Back to results
US 2024/0199585 A1Published application
Solid forms of (3r)-n-[2-cyano-4-fluoro-3-(3-methyl-4-oxo-quinazolin-6-yl)oxy-phenyl]-3-fluoro-pyrrolidine-1-sulfonamide
AssigneeHoffmann-La Roche Inc.
InventorsBengt ÅSLUND, Manuel KONRATH, Ulf Goeran LARSSON, Johan Salman MALMBERG, Alexander Bogdan Emil MINIDIS, Isabelle Georgette Huguette MODOLO-CHELLAT
Life of this patent
Estimating the term…
Abstract
The present invention provides solid forms of (3R)-N-[2-cyano-4-fluoro-3-(3-methyl-4-oxo-quinazolin-6-yl)oxy-phenyl]-3-fluoro-pyrrolidine-1-sulfonamide and solvates thereof, as well as therapeutic uses and processes to manufacture the new solid forms.
Claims23
A solid form of a compound of formula (I):
- wherein the solid form is crystalline polymorphic Form A characterized by a X-ray powder diffraction pattern comprising a peak at an angle of diffraction at about 10.22 degrees 2-theta and at least one additional peak expressed in values of degrees 2-theta at approximately 7.90, 8.92, 11.58, 12.16, 12.66, 14.66, 17.50, 18.06, 19.64 or 20.54.
A solid form of a compound of formula (I), or a solvate thereof:
- wherein the solid form is amorphous.
-19. (canceled)
-22. (canceled)
A process for the preparation of a compound of formula (I):
- comprising the following steps:
- (a) reacting a compound of formula (A1):
- with a compound of formula (A2)
- in presence of suitable base in presence of a suitable solvent, to arrive at a compound of formula (B1)
- (b) reacting the compound of formula (B1) with a compound of formula (B2):
- in presence of a suitable base in presence of a suitable solvent to arrive at a compound of formula (I):
- (c) purifying by filtration a suspension of the crude product of the compound of formula (I) in a suitable solvent and a suitable acid to remove substantial amounts of dimer sulfate and to obtain a filtrate comprising substantial amounts of the compound of formula (I).
4 more elements
(canceled)
Dependencies are inferred from the claim text.