DK3351539T3 - Krystallinsk monohydratkompleks af 1-cyan-2-(4-cyklopropyl-benzyl)-4-(beta-d-glucopyranos-1-yl)-benzen og prolin i krystalvand (1:1:1), fremgangsmåder til fremstilling deraf og dets anvendelse som SGLT-hæmmer - Google Patents
Krystallinsk monohydratkompleks af 1-cyan-2-(4-cyklopropyl-benzyl)-4-(beta-d-glucopyranos-1-yl)-benzen og prolin i krystalvand (1:1:1), fremgangsmåder til fremstilling deraf og dets anvendelse som SGLT-hæmmer Download PDFInfo
- Publication number
- DK3351539T3 DK3351539T3 DK18155079.9T DK18155079T DK3351539T3 DK 3351539 T3 DK3351539 T3 DK 3351539T3 DK 18155079 T DK18155079 T DK 18155079T DK 3351539 T3 DK3351539 T3 DK 3351539T3
- Authority
- DK
- Denmark
- Prior art keywords
- glucopyranos
- proline
- cyclopropyl
- cyano
- beta
- Prior art date
Links
- 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
- ONIBWKKTOPOVIA-BYPYZUCNSA-N L-Proline Chemical compound OC(=O)[C@@H]1CCCN1 ONIBWKKTOPOVIA-BYPYZUCNSA-N 0.000 title 1
- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 title 1
- 239000013078 crystal Substances 0.000 title 1
- 150000004682 monohydrates Chemical class 0.000 title 1
- 229940121377 sodium-glucose co-transporter inhibitor Drugs 0.000 title 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 title 1
Classifications
-
- 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)
- Pyrane Compounds (AREA)
- Saccharide Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12177944 | 2012-07-26 | ||
| EP13740309.3A EP2877460B1 (en) | 2012-07-26 | 2013-07-25 | 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 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK3351539T3 true DK3351539T3 (da) | 2023-01-30 |
Family
ID=48874313
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK18155079.9T DK3351539T3 (da) | 2012-07-26 | 2013-07-25 | Krystallinsk monohydratkompleks af 1-cyan-2-(4-cyklopropyl-benzyl)-4-(beta-d-glucopyranos-1-yl)-benzen og prolin i krystalvand (1:1:1), fremgangsmåder til fremstilling deraf og dets anvendelse som SGLT-hæmmer |
| DK13740309.3T DK2877460T3 (en) | 2012-07-26 | 2013-07-25 | 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. |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK13740309.3T DK2877460T3 (en) | 2012-07-26 | 2013-07-25 | 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. |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US9145434B2 (enExample) |
| EP (3) | EP2877460B1 (enExample) |
| JP (2) | JP6538556B2 (enExample) |
| CN (2) | CN104470908A (enExample) |
| AR (1) | AR091908A1 (enExample) |
| AU (1) | AU2013294947B2 (enExample) |
| BR (1) | BR112015001327B1 (enExample) |
| CA (1) | CA2878698C (enExample) |
| DK (2) | DK3351539T3 (enExample) |
| EA (2) | EA025438B1 (enExample) |
| ES (2) | ES2694675T3 (enExample) |
| FI (1) | FI3351539T3 (enExample) |
| HR (2) | HRP20181972T1 (enExample) |
| HU (1) | HUE061450T2 (enExample) |
| LT (1) | LT3351539T (enExample) |
| MX (1) | MX357906B (enExample) |
| PL (2) | PL2877460T3 (enExample) |
| PT (2) | PT2877460T (enExample) |
| RS (1) | RS63881B1 (enExample) |
| SG (1) | SG11201500574QA (enExample) |
| SI (2) | SI3351539T1 (enExample) |
| TW (1) | TW201418275A (enExample) |
| WO (1) | WO2014016381A1 (enExample) |
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 |
