Claims for Patent: 10,391,094

Summary for Patent: 10,391,094

Title:	Compositions and methods for treating myelofibrosis
Abstract:	Provided herein are compositions and methods for treating myelofibrosis in a subject. The methods comprise administering to the subject an effective amount of compound which is which is N-tert-butyl-3-[(5-methyl-2-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}pyr- imidin-4-yl)amino]benzenesulfonamide or a pharmaceutical salt thereof or a hydrate thereof.
Inventor(s):	Jayan; Arvind (La Jolla, CA), Cacace; Janice (Miami, FL)
Assignee:	Impact Biomedicines, Inc. (Summit, NJ)
Application Number:	13/888,096
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 10,391,094
Patent Claims:	1. A capsule comprising a formulation comprising (i) a compound that is N-tert-butyl-3-[(5-methyl-2-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}pyr- imidin-4-yl)amino]benzenesulfonamide dihydrochloride monohydrate, (ii) a microcrystalline cellulose, and (iii) sodium stearyl fumarate, wherein: the weight ratio of N-tert-butyl-3-[(5-methyl-2-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}pyr- imidin-4-yl)amino]benzenesulfonamide to microcrystalline cellulose in the formulation is about 1:1.5 to about 1:9, and sodium stearyl fumarate is about 1% by weight of the formulation. 2. The capsule unit of claim 1, wherein the microcrystalline cellulose is silicified microcrystalline cellulose. 3. The capsule of claim 1, wherein the to formulation comprises about 117 mg of N-tert-butyl-3-[(5-methyl-2-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]ami- no}pyrimidin-4-yl)amino]benzenesulfonamide dihydrochloride monohydrate. 4. The capsule of claim 1, wherein the formulation comprises about 235 mg of N-tert-butyl-3-[(5-methyl-2-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}- pyrimidin-4-yl)amino]benzenesulfonamide dihydrochloride monohydrate, about 357 mg of silicified microcrystalline cellulose, and about 6 mg of sodium stearyl fumarate. 5. The capsule of claim 1, wherein the capsule is a hard gelatin capsule. 6. A method of treating myelofibrosis in a subject comprising administering a capsule comprising a formulation comprising (i) a compound that is N-tert-butyl-3-[(5-methyl-2-{[4(2-pyrrolidin-1-ylethoxy)phenyl]amino}pyri- midin-4-yl)amino]benzenesulfonamide dihydrochloride monohydrate, (ii) a microcrystalline cellulose, and (iii) sodium stearyl fumarate, wherein: the weight ratio of N-tert-butyl-3-[(5-methyl-2-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}pyr- imidin-4-yl)amino]benzenesulfonamide to microcrystalline cellulose in the formulation is about 1:1.5 to about 1:9, and sodium stearyl fumarate is about 1% by weight of the formulation. 7. A method of preparing a capsule comprising a formulation, wherein the method comprises blending a microcrystalline cellulose and sodium stearyl fumarate with a compound that is N-tert-butyl-3-[(5-methyl-2-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}pyr- imidin-4-yl)amino]benzenesulfonamide dihydrochloride monohydrate, wherein: the weight ratio of N-tert-butyl-3-[(5-methyl-2-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}pyr- imidin-4-yl)amino]benzenesulfonamide to microcrystalline cellulose in the formulation is about 1:1.5 to about 1:9, and sodium stearyl fumarate is about 1% by weight of the formulation. 8. An article of manufacture comprising: (a) a capsule comprising a formulation comprising (i) a compound that is N-tert-butyl-3-[(5-methyl-2-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}pyr- imidin-4-yl)amino]benzenesulfonamide dihydrochloride monohydrate, (ii) a microcrystalline cellulose, and (iii) sodium stearyl fumarate, wherein: the weight ratio of N-tert-butyl-3-[(5-methyl-2-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}pyr- imidin-4-yl)amino]benzenesulfonamide to microcrystalline cellulose in the formulation is about 1:1.5 to about 1:9, and sodium stearyl fumarate is about 1% by weight of the formulation; and (b) a package insert or a label indicating that the formulation is useful for treating myelofibrosis in a subject. 9. The capsule or claim 3, wherein the microcrystalline cellulose is silicified microcrystalline cellulose. 10. The article of manufacture of claim 8, wherein the microcrystalline cellulose is silicified microcrystalline cellulose. 11. The method of claim 7, wherein the microcrystalline cellulose is silicified microcrystalline cellulose. 12. The capsule of claim 1, wherein the weight ratio or N-tert-butyl-3-[(5-methyl-2-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}pyr- imidin-4-yl)amino]benzenesulfonamide to microcrystalline cellulose in the formulation is about 1:1.5 to about 1:2. 13. The capsule of claim 12, wherein the formulation comprises about 117 mg of N-tert-butyl-3-[(5-methyl-2-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]ami- no}pyrimidin-4-yl)amino]benzenesulfonamide dihydrochloride monohydrate. 14. The capsule of claim 12, wherein the formulation comprises about 235 mg of N-tert-butyl-3-[(5-methyl-2-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]ami- no}pyrimidin-4-yl)amino]benzenesulfonamide dihydrochloride monohydrate. 15. The capsule of claim 12, wherein the microcrystalline cellulose is silicified microcrystalline cellulose. 16. The capsule of claim 15, wherein the formulation comprises about 117 mg of N-tert-butyl-3-[(5-methyl-2-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]ami- no}pyrimidin-4-yl)amino]benzenesulfonamide dihydrochloride monohydrate. 17. The capsule of claim 15, wherein the formulation comprises about 235 mg of N-tert-butyl-3-[(5-methyl-2-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]ami- no}pyrimidin-4-yl)amino]benzenesulfonamide dihydrochloride monohydrate. 18. The capsule of claim 4, wherein the microcrystalline cellulose is silicified microcrystalline cellulose. 19. The article of manufacture of claim 8, wherein the formulation comprises about 117 mg of N-tert-butyl-3-[(5-methyl-2-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}pyr- imidin-4-yl)amino]benzenesulfonamide dihydrochloride monohydrate. 20. The article of manufacture of claim 19, wherein the microcrystalline cellulose is silicified microcrystalline cellulose. 21. The article of manufacture of claim 8, wherein the weight ratio of N-tert-butyl-3-[(5-methyl-2-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}pyr- imidin-4-yl)amino]benzenesulfonamide to microcrystalline cellulose in the formulation is about 1:1.5 to about 1:2. 22. The article of manufacture of claim 21, wherein the microcrystalline cellulose is silicified microcrystalline cellulose. 23. The article or manufacture of claim 22, wherein the formulation comprises about 117 mg of N-tert-butyl-3-[(5-methyl-2-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino)}py- rimidin-4-yl)amino]benzenesulfonamide dihydrochloride monohydrate. 24. The article of manufacture of claim 8, wherein the formulation comprises about 235 mg of N-tert-butyl-3-[(5-methyl-2-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}pyr- imidin-4-yl)amino]benzenesulfonamide dihydrochloride monohydrate. 25. The article of manufacture of claim 22, wherein the formulation comprises about 235 mg of N-tert-butyl-3-[(5-methyl-2-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}pyr- imidin-4-yl)amino]benzenesulfonamide dihydrochloride monohydrate. 26. The article of manufacture of claim 24, wherein the microcrystalline cellulose is silicified microcrystalline cellulose.