FI3351539T3 - Kiteinen monohydraattikompleksi 1-syaani-2-(4-syklopropyylibentsyyli)-4-(ß-D-glukopyranos-1-yyli)bentseenistä ja L-proliinista kidevedessä (1:1:1), menetelmät sen valmistamiseksi ja sen käyttö SGLT-estäjänä - Google Patents
Kiteinen monohydraattikompleksi 1-syaani-2-(4-syklopropyylibentsyyli)-4-(ß-D-glukopyranos-1-yyli)bentseenistä ja L-proliinista kidevedessä (1:1:1), menetelmät sen valmistamiseksi ja sen käyttö SGLT-estäjänä Download PDFInfo
- Publication number
- FI3351539T3 FI3351539T3 FIEP18155079.9T FI18155079T FI3351539T3 FI 3351539 T3 FI3351539 T3 FI 3351539T3 FI 18155079 T FI18155079 T FI 18155079T FI 3351539 T3 FI3351539 T3 FI 3351539T3
- Authority
- FI
- Finland
- Prior art keywords
- degrees
- diffraction pattern
- powder diffraction
- ray powder
- proline
- Prior art date
Links
- ONIBWKKTOPOVIA-BYPYZUCNSA-N L-Proline Chemical compound OC(=O)[C@@H]1CCCN1 ONIBWKKTOPOVIA-BYPYZUCNSA-N 0.000 title claims 4
- 239000013078 crystal Substances 0.000 title claims 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 title claims 2
- PESZPPAQWQMZAM-XNBWIAOKSA-N 2-[(4-cyclopropylphenyl)methyl]-4-[(2r,3r,4s,5s,6r)-2,3,4,5-tetrahydroxy-6-(hydroxymethyl)oxan-2-yl]benzonitrile Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@]1(O)C1=CC=C(C#N)C(CC=2C=CC(=CC=2)C2CC2)=C1 PESZPPAQWQMZAM-XNBWIAOKSA-N 0.000 title 1
- 150000004682 monohydrates Chemical class 0.000 title 1
- 229940121377 sodium-glucose co-transporter inhibitor Drugs 0.000 title 1
- 238000000634 powder X-ray diffraction Methods 0.000 claims 10
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 claims 9
- 230000005855 radiation Effects 0.000 claims 5
- 229930182821 L-proline Natural products 0.000 claims 3
- 229960002429 proline Drugs 0.000 claims 3
- 229940024606 amino acid Drugs 0.000 claims 2
- 150000001413 amino acids Chemical class 0.000 claims 2
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
- C07H15/26—Acyclic or carbocyclic radicals, substituted by hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
- C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D309/10—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H7/00—Compounds containing non-saccharide radicals linked to saccharide radicals by a carbon-to-carbon bond
- C07H7/04—Carbocyclic radicals
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Diabetes (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Hematology (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Emergency Medicine (AREA)
- Obesity (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Endocrinology (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Pyrane Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12177944 | 2012-07-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| FI3351539T3 true FI3351539T3 (fi) | 2023-02-19 |
Family
ID=48874313
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| FIEP18155079.9T FI3351539T3 (fi) | 2012-07-26 | 2022-07-25 | Kiteinen monohydraattikompleksi 1-syaani-2-(4-syklopropyylibentsyyli)-4-(ß-D-glukopyranos-1-yyli)bentseenistä ja L-proliinista kidevedessä (1:1:1), menetelmät sen valmistamiseksi ja sen käyttö SGLT-estäjänä |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US9145434B2 (OSRAM) |
| EP (3) | EP4166548A1 (OSRAM) |
| JP (2) | JP6538556B2 (OSRAM) |
| CN (2) | CN104470908A (OSRAM) |
