Traitement en cours

Veuillez attendre...

Paramétrages

Paramétrages

Aller à Demande

1. WO2020115213 - SOLVATE D'UN INHIBITEUR SÉLECTIF DE JAK1

Note: Texte fondé sur des processus automatiques de reconnaissance optique de caractères. Seule la version PDF a une valeur juridique

[ EN ]

CLAIMS

1) A solvate comprising upadacitinib and acetic acid.

2) Upadacitinib acetic acid solvate of claim 1, characterized by the chemical structure according to Formula (II)


(P),

wherein n is in the range of from 0.8 to 1.2.

3) Upadacitinib acetic acid solvate (Form BHOAC) of claim 1 or 2, characterized by having a powder X-ray diffractogram comprising reflections at 2-Theta angles of (11.3 ± 0.2)°, (16.9 ± 0.2)° and (27.0 ± 0.2)°, when measured at a temperature in the range of from 20 to 30 °C with Cu-Kalphai,2 radiation having a wavelength of 0.15419 nm.

4) Upadacitinib acetic acid solvate (Form BHOAC) of claim 3, characterized by having a powder X-ray diffractogram comprising additional reflections at 2-Theta angles of (9.8 ± 0.2)° and (13.1 ± 0.2)°, when measured at a temperature in the range of from 20 to 30 °C with Cu-Kalphai,2 radiation having a wavelength of 0.15419 nm.

5) Upadacitinib acetic acid solvate of claim 1, characterized by the chemical structure according to Formula (II)

wherein n is in the range of from 1.8 to 2.2.

6) Upadacitinib acetic acid solvate (Form AHOAC) of claim 1 or 5, characterized by having a powder X-ray diffractogram comprising reflections at 2-Theta angles of (3.3 ± 0.2)°, (11.0 ± 0.2)° and (27.3 ± 0.2)°, when measured at a temperature in the range of from 20 to 30 °C with Cu-Kalphai,2 radiation having a wavelength of 0.15419 nm.

7) Upadacitinib acetic acid solvate of claim 6 characterized by having a powder X-ray diffractogram comprising additional reflections at 2-Theta angles of (17.7 ± 0.2)° and (22.4 ± 0.2)°, when measured at a temperature in the range of from 20 to 30 °C with Cu-Kalphai,2 radiation having a wavelength of 0.15419 nm.

8) Use of the upadactinib acetic acid solvate (Form AHOAC) as defined in any one of claims 5 to 7 for the preparation of the upadacitinib acetic acid solvate (Form BHOAC) as defined in any one of claims 2 to 4.

9) Use of the upadacitinib acetic acid solvate as defined in any one of claims 1 to 7 for the preparation of a pharmaceutical composition.

10) A pharmaceutical composition comprising the upadacitinib acetic acid solvate as defined in any one of claims 1 to 4 and at least one pharmaceutically acceptable excipient.

11) The pharmaceutical composition of claim 10, wherein the at least one pharmaceutically acceptable excipient comprises a release control polymer.

12) The pharmaceutical composition of claim 10 or 11, wherein the at least one pharmaceutically acceptable excipient does not comprise a pH-modifier.

13) The pharmaceutical composition as defined in any one of claims 10 to 12, wherein the pharmaceutical composition is an oral solid dosage form.

14) The pharmaceutical composition as defined in any one of claims 10 to 13, comprising 15 or 30 mg of the upadacitinib acetic acid solvate (Form BHOAC) as defined in any one of claims 1 to 4, calculated as upadacitinib.

15) The pharmaceutical composition as defined in any one of claims 10 to 14 for use in the treatment of rheumatoid arthritis.