Claims for Patent: 10,183,020

Summary for Patent: 10,183,020

Title:	Pharmaceutical compositions comprising AZD9291
Abstract:	The present invention relates to pharmaceutical compositions suitable for oral administration, and more particularly to pharmaceutical compositions, including pharmaceutical tablet compositions, containing N-(2-{2-dimethylaminoethyl-methyl-amino}-4-methoxy-5-{[4-(1-methylindol-3- -yl)pyrimidin-2-yl]amino}phenyl)prop-2-enamide ("AZD9291") or a pharmaceutically acceptable salt thereof, wherein such compositions comprise a certain amount of microcrystalline cellulose and at least one other pharmaceutical diluent.
Inventor(s):	Finnie; Cindy (Macclesfield, GB), Raw; Steven Anthony (Macclesfield, GB), Wilson; David (Macclesfield, GB)
Assignee:	AstraZeneca AB (Sodertalje, SE)
Application Number:	15/109,170
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 10,183,020
Patent Claims:	1. A pharmaceutical composition comprising: (a) from 2 to 70 parts of the mesylate salt of N-(2-{2-dimethylaminoethyl-methylamino}-4-methoxy-5-{[4-(1-methylindo-3-y- l)pyrimidin-2-yl]amino}phenyl)prop-2-enamide; (b) from 5 to 96 parts of two or more pharmaceutical diluents; (c) from 2 to 15 parts of one or more pharmaceutical disintegrants; (d) from 0 to 0.75 parts of one or more pharmaceutical solubilising agents; and (e) from 0 to 3 parts of one or more pharmaceutical lubricants; wherein all parts are by weight and the sum of the parts (a)+(b)+(c)+(d)+(e)=100; and wherein one of the two or more pharmaceutical diluents is microcrystalline cellulose wherein the microcrystalline cellulose makes up from 7 to 30 wt % of the two or more pharmaceutical diluents (b). 2. The pharmaceutical composition according to claim 1 wherein the pharmaceutical composition comprises from 1 to 2.5 parts of the one or more pharmaceutical lubricants (e). 3. The pharmaceutical composition according to claim 2 wherein the one or more pharmaceutical lubricants (e) comprises sodium stearyl fumarate and/or one or more behenate esters of glycerine. 4. The pharmaceutical composition according to claim 3, wherein the pharmaceutical composition comprises from 2 to 10 parts of the one or more pharmaceutical disintegrants (c). 5. The pharmaceutical composition according to claim 4 wherein the one or more pharmaceutical disintegrants (c) comprises low-substituted hydroxypropyl cellulose. 6. The pharmaceutical composition according to claim 5, wherein the pharmaceutical composition comprises from 0 to 0.25 parts of one or more pharmaceutical solubilising agents (d). 7. The pharmaceutical composition according to claim 6, wherein the pharmaceutical composition comprises from 5 to 50 parts of the mesylate salt of N-(2-{2-dimethylaminoethyl-methylamino}-4-methoxy-5-{[4-(1-methyl- indol-3-yl)pyrimidin-2-yl]amino}phenyl)prop-2-enamide. 8. A method of treating cancer in a patient in need thereof, which method comprises the oral administration to the patient of an effective amount of the pharmaceutical composition as claimed in claim 1. 9. A pharmaceutical tablet comprising the pharmaceutical composition as claimed in claim 1. 10. A pharmaceutical tablet comprising a tablet core wherein the tablet core comprises the pharmaceutical composition as claimed in claim 1, wherein the tablet core has a coating. 11. A method of treating cancer in a patient in need thereof, which method comprises the oral administration of an effective number of the pharmaceutical tablet(s), as claimed in claim 9, to the patient. 12. The method of claim 8, wherein the cancer is non-small cell lung cancer. 13. The method of claim 11, wherein the cancer is non-small cell lung cancer. 14. The pharmaceutical composition as claimed in claim 6, wherein a pharmaceutical solubilising agent (d) is not present. 15. The pharmaceutical composition as claimed in claim 7, wherein the pharmaceutical composition comprises from 7 to 30 parts of the mesylate salt of N-(2-{2-dimethylaminoethyl-methylamino}-4-methoxy-5-{[4-(1-methyl- indo-3-yl)pyrimidin-2-yl]amino}phenyl)prop-2-enamide. 