| AR (1) | AR091908A1 (OSRAM) |
| AU (1) | AU2013294947B2 (OSRAM) |
| BR (1) | BR112015001327B1 (OSRAM) |
| CA (1) | CA2878698C (OSRAM) |
| DK (2) | DK2877460T3 (OSRAM) |
| EA (2) | EA201600506A1 (OSRAM) |
| ES (2) | ES2694675T3 (OSRAM) |
| FI (1) | FI3351539T3 (OSRAM) |
| HR (2) | HRP20230081T1 (OSRAM) |
| HU (1) | HUE061450T2 (OSRAM) |
| LT (1) | LT3351539T (OSRAM) |
| MX (1) | MX357906B (OSRAM) |
| PL (2) | PL2877460T3 (OSRAM) |
| PT (2) | PT2877460T (OSRAM) |
| RS (1) | RS63881B1 (OSRAM) |
| SG (1) | SG11201500574QA (OSRAM) |
| SI (2) | SI3351539T1 (OSRAM) |
| TW (1) | TW201418275A (OSRAM) |
| WO (1) | WO2014016381A1 (OSRAM) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9145434B2 (en) | 2012-07-26 | 2015-09-29 | Boehringer Ingelheim International Gmbh | Crystalline complex of 1-cyano-2-(4-cyclopropyl-benzyl)-4-(ss-d-glucopyranos-1-yl)-benzene, methods for its preparation and the use thereof for preparing medicaments |
| WO2014161836A1 (en) | 2013-04-04 | 2014-10-09 | Boehringer Ingelheim Vetmedica Gmbh | Treatment of metabolic disorders in equine animals |
| CN105828815B (zh) * | 2013-12-17 | 2020-03-27 | 勃林格殷格翰动物保健有限公司 | 猫科动物中代谢紊乱的治疗 |
| ES2951127T3 (es) | 2014-01-23 | 2023-10-18 | Boehringer Ingelheim Vetmedica Gmbh | Inhibidores de SGLT2 para el tratamiento de trastornos metabólicos en animales caninos |
| AU2015239655B2 (en) | 2014-04-01 | 2019-10-24 | Boehringer Ingelheim Vetmedica Gmbh | Treatment of metabolic disorders in equine animals |
| CN103965020B (zh) * | 2014-05-06 | 2015-09-09 | 启东东岳药业有限公司 | 制备5-碘-2-溴苄醇的方法 |
| NZ728804A (en) | 2014-09-25 | 2022-10-28 | Boehringer Ingelheim Vetmedica Gmbh | Combination treatment of sglt2 inhibitors and dopamine agonists for preventing metabolic disorders in equine animals |
| BR112017005454A2 (pt) * | 2014-09-30 | 2017-12-12 | Jiangsu Hengrui Medicine Co | composto de l-prolina do inibidor 2 do cotransportador de sódio-glicose, e mono-hidrato e cristal do composto de l-prolina |
| CZ2015110A3 (cs) * | 2015-02-18 | 2016-08-31 | Zentiva, K.S. | Pevné formy empagliflozinu |
| RS66325B1 (sr) | 2015-08-27 | 2025-01-31 | Boehringer Ingelheim Vetmedica Gmbh | Tečne farmaceutske kompozicije koje obuhvataju inhibitore sglt 2 |
| WO2017203457A1 (en) * | 2016-05-26 | 2017-11-30 | Dr. Reddy's Laboratories Limited | Solid state forms of empagliflozin |
| EP3466940B1 (en) | 2016-05-28 | 2021-11-17 | Ji Lin Hui Sheng Bio-Pharmaceutical Co., Ltd. | Crystal form of sodium-glucose cotransporter 2 inhibitor |
| JP2021506962A (ja) | 2017-12-19 | 2021-02-22 | ベーリンガー インゲルハイム フェトメディカ ゲーエムベーハーＢｏｅｈｒｉｎｇｅｒ Ｉｎｇｅｌｈｅｉｍ Ｖｅｔｍｅｄｉｃａ ＧｍｂＨ | １−シアノ−２−（４−シクロプロピル−ベンジル）−４−（β−Ｄ−グルコピラノス−１−イル）−ベンゼン、Ｌ−プロリンおよび水からなる１：１：１共結晶の合成 |
| AU2020394498A1 (en) | 2019-11-28 | 2022-06-09 | Boehringer Ingelheim Vetmedica Gmbh | Use of SGLT-2 inhibitors in the drying-off of non-human mammals |
| AU2021222297A1 (en) | 2020-02-17 | 2022-08-04 | Boehringer Ingelheim Vetmedica Gmbh | Use of SGLT-2 inhibitors for the prevention and/or treatment of cardiac diseases in felines |
| MX2024001184A (es) | 2021-07-28 | 2024-02-27 | Boehringer Ingelheim Vetmedica Gmbh | Uso de inhibidores de sglt-2 para la prevencion y/o tratamiento de cardiopatias en mamiferos no humanos, que excluye felinos, en particular, caninos. |
