UNSOLVATED AND HOST-GUEST SOLVATED CRYSTALLINE FORMS OF (2E,4S)-4-[(N-{[(2R)-1-ISOPROPYLPIPERIDIN-2-YL]-CARBONYL}-3-METHYL-L-VALYL)(METHYL)AMINO]-2,5-DIMETHYLHEX-2-ENOIC ACID AND THEIR PHARMACEUTICAL USES

摘要

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.