Claims for Patent: 10,435,404

Summary for Patent: 10,435,404

Title:	Formulations of a compound modulating kinases
Abstract:	Provided are compositions comprising Compound I having the following structure: ##STR00001## or a pharmaceutically acceptable salt thereof, and a solubilizing agent; methods of making the same; and methods of using the same.
Inventor(s):	Ibrahim; Prabha N. (Mountain View, CA), Rezaei; Hamid (Berkeley, CA), Visor; Gary Conard (Castro Valley, CA), Kamo; Tomoari (Tokyo, JP), Yamakose; Hiroshi (Tokyo, JP)
Assignee:	Plexxikon Inc. (Berkeley, CA) Daiichi Sankyo Company, Limited (Tokyo, JP)
Application Number:	16/043,821
Patent Claims:	1. A composition comprising: 40% to 60% W/W of Compound I having the following structure: ##STR00005## and wherein Compound I is a crystalline HCl salt characterized by an X-ray powder diffractogram comprising peaks (.+-.0.2.degree.) at 7.3, 23.3 and 28.2.degree. 2.theta. as determined on a diffractometer using Cu-K.alpha. radiation; 20% to 35% W/W of a poloxamer; 10% to 22% W/W of an excipient; 1% to 5% W/W of a disintegrant; and 0.5% to 3% W/W of a lubricant. 2. The composition of claim 1, wherein the poloxamer is poloxamer 407. 3. The composition of claim 1, wherein the diffractogram further comprises peaks at 16.6 and 20.9.degree. 2.theta..+-.0.2.degree.. 4. The composition of claim 1, wherein Compound I is characterized by: i) a diffractogram substantially as shown in FIG. 1; ii) a differential scanning calorimetry (DSC) thermogram comprising an endotherm at 234.degree. C.; iii) a DSC thermogram substantially as shown in FIG. 2; iv) thermogravimetric analysis (TGA) comprising a thermogram substantially as shown in FIG. 3; or v) a dynamic vapor sorption (DVS) curve substantially as shown in FIG. 4. 5. The composition of claim 1, comprising 45% to 55% W/W of Compound I; 24% to 32% W/W of the poloxamer; 14% to 20% W/W of the excipient; 2% to 4% W/W of the disintegrant; and 1.0% to 2.5% W/W of the lubricant. 6. The composition of claim 1, comprising 48% to 53% W/W of Compound I; 26% to 29% W/W of the poloxamer; 15% to 18% W/W of the excipient; 2.5% to 3.5% W/W of the disintegrant; and 1.2% to 1.8% W/W of the lubricant. 7. The composition of claim 1, comprising 51.2% (.+-.3%) W/W of Compound I; 27.6% (.+-.3%) W/W of the poloxamer; 16.8% (.+-.3%) W/W of the excipient; 3% (.+-.1%) W/W of the disintegrant; and 1.5% (.+-.1%) W/W of the lubricant. 8. The composition of claim 1, wherein the excipient is mannitol; the disintegrant is crospovidone; and the lubricant is magnesium stearate. 9. The composition of claim 8, wherein the crospovidone is Polyplasdone.RTM. Ultra or Polyplasdone.RTM. Ultra-10. 10. The composition of claim 1, wherein the poloxamer is poloxamer 407; the excipient is mannitol; the disintegrant is crospovidone; and the lubricant is magnesium stearate. 11. The composition of claim 10, comprising 45% to 55% W/W of Compound I; 24% to 32% W/W of poloxamer 407; 14% to 20% W/W of mannitol; 2% to 4% W/W of crospovidone; and 1.0% to 2.5% W/W of magnesium stearate. 12. The composition of claim 10, comprising 48% to 53% W/W of Compound I; 26% to 29% W/W of poloxamer 407; 15% to 18% W/W of mannitol; 2.5% to 3.5% W/W of crospovidone; and 1.2% to 1.8% W/W magnesium stearate. 13. The composition of claim 10, comprising 51.2% W/W (.+-.3%) of Compound I; 27.6% W/W (.+-.3%) of poloxamer 407; 16.8% (.+-.3%) W/W of mannitol; 3% W/W (.+-.1%) of crospovidone; and 1.5% (.+-.1%) W/W of magnesium stearate. 14. The composition of claim 10, wherein the crospovidone is Polyplasdone.RTM. Ultra or Polyplasdone.RTM. Ultra-10. 15. The composition of claim 1, wherein the composition is in a capsule form suitable for oral dosage. 16. The composition of claim 15, wherein the capsule comprises hard gelatin or hypromellose. 17. The composition of claim 16, wherein the capsule comprises hypromellose. 18. A method for preparing the composition of claim 1 comprising mixing Compound I, and a poloxamer in a convection mixer. 19. The method of claim 18, wherein the convection mixer is a vertical high intensity mixer. 20. A composition prepared by the method of claim 18.