Formulations of (S)-3-(1-(9H-purin-6-ylamino)ethyl)-8-chloro-2-phenylisoquinolin-1(2H)-one

Patent metadata

Field	Value
Publication number	US-11312718-B2
Application number	US-202016734135-A
Country	US
Kind code	B2
Filing date	Jan 3, 2020
Priority date	Jan 10, 2011
Publication date	Apr 26, 2022
Grant date	Apr 26, 2022

Abstract

Polymorphs of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphs thereof, and pharmaceutical compositions thereof.

First claim

What is claimed is:

1. A formulation comprising polymorph Form C of a compound of Formula (I):

and a filler, glidant, or a combination thereof, wherein polymorph Form C of the compound of Formula (I) is a hydrate and has the following characteristic X-ray Powder Diffraction (XRPD) peaks: 2θ=10.4°±0.2°, 13.3°±0.2°, and 24.3°±0.2°.

2. The formulation of claim 1 , wherein the formulation further comprises a disintegrant.

3. The formulation of claim 1 , wherein the formulation further comprises a lubricant.

4. The formulation of claim 1 , wherein the filler is lactose, mannitol, starch, sorbitol, sucrose, dicalcium phosphate, or microcrystalline cellulose.

5. The formulation of claim 1 , wherein the glidant is silicon dioxide, magnesium silicate, or talc.

6. The formulation of claim 2 , wherein the disintegrant is crospovidone, croscarmellose sodium or sodium starch glycolate.

7. The formulation of claim 3 , wherein the lubricant is sodium stearyl fumarate, stearic acid, talc, calcium stearate, magnesium stearate, solid polyethylene glycols, or sodium lauryl sulfate.

8. The formulation of claim 1 , wherein the formulation is for oral administration.

9. The formulation of claim 1 , wherein the formulation is a solid dosage form.

10. The formulation of claim 1 , wherein the formulation is a tablet or a capsule.

11. The formulation of claim 1 , wherein the formulation is a capsule.

12. The formulation of claim 1 , wherein the filler is microcrystalline cellulose and the formulation further comprises crospovidone and magnesium stearate.

13. The formulation of claim 11 , wherein the filler is microcrystalline cellulose and the formulation further comprises crospovidone and magnesium stearate.

14. An oral dosage form comprising polymorph Form C of a compound of Formula (I):

and a filler, glidant, or a combination thereof, wherein polymorph Form C is a hydrate with the following characteristic X-ray Powder Diffraction (XRPD) peaks: 2θ=10.4°±0.2°, 13.3°±0.2°, and 24.3°±0.2°;
wherein the oral dosage form comprises about 5 mg to about 75 mg of polymorph Form C.

15. The oral dosage form of claim 14 , wherein polymorph Form C is present in an amount of about 25 mg.

16. The oral dosage form of claim 14 , wherein polymorph Form C is present in an amount of about 15 mg.

17. The oral dosage form of claim 14 , wherein the oral dosage form further comprises a disintegrant, a lubricant, or combination thereof.

18. The oral dosage form of claim 14 , wherein the filler is lactose, mannitol, starch, sorbitol, sucrose, dicalcium phosphate, or microcrystalline cellulose; and wherein the glidant is silicon dioxide, magnesium silicate, or talc.

19. The oral dosage form of claim 17 , wherein the disintegrant is crospovidone, croscarmellose sodium or sodium starch glycolate; and wherein the lubricant is sodium stearyl fumarate, stearic acid, talc, calcium stearate, magnesium stearate, solid polyethylene glycols, or sodium lauryl sulfate.

20. The oral dosage form of claim 14 , wherein the oral dosage form is a tablet or a capsule.

21. The oral dosage form of claim 14 , wherein the oral dosage form is a capsule.

22. The oral dosage form of claim 21 , wherein the polymorph Form C is present in an amount of about 15 mg.

23. The oral dosage form of claim 21 , wherein the polymorph Form C is present in an amount of about 25 mg.

24. The oral dosage form of claim 21 , wherein the filler is microcrystalline cellulose and the oral dosage form further comprises crospovidone and magnesium stearate.

25. The oral dosage form of claim 24 , wherein the polymorph Form C is present in an amount of about 15 mg.

26. The oral dosage form of claim 24 , wherein the polymorph Form C is present in an amount of about 25 mg.

27. The formulation of claim 5 , wherein the silicon dioxide is colloidal silicon dioxide.

28. The formulation of claim 11 , wherein the filler is microcrystalline cellulose, the glidant is silicon dioxide, and the formulation further comprises crospovidone and magnesium stearate.

29. The formulation of claim 28 , wherein polymorph Form C is present in an amount of about 15 mg.

30. The formulation of claim 28 , wherein polymorph Form C is present in an amount of about 25 mg.

31. The oral dosage form of claim 18 , wherein the silicon dioxide is colloidal silicon dioxide.

32. The oral dosage form of claim 21 , wherein the filler is microcrystalline cellulose, the glidant is silicon dioxide, and the oral dosage form further comprises crospovidone and magnesium stearate.

33. The oral dosage form of claim 32 , wherein polymorph Form C is present in an amount of about 15 mg.

34. The oral dosage form of claim 32 , wherein polymorph Form C is present in an amount of about 25 mg.

Assignees

• Infinity Pharmaceuticals Inc

Inventors

• Ren Pingda
• Martin Michael
• Isbester Paul
• Lane Benjamin S
• Kropp Jason

Classifications

• A61P29/00

  Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• C07B2200/13

  Crystalline forms, e.g. polymorphs · CPC title

• C07B2200/07

  Optical isomers · CPC title

• A61K31/519 Primary

  ortho- or peri-condensed with heterocyclic rings · CPC title