JP2016536321A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2016536321A5 JP2016536321A5 JP2016530967A JP2016530967A JP2016536321A5 JP 2016536321 A5 JP2016536321 A5 JP 2016536321A5 JP 2016530967 A JP2016530967 A JP 2016530967A JP 2016530967 A JP2016530967 A JP 2016530967A JP 2016536321 A5 JP2016536321 A5 JP 2016536321A5
- Authority
- JP
- Japan
- Prior art keywords
- ray diffraction
- diffraction pattern
- measured
- canagliflozin
- pharmaceutical composition
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 239000013078 crystal Substances 0.000 claims 11
- 238000002441 X-ray diffraction Methods 0.000 claims 7
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 6
- 229960001713 canagliflozin Drugs 0.000 claims 6
- VHOFTEAWFCUTOS-TUGBYPPCSA-N canagliflozin hydrate Chemical compound O.CC1=CC=C([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)C=C1CC(S1)=CC=C1C1=CC=C(F)C=C1.CC1=CC=C([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)C=C1CC(S1)=CC=C1C1=CC=C(F)C=C1 VHOFTEAWFCUTOS-TUGBYPPCSA-N 0.000 claims 6
- 238000000034 method Methods 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 230000005855 radiation Effects 0.000 claims 6
- 239000003960 organic solvent Substances 0.000 claims 5
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims 3
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 3
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 3
- 102000000070 Sodium-Glucose Transport Proteins Human genes 0.000 claims 2
- 108010080361 Sodium-Glucose Transport Proteins Proteins 0.000 claims 2
- 230000036765 blood level Effects 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 238000000634 powder X-ray diffraction Methods 0.000 claims 2
- 239000002904 solvent Substances 0.000 claims 2
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 2
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000002249 Diabetes Complications Diseases 0.000 claims 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 1
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 1
- 206010012655 Diabetic complications Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 206010060378 Hyperinsulinaemia Diseases 0.000 claims 1
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 230000003111 delayed effect Effects 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 208000033679 diabetic kidney disease Diseases 0.000 claims 1
- 235000014113 dietary fatty acids Nutrition 0.000 claims 1
- 238000000113 differential scanning calorimetry Methods 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 239000000194 fatty acid Substances 0.000 claims 1
- 229930195729 fatty acid Natural products 0.000 claims 1
- 150000004665 fatty acids Chemical class 0.000 claims 1
- 201000001421 hyperglycemia Diseases 0.000 claims 1
- 230000003451 hyperinsulinaemic effect Effects 0.000 claims 1
- 201000008980 hyperinsulinism Diseases 0.000 claims 1
- 208000006575 hypertriglyceridemia Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000002844 melting Methods 0.000 claims 1
- 230000008018 melting Effects 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- -1 or a hydrate thereof Substances 0.000 claims 1
- 230000001376 precipitating effect Effects 0.000 claims 1
- 102000004169 proteins and genes Human genes 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 238000001757 thermogravimetry curve Methods 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
- 230000029663 wound healing Effects 0.000 claims 1
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310556655.2A CN103554092A (zh) | 2013-11-11 | 2013-11-11 | 1-(β-D-吡喃葡糖基)-4-甲基-3-[5-(4-氟苯基)-2-噻吩基甲基]苯的新晶型B及其制备方法 |
