US 12,465,614 B2
Budesonide 21-phosphate salts and pharmaceutical compositions containing the same
Giuseppe Caliendo, Marigliano (IT); Giuseppe Cirino, Naples (IT); Ferdinando Fiorino, Benevento (IT); Francesco Frecentese, Aversa (IT); Marcelo Nicolas Muscarà, Campinas (BR); Elisa Perissutti, Venafro (IT); Antonio Petti, Battipaglia (IT); Fiorentina Roviezzo, Bonea (IT); Vincenzo Santagada, Naples (IT); Beatrice Severino, Mugnano di Napoli (IT); and Elisa Magli, Portici (IT)
Assigned to GENETIC S.P.A., Castel San Giorgio (IT)
Appl. No. 17/906,997
Filed by GENETIC S.P.A., Castel San Giorgio (IT)
PCT Filed Mar. 25, 2021, PCT No. PCT/EP2021/057780
§ 371(c)(1), (2) Date Sep. 22, 2022,
PCT Pub. No. WO2021/191366, PCT Pub. Date Sep. 30, 2021.
Claims priority of application No. 102020000006442 (IT), filed on Mar. 27, 2020.
Prior Publication US 2023/0115869 A1, Apr. 13, 2023
Int. Cl. A61K 31/665 (2006.01); A61K 31/167 (2006.01); A61P 11/06 (2006.01); A61P 11/08 (2006.01); C07C 231/12 (2006.01); C07C 233/25 (2006.01); C07J 71/00 (2006.01)
CPC A61K 31/665 (2013.01) [A61K 31/167 (2013.01); A61P 11/06 (2018.01); A61P 11/08 (2018.01); C07C 231/12 (2013.01); C07C 233/25 (2013.01); C07J 71/0026 (2013.01); C07B 2200/13 (2013.01)] 20 Claims
 
1. A salt of budesonide 21-phosphate with a β2 adrenergic agonist, wherein the β2 adrenergic agonist is Formoterol, which is in crystalline form IV characterized by an X-ray powder diffraction spectrum, which is obtained by using CuKα radiation and represented by °2θ angle, having characteristic peaks at about 5.82, 8.21, 11.67, 13.02, 13.54, 14.17, 14.87, 16.40, 16.92, 18.39, 19.69, 20.15, 20.65, 21.41, 22.28, 23.41, 23.69, 24.16, 24.77, 25.27, 26.41, 27.38, 27.84, 28.58, 30.15, 31.69, 33.58, 34.41, 35.47, 36.02, 37.59, 38.63 2theta±0.20 degrees.