JP2009507809A5 - - Google Patents
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- Publication number
- JP2009507809A5 JP2009507809A5 JP2008529633A JP2008529633A JP2009507809A5 JP 2009507809 A5 JP2009507809 A5 JP 2009507809A5 JP 2008529633 A JP2008529633 A JP 2008529633A JP 2008529633 A JP2008529633 A JP 2008529633A JP 2009507809 A5 JP2009507809 A5 JP 2009507809A5
- Authority
- JP
- Japan
- Prior art keywords
- crystal
- glucopyranos
- ethynyl
- chloro
- benzyl
- 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.)
- Granted
Links
- 239000013078 crystal Substances 0.000 claims 12
- 239000002904 solvent Substances 0.000 claims 10
- 238000000634 powder X-ray diffraction Methods 0.000 claims 8
- GXGRVEFOJXINFI-YMQHIKHWSA-N (2r,3r,4s,5s,6r)-2-[4-chloro-3-[(4-ethynylphenyl)methyl]phenyl]-6-(hydroxymethyl)oxane-2,3,4,5-tetrol Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@]1(O)C1=CC=C(Cl)C(CC=2C=CC(=CC=2)C#C)=C1 GXGRVEFOJXINFI-YMQHIKHWSA-N 0.000 claims 7
- 239000000203 mixture Substances 0.000 claims 5
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 239000002244 precipitate Substances 0.000 claims 4
- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 claims 3
- 150000001413 amino acids Chemical class 0.000 claims 3
- 150000004677 hydrates Chemical class 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- -1 β-D-glucopyranos-1-yl Chemical group 0.000 claims 3
- ONIBWKKTOPOVIA-BYPYZUCNSA-N L-Proline Chemical compound OC(=O)[C@@H]1CCCN1 ONIBWKKTOPOVIA-BYPYZUCNSA-N 0.000 claims 2
- 238000001035 drying Methods 0.000 claims 2
- 208000030159 metabolic disease Diseases 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 2
- 208000010444 Acidosis Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 206010007558 Cardiac failure chronic Diseases 0.000 claims 1
- 208000002249 Diabetes Complications Diseases 0.000 claims 1
- 206010012655 Diabetic complications Diseases 0.000 claims 1
- 208000032928 Dyslipidaemia Diseases 0.000 claims 1
- 206010060378 Hyperinsulinaemia Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 201000001431 Hyperuricemia Diseases 0.000 claims 1
- 208000013016 Hypoglycemia Diseases 0.000 claims 1
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
- 208000007976 Ketosis Diseases 0.000 claims 1
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 206010027417 Metabolic acidosis Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 206010030113 Oedema Diseases 0.000 claims 1
- 108091006269 SLC5A2 Proteins 0.000 claims 1
- 102100020888 Sodium/glucose cotransporter 2 Human genes 0.000 claims 1
- 102100037202 Sodium/myo-inositol cotransporter 2 Human genes 0.000 claims 1
- 101710090560 Sodium/myo-inositol cotransporter 2 Proteins 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 239000002131 composite material Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 208000018914 glucose metabolism disease Diseases 0.000 claims 1
- 230000003451 hyperinsulinaemic effect Effects 0.000 claims 1
- 201000008980 hyperinsulinism Diseases 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000004140 ketosis Effects 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 239000000047 product Substances 0.000 claims 1
- 230000005855 radiation Effects 0.000 claims 1
- 239000007858 starting material Substances 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP05019527 | 2005-09-08 | ||
| EP05019527.0 | 2005-09-08 | ||
| PCT/EP2006/066107 WO2007028814A1 (en) | 2005-09-08 | 2006-09-07 | CRYSTALLINE FORMS OF 1-CHLORO-4-(ß-D-GLUCOPYRANOS-1-YL)-2-(4-ETHYNYL-BENZYL)-BENZENE, METHODS FOR ITS PREPARATION AND THE USE THEREOF FOR PREPARING MEDICAMENTS |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2009507809A JP2009507809A (ja) | 2009-02-26 |
