发明名称 CRYSTALLINE FORMS OF AN ANTIVIRAL COMPOUND
摘要 Crystalline forms of the anti-HCV compound (1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-{[(1-methylcyclopropyl)sulfonyl]carbamoyl}cyclopropyl]-9-ethyl-18,18-difluoro-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide (Compound I) were prepared and characterized in the solid state:;;Also provided are processes of manufacture and methods of using the crystalline forms.
申请公布号 US2015175625(A1) 申请公布日期 2015.06.25
申请号 US201414575966 申请日期 2014.12.18
申请人 GILEAD SCIENCES, INC. 发明人 Bringley Dustin;Chan Johann;Fung Peter;Keaton Katie;Lapina Olga;Morrison Henry;Pcion Dominika
分类号 C07D498/16;A61K45/06;A61K31/4985 主分类号 C07D498/16
代理机构 代理人
主权项 1. A crystalline form of compound I: wherein, the crystalline form is: i) an ethanol solvate (Compound I Form I), characterized by an X-ray powder diffractogram comprising peaks (±0.2°) at 8.6, 11.1, and 15.5 °2θ as determined on a diffractometer using Cu—Kα radiation; ii) an ethyl acetate solvate (Compound I Form II) characterized by an X-ray powder diffractogram comprising peaks (±0.2°) at 8.7, 13.0, and 17.4 °2θ as determined on a diffractometer using Cu—Kα radiation, iii) an isopropanol solvate (Compound I Form III), characterized by an X-ray powder diffractogram comprising peaks (±0.2°) at 11.1, 12.8, and 19.7 °2θ as determined on a diffractometer using Cu—Kα radiation; iv) a dihydrate (Compound I Form IV), characterized by an X-ray powder diffractogram comprising peaks (±0.2°) at 8.7, 8.9, and 16.0 °2θ as determined on a diffractometer using Cu—Kα radiation; v) a methanol solvate (Compound I Form V), characterized by an X-ray powder diffractogram comprising peaks (+0.2°) at 6.2, 12.4, and 19.6 °2θ as determined on a diffractometer using Cu—Kα radiation; vi) anhydrous (Compound I Form VI), characterized by an X-ray powder diffractogram comprising peaks (±0.2°) at 14.6, 15.4, and 20.0 °2θ as determined on a diffractometer using Cu—Kα radiation; vii) anhydrous (Compound I Form VII), characterized by an X-ray powder diffractogram comprising peaks (±0.2°) at 6.5, 8.5, and 18.7 °2θ as determined on a diffractometer using Cu—Kα radiation; viii) anhydrous (Compound I Form VIII), characterized by an X-ray powder diffractogram comprising peaks (±0.2°) at 7.8, 8.2, and 20.2 °2θ as determined on a diffractometer using Cu—Kα radiation; ix) anhydrous (Compound I Form IX), characterized by an X-ray powder diffractogram comprising peaks (±0.2°) at 6.1, 9.5, and 19.4 °2θ as determined on a diffractometer using Cu—Kα radiation; x) hemihydrate (Compound I Form X), characterized by an X-ray powder diffractogram comprising peaks (±0.2°) at 8.0, 19.0, and 20.4 °2θ as determined on a diffractometer using Cu—Kα radiation; xi) a dihydrate (Compound I Form XI), characterized by an X-ray powder diffractogram comprising peaks (+0.2°) at 11.0, 13.9, and 20.9 °2θ as determined on a diffractometer using Cu—Kα radiation; or xii) a tetrahydrate (Compound I Form XII), characterized by an X-ray powder diffractogram comprising peaks (±0.2°) at 12.4, 14.6, and 19.3 °2θ as determined on a diffractometer using Cu—Kα radiation.
地址 Foster City CA US