Claims for Patent: 9,802,932

Summary for Patent: 9,802,932

Title:	Solid forms of a compound modulating kinases
Abstract:	Solid forms of the compound, [5-(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-ylmethyl)-pyridin-2-yl]-(6-triflu- oromethyl-pyridin-3-ylmethyl)-amine HCl salt (Compound I) and its free base, active on the receptor protein kinases c-Kit and/or c-Fms and/or Flt3, were prepared and characterized: ##STR00001## Also provided are methods of using the solid forms.
Inventor(s):	Ibrahim; Prabha N. (Mountain View, CA), Visor; Gary Conard (Castro Valley, CA)
Assignee:	Plexxikon Inc. (Berkeley, CA)
Application Number:	15/147,692
Patent Claims:	1. A crystalline form of Compound I: ##STR00005## which is Compound I Form A, characterized by an X-ray powder diffractogram comprising peaks (.+-.0.2.degree.) at 7.1, 22.9 and 27.6 .degree.2.theta. as determined on a diffractometer usino Cu--K.alpha. radiation. 2. Compound I Form A according to claim 1, further characterized by: i) peaks at 21.7 and 23.7 .degree.2.theta..+-.0.2.degree. as determined on a diffractometer using Cu--K.alpha. radiation; ii) a diffractogram substantially as shown in FIG. 1; iii) a differential scanning calorimetry (DSC) thermogram comprising an endotherm at about 231.degree. C; iv) a DSC thermogram substantially as shown in FIG. 2; v) thermogravimetric analysis (TGA) comprising a thermogram substantially as shown in FIG. 3; vi) a dynamic vapor sorption (DVS) curve substantially as shown in FIG. 4; or vii) a Raman spectrum substantially as shown in FIG. 5. 3. A crystalline form of Compound I: ##STR00006## which is Compound I Form B, characterized by an X-ray powder diffractoaram comprising peaks (.+-.0.2.degree.) at 6.6, 23.2 and 28.1 .degree.2.theta. as determined on a diffractometer using Cu--K.alpha. radiation. 4. Compound I Form B according to claim 3, further characterized by: i) peaks at 22.3 and 26.7 .degree.2.theta..+-.0.2.degree. as determined on a diffractometer using Cu--K.alpha. radiation; ii) a diffractogram substantially as shown in FIG. 6; iii) a differential scanning calorimetry (DSC) thermogram comprising endotherms at about 127.degree. C. and 233.degree. C; iv) a DSC thermogram substantially as shown in FIG. 7; v) thermogravimetric analysis (TGA) comprising a thermogram substantially as shown in FIG. 8; or vi) a Raman spectrum substantially as shown in FIG. 9. 5. A crystalline form of Compound I: ##STR00007## which is Compound I Form C, 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. 6. Compound I Form C according to claim 5, further characterized by: i) peaks at 16.6 and 20.9 .degree.2.theta..+-.0.2.degree. as determined on a diffractometer using Cu--K.alpha. radiation; ii) a diffractogram substantially as shown in FIG. 10; iii) a differential scanning calorimetry (DSC) thermogram comprising an endotherm at about 234.degree. C; iv) a DSC thermogram substantially as shown in FIG. 11; v) thermogravimetric analysis (TGA) comprising a thermogram substantially as shown in FIG. 12; or vi) a dynamic vapor sorption (DVS) curve substantially as shown in FIG. 13. 7. A crystalline form of Compound I: ##STR00008## which is Compound I Form D, wherein the crystalline form is a methanol solvate, characterized by an X-ray powder diffractogram comprising peaks (.+-.0.2.degree.) at 6.9, 20.9 and 26.7 .degree.2.theta. as determined on a diffractometer using Cu--K.alpha. radiation. 8. Compound I Form D according to claim 7, further characterized by: i) peaks at 12.9 and 24.0 .degree.2.theta..+-.0.2.degree. as determined on a diffractometer using Cu--K.alpha. radiation; ii) a diffractogram substantially as shown in FIG. 17; or iii) thermogravimetric analysis (TGA) comprising a thermogram substantially as shown in FIG. 23. 9. A crystalline form of Compound II: ##STR00009## characterized by an X-ray powder diffractogram comprising peaks (.+-.0.2.degree.) at 10.9, 19.7 and 26.4 .degree.2.theta. as determined on a diffractometer using Cu--K.alpha. radiation. 10. The crystalline form according to claim 9, further characterized by: i) peaks at 20.8 and 25.3 .degree.2.theta..+-.0.2.degree. as determined on a diffractometer using Cu--K.alpha. radiation; ii) a diffractogram substantially as shown in FIG. 20; iii) a differential scanning calorimetry (DSC) thermogram comprising an endotherm at about 192.degree. C.; iv) a DSC thermogram substantially as shown in FIG. 21; or v) a dynamic vapor sorption (DVS) curve substantially as shown in FIG. 22. 11. A pharmaceutical composition comprising Compound I Form C according to claim 5 and a pharmaceutically acceptable excipient. 12. The composition of claim 11, wherein the composition comprises at least 50% w/w of Compound I Form C. 13. A process of preparing a capsule comprising Compound I Form C comprising combining Compound I Form C with a pharmaceutically acceptable carrier or excipient. 14. A process of preparing a tablet comprising Compound I Form C comprising combining Compound I Form C with a pharmaceutically acceptable carrier or excipient.