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Last Updated: August 14, 2024

Claims for Patent: 8,987,323


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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):Cai Mengzhuang, Liu Qian, Xu Ge, Lv Binhua, Seed Brian, Roberge Jacques Y.
Assignee:Theracos, Inc.
Application Number:US13158724
Patent Claims: 2. The crystalline form in accordance with claim 1 , characterized by an XRPD that further comprises one or more peaks at 5.4 claim 1 , 11.3 claim 1 , 11.9 claim 1 , 16.3 claim 1 , 20.6 claim 1 , 21.2 claim 1 , 22.8 claim 1 , 23.0 claim 1 , 23.4 claim 1 , 23.6 claim 1 , 23.9 claim 1 , 24.7 claim 1 , 25.4 claim 1 , 25.8 claim 1 , 27.8 and 28.2 degrees 2θ claim 1 , ±0.1 degrees 2θ claim 1 , wherein said XRPD is made using CuKradiation.3. The crystalline form in accordance with claim 2 , characterized by an XRPD that comprises peaks at 11.2 claim 2 , 12.9 claim 2 , 15.5 claim 2 , 17.8 claim 2 , 19.1 claim 2 , 20.0 claim 2 , 20.6 claim 2 , 20.7 claim 2 , 21.2 and 22.8 degrees 2θ claim 2 , ±0.1 degrees 2θ claim 2 , wherein said XRPD is made using CuKradiation.4. The crystalline form in accordance with claim 2 , characterized by an XRPD that comprises peaks at 5.4 claim 2 , 11.2 claim 2 , 11.9 claim 2 , 12.9 claim 2 , 15.5 claim 2 , 16.3 claim 2 , 17.8 claim 2 , 19.1 claim 2 , 20.0 and 20.7 degrees 2θ claim 2 , ±0.1 degrees 2θ claim 2 , wherein said XRPD is made using CuKradiation.5. The crystalline form in accordance with claim 1 , characterized by an XRPD that comprises peaks at 5.4 claim 1 , 10.7 claim 1 , 11.2 claim 1 , 11.3 claim 1 , 11.9 claim 1 , 12.9 claim 1 , 14.7 claim 1 , 15.0 claim 1 , 15.5 claim 1 , 16.1 claim 1 , 16.3 claim 1 , 17.8 claim 1 , 18.7 claim 1 , 19.1 claim 1 , 20.0 claim 1 , 20.6 claim 1 , 20.7 claim 1 , 21.2 claim 1 , 21.6 claim 1 , 22.4 claim 1 , 22.8 claim 1 , 23.0 claim 1 , 23.4 claim 1 , 23.6 claim 1 , 23.9 claim 1 , 24.7 claim 1 , 25.4 claim 1 , 25.8 claim 1 , 27.0 claim 1 , 27.5 claim 1 , 27.8 claim 1 , 28.2 claim 1 , 28.9 claim 1 , 29.0 and 29.6 degrees 2θ claim 1 , ±0.1 degrees 2θ claim 1 , wherein said XRPD is made using CuKradiation.6. The crystalline form in accordance with claim 1 , characterized by a Raman spectra that comprises one or more peaks at about 353 claim 1 , 688 claim 1 , 825 claim 1 , 1178 claim 1 , 1205 claim 1 , 1212 claim 1 , 1608 claim 1 , 2945 claim 1 , 3010 and 3063 cm.7. The crystalline form in accordance with claim 1 , characterized by a Raman spectra that comprises peaks at about 353 claim 1 , 688 claim 1 , and 825 cm.8. The crystalline form in accordance with claim 1 , characterized by a Raman spectra that comprises peaks at about 144 claim 1 , 189 claim 1 , 216 claim 1 , 226 claim 1 , 284 claim 1 , 315 claim 1 , 353 claim 1 , 387 claim 1 , 419 claim 1 , 432 claim 1 , 449 claim 1 , 503 claim 1 , 530 claim 1 , 565 claim 1 , 594 claim 1 , 638 claim 1 , 688 claim 1 , 716 claim 1 , 728 claim 1 , 755 claim 1 , 790 claim 1 , 825 claim 1 , 850 claim 1 , 884 claim 1 , 901 claim 1 , 919 claim 1 , 934 claim 1 , 974 claim 1 , 984 claim 1 , 1014 claim 1 , 1030 claim 1 , 1052 claim 1 , 1070 claim 1 , 1120 claim 1 , 1134 claim 1 , 1178 claim 1 , 1205 claim 1 , 1212 claim 1 , 1229 claim 1 , 1302 claim 1 , 1323 claim 1 , 1343 claim 1 , 1380 claim 1 , 1422 claim 1 , 1438 claim 1 , 1457 claim 1 , 1572 claim 1 , 1585 claim 1 , 1608 claim 1 , 2844 claim 1 , 2919 claim 1 , 2945 claim 1 , 2963 claim 1 , 2997 claim 1 , 3010 claim 1 , 3028 claim 1 , 3051 claim 1 , 3063 claim 1 , 3085 claim 1 , and 3095 cm.9. The crystalline form in accordance with claim 1 , characterized by{'sub': 'α1', '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 CuKradiation; and'}{'sup': '−1', 'a Raman spectra that comprises one or more peaks at about 353, 688, 825, 1178, 1205, 1212, 1608, 2945, 3010 and 3063 cm.'}10. The crystalline form in accordance with claim 1 , characterized by{'sub': 'α1', '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 CuKradiation; and'}{'sup': '−1', 'a Raman spectra that comprises one or more peaks at about 353, 688, and 825 cm.'}11. The crystalline form in accordance with claim 1 , characterized by a differential scanning calorimetry (DSCI) endotherm at about 136° C.13. The crystalline form of the compound of which is isotopically labeled.14. A pharmaceutical composition comprising a pharmaceutically acceptable excipient and the crystalline form of the compound in accordance with .

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