Novel solid forms
AssigneeHoffmann-La Roche Inc.
InventorsPascal Dott, Olaf Grassmann, Michael Kammerer, Joachim Manns, Urs Schwitter, Andrew Thomas, Nicole Wyttenbach
Life of this patent
Estimating the term…
Abstract
The instant invention relates to novel solid forms of the compound of formula (I) as well as solvates, inclusion complexes with other suitable compounds, processes for their manufacture, pharmaceutical compositions containing these solid forms, and their use as pharmaceuticals.
Claims29
A solid form of the compound of formula (I)
- or a solvate thereof;
- or an inclusion complex thereof with one or more inclusion complex forming agents;
- or a solvate of an inclusion complex thereof with one or more inclusion complex forming agents;
- having an XRPD pattern comprising at least one XRPD peak in the range of angles of diffraction 2Theta of 10.3° to 13.3°.
Amorphous Form of (1,1-dioxo-1λ6-thiomorpholin-4-yl)-{6-[3-(4-fluoro-phenyl)-5-methyl-isoxazol-4-ylmethoxy]-pyridin-3-yl}-methanone, having at least one amorphous halo and a lack of a sharp Bragg diffraction peak in the XRPD diffraction pattern.
Amorphous Form of (1,1-dioxo-1λ6-thiomorpholin-4-yl)-{6-[3-(4-fluoro-phenyl)-5-methyl-isoxazol-4-ylmethoxy]-pyridin-3-yl}-methanone, having the FTIR spectrum of FIG. 12.
Amorphous Form of (1,1-dioxo-1λ6-thiomorpholin-4-yl)-{6-[3-(4-fluoro-phenyl)-5-methyl-isoxazol-4-ylmethoxy]-pyridin-3-yl}-methanone, having the Raman spectrum of FIG.
Amorphous Form of (1,1-dioxo-1λ6-thiomorpholin-4-yl)-{6-[3-(4-fluoro-phenyl)-5-methyl-isoxazol-4-ylmethoxy]-pyridin-3-yl}-methanone, having a glass transition temperature Tg of 60° C. to 70° C.
A high-shear process for preparing a solid form of a compound of formula (I)
- having an XRPD pattern comprising at least one XRPD peak in the range of angles of diffraction 2Theta of 10.3° to 13.3° comprising:
- a) injecting a solution of an educt solid form of compound (I) in a solvent into a high-shear mixer having a rotor-stator system comprising an antisolvent;
- b) agitating the rotor-stator system of the high-shear mixer to form a suspension;
- and
- c) physically separating the solid form from the suspension.
A pharmaceutical composition comprising a solid form of a compound of formula (I) the compound of formula (I)
- or a solvate thereof;
- or an inclusion complex thereof with one or more inclusion complex forming agents;
- or a solvate of an inclusion complex thereof with one or more inclusion complex forming agents;
- having an XRPD pattern comprising at least one XRPD peak in the range of angles of diffraction 2Theta of 10.3° to 13.3°
- and a pharmaceutically acceptable excipient.
Dependencies are inferred from the claim text.