| JP2009507809A5 true JP2009507809A5 (enExample) | 2009-10-22 |
| JP5345846B2 JP5345846B2 (ja) | 2013-11-20 |
Family
ID=37478909
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008529633A Active JP5345846B2 (ja) | 2005-09-08 | 2006-09-07 | 1−クロロ−4−(β−D−グルコピラノス−1−イル)−2−(4−エチニル−ベンジル)−ベンゼンの結晶形態、その製造方法及び薬剤製造のためのそれらの使用 |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US8507450B2 (enExample) |
| EP (1) | EP1926720B1 (enExample) |
| JP (1) | JP5345846B2 (enExample) |
| KR (1) | KR20080053369A (enExample) |
| CN (1) | CN101238112A (enExample) |
| AR (1) | AR056055A1 (enExample) |
| AT (1) | ATE491700T1 (enExample) |
| AU (1) | AU2006289093A1 (enExample) |
| BR (1) | BRPI0615882A2 (enExample) |
| CA (1) | CA2621314A1 (enExample) |
| DE (1) | DE602006018961D1 (enExample) |
| ES (1) | ES2358051T3 (enExample) |
| IL (1) | IL189950A0 (enExample) |
| MX (1) | MX2008002457A (enExample) |
| NZ (1) | NZ566787A (enExample) |
| RU (1) | RU2008113050A (enExample) |
| TW (1) | TW200745075A (enExample) |
| WO (1) | WO2007028814A1 (enExample) |
| ZA (1) | ZA200800681B (enExample) |
Families Citing this family (73)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103435581B (zh) | 2004-03-16 | 2015-08-19 | 贝林格尔.英格海姆国际有限公司 | 吡喃葡萄糖基取代的苯基衍生物、含该化合物的药物、其用途及其制造方法 |
| ES2314743T3 (es) | 2004-12-16 | 2009-03-16 | Boehringer Ingelheim International Gmbh | Derivados de benceno sustituidos con glucopiranosilo, medicamentos que contienen a este tipo de compuestos, su uso y procedimiento para su fabricacion. |
| EP1856082B1 (en) | 2005-02-23 | 2009-10-14 | Boehringer Ingelheim International GmbH | Glucopyranosyl-substituted ((hetero)arylethynyl-benzyl)-benzene derivatives and use thereof as sodium-dependent glucose cotransporter 2 (sglt2) inhibitors |
| CA2605245A1 (en) | 2005-04-15 | 2006-10-19 | Boehringer Ingelheim International Gmbh | Glucopyranosyl-substituted (heteroaryloxy-benzyl)-benzene derivatives as sglt inhibitors |
| UA91546C2 (uk) * | 2005-05-03 | 2010-08-10 | Бьорінгер Інгельхайм Інтернаціональ Гмбх | КРИСТАЛІЧНА ФОРМА 1-ХЛОР-4-(β-D-ГЛЮКОПІРАНОЗ-1-ИЛ)-2-[4-((S)-ТЕТРАГІДРОФУРАН-3-ІЛОКСИ)-БЕНЗИЛ]-БЕНЗОЛУ, СПОСІБ ЇЇ ОДЕРЖАННЯ ТА ЇЇ ЗАСТОСУВАННЯ ПРИ ПРИГОТУВАННІ ЛІКАРСЬКИХ ЗАСОБІВ |
| US7723309B2 (en) | 2005-05-03 | 2010-05-25 | Boehringer Ingelheim International Gmbh | Crystalline forms of 1-chloro-4-(β-D-glucopyranos-1-yl)-2-[4-((R)-tetrahydrofuran-3-yloxy)-benzyl]-benzene, a method for its preparation and the use thereof for preparing medicaments |
| US7772191B2 (en) | 2005-05-10 | 2010-08-10 | Boehringer Ingelheim International Gmbh | Processes for preparing of glucopyranosyl-substituted benzyl-benzene derivatives and intermediates therein |
| DE602006014411D1 (de) * | 2005-07-27 | 2010-07-01 | Boehringer Ingelheim Pharma | Glucopyranosyl-substituierte ((hetero)cycloalyklethynyl-benzyl)-benzenderivative und deren verwendung als inhibitoren des natriumabhängigen glucose-cotransporters (sglt) |
| EP1924571B1 (en) * | 2005-08-30 | 2010-10-13 | Boehringer Ingelheim International Gmbh | Glucopyranosyl-substituted benzyl-benzene derivatives, medicaments containing such compounds, their use and process for their manufacture |
| DE602006018961D1 (de) | 2005-09-08 | 2011-01-27 | Boehringer Ingelheim Pharma | KRISTALLINE FORMEN VON 1-CHLORO-4-(ß-D-GLUCOPYRANOS-1-YL)-2-(4-ETHYNYL-BENZYL)-BENZOL, ZUBEREITUNGSVERFAHREN DAFÜR UND DESSEN VERWENDUNG ZUR ARZNEIMITTELHERSTELLUNG |
| AR056195A1 (es) | 2005-09-15 | 2007-09-26 | Boehringer Ingelheim Int | Procedimientos para preparar derivados de (etinil-bencil)-benceno sustituidos de glucopiranosilo y compuestos intermedios de los mismos |
