C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 487/04 (2006.01) A61K 31/519 (2006.01) A61P 9/06 (2006.01)
Patent
CA 2589468
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-5~methylpyrazolo[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.
L'invention concerne un procédé de préparation de nouvelles formes cristallines, à savoir un procédé de préparation sélective et uniforme de la forme cristalline dihydrate H2-1, de la forme cristalline dihydrate H2-2, de la forme cristalline anhydrate N-3 et de la forme cristalline solvate MTBE du composé Ikur (2S)-1-[[(7R)-7-(3,4-dichlorophényl)-4,7-dihydro-5-méthylpyrazolo[1,5]pyrimidine-6-yl]carbonyl]-2-(4-fluorophényl)pyrrolidine. Ce procédé consiste à préparer des formes H2-1 et H2-2 utilisées dans la préparation de la forme anhydrate N-3 qui est particulièrement stable et qui possède des propriétés de fluidité adaptées ainsi que la dimension de particule souhaitée. L'invention porte également sur de nouvelles formes de dihydrate H2-1 et H2-2, sur la forme anhydrate N-3 et sur la forme solvate MTBE du composé Ikur décrit précédemment, sur des compositions pharmaceutiques renfermant ces formes nouvelles et sur un procédé de prévention ou de traitement des arythmies, y compris de la fibrillation auriculaire et des états liés à Ikur, au moyen de ces nouvelles formes.
Burton Lori S.
Dimarco John D.
Gandhi Rajesh Babulal
Gougoutas Jack Z.
Lai Chiajen
Bristol-Myers Squibb Company
Gowling Lafleur Henderson Llp
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