Stable solid dispersion of a B-RAF kinase dimer inhibitor, methods of preparation, and uses therefor
AssigneeBeiGene, Ltd.
InventorsGuoliang Zhang, Changyou Zhou, Huangbin Sun
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Abstract
Disclosed herein is a physically stable solid dispersion comprising Compound 1, i.e., the B-RAF kinase dimer inhibitor 1-((1S, 1aS, 6bS)-5-((7-oxo-5, 6, 7, 8-tetrahydro-1, 8-naphthyridin-4-yl)oxy)-1a,6b-dihydro-1H-cyclopropa [b] benzofuran-1-yl)-3-(2, 4, 5-trifluorophenyl) urea and a specific stabilizing polymer, the method for preparing the same, and the uses of the solid dispersion. Also disclosed herein is the crystalline form of Compound 1.
Claims4
A stable amorphous solid dispersion comprising Compound 1 and a stabilizing polymer, wherein Compound 1 is 1-((1S,1aS,6bS)-5-((7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-4-yl)oxy)-1a,6b-dihydro-1H-cyclopropa[b]benzofuran-1-yl)-3-(2,4,5-trifluorophenyl) urea, and Compound 1 is molecularly dispersed within a polymer matrix formed by the stabilizing polymer in its solid state, wherein the stabilizing polymer is hydroxypropyl methylcellulose acetate succinate, type LF (HPMCAS-LF), and the weight ratio of Compound 1 in the form of freebase and the polymer is 1:4, and wherein HPMCAS-LF has 5.0-9.0% of acetyl group and 14.0-18.0% of succinoyl group.
Dependencies are inferred from the claim text.