Unsolvated and host-guest solvated crystalline forms of...

C - Chemistry – Metallurgy – 07 – K

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Details

C07K 5/027 (2006.01) A61K 38/06 (2006.01) A61P 35/00 (2006.01) C07K 5/097 (2006.01)

Patent

CA 2607257

The invention relates to unsolvated and host-guest solvated crystalline forms of (2E,4S)-4-[(N-{[(2R)-l-isopropylpiperidin-2-yl]- carbonyl}-3-methyl -L- valyl) (methyl)amino]-2,5-dimethylhex-2-enoic acid, E7974, and their therapeutic uses. Pharmaceutical compositions containing crystalline forms of E7974 and a pharmaceuticall acceptable carrier represent one embodiment of the invention. The invention also relates t methods for treating cancer, an inflammatory disorder, an autoimmune disorder, or a proliferative disorder as well as restenosis of blood vessels comprising the step of administering to a patient in need thereof a therapeutically effective amount of crystalline E7974.

Cette invention concerne des formes cristallines solvatées par complexe hôte-invité et non solvatées de (2E,4S)-4-[(N-{[(2R)-l-isopropylpiperidin-2-yl]- carbonyl}-3-methyl -L-valyl) (methyl)amino]-2,5-dimethylhex-2-enoïque acide, E7974, ainsi que leurs utilisations à des fins thérapeutiques. Cette invention concerne également des compositions pharmaceutiques contenant des formes cristallines de E7974 ainsi qu'un excipient pharmaceutiquement acceptable. Cette invention concerne également des méthodes permettant de traiter un cancer, un trouble inflammatoire, un trouble autoimmun, ou un trouble proliférant ainsi que la resténose des vaisseaux sanguins; ces méthodes consistent à administrer à un patient qui en a besoin, une quantité efficace de la forme cristalline de E7974.

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