Invention Application
US20150366872A1 CRYSTALLINE FORMS OF (2R,5S,13AR)-8-HYDROXY-7,9-DIOXO-N-(2,4,6-TRIFLUOROBENZYL)-2,3,4,5,7,9,13,13A-OCTAHYDRO-2,5-METHANOPYRIDO[1',2':4,5]PYRAZINO[2,1-B][1,3]OXAZEPINE-10-CARBOXAMIDE 有权
(2R,5S,13AR)-8-羟基-7,9-二氧代-N-(2,4,6-三氟硼酸)-2,3,4,5,7,9,13,13a-八氢噻吩的结晶形式 -2,5-甲基吡咯并[1',2':4,5]吡咯并[2,1-B] [1,3]氧杂氮杂-10-羧酰胺

  • Patent Title: CRYSTALLINE FORMS OF (2R,5S,13AR)-8-HYDROXY-7,9-DIOXO-N-(2,4,6-TRIFLUOROBENZYL)-2,3,4,5,7,9,13,13A-OCTAHYDRO-2,5-METHANOPYRIDO[1',2':4,5]PYRAZINO[2,1-B][1,3]OXAZEPINE-10-CARBOXAMIDE
  • Patent Title (中): (2R,5S,13AR)-8-羟基-7,9-二氧代-N-(2,4,6-三氟硼酸)-2,3,4,5,7,9,13,13a-八氢噻吩的结晶形式 -2,5-甲基吡咯并[1',2':4,5]吡咯并[2,1-B] [1,3]氧杂氮杂-10-羧酰胺
  • Application No.: US14745121
    Application Date: 2015-06-19
  • Publication No.: US20150366872A1
    Publication Date: 2015-12-24
  • Inventor: Ernest A. CarraIrene ChenKatie Ann KeatonVahid Zia
  • Applicant: Gilead Sciences, Inc.
  • Main IPC: A61K31/5365
  • IPC: A61K31/5365 A61K45/06 A61K9/20 C07D498/18
CRYSTALLINE FORMS OF (2R,5S,13AR)-8-HYDROXY-7,9-DIOXO-N-(2,4,6-TRIFLUOROBENZYL)-2,3,4,5,7,9,13,13A-OCTAHYDRO-2,5-METHANOPYRIDO[1',2':4,5]PYRAZINO[2,1-B][1,3]OXAZEPINE-10-CARBOXAMIDE
Abstract:
The present invention relates to crystalline forms and co-crystals of (2R,5S,13aR)-8-hydroxy-7,9-dioxo-N-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1′,2′:4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide, the pharmaceutical formulations, and the therapeutic uses thereof. The present invention also relates to novel crystalline forms of sodium (2R,5S,13aR)-7,9-dioxo-10-((2,4,6-trifluorobenzyl)carbamoyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1′,2′:4,5]pyrazino[2,1-b][1,3]oxazepin-8-olate Form I.
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