| EP4245765A3 (en) | 2013-04-04 | 2024-03-20 | Boehringer Ingelheim Vetmedica GmbH | Treatment of metabolic disorders in equine animals |
| ES2969764T3 (es) | 2013-12-17 | 2024-05-22 | Boehringer Ingelheim Vetmedica Gmbh | Un inhibidor de SGLT-2 para usar en el tratamiento de un trastorno metabólico en animales felinos |
| CN115282284A (zh) | 2014-01-23 | 2022-11-04 | 勃林格殷格翰动物保健有限公司 | 犬科动物中代谢紊乱的治疗 |
| ES2811261T3 (es) | 2014-04-01 | 2021-03-11 | Boehringer Ingelheim Vetmedica Gmbh | Tratamiento de trastornos metabólicos en animales equinos |
| 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 |
| HUE068152T2 (hu) | 2014-09-25 | 2024-12-28 | Boehringer Ingelheim Vetmedica Gmbh | SGLT2-gátlók és dopamin agonisták kombinációs kezelése anyagcserezavarok megelõzésére lófélékben |
| PL3202772T3 (pl) * | 2014-09-30 | 2021-02-22 | Jiangsu Hengrui Medicine Co. Ltd. | Kryształ kompleksu inhibitora l-proliny/glukozy sodowej 2 |
| CZ2015110A3 (cs) * | 2015-02-18 | 2016-08-31 | Zentiva, K.S. | Pevné formy empagliflozinu |
| MX389367B (es) | 2015-08-27 | 2025-03-20 | Boehringer Ingelheim Vetmedica Gmbh | Composiciones farmaceuticas liquidas que comprenden inhibidores de sglt-2. |
| WO2017203457A1 (en) * | 2016-05-26 | 2017-11-30 | Dr. Reddy's Laboratories Limited | Solid state forms of empagliflozin |
| CN109476624B (zh) | 2016-05-28 | 2021-07-09 | 吉林惠升生物制药有限公司 | 钠-葡萄糖协同转运蛋白2抑制剂的晶型 |
| CN111511725B (zh) | 2017-12-19 | 2024-04-09 | 勃林格殷格翰维特梅迪卡有限公司 | 1-氰基-2-(4-环丙基-苄基)-4-(β-D-吡喃葡萄糖-1-基)-苯、L-脯氨酸和水的1:1:1共晶体的合成 |
| CN114727624A (zh) | 2019-11-28 | 2022-07-08 | 勃林格殷格翰动物保健有限公司 | Sglt-2抑制剂在非人哺乳动物的停奶中的用途 |
| KR20220143732A (ko) | 2020-02-17 | 2022-10-25 | 베링거잉겔하임베트메디카게엠베하 | 고양이과에서 심장 질환을 예방 및/또는 치료하기 위한 sglt-2 억제제의 사용 |
| 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. |
| 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 |
| MX2024001185A (es) | 2021-07-28 | 2024-02-27 | Boehringer Ingelheim Vetmedica Gmbh | Uso de inhibidores de sglt-2 para la prevencion y/o tratamiento de enfermedades renales en mamiferos no humanos. |
| EP4531810A1 (en) | 2022-05-25 | 2025-04-09 | Boehringer Ingelheim Vetmedica GmbH | Aqueous pharmaceutical compositions comprising sglt-2 inhibitors |
| US20240307628A1 (en) | 2023-03-06 | 2024-09-19 | Boehringer Ingelheim Vetmedica Gmbh | Systems and methods for delivery of liquid pharmaceutical compositions in particular comprising one or more sglt-2 inhibitor(s) |
| EP4702012A1 (en) | 2023-04-24 | 2026-03-04 | Boehringer Ingelheim Vetmedica GmbH | Crystalline complexes between velagliflozin and selected co-crystal forming agents, methods for their preparation and the use thereof for preparing medicaments |
| WO2024240632A1 (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 |
| KR20260019532A (ko) | 2023-05-24 | 2026-02-10 | 베링거잉겔하임베트메디카게엠베하 | 하나 이상의 sglt-2 억제제와 텔미사르탄을 포함하는 비인간 포유류의 신장 질환 및/또는 고혈압의 병용 치료 및/또는 예방 |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2258141T3 (es) | 2001-04-11 | 2006-08-16 | Bristol-Myers Squibb Company | Complejos de aminoacidos de glucosidos c-arilo para el tratamiento de la diabetes y procedimiento. |
| US7927613B2 (en) * | 2002-02-15 | 2011-04-19 | University Of South Florida | Pharmaceutical co-crystal compositions |
| AU2003299966A1 (en) * | 2003-01-03 | 2004-08-10 | Bristol-Myers Squibb Company | Methods of producing c-aryl glucoside sglt2 inhibitors |