16. A pharmaceutical composition as claimed in claim 1 comprising: (a) from 5 to 50 parts of the mesylate salt of N-(2-{2-dimethylaminoethyl-methylamino}-4-methoxy-5-{[4-(1-methylindol-3-- yl)pyrimidin-2-yl]amino}phenyl)prop-2-enamide; (b) from 5to 96 parts of two or more pharmaceutical diluents; (c) from 2 to 15 parts of one or more pharmaceutical disintegrants; (d) from 0 to 0.75 parts of one or more pharmaceutical solubilising agents; and (e) from 0.5 to 3 parts of one or more pharmaceutical lubricants; wherein all parts are by weight and the sum of the parts (a)+(b)+(c)+(d)+(e)=100; wherein one of the two or more pharmaceutical diluents is microcrystalline cellulose wherein the microcrystalline cellulose makes up from 7 to 30 wt % of the two or more pharmaceutical diluents (b) and wherein in addition to microcrystalline cellulose, the other pharmaceutical diluent(s) within the two or more pharmaceutical diluents is/are selected from cellulose acetate, erythritol, ethylcellulose, fructose, inulin, isomalt, lactitol, lactose, maltitol, maltodextrin, maltose, mannitol, polydextrose, polyethylene glycol, pullulan, simethicone, sodium chloride, sorbitol, starch, sucrose, trehalose and xylitol; and wherein the one or more pharmaceutical disintegrants (c) comprises low-substituted hydroxypropyl cellulose and wherein the one or more pharmaceutical lubricants (e) comprises sodium stearyl fumarate and/or one or more behenate esters of glycerine. 17. A method of treating cancer in a patient in need thereof, which method comprises the oral administration to the patient of an effective amount of the pharmaceutical composition as claimed in claim 16. 18. A pharmaceutical tablet comprising the pharmaceutical composition as claimed in claim 16. 19. A pharmaceutical tablet comprising a tablet core wherein the tablet core comprises the pharmaceutical composition as claimed in claim 16, wherein the tablet core has a coating. 20. A method of treating cancer in a patient in need thereof, which method comprises the oral administration of an effective number of the pharmaceutical tablet(s), as claimed in claim 19, to the patient. 21. A pharmaceutical composition according to claim 1 comprising: (a) from 7 to 25 parts of the mesylate salt of N-(2-{2-dimethylaminoethyl-methylamino}-4-methoxy-5-{[4-(1-methylindol-3-- yl)pyrimidin-2-yl]amino}phenyl)prop-2-enamide; (b) from 55 to 85 parts of two pharmaceutical diluents; (c) from 2 to 8 parts of a pharmaceutical disintegrant; and (e) from 1.5 to 2.5 parts of a pharmaceutical lubricant; wherein a pharmaceutical solubilising agent (d) is not present; wherein all parts are by weight and the sum of the parts (a)+(b)+(c)+(e)=100; and wherein one of the two pharmaceutical diluents is microcrystalline cellulose wherein the microcrystalline cellulose makes up from 7 to 30 wt % of the two pharmaceutical diluents (b). 22. A pharmaceutical composition according to claim 21 comprising: (a) from 7 to 25 parts of the mesylate salt of N-(2-{2-dimethylaminoethyl-methylamino}-4-methoxy-5-{[4-(1-methylindol-3-- yl)pyrimidin-2-yl]amino}phenyl)prop-2-enamide; (b) from 55 to 85 parts of two pharmaceutical diluents, wherein the pharmaceutical diluents are microcrystalline cellulose and mannitol; (c) from 2 to 8 parts of a pharmaceutical disintegrant, wherein the pharmaceutical disintegrant is low-substituted hydroxypropyl cellulose; and (e) from 1.5 to 2.5 parts of a pharmaceutical lubricant, wherein the pharmaceutical lubricant is sodium stearyl fumarate; wherein a pharmaceutical solubilising agent (d) is not present; wherein all parts are by weight and the sum of the parts (a)+(b)+(c)+(e)=100; and wherein the microcrystalline cellulose makes up from 7 to 30 wt % of the two pharmaceutical diluents (b). 23. A pharmaceutical composition according to claim 22 comprising: (a) about 19 parts of the mesylate salt of N-(2-{2-dimethylaminoethyl-methylamino}-4-methoxy-5-{[4-(1-methylindol-3-- yl)pyrimidin-2-yl]amino}phenyl)prop-2-enamide; (b) about 59 parts of mannitol; (c) about 15 parts of microcrystalline cellulose; (d) about 5 parts of low-substituted hydroxypropyl cellulose; and (e) about 2 parts of sodium stearyl fumarate.