| US20240307426A1 (en) | 2021-07-28 | 2024-09-19 | Boehringer Ingelheim Vetmedica Gmbh | Use of sglt-2 inhibitors for the prevention and/or treatment of renal diseases in non-human mammals |
| EP4376819A1 (en) | 2021-07-28 | 2024-06-05 | Boehringer Ingelheim Vetmedica GmbH | Use of sglt-2 inhibitors for the prevention and/or treatment of hypertension in non-human mammals |
| US20230381101A1 (en) | 2022-05-25 | 2023-11-30 | Boehringer Ingelheim Vetmedica Gmbh | Aqueous pharmaceutical compositions comprising sglt-2 inhibitors |
| WO2024184293A1 (en) | 2023-03-06 | 2024-09-12 | Boehringer Ingelheim Vetmedica Gmbh | Systems for delivery of liquid pharmaceutical compositions in particular comprising one or more sglt-2 inhibitor(s) |
| CN121039113A (zh) | 2023-04-24 | 2025-11-28 | 勃林格殷格翰动物保健有限公司 | 维格列净与所选共晶形成剂的结晶复合物、其制备方法及其在制备药物中的用途 |
| US20240390317A1 (en) | 2023-05-24 | 2024-11-28 | Boehringer Ingelheim Vetmedica Gmbh | Combination treatment and/or prevention of cardiac diseases in non-human mammals comprising one or more sglt-2 inhibitors and pimobendan and/or telmisartan |
| WO2024240633A1 (en) | 2023-05-24 | 2024-11-28 | Boehringer Ingelheim Vetmedica Gmbh | Combination treatment and/or prevention of renal diseases and/or hypertension in non-human mammals comprising one or more sglt-2 inhibitors and telmisartan |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2444481A1 (en) * | 2001-04-11 | 2002-10-24 | Bristol-Myers Squibb Company | Amino acid complexes of c-aryl glucosides for treatment of diabetes and method |
| US7927613B2 (en) * | 2002-02-15 | 2011-04-19 | University Of South Florida | Pharmaceutical co-crystal compositions |
| EP1581543A4 (en) * | 2003-01-03 | 2008-03-19 | Bristol Myers Squibb Co | METHODS FOR PRODUCING SGLT2 GLYCOSIS C-ARYL INHIBITORS |
| EP2360164A3 (de) * | 2004-03-16 | 2012-01-04 | Boehringer Ingelheim International GmbH | Glucopyranosyl-substituierte Benzol-Derivate, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
| NZ566787A (en) * | 2005-09-08 | 2010-02-26 | Boehringer Ingelheim Int | Crystalline forms of 1-chloro-4-(beta-D-glucopyranos-1-yl)-2-(4-ethynyl-benzyl)-benzene, methods for its preparation and the use thereof for preparing medicaments |
| EP1989191B1 (en) * | 2006-02-15 | 2011-07-20 | Boehringer Ingelheim International GmbH | Glucopyranosyl-substituted benzonitrile derivatives, pharmaceutical compositions containing such compounds, their use and process for their manufacture |
| TWI370818B (en) * | 2006-04-05 | 2012-08-21 | Astellas Pharma Inc | Cocrystal of c-glycoside derivative and l-proline |
| PE20080697A1 (es) * | 2006-05-03 | 2008-08-05 | Boehringer Ingelheim Int | Derivados de benzonitrilo sustituidos con glucopiranosilo, composiciones farmaceuticas que contienen compuestos de este tipo, su uso y procedimiento para su fabricacion |
| US7919598B2 (en) * | 2006-06-28 | 2011-04-05 | Bristol-Myers Squibb Company | Crystal structures of SGLT2 inhibitors and processes for preparing same |
| TW200817424A (en) | 2006-08-04 | 2008-04-16 | Daiichi Sankyo Co Ltd | Benzylphenyl glucopyranoside derivatives |
| TW200904405A (en) | 2007-03-22 | 2009-02-01 | Bristol Myers Squibb Co | Pharmaceutical formulations containing an SGLT2 inhibitor |
| EP2147008A2 (en) * | 2007-05-18 | 2010-01-27 | Bristol-Myers Squibb Company | Crystal structures of sglt2 inhibitors and processes for preparing same |
