发明名称 Crystalline forms of an 8-azabicyclo[3.2.1]octane compound
摘要 The invention provides a crystalline sulfate salt of 3-endo-(8-{2-[cyclohexylmethyl-((S)-2,3-dihydroxy-propionyl)amino]ethyl}-8-aza-bicyclo[3.2.1]oct-3-yl)benzamide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with mu opioid receptor activity, and processes useful for preparing such crystalline salt forms.
申请公布号 US9290491(B2) 申请公布日期 2016.03.22
申请号 US201414333003 申请日期 2014.07.16
申请人 Theravance Biopharma R&D IP, LLC 发明人 Dalziel Sean M.;Preza Leticia M.;Rapta Miroslav;Colson Pierre-Jean
分类号 C07D221/02;C07D451/02;A61K31/46;A61K31/485;A61K45/06 主分类号 C07D221/02
代理机构 代理人 Hagenah Jeffrey A.;Saxon Roberta P.
主权项 1. A crystalline sulfate salt of 3-endo-(8-{2-[cyclohexylmethyl-((S)-2,3-dihydroxy-propionyl)amino]ethyl}-8-aza-bicyclo[3.2.1]oct-3-yl)benzamide wherein a single crystal of the sulfate salt, analyzed at a temperature of −153±1° C., is characterized by an orthorhombic unit cell with dimensions a=6.824 Å, b=16.228 Å, c=24.202 Å, α=β=γ=90°; cell volume (V) of 2680.0 Å3, and a space group of P212121(#19).
地址 South San Francisco CA US