Patent ID: 6982276
Filing Date: 2006-01-03
Classification: A61P,C07D

Abstract:
1. A method for treating cancer or other proliferative diseases in a mammal, comprising: a) preparing a pharmaceutical composition comprising an active ingredient and one or more pharmaceutically acceptable carriers, excipients or diluents thereof; wherein the active ingredient comprises an effective amount of a crystalline material of an epothilone analog represented by formula I: wherein the crystalline material is Form A and optionally Form B; and b) administrating the pharmaceutical composition to the mammal; wherein the Form A is characterized by: i) unit cell parameters approximately equal to the following: and characteristic peaks in the powder x-ray diffraction pattern at values of two theta (CuKα λ=1.5406 Å at 22° C.): 5.69, 6.76, 8.38, 11.43, 12.74, 13.62, 14.35, 15.09, 15.66, 16.43, 17.16, 17.66, 18.31, 19.03, 19.54, 20.57, 21.06, 21.29, 22.31, 23.02, 23.66, 24.18, 14.98, 25.50, 26.23, 26.23, 26.46, 27.59, 28.89, 29.58, 30.32, 31.08 and 31.52; and/or ii) a powder x-ray diffraction substantially as shown in iii) a solubility in water of 0.1254, a solubility in a 3% aqueous solution of polysorbate 80 of 0.2511, a melting point with decomposition between 182-185° C. and a heat of solution of 20.6 kJ/mol; and wherein the Form B, if present, is characterized by: i) unit cell parameters approximately equal to the following: and characteristic peaks in the powder x-ray diffraction pattern at values of two theta (CuKα λ=1.5406 Å at 22° C.): 6.17, 10.72, 12.33, 14.17, 14.93, 15.88, 16.17, 17.11, 17.98, 19.01, 19.61, 20.38, 21.55, 21.73, 22.48, 23.34, 23.93, 24.78, 25.15, 25.90, 26.63, 27.59, 28.66, 29.55, 30.49 and 31.22; and/or ii) a powder x-ray diffraction substantially as shown in iii) a solubility in water of 0.1907, a solubility in a 3% aqueous solution of polysorbate 80 of 0.5799, a melting point with decomposition between 191-199° C. and a heat of solution of 9.86 kJ/mol.