JP5758900B2 - グルコピラノシル置換ベンジルベンゼン誘導体の調製方法 - Google Patents
グルコピラノシル置換ベンジルベンゼン誘導体の調製方法 Download PDFInfo
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- JP5758900B2 JP5758900B2 JP2012531333A JP2012531333A JP5758900B2 JP 5758900 B2 JP5758900 B2 JP 5758900B2 JP 2012531333 A JP2012531333 A JP 2012531333A JP 2012531333 A JP2012531333 A JP 2012531333A JP 5758900 B2 JP5758900 B2 JP 5758900B2
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- 0 *OCC([C@@](C([C@]1O*)O*)O*)OC1(c(cc1Cc(cc2)ccc2O*)ccc1Cl)O* Chemical compound *OCC([C@@](C([C@]1O*)O*)O*)OC1(c(cc1Cc(cc2)ccc2O*)ccc1Cl)O* 0.000 description 1
Classifications
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- 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
- C07D309/12—Oxygen atoms only hydrogen atoms and one oxygen atom directly attached to ring carbon atoms, e.g. tetrahydropyranyl ethers
-
- 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
-
- 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
- C07H1/00—Processes for the preparation of sugar derivatives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H1/00—Processes for the preparation of sugar derivatives
- C07H1/06—Separation; Purification
-
- 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
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Molecular Biology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- General Health & Medical Sciences (AREA)
- Genetics & Genomics (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Saccharide Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Packaging Of Annular Or Rod-Shaped Articles, Wearing Apparel, Cassettes, Or The Like (AREA)
- Wrapping Of Specific Fragile Articles (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24714409P | 2009-09-30 | 2009-09-30 | |
| US61/247,144 | 2009-09-30 | ||
| PCT/EP2010/064120 WO2011039108A2 (en) | 2009-09-30 | 2010-09-24 | Processes for preparing of glucopyranosyl-substituted benzyl-benzene derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013505975A JP2013505975A (ja) | 2013-02-21 |
| JP5758900B2 true JP5758900B2 (ja) | 2015-08-05 |
Family
ID=43736212
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012531333A Active JP5758900B2 (ja) | 2009-09-30 | 2010-09-24 | グルコピラノシル置換ベンジルベンゼン誘導体の調製方法 |
Country Status (25)
| Country | Link |
|---|---|
| US (2) | US9024010B2 (enEXAMPLES) |
| EP (1) | EP2486029B1 (enEXAMPLES) |
| JP (1) | JP5758900B2 (enEXAMPLES) |
| KR (1) | KR101813025B1 (enEXAMPLES) |
| CN (1) | CN102574829B (enEXAMPLES) |
| AR (1) | AR078193A1 (enEXAMPLES) |
| AU (1) | AU2010303124B2 (enEXAMPLES) |
| BR (1) | BR112012007085B8 (enEXAMPLES) |
| CA (1) | CA2775962C (enEXAMPLES) |
| CL (1) | CL2012000581A1 (enEXAMPLES) |
| DK (1) | DK2486029T3 (enEXAMPLES) |
| EA (1) | EA022032B1 (enEXAMPLES) |
| ES (1) | ES2546762T3 (enEXAMPLES) |
| HR (1) | HRP20150945T1 (enEXAMPLES) |
| HU (1) | HUE026133T2 (enEXAMPLES) |
| IL (1) | IL218101A0 (enEXAMPLES) |
| IN (1) | IN2012DN02751A (enEXAMPLES) |
| MX (1) | MX2012003048A (enEXAMPLES) |
| NZ (1) | NZ598366A (enEXAMPLES) |
| PH (1) | PH12012500634A1 (enEXAMPLES) |
| PL (1) | PL2486029T3 (enEXAMPLES) |
| PT (1) | PT2486029E (enEXAMPLES) |
| SI (1) | SI2486029T1 (enEXAMPLES) |
| TW (1) | TWI465458B (enEXAMPLES) |
| WO (1) | WO2011039108A2 (enEXAMPLES) |
Families Citing this family (79)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005092877A1 (de) * | 2004-03-16 | 2005-10-06 | Boehringer Ingelheim International Gmbh | Glucopyranosyl-substituierte benzol-derivate, diese verbindungen enthaltende arzneimittel, deren verwendung und verfahren zu ihrer herstellung |
| 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 |
| US7772191B2 (en) | 2005-05-10 | 2010-08-10 | Boehringer Ingelheim International Gmbh | Processes for preparing of glucopyranosyl-substituted benzyl-benzene derivatives and intermediates therein |
| AU2006289093A1 (en) * | 2005-09-08 | 2007-03-15 | Boehringer Ingelheim International Gmbh | 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 |
| 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 |
| 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 |
| CL2008002427A1 (es) | 2007-08-16 | 2009-09-11 | Boehringer Ingelheim Int | Composicion farmaceutica que comprende 1-cloro-4-(b-d-glucopiranos-1-il)-2-[4-((s)-tetrahidrofurano-3-iloxi)bencil]-benceno combinado con 1-[(4-metilquinazolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-(3-(r)-aminopiperidin-1-il)xantina; y su uso para tratar diabetes mellitus tipo 2. |
| JP5498392B2 (ja) | 2007-11-30 | 2014-05-21 | 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 | １，５−ジヒドロ−ピラゾロ［３，４−ｄ］ピリミジン−４−オン誘導体及びｃｎｓ障害の治療のためのｐｄｅ９ａモジュレーターとしてのそれらの使用 |
| UA105362C2 (en) | 2008-04-02 | 2014-05-12 | Бьорингер Ингельхайм Интернациональ Гмбх | 1-heterocyclyl-1, 5-dihydro-pyrazolo [3, 4-d] pyrimidin-4-one derivatives and their use as pde9a modulators |
| JP5453431B2 (ja) | 2008-09-08 | 2014-03-26 | 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 | ピラゾロピリミジン及びｃｎｓ障害の治療のためのそれらの使用 |
| CN104906582A (zh) | 2009-02-13 | 2015-09-16 | 勃林格殷格翰国际有限公司 | 包含sglt2抑制剂、dpp-iv抑制剂和任选的另一种抗糖尿病药的药物组合物及其用途 |
| PE20120505A1 (es) | 2009-03-31 | 2012-05-09 | Boehringer Ingelheim Int | Derivados de 1-heterociclil-1,5-dihidro-pirazolo[3,4-d]pirimidin-4-ona como moduladores de pde9a |
| PL2486029T3 (pl) | 2009-09-30 | 2015-11-30 | Boehringer Ingelheim Int | Sposoby otrzymywania podstawionych glukopiranozylem pochodnych benzylo-benzenowych |
| EA020798B1 (ru) | 2009-09-30 | 2015-01-30 | Бёрингер Ингельхайм Интернациональ Гмбх | СПОСОБ ПОЛУЧЕНИЯ КРИСТАЛЛИЧЕСКОЙ ФОРМЫ 1-ХЛОР-4-(β-D-ГЛЮКОПИРАНОЗ-1-ИЛ)-2-[4-((S)-ТЕТРАГИДРОФУРАН-3-ИