Claims for Patent: 10,385,008

Summary for Patent: 10,385,008

Title:	Polymorphic forms of RAD1901-2HCL
Abstract:	Various polymorphic forms of RAD1901-2HCl, including three crystalline and amorphous forms, are prepared and characterized. Uses of the various polymorphic forms of RAD1901-2HCl for cancer treatment are also disclosed.
Inventor(s):	Cruskie, Jr. Michael Paul, Bolger Joshua Kyle, McKenzie Jonathan Blake, Sheth Pratik, Edwards Richard, Eberlin Alex, Markey Michael
Assignee:	Radius Pharmaceuticals, Inc.
Application Number:	US15863850
Patent Claims:	2. The solid form of claim 1 , having an X-ray powder diffraction pattern comprising peaks claim 1 , in terms of 2-theta claim 1 , at 7.1 degrees 2θ±0.2 degree 2θ and 14.3 degrees 2θ±0.2 degree 2θ at about relative humidity 0%.3. The solid form of claim 1 , having an X-ray powder diffraction pattern further comprising at least one peak claim 1 , in terms of 2-theta claim 1 , selected from the group consisting of 14.3 degrees 2θ±0.2 degree 2θ and 18.3 degrees 2θ±0.2 degree 2θ at about relative humidity 0%.4. The solid form of claim 1 , having an X-ray powder diffraction pattern further comprising at least two peaks claim 1 , in terms of 2-theta claim 1 , selected from the group consisting of 14.3 degrees 2θ±0.2 degree 2θ claim 1 , 18.3 degrees 2θ±0.2 degree 2θ claim 1 , 13.8 degrees 2θ±0.2 degree 2θ and 12.0 degrees 2θ±0.2 degree 2θ claim 1 , at about relative humidity 0%.5. The solid form of claim 1 , having an X-ray powder diffraction pattern further comprising at least three peaks claim 1 , in terms of 2-theta claim 1 , selected from the group consisting of 14.3 degrees 2θ±0.2 degree 2θ claim 1 , 18.3 degrees 2θ±0.2 degree 2θ claim 1 , 13.8 degrees 2θ±0.2 degree 2θ claim 1 , 12.0 degrees 2θ±0.2 degree 2θ claim 1 , 25.1 degrees 2θ±0.2 degree 2θ and 18.9 degrees 2θ±0.2 degree 2θ claim 1 , at about relative humidity 0%.6. The solid form of claim 1 , having an X-ray powder diffraction pattern further comprising at least four peaks claim 1 , in terms of 2-theta claim 1 , selected from the group consisting of 14.3 degrees 2θ±0.2 degree 2θ claim 1 , 18.3 degrees 2θ±0.2 degree 2θ claim 1 , 13.8 degrees 2θ±0.2 degree 2θ claim 1 , 12.0 degrees 2θ±0.2 degree 2θ claim 1 , 25.1 degrees 2θ±0.2 degree 2θ claim 1 , 18.9 degrees 2θ±0.2 degree 2θ claim 1 , 27.2 degrees 2θ±0.2 degree 2θ and 11.0 degrees 2θ±0.2 degree 2θ claim 1 , at about relative humidity 0%.7. The solid form of claim 1 , having an X-ray powder diffraction pattern further comprising at least four peaks claim 1 , in terms of 2-theta claim 1 , selected from the group consisting of 14.3 degrees 2θ±0.2 degree 2θ claim 1 , 18.3 degrees 2θ±0.2 degree 2θ claim 1 , 13.8 degrees 2θ±0.2 degree 2θ claim 1 , 12.0 degrees 2θ±0.2 degree 2θ claim 1 , 25.1 degrees 2θ±0.2 degree 2θ claim 1 , 18.9 degrees 2θ±0.2 degree 2θ claim 1 , 27.2 degrees 2θ±0.2 degree 2θ claim 1 , 11.0 degrees 2θ±0.2 degree 2θ and 16.2 degrees 2θ±0.2 degree 2θ claim 1 , at about relative humidity 0%.8. The solid form of claim 1 , having an X-ray powder diffraction pattern further comprising at least six peaks claim 1 , in terms of 2-theta claim 1 , selected from the group consisting of 14.3 degrees 2θ±0.2 degree 2θ claim 1 , 18.3 degrees 2θ±0.2 degree 2θ claim 1 , 13.8 degrees 2θ±0.2 degree 2θ claim 1 , 12.0 