| EP2360165A3 (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 |
| CN101238112A (zh) * | 2005-09-08 | 2008-08-06 | 贝林格尔·英格海姆国际有限公司 | 1-氯-4-(β-D-吡喃葡萄糖-1-基)-2-(4-乙炔基-苄基)-苯的晶形、其制备方法及其用于制备药物中的用途 |
| AU2007216452A1 (en) * | 2006-02-15 | 2007-08-23 | 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 |
| AR065809A1 (es) | 2007-03-22 | 2009-07-01 | Bristol Myers Squibb Co | Formulaciones farmaceuticas que contienen un inhibidor sglt2 |
| JP2010528023A (ja) * | 2007-05-18 | 2010-08-19 | ブリストル−マイヤーズ スクイブ カンパニー | Ｓｇｌｔ２阻害剤の結晶構造およびその製造方法 |
| 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 |
| PT2324002T (pt) * | 2008-08-22 | 2016-11-09 | Theracos Sub Llc | Processos para a preparação de inibidores de sglt2 |
| MX2011002166A (es) | 2008-08-28 | 2011-04-07 | Pfizer | Derivados de dioxa-biciclo[3.2.1]octano-2,3,1-triol. |
| 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 |
| EP4245765A3 (en) | 2013-04-04 | 2024-03-20 | Boehringer Ingelheim Vetmedica GmbH | Treatment of metabolic disorders in equine animals |
-
2013
- 2013-07-23 US US13/948,751 patent/US9145434B2/en active Active
- 2013-07-25 HR HRP20181972TT patent/HRP20181972T1/hr unknown
- 2013-07-25 EA EA201500038A patent/EA025438B1/ru not_active IP Right Cessation
- 2013-07-25 CA CA2878698A patent/CA2878698C/en active Active
- 2013-07-25 SG SG11201500574QA patent/SG11201500574QA/en unknown
- 2013-07-25 PT PT13740309T patent/PT2877460T/pt unknown
- 2013-07-25 PL PL13740309T patent/PL2877460T3/pl unknown
- 2013-07-25 RS RS20230025A patent/RS63881B1/sr unknown
- 2013-07-25 HU HUE18155079A patent/HUE061450T2/hu unknown
- 2013-07-25 SI SI201332031T patent/SI3351539T1/sl unknown
- 2013-07-25 HR HRP20230081TT patent/HRP20230081T1/hr unknown
- 2013-07-25 LT LTEP18155079.9T patent/LT3351539T/lt unknown
- 2013-07-25 DK DK18155079.9T patent/DK3351539T3/da active
- 2013-07-25 CN CN201380037186.1A patent/CN104470908A/zh active Pending
- 2013-07-25 DK DK13740309.3T patent/DK2877460T3/en active
- 2013-07-25 EP EP13740309.3A patent/EP2877460B1/en active Active
- 2013-07-25 AR ARP130102660A patent/AR091908A1/es unknown
- 2013-07-25 SI SI201331237T patent/SI2877460T1/sl unknown
- 2013-07-25 TW TW102126724A patent/TW201418275A/zh unknown
- 2013-07-25 PT PT181550799T patent/PT3351539T/pt unknown
- 2013-07-25 ES ES13740309.3T patent/ES2694675T3/es active Active
- 2013-07-25 EA EA201600506A patent/EA201600506A1/ru unknown
- 2013-07-25 AU AU2013294947A patent/AU2013294947B2/en active Active
- 2013-07-25 JP JP2015523552A patent/JP6538556B2/ja active Active
- 2013-07-25 WO PCT/EP2013/065736 patent/WO2014016381A1/en not_active Ceased
- 2013-07-25 MX MX2015000962A patent/MX357906B/es active IP Right Grant
- 2013-07-25 ES ES18155079T patent/ES2937665T3/es active Active
- 2013-07-25 PL PL18155079.9T patent/PL3351539T3/pl unknown
- 2013-07-25 EP EP18155079.9A patent/EP3351539B1/en active Active
- 2013-07-25 BR BR112015001327-9A patent/BR112015001327B1/pt active IP Right Grant
- 2013-07-25 CN CN201810468431.9A patent/CN108774200A/zh active Pending
- 2013-07-25 EP EP22202153.7A patent/EP4166548A1/en active Pending
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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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