Process for preparing novel crystalline forms of (2S)-1-[[(7R)-7-(3,4-dichlorophenyl)-4,7-dihydro-5-methylpyrazolo[1,5]pyrimidine-6-yl]carbonyl]-2-(4-fluorophenyl)pyrrolidine, novel stable forms produced therein and formulations
First Claim
1. a) The H2-1 dihydrate crystalline form of the free base of the structure b) the H2-2 dihydrate crystalline form of the free base of the structure as defined above;
- c) the N-3 anhydrate crystalline form of the free base of the structure as defined above;
or d) the MTBE solvate of the free base of the solvate as defined above.
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Accused Products
Abstract
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.
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Citations
36 Claims
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1. a) The H2-1 dihydrate crystalline form of the free base of the structure
b) the H2-2 dihydrate crystalline form of the free base of the structure as defined above; -
c) the N-3 anhydrate crystalline form of the free base of the structure as defined above;
ord) the MTBE solvate of the free base of the solvate as defined above. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36)
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Specification