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Last Updated: August 13, 2020

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Claims for Patent: 10,294,231

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Summary for Patent: 10,294,231
Title:Crystalline forms of a Bruton's tyrosine kinase inhibitor
Abstract: Described herein is the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pi- peridin-1-yl)prop-2-en-1-one, including crystalline forms, solvates and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include the Btk inhibitor, as well as methods of using the Btk inhibitor, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
Inventor(s): Purro; Norbert (Los Gatos, CA), Smyth; Mark S. (Foster City, CA), Goldman; Erick (Concord, CA), Wirth; David D. (Oak Ridge, NC)
Assignee: Pharmacyclics LLC (Sunnyvale, CA)
Application Number:16/110,999
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 10,294,231
Patent Claims: 1. A pharmaceutical formulation for oral administration comprising: (a) about 40 mg to about 200 mg of 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pi- peridin-1-yl)prop-2-en-1-one; (b) about 40 wt % to about 50 wt % of one or more diluents; (c) about 3 wt % to about 10 wt % of one or more disintegrating agents; (d) about 2 wt % to about 7 wt % of one or more surfactants; and (e) one or more lubricants.

2. The pharmaceutical formulation of claim 1, wherein the formulation is in the form of a capsule comprising about 140 mg of 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pi- peridin-1-yl)prop-2-en-1-one.

3. The pharmaceutical formulation of claim 1, wherein the one or more diluents are selected from the group consisting of lactose, sucrose, dextrose, dextrates, maltodextrin, mannitol, xylitol, sorbitol, cyclodextrins, calcium phosphate, calcium sulfate, starches, modified starches, microcrystalline cellulose, microcellulose, and talc.

4. The pharmaceutical formulation of claim 1, wherein the one or more diluents are selected from the group consisting of lactose, sucrose, dextrose, mannitol, xylitol, sorbitol, calcium phosphate, starches, modified starches, microcrystalline cellulose, and microcellulose.

5. The pharmaceutical formulation of claim 1, wherein the one or more diluents are diluent is selected from the group consisting of lactose, sucrose, mannitol, calcium phosphate, starches, modified starches, and microcrystalline cellulose.

6. The pharmaceutical formulation of claim 1, wherein the one or more diluent is microcrystalline cellulose.

7. The pharmaceutical formulation of claim 1, wherein the one or more disintegrating agents are selected from the group consisting of natural starch, a pregelatinized starch, a sodium starch, methylcrystalline cellulose, methylcellulose, croscarmellose, croscarmellose sodium, cross-linked sodium carboxymethylcellulose, cross-linked carboxymethylcellulose, cross-linked croscarmellose, cross-linked starch, cross-linked polymer, cross-linked polyvinylpyrrolidone, sodium alginate, a clay, and a gum.

8. The pharmaceutical formulation of claim 1, wherein the one or more disintegrating agents are selected from the group consisting of natural starch, a pregelatinized starch, a sodium starch, methylcrystalline cellulose, methylcellulose, croscarmellose, croscarmellose sodium, sodium starch glycolate, crospovidone, sodium alginate, a clay, and a gum.

9. The pharmaceutical formulation of claim 1, wherein the one or more disintegrating agents are selected from the group consisting of natural starch, a pregelatinized starch, a sodium starch, methylcrystalline cellulose, croscarmellose, croscarmellose sodium, sodium starch glycolate, and crospovidone.

10. The pharmaceutical formulation of claim 1, wherein the one or more disintegrating agents are selected from the group consisting of croscarmellose sodium, sodium starch glycolate, and crospovidone.

11. The pharmaceutical formulation of claim 1, the one or more disintegrating agent is croscarmellose sodium.

12. The pharmaceutical formulation of claim 1, wherein the one or more surfactants are selected from the group consisting of sodium lauryl sulfate, sorbitan monooleate, polyoxyethylene sorbitan monooleate, polysorbates, poloxamers, bile salts, glyceryl monostearate, and copolymers of ethylene oxide and propylene oxide.

13. The pharmaceutical formulation of claim 1, wherein the one or more surfactants are selected from the group consisting of sodium lauryl sulfate, polyoxyethylene sorbitan monooleate, polysorbates, poloxamers, and copolymers of ethylene oxide and propylene oxide.

