公开(公告)号：EP1814884A1

公开(公告)日：2007-08-08

申请号：EP05851950.5

申请日：2005-11-22

申请人： Bristol-Myers Squibb Company

发明人： WANG, Xuebao ,  LAI, Chiajen ,  SOUNDARARAJAN, Nachimuthu ,  NGUYEN, Nina ,  YING, Weiming ,  BURTON, Lori, S. ,  GANDHI, Rajesh, Babulal ,  RAGHAVAN, Krishnaswamy Srinivas ,  WEST, Ronald, C. ,  ZHOU, Yuji, Simon ,  YAN, Lin ,  YIN, Xiaotian ,  DIMARCO, John, D. ,  GOUGOUTAS, Jack, Z.

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P9/06

CPC分类号： C07D487/04

摘要： A process is provided for preparing novel crystalline forms, namely selectively and consistently preparing the H2-1 dihydrate crystalline form, the H2-2 dihydrate crystalline form, the N-3 anhydrate crystalline form and the MTBE solvate crystalline form of the IKur compound (2S)-1-[[(7R)-7-(3,4-dichlorophenyl)-4,7-dihydro-5­methylpyrazolo[1,5]pyrimidine-6-yl]carbonyl]-2-(4-fluorophenyl)pyrrolidine. The process includes preparation of the H2-1 and H2-2 forms which are used in preparing the N-3 anhydrate form which is particularly stable and has suitable flow properties and desired particle size. Novel H2-1 dihydrate and H2-2 dihydrate forms, the N-3 anhydrate form and the MTBE solvate form of the above IKur compound, pharmaceutical compositions containing such novel forms and a method for preventing or treating arrhythmias including atrial fibrillation and IKur related conditions employing such novel forms are also provided.