| EA200801773A1 (ru) * | 2006-02-15 | 2009-02-27 | Бёрингер Ингельхайм Интернациональ Гмбх | Глюкопиранозилзамещенные производные бензонитрила, фармацевтические композиции, содержащие такие соединения, их применение и способ их получения |
| 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 |
| US8039441B2 (en) * | 2006-08-15 | 2011-10-18 | Boehringer Ingelheim International Gmbh | Glucopyranosyl-substituted cyclopropylbenzene derivatives, pharmaceutical compositions containing such compounds, their use as SGLT inhibitors and process for their manufacture |
| EP2074130A1 (en) * | 2006-09-21 | 2009-07-01 | Boehringer Ingelheim International GmbH | Glucopyranosyl-substituted difluorobenzyl-benzene derivatives, medicaments containing such compounds, their use and process for their manufacture |
| US8283326B2 (en) * | 2006-10-27 | 2012-10-09 | Boehringer Ingelheim International Gmbh | Crystalline form of 4-(beta-D-glucopyranos-1-yl)-1-methyl-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene, a method for its preparation and the use thereof for preparing medicaments |
| TW200829258A (en) | 2006-11-06 | 2008-07-16 | Boehringer Ingelheim Int | Glucopyranosyl-substituted benzyl-benzonitrile derivatives, medicaments containing such compounds, their use and process for their manufacture |
| WO2008101939A1 (en) | 2007-02-21 | 2008-08-28 | Boehringer Ingelheim International Gmbh | Tetrasubstituted glucopyranosylated benzene derivatives, medicaments containing such compounds, their use and process for their manufacture |
| PE20090938A1 (es) * | 2007-08-16 | 2009-08-08 | Boehringer Ingelheim Int | Composicion farmaceutica que comprende un derivado de benceno sustituido con glucopiranosilo |
| EP3318562A3 (en) | 2007-08-23 | 2018-09-12 | Theracos Sub, LLC | Benzylbenzene derivatives and methods of use |
| UA101004C2 (en) | 2007-12-13 | 2013-02-25 | Теракос, Инк. | Derivatives of benzylphenylcyclohexane and use thereof |
| HRP20161648T1 (hr) | 2008-08-22 | 2017-02-10 | Theracos Sub, Llc | Postupak za pripravu sglt2 inhibitora |
| ATE540040T1 (de) * | 2008-08-28 | 2012-01-15 | Pfizer | Dioxabicycloä3.2.1üoctan-2,3,4-triolderivate |
| UY32427A (es) | 2009-02-13 | 2010-09-30 | Boheringer Ingelheim Internat Gmbh | Composicion farmaceutica, forma farmaceutica, procedimiento para su preparacion, metodos de tratamiento y usos de la misma |
| LT2395968T (lt) | 2009-02-13 | 2024-02-26 | Boehringer Ingelheim International Gmbh | Farmacinė kompozicija, apimanti gliukopiranozildifenilmetano darinius, jų farmacines dozavimo formas, jų gamybos būdą ir naudojimą patobulintai glikeminei kontrolei paciento organizme |
| SG173619A1 (en) | 2009-02-13 | 2011-09-29 | Boehringer Ingelheim Int | Pharmaceutical composition comprising a sglt2 inhibitor, a dpp-iv inhibitor and optionally a further antidiabetic agent and uses thereof |
| GEP20146120B (en) | 2009-02-13 | 2014-07-25 | Boehringer Ingelheim Int | Sglt-2 inhibitor for treating type i diabetes mellitus, type ii diabetes mellitus, impaired glucose tolerance or hyperglycemia |
| CN102574829B (zh) | 2009-09-30 | 2015-07-01 | 贝林格尔.英格海姆国际有限公司 | 吡喃葡萄糖基取代的苄基-苯衍生物的制备方法 |
| MX2012002942A (es) | 2009-09-30 | 2012-04-11 | Boehringer Ingelheim Int | Metodo para la preparacion de una forma cristalina de 1-cloro-4-(beta-d-glucopiranos-1-il)-2-(4-((s)-teteahidrofuran-3- iloxi)bencil)-benceno. |
| US10610489B2 (en) | 2009-10-02 | 2020-04-07 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, pharmaceutical dosage form, process for their preparation, methods for treating and uses thereof |
| ME02016B (me) | 2009-11-02 | 2015-05-20 | Pfizer | Derivati dioksabiciklo[3.2.1]oktan-2,3,4-triola |
| JP2013523681A (ja) | 2010-03-30 | 2013-06-17 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Sglt2インヒビター及びppar−ガンマアゴニストを含む医薬組成物並びにその使用 |
