Claims for Patent: 12,071,402

Summary for Patent: 12,071,402

Title:	Immunosuppressant formulations
Abstract:	The present invention relates to a solid phase pharmaceutical composition comprising one or more pharmaceutically acceptable excipients and an active pharmaceutical ingredient (“API”) which is a compound of formula A1 or A2 or a pharmacologically acceptable salt, solvate or hydrate thereof, wherein the API is not exposed to a basic compound.
Inventor(s):	Philippe Michel Rene Bouillot, Emeric Reynaud
Assignee:	Novartis AG
Application Number:	US17/230,175
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 12,071,402
Patent Claims:	1. A solid phase pharmaceutical composition comprising one or more pharmaceutically acceptable non-basic excipients and 1-{4-[1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl-benzyl}-azetidine-3-carboxylic acid or a pharmacologically acceptable salt thereof, wherein at least one of the one or more pharmaceutically acceptable non-basic excipients is glyceryl behenate, and wherein the solid phase pharmaceutical composition does not comprise magnesium stearate. 2. The composition of claim 1, wherein the composition comprises 1-{4-[1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl-benzyl}-azetidine-3-carboxylic acid and fumaric acid. 3. The composition of claim 1, wherein the composition comprises 1-{4-[1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl-benzyl}-azetidine-3-carboxylic acid and fumaric acid in the form of particles having an X90 diameter of 8 μm to 121 μm, wherein 0.25 mg of 1-{4-[1-(4-cyclohexyl-3-trifluoromethyl-benzoyloxyimino)-ethyl]-2-ethyl-benzyl}-azetidine-3-carboxylic acid is present in the composition. 4. The composition of claim 3, wherein the particles have an X90 diameter of 8 μm to 40 μm. 5. The composition of claim 1, which is in unit dosage form and complies with the US Pharmacopeia, European Pharmacopeia and Japanese Pharmacopeia harmonized content uniformity requirements as in force on 1 Jan. 2011. 6. A tablet comprising a compressed mixture comprising 1-{4-[1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl-benzyl}-azetidine-3-carboxylic acid and one or more non-basic excipients, wherein at least one of the one or more pharmaceutically acceptable non-basic excipients is glyceryl behenate, and wherein the tablet does not comprise magnesium stearate. 7. The tablet of claim 6, wherein the compressed mixture comprises 1-{4-[1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl-benzyl}-azetidine-3-carboxylic acid and fumaric acid. 8. The tablet of claim 6, wherein the tablet includes colloidal silica. 9. The tablet of claim 8, wherein the one or more non-basic excipients are chosen from binders, disintegrants, glidants, fillers, diluents, and sorbents. 10. The composition of claim 1, wherein the one or more pharmaceutically acceptable non-basic excipients are chosen from binders, disintegrants, glidants, fillers, diluents, and sorbents. 11. The tablet of claim 9, wherein the compressed mixture comprises 1-{4-[1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl-benzyl}-azetidine-3-carboxylic acid and fumaric acid in the form of particles having an X90 diameter of 8 μm to 121 μm, wherein 0.25 mg of 1-{4-[1-(4-cyclohexyl-3-trifluoromethyl-benzoyloxyimino)-ethyl]-2-ethyl-benzyl}-azetidine-3-carboxylic acid is present in the tablet. 12. The tablet of claim 11, wherein the particles have an X90 diameter of 8 μm to 40 μm.