14. The pharmaceutical formulation of claim 1, wherein the one or more surfactants are selected from the group consisting of sodium lauryl sulfate, poloxamers, and copolymers of ethylene oxide and propylene oxide.

15. The pharmaceutical formulation of claim 1, wherein the one or more surfactant is sodium lauryl sulfate.

16. The pharmaceutical formulation of claim 1, wherein the one or more lubricants are selected from the group consisting of stearic acid, calcium hydroxide, talc, corn starch, sodium stearyl fumarate, sodium stearate, magnesium stearate, zinc stearate, and waxes.

17. The pharmaceutical formulation of claim 1, wherein the one or more lubricants are selected from the group consisting of stearic acid, talc, sodium stearyl fumarate, magnesium stearate, and zinc stearate.

18. The pharmaceutical formulation of claim 1, wherein the one or more lubricants are selected from the group consisting of stearic acid, talc, sodium stearyl fumarate, and magnesium stearate.

19. The pharmaceutical formulation of claim 1, wherein the one or more lubricant is magnesium stearate.

20. The pharmaceutical formulation of claim 1, wherein: i. the one or more diluents are selected from the group consisting of lactose, sucrose, dextrose, dextrates, maltodextrin, mannitol, xylitol, sorbitol, cyclodextrins, calcium phosphate, calcium sulfate, starches, modified starches, microcrystalline cellulose, microcellulose, and talc; ii. the one or more disintegrating agents are selected from the group consisting of natural starch, a pregelatinized starch, a sodium starch, methylcrystalline cellulose, methylcellulose, croscarmellose, croscarmellose sodium, sodium starch glycolate, crospovidone, sodium alginate, a clay, and a gum; and iii. the one or more surfactants are selected from the group consisting of sodium lauryl sulfate, polyoxyethylene sorbitan monooleate, polysorbates, poloxamers, and copolymers of ethylene oxide and propylene oxide.

21. The pharmaceutical formulation of claim 20, wherein the dosage form is a hard gelatin capsule.

22. The pharmaceutical formulation of claim 1, wherein: i. the one or more diluents are selected from the group consisting of lactose, sucrose, dextrose, mannitol, xylitol, sorbitol, calcium phosphate, starches, modified starches, microcrystalline cellulose, and microcellulose; ii. the one or more disintegrating agents are selected from the group consisting of croscarmellose sodium, sodium starch glycolate, and crospovidone; and iii. the one or more surfactants are selected from the group consisting of sodium lauryl sulfate, poloxamers, and copolymers of ethylene oxide and propylene oxide.

23. The pharmaceutical formulation of claim 22, wherein the dosage form is a hard gelatin capsule.

24. The pharmaceutical formulation of claim 1, wherein: i. the one or more diluents are selected from the group consisting of lactose, sucrose, mannitol, calcium phosphate, starches, modified starches, and microcrystalline cellulose; ii. the one or more disintegrating agents are selected from the group consisting of natural starch, a pregelatinized starch, a sodium starch, methylcrystalline cellulose, methylcellulose, croscarmellose, croscarmellose sodium, cross-linked sodium carboxymethylcellulose, cross-linked carboxymethylcellulose, cross-linked croscarmellose, cross-linked starch, cross-linked polymer, cross-linked polyvinylpyrrolidone, sodium alginate, a clay, and a gum; and iii. the one or more surfactants are selected from the group consisting of sodium lauryl sulfate, sorbitan monooleate, polyoxyethylene sorbitan monooleate, polysorbates, poloxamers, bile salts, glyceryl monostearate, and copolymers of ethylene oxide and propylene oxide.

25. The pharmaceutical formulation of claim 24, wherein the dosage form is a hard gelatin capsule.

26. The pharmaceutical formulation of claim 1, wherein: i. the one or more diluent is microcrystalline cellulose; ii. the one or more disintegrating agent is croscarmellose sodium; and iii. the one or more surfactant is sodium lauryl sulfate.

27. The pharmaceutical formulation of claim 1 comprising: (a) about 40 wt % to about 50 wt % of 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pi- peridin-1-yl)prop-2-en-1-one; (b) microcrystalline cellulose; (c) croscarmellose sodium; and (d) sodium lauryl sulfate.

28. The pharmaceutical formulation of claim 27, wherein the dosage form is a hard gelatin capsule.

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