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 |