发明名称 Crystalline form of pyrimido[6,1-A] isoquinolin-4-one compound
摘要 The current invention is directed towards a polymorph of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, in the form of a crystalline solid consisting of greater than 99% by weight of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, at least 95% in the polymorphic form of a thermodynamically stable polymorph (I) of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, wherein said polymorph is determined by single crystal X-ray structural analysis and X-ray powder diffraction pattern.;
申请公布号 US9062047(B2) 申请公布日期 2015.06.23
申请号 US201113814877 申请日期 2011.08.09
申请人 Verona Pharma plc 发明人 Walker Michael J. A.;Plouvier Bertrand M. C.;Northen Julian S.;Fernandes Philippe
分类号 A61K31/519;C07D471/04;A61K45/06 主分类号 A61K31/519
代理机构 Kilpatrick Townsend & Stockton LLP 代理人 Kilpatrick Townsend & Stockton LLP
主权项 1. A compound N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, in the form of a crystalline solid consisting of greater than 99% by weight of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, at least 95% in the polymorphic form of a thermodynamically stable polymorph (I) of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, said polymorph (I) having the following structural parameters obtained by single crystal analysis:Wavelength0.71073 ÅCrystal systemTriclinicSpace groupP-1Unit cell dimensionsa = 8.1246(4) Å α = 91.583(4)°.b = 11.4573(5) Å β = 90.299(4)°.c = 13.2398(6) Å γ = 99.628(4)°.Volume1214.56(10) Å3.Z2.
地址 London GB