| WO2011153712A1 (en) | 2010-06-12 | 2011-12-15 | Theracos, Inc. | Crystalline form of benzylbenzene sglt2 inhibitor |
| WO2012041898A1 (en) | 2010-09-29 | 2012-04-05 | Celon Pharma Sp. Z O.O. | Combination of sglt2 inhibitor and a sugar compound for the treatment of diabetes |
| US20120283169A1 (en) | 2010-11-08 | 2012-11-08 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
| US20130035281A1 (en) | 2011-02-09 | 2013-02-07 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
| AR085689A1 (es) | 2011-03-07 | 2013-10-23 | Boehringer Ingelheim Int | Composiciones farmaceuticas de metformina, linagliptina y un inhibidor de sglt-2 |
| EA201301354A1 (ru) | 2011-06-03 | 2014-05-30 | Бёрингер Ингельхайм Интернациональ Гмбх | Ингибиторы sglt-2, предназначенные для лечения метаболических нарушений у пациентов, леченных нейролептиками |
| US20130035298A1 (en) | 2011-07-08 | 2013-02-07 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
| EP2597090A1 (en) | 2011-11-28 | 2013-05-29 | Sandoz AG | Crystalline dapagliflozin hydrate |
| US9555001B2 (en) | 2012-03-07 | 2017-01-31 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition and uses thereof |
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| 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 |
| CN103910769B (zh) * | 2012-12-31 | 2018-10-02 | 上海璎黎药业有限公司 | 葡萄糖衍生物和脯氨酸的复合物、晶体、制备方法及应用 |
| CN103910719B (zh) * | 2012-12-31 | 2018-05-01 | 上海璎黎药业有限公司 | 葡萄糖衍生物与苯丙氨酸复合物、晶体、制备方法及应用 |
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| HUE041709T2 (hu) | 2013-04-05 | 2019-05-28 | Boehringer Ingelheim Int | Az empagliflozin terápiás alkalmazásai |
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| HK1213818A1 (zh) | 2013-04-05 | 2016-07-15 | 勃林格殷格翰国际有限公司 | 依帕列净的治疗用途 |
| PT2986304T (pt) | 2013-04-18 | 2022-02-25 | Boehringer Ingelheim Int | Composição farmacêutica, métodos para o tratamento e suas utilizações |
| WO2015051484A1 (en) | 2013-10-12 | 2015-04-16 | Theracos, Inc. | Preparation of hydroxy-benzylbenzene derivatives |
| PL3082829T3 (pl) * | 2013-12-17 | 2021-09-06 | Boehringer Ingelheim Vetmedica Gmbh | Inhibitory sglt2 do leczenia zaburzeń metabolicznych u zwierząt kotowatych |
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| KR102662473B1 (ko) | 2014-04-01 | 2024-05-03 | 베링거잉겔하임베트메디카게엠베하 | 말과 동물에서 대사 장애의 치료 |
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-
2006
- 2006-09-07 DE DE602006018961T patent/DE602006018961D1/de active Active
- 2006-09-07 KR KR1020087008490A patent/KR20080053369A/ko not_active Withdrawn
- 2006-09-07 ES ES06793305T patent/ES2358051T3/es active Active
- 2006-09-07 CA CA002621314A patent/CA2621314A1/en not_active Withdrawn
- 2006-09-07 CN CNA2006800287058A patent/CN101238112A/zh active Pending
- 2006-09-07 AU AU2006289093A patent/AU2006289093A1/en not_active Abandoned
- 2006-09-07 US US11/470,684 patent/US8507450B2/en active Active
- 2006-09-07 TW TW095133001A patent/TW200745075A/zh unknown
- 2006-09-07 MX MX2008002457A patent/MX2008002457A/es not_active Application Discontinuation
- 2006-09-07 WO PCT/EP2006/066107 patent/WO2007028814A1/en not_active Ceased
- 2006-09-07 EP EP06793305A patent/EP1926720B1/en active Active
- 2006-09-07 RU RU2008113050/04A patent/RU2008113050A/ru not_active Application Discontinuation
- 2006-09-07 AT AT06793305T patent/ATE491700T1/de active
- 2006-09-07 BR BRPI0615882-0A patent/BRPI0615882A2/pt not_active IP Right Cessation
- 2006-09-07 JP JP2008529633A patent/JP5345846B2/ja active Active
- 2006-09-07 NZ NZ566787A patent/NZ566787A/en unknown
- 2006-09-08 AR ARP060103906A patent/AR056055A1/es unknown
-
2008
- 2008-01-23 ZA ZA200800681A patent/ZA200800681B/xx unknown
- 2008-03-05 IL IL189950A patent/IL189950A0/en unknown
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