| CN101468976B (zh) * | 2007-12-27 | 2013-11-20 | 百时美施贵宝公司 | Sglt2抑制剂的晶体结构及其制备方法 |
| TWI482779B (zh) * | 2008-08-22 | 2015-05-01 | Theracos Inc | Ｓｇｌｔ２抑制劑之結晶型 |
| CN102149717B (zh) | 2008-08-28 | 2014-05-14 | 辉瑞大药厂 | 二氧杂-双环[3.2.1]辛烷-2，3，4-三醇衍生物 |
| WO2010048358A2 (en) | 2008-10-22 | 2010-04-29 | Auspex Pharmaceutical, Inc. | Ethoxyphenylmethyl inhibitors of sglt2 |
| WO2011153712A1 (en) * | 2010-06-12 | 2011-12-15 | Theracos, Inc. | Crystalline form of benzylbenzene sglt2 inhibitor |
| US9145434B2 (en) | 2012-07-26 | 2015-09-29 | Boehringer Ingelheim International Gmbh | Crystalline complex of 1-cyano-2-(4-cyclopropyl-benzyl)-4-(ss-d-glucopyranos-1-yl)-benzene, methods for its preparation and the use thereof for preparing medicaments |
| WO2014161836A1 (en) | 2013-04-04 | 2014-10-09 | Boehringer Ingelheim Vetmedica Gmbh | Treatment of metabolic disorders in equine animals |
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2013
- 2013-07-23 US US13/948,751 patent/US9145434B2/en active Active
- 2013-07-25 EA EA201600506A patent/EA201600506A1/ru unknown
- 2013-07-25 SG SG11201500574QA patent/SG11201500574QA/en unknown
- 2013-07-25 MX MX2015000962A patent/MX357906B/es active IP Right Grant
- 2013-07-25 PT PT13740309T patent/PT2877460T/pt unknown
- 2013-07-25 BR BR112015001327-9A patent/BR112015001327B1/pt active IP Right Grant
- 2013-07-25 TW TW102126724A patent/TW201418275A/zh unknown
- 2013-07-25 EP EP22202153.7A patent/EP4166548A1/en active Pending
- 2013-07-25 EP EP18155079.9A patent/EP3351539B1/en active Active
- 2013-07-25 HU HUE18155079A patent/HUE061450T2/hu unknown
- 2013-07-25 HR HRP20230081TT patent/HRP20230081T1/hr unknown
- 2013-07-25 LT LTEP18155079.9T patent/LT3351539T/lt unknown
- 2013-07-25 PL PL13740309T patent/PL2877460T3/pl unknown
- 2013-07-25 AU AU2013294947A patent/AU2013294947B2/en active Active
- 2013-07-25 SI SI201332031T patent/SI3351539T1/sl unknown
- 2013-07-25 ES ES13740309.3T patent/ES2694675T3/es active Active
- 2013-07-25 CN CN201380037186.1A patent/CN104470908A/zh active Pending
- 2013-07-25 HR HRP20181972TT patent/HRP20181972T1/hr unknown
- 2013-07-25 AR ARP130102660A patent/AR091908A1/es unknown
- 2013-07-25 SI SI201331237T patent/SI2877460T1/sl unknown
- 2013-07-25 PL PL18155079.9T patent/PL3351539T3/pl unknown
- 2013-07-25 EP EP13740309.3A patent/EP2877460B1/en active Active
- 2013-07-25 CN CN201810468431.9A patent/CN108774200A/zh active Pending
- 2013-07-25 WO PCT/EP2013/065736 patent/WO2014016381A1/en not_active Ceased
- 2013-07-25 DK DK13740309.3T patent/DK2877460T3/en active
- 2013-07-25 JP JP2015523552A patent/JP6538556B2/ja active Active
- 2013-07-25 RS RS20230025A patent/RS63881B1/sr unknown
- 2013-07-25 EA EA201500038A patent/EA025438B1/ru not_active IP Right Cessation
- 2013-07-25 ES ES18155079T patent/ES2937665T3/es active Active
- 2013-07-25 CA CA2878698A patent/CA2878698C/en active Active
- 2013-07-25 DK DK18155079.9T patent/DK3351539T3/da active
- 2013-07-25 PT PT181550799T patent/PT3351539T/pt unknown
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2018
- 2018-05-08 JP JP2018089968A patent/JP2018135384A/ja active Pending
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2022
- 2022-07-25 FI FIEP18155079.9T patent/FI3351539T3/fi active
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