Claims for Patent: 8,987,323

Summary for Patent: 8,987,323

Title:	Crystalline form of benzylbenzene SGLT2 inhibitor
Abstract:	Provided are crystalline forms of a compound having an inhibitory effect on sodium-dependent glucose cotransporter SGLT2. The invention also provides pharmaceutical compositions, methods of preparing the crystalline compound, and methods of using the crystalline compound, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT or SGLT2 inhibition.
Inventor(s):	Mengzhuang Cai, Qian Liu, Ge Xu, Binhua Lv, Brian Seed, Jacques Y. Roberge
Assignee:	Theracosbio LLC
Application Number:	US13/158,724
Patent Claims:	1. A crystalline form of the compound of the formula: characterized by an X-ray powder diffraction (XRPD) pattern that comprises peaks at 11.2, 12.9, 15.5, 17.8, 19.1, 20.0 and 20.7 degrees 2θ, ±0.1 degrees 2θ, wherein said XRPD is made using CuKα1 radiation. 2. The crystalline form in accordance with claim 1, characterized by an XRPD that further comprises one or more peaks at 5.4, 11.3, 11.9, 16.3, 20.6, 21.2, 22.8, 23.0, 23.4, 23.6, 23.9, 24.7, 25.4, 25.8, 27.8 and 28.2 degrees 2θ, ±0.1 degrees 2θ, wherein said XRPD is made using CuKα1 radiation. 3. The crystalline form in accordance with claim 2, characterized by an XRPD that comprises peaks at 11.2, 12.9, 15.5, 17.8, 19.1, 20.0, 20.6, 20.7, 21.2 and 22.8 degrees 2θ, ±0.1 degrees 2θ, wherein said XRPD is made using CuKα1 radiation. 4. The crystalline form in accordance with claim 2, characterized by an XRPD that comprises peaks at 5.4, 11.2, 11.9, 12.9, 15.5, 16.3, 17.8, 19.1, 20.0 and 20.7 degrees 2θ, ±0.1 degrees 2θ, wherein said XRPD is made using CuKα1 radiation. 5. The crystalline form in accordance with claim 1, characterized by an XRPD that comprises peaks at 5.4, 10.7, 11.2, 11.3, 11.9, 12.9, 14.7, 15.0, 15.5, 16.1, 16.3, 17.8, 18.7, 19.1, 20.0, 20.6, 20.7, 21.2, 21.6, 22.4, 22.8, 23.0, 23.4, 23.6, 23.9, 24.7, 25.4, 25.8, 27.0, 27.5, 27.8, 28.2, 28.9, 29.0 and 29.6 degrees 2θ, ±0.1 degrees 2θ, wherein said XRPD is made using CuKα1 radiation. 6. The crystalline form in accordance with claim 1, characterized by a Raman spectra that comprises one or more peaks at about 353, 688, 825, 1178, 1205, 1212, 1608, 2945, 3010 and 3063 cm−1. 7. The crystalline form in accordance with claim 1, characterized by a Raman spectra that comprises peaks at about 353, 688, and 825 cm−1. 8. The crystalline form in accordance with claim 1, characterized by a Raman spectra that comprises peaks at about 144, 189, 216, 226, 284, 315, 353, 387, 419, 432, 449, 503, 530, 565, 594, 638, 688, 716, 728, 755, 790, 825, 850, 884, 901, 919, 934, 974, 984, 1014, 1030, 1052, 1070, 1120, 1134, 1178, 1205, 1212, 1229, 1302, 1323, 1343, 1380, 1422, 1438, 1457, 1572, 1585, 1608, 2844, 2919, 2945, 2963, 2997, 3010, 3028, 3051, 3063, 3085, and 3095 cm−1. 9. The crystalline form in accordance with claim 1, characterized by an XRPD that further comprises one or more peaks at 5.4, 11.3, 11.9, 16.3, 20.6, 21.2, 22.8, 23.0, 23.4, 23.6, 23.9, 24.7, 25.4, 25.8, 27.8 and 28.2 degrees 2θ, ±0.1 degrees 2θ, wherein said XRPD is made using CuKα1 radiation; and a Raman spectra that comprises one or more peaks at about 353, 688, 825, 1178, 1205, 1212, 1608, 2945, 3010 and 3063 cm−1. 10. The crystalline form in accordance with claim 1, characterized by an XRPD that further comprises one or more peaks at 20.6, 21.2, 22.8 and 28.2 degrees 2θ, ±0.1 degrees 2θ, wherein said XRPD is made using CuKα1 radiation; and a Raman spectra that comprises one or more peaks at about 353, 688, and 825 cm−1. 11. The crystalline form in accordance with claim 1, characterized by a differential scanning calorimetry (DSCI) endotherm at about 136° C. 12. The crystalline form in accordance with claim 1, characterized by the following unit cell data: Family and Space Group Monoclinic P21 (#4) Z’/Z 1/2 a (Å) 7.960 b (Å) 8.860 c (Å) 16.560 α (deg) 90 β (deg) 95.71 γ (deg) 90 Volume (Å3/cell) 1162.1 V/Z (Å3/asym. unit) 581.1 Assumed Composition C24H29O7Cl Density (g/cm3) 1.329 Weight Fraction Solvent (%) N/A. 13. The crystalline form of the compound of claim 1 which is isotopically labeled. 14. A pharmaceutical composition comprising a pharmaceutically acceptable excipient and the crystalline form of the compound in accordance with claim 1.