutegraviru a jeho stabilizaci z hlediska chemické i polymorfní čistoty.
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. |
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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.</description><language>cze ; eng</language><subject>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</subject><creationdate>2016</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20160824&DB=EPODOC&CC=CZ&NR=201599A3$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25564,76547</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20160824&DB=EPODOC&CC=CZ&NR=201599A3$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>Dammer Ondřej</creatorcontrib><creatorcontrib>Obadalová Iva</creatorcontrib><creatorcontrib>Krejčík Lukáš</creatorcontrib><creatorcontrib>Svobodová Jaroslava</creatorcontrib><creatorcontrib>Havlíček Jaroslav</creatorcontrib><title>Solid forms of dolutegravir salts and process for preparing thereof</title><description>Řešení se týká pevných forem solí dolutegraviru vzorce I, (4R,12aS)-N-(2,4-difluorbenzyl)-7-hydroxy-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyridol[1´,2´:4,5]pyrazinol[2,1-b][1,3]oxazin-9-karboxamidu, způsobu jejich přípravy a použití do lékové formy. Dobře využitelné jsou například pevné formy dolutegraviru s aminy (např. diethylaminem, N,N´-dibenzylethylendiaminem, megluminem, ethanolaminem, diethanolaminem, tromethaminem, terc-butylaminem), draslíkem, hořčíkem a vápníkem. Tyto soli mohou být s výhodou použity pro zvýšení čistoty dolutegraviru a jeho stabilizaci z hlediska chemické i polymorfní čistoty.
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.</description><subject>CHEMISTRY</subject><subject>HETEROCYCLIC COMPOUNDS</subject><subject>HUMAN NECESSITIES</subject><subject>HYGIENE</subject><subject>MEDICAL OR VETERINARY SCIENCE</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><subject>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</subject><subject>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>2016</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZHAOzs_JTFFIyy_KLVbIT1NIyc8pLUlNL0osyyxSKE7MKSlWSMxLUSgoyk9OLS4GqQOyUwsSizLz0hVKMlKLUvPTeBhY0xJzilN5oTQ3g7yba4izh25qQX58anFBYnJqXmpJvHOUkYGhqaWlo7ExYRUA09sx_A</recordid><startdate>20160824</startdate><enddate>20160824</enddate><creator>Dammer Ondřej</creator><creator>Obadalová Iva</creator><creator>Krejčík Lukáš</creator><creator>Svobodová Jaroslava</creator><creator>Havlíček Jaroslav</creator><scope>EVB</scope></search><sort><creationdate>20160824</creationdate><title>Solid forms of dolutegravir salts and process for preparing thereof</title><author>Dammer Ondřej ; Obadalová Iva ; Krejčík Lukáš ; Svobodová Jaroslava ; Havlíček Jaroslav</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_CZ201599A33</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>cze ; eng</language><creationdate>2016</creationdate><topic>CHEMISTRY</topic><topic>HETEROCYCLIC COMPOUNDS</topic><topic>HUMAN NECESSITIES</topic><topic>HYGIENE</topic><topic>MEDICAL OR VETERINARY SCIENCE</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><topic>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</topic><topic>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</topic><toplevel>online_resources</toplevel><creatorcontrib>Dammer Ondřej</creatorcontrib><creatorcontrib>Obadalová Iva</creatorcontrib><creatorcontrib>Krejčík Lukáš</creatorcontrib><creatorcontrib>Svobodová Jaroslava</creatorcontrib><creatorcontrib>Havlíček Jaroslav</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>Dammer Ondřej</au><au>Obadalová Iva</au><au>Krejčík Lukáš</au><au>Svobodová Jaroslava</au><au>Havlíček Jaroslav</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>Solid forms of dolutegravir salts and process for preparing thereof</title><date>2016-08-24</date><risdate>2016</risdate><abstract>Řešení se týká pevných forem solí dolutegraviru vzorce I, (4R,12aS)-N-(2,4-difluorbenzyl)-7-hydroxy-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyridol[1´,2´:4,5]pyrazinol[2,1-b][1,3]oxazin-9-karboxamidu, způsobu jejich přípravy a použití do lékové formy. Dobře využitelné jsou například pevné formy dolutegraviru s aminy (např. diethylaminem, N,N´-dibenzylethylendiaminem, megluminem, ethanolaminem, diethanolaminem, tromethaminem, terc-butylaminem), draslíkem, hořčíkem a vápníkem. Tyto soli mohou být s výhodou použity pro zvýšení čistoty dolutegraviru a jeho stabilizaci z hlediska chemické i polymorfní čistoty.
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.</abstract><oa>free_for_read</oa></addata></record> |
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| 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 |
| title | Solid forms of dolutegravir salts and process for preparing thereof |
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