degrees 2θ±0.2 degree 2θ claim 1 , 25.1 degrees 2θ±0.2 degree 2θ claim 1 , 18.9 degrees 2θ±0.2 degree 2θ claim 1 , 27.2 degrees 2θ±0.2 degree 2θ claim 1 , 11.0 degrees 2θ±0.2 degree 2θ and 16.2 degrees 2θ±0.2 degree 2θ claim 1 , at about relative humidity 0%.9. The solid form of claim 1 , having an X-ray powder diffraction pattern further comprising at least seven peaks claim 1 , in terms of 2-theta claim 1 , selected from the group consisting of 14.3 degrees 2θ±0.2 degree 2θ claim 1 , 18.3 degrees 2θ±0.2 degree 2θ claim 1 , 13.8 degrees 2θ±0.2 degree 2θ claim 1 , 12.0 degrees 2θ±0.2 degree 2θ claim 1 , 25.1 degrees 2θ±0.2 degree 2θ claim 1 , 18.9 degrees 2θ±0.2 degree 2θ claim 1 , 27.2 degrees 2θ±0.2 degree 2θ claim 1 , 11.0 degrees 2θ±0.2 degree 2θ and 16.2 degrees 2θ±0.2 degree 2θ claim 1 , at about relative humidity 0%.10. The solid form of claim 1 , having an X-ray powder diffraction pattern further comprising at least eight peaks claim 1 , in terms of 2-theta claim 1 , selected from the group consisting of 14.3 degrees 2θ±0.2 degree 2θ claim 1 , 18.3 degrees 2θ±0.2 degree 2θ claim 1 , 13.8 degrees 2θ±0.2 degree 2θ claim 1 , 12.0 degrees 2θ±0.2 degree 2θ claim 1 , 25.1 degrees 2θ±0.2 degree 2θ claim 1 , 18.9 degrees 2θ±0.2 degree 2θ claim 1 , 27.2 degrees 2θ±0.2 degree 2θ claim 1 , 11.0 degrees 2θ±0.2 degree 2θ and 16.2 degrees 2θ±0.2 degree 2θ claim 1 , at about relative humidity 0%.11. The solid form of claim 1 , having an X-ray powder diffraction pattern comprising the peaks claim 1 , in terms of 2-theta claim 1 , of 7.1 degrees 2θ±0.2 degree 2θ claim 1 , 14.3 degrees 2θ±0.2 degree 2θ claim 1 , 18.3 degrees 2θ±0.2 degree 2θ claim 1 , 13.8 degrees 2θ±0.2 degree 2θ claim 1 , 12.0 degrees 2θ±0.2 degree 2θ claim 1 , 25.1 degrees 2θ±0.2 degree 2θ claim 1 , 18.9 degrees 2θ±0.2 degree 2θ claim 1 , 27.2 degrees 2θ±0.2 degree 2θ claim 1 , 11.0 degrees 2θ±0.2 degree 2θ and 16.2 degrees 2θ±0.2 degree 2θ claim 1 , at about relative humidity 0%.12. The solid form of claim 1 , having an X-ray powder diffraction pattern as shown in at about relative humidity 0%.14. The solid form of claim 13 , having a differential scanning calorimetry (DSC) thermogram as shown in the bottom figure of .15. A solid form of RAD1901-2HCl claim 13 , having a thermogravimetric analysis (TGA) as shown in the top graph of .16. A pharmaceutical composition comprising the solid form of and one or more pharmaceutically acceptable excipients.17. A process for preparing the solid form of comprising precipitating from a solution comprising RAD1901-2HCl and a solvent claim 1 , or slurrying RAD1901-2HCl in a solvent claim 1 , wherein the solvent comprises an organic solvent excluding methanol claim 1 , and the content of water is at or below 5% v/v.18. The process according to wherein the organic solvent is selected from the group consisting of n-heptane claim 17 , propyl acetate claim 17 , ethyl acetate claim 17 , isopropyl acetate claim 17 , methyl isobutyl ketone (MIBK) claim 17 , methyl ethyl ketone (MEK) claim 17 , 1-propanol claim 17 , ethanol claim 17 , t-butyl methyl ether (TBME) claim 17 , 1 claim 17 ,4-dioxane claim 17 , toluene claim 17 , 1 claim 17 ,2-dimethoxyethane claim 17 , tetrahydrofuran claim 17 , dichloromethane claim 17 , acetonitrile claim 17 , nitromethane claim 17 , and mixtures thereof.