| CN201310556655.2 | 2013-11-11 | ||
| CN201310617597.X | 2013-11-27 | ||
| CN201310617597.XA CN103588762A (zh) | 2013-11-27 | 2013-11-27 | 坎格列净的新晶型及其制备方法 |
| CN201410542984.6A CN104356121A (zh) | 2013-11-11 | 2014-10-14 | 1-(β-D-吡喃葡糖基)-4-甲基-3-[5-(4-氟苯基)-2-噻吩基甲基]苯的晶型B及其制备方法 |
| CN201410542984.6 | 2014-10-14 | ||
| CN201410593413.5A CN104356122B (zh) | 2013-11-27 | 2014-10-29 | 坎格列净的晶型及其制备方法 |
| CN201410593413.5 | 2014-10-29 | ||
| PCT/IB2014/003013 WO2015071761A2 (en) | 2013-11-11 | 2014-11-11 | Crystalline forms b, c, and d of canagliflozin |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016536321A JP2016536321A (ja) | 2016-11-24 |
| JP2016536321A5 true JP2016536321A5 (https=) | 2017-12-07 |
Family
ID=53141472
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016530967A Pending JP2016536321A (ja) | 2013-11-11 | 2014-11-11 | カナグリフロジンのｂ形結晶、ｃ形およびｄ形 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US20160280731A1 (https=) |
| EP (1) | EP3068779A4 (https=) |
| JP (1) | JP2016536321A (https=) |
| WO (1) | WO2015071761A2 (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015139386A1 (zh) | 2014-03-19 | 2015-09-24 | 杭州普晒医药科技有限公司 | 坎格列净一水合物及其晶型、它们的制备方法和用途 |
| WO2016016774A1 (en) * | 2014-07-31 | 2016-02-04 | Sun Pharmaceutical Industries Limited | Crystalline forms of canagliflozin |
| CN104530024B (zh) * | 2015-02-04 | 2017-08-08 | 上海迪赛诺药业有限公司 | 1‑(β‑D‑吡喃葡糖基)‑4‑甲基‑3‑[5‑(4‑氟苯基)‑2‑噻吩基甲基]苯的晶型及其制备方法 |
| ES2896101T3 (es) | 2015-09-15 | 2022-02-23 | Laurus Labs Ltd | Cocristales de inhibidores de SGLT2, procedimiento para su preparación y composiciones farmacéuticas de los mismos |
| CZ2015824A3 (cs) | 2015-11-20 | 2017-05-31 | Zentiva, K.S. | Krystalická forma Canagliflozinu a způsob její přípravy |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001051919A2 (en) * | 2000-01-07 | 2001-07-19 | Transform Pharmaceuticals, Inc. | High-throughput formation, identification, and analysis of diverse solid-forms |
| UY30730A1 (es) * | 2006-12-04 | 2008-07-03 | Mitsubishi Tanabe Pharma Corp | Forma cristalina del hemihidrato de 1-(b (beta)-d-glucopiranosil) -4-metil-3-[5-(4-fluorofenil) -2-tienilmetil]benceno |
| MX2010002695A (es) * | 2007-09-10 | 2010-04-01 | Janssen Pharmaceutica Nv | Proceso para la preparacion de compuestos utiles como inhibidores de transportador de glucosa dependiente de sodio (sglt). |
| SI2488515T1 (sl) * | 2009-10-14 | 2017-04-26 | Janssen Pharmaceutica Nv | Postopek za pripravo spojin, ki so uporabne kot inhibitorji SGLT2 |
| JP5596799B2 (ja) * | 2010-05-11 | 2014-09-24 | 田辺三菱製薬株式会社 | カナグリフロジン含有錠剤 |
| CA2911261A1 (en) * | 2013-05-08 | 2014-11-13 | Lek Pharmaceuticals D.D. | Novel crystalline hydrates of 1-(.beta.-d-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene |
| CN103588762A (zh) * | 2013-11-27 | 2014-02-19 | 苏州晶云药物科技有限公司 | 坎格列净的新晶型及其制备方法 |
| CN103554092A (zh) * | 2013-11-11 | 2014-02-05 | 苏州晶云药物科技有限公司 | 1-(β-D-吡喃葡糖基)-4-甲基-3-[5-(4-氟苯基)-2-噻吩基甲基]苯的新晶型B及其制备方法 |
| CN103980262B (zh) * | 2014-04-01 | 2016-06-22 | 天津大学 | 卡格列净的b晶型及其结晶制备方法 |
| CN104119324B (zh) * | 2014-07-23 | 2016-03-30 | 齐鲁天和惠世制药有限公司 | 一种卡格列净的制备方法 |
| WO2016016774A1 (en) * | 2014-07-31 | 2016-02-04 | Sun Pharmaceutical Industries Limited | Crystalline forms of canagliflozin |
-
2014
- 2014-11-11 US US15/035,751 patent/US20160280731A1/en not_active Abandoned
- 2014-11-11 WO PCT/IB2014/003013 patent/WO2015071761A2/en not_active Ceased
- 2014-11-11 JP JP2016530967A patent/JP2016536321A/ja active Pending
- 2014-11-11 EP EP14862830.8A patent/EP3068779A4/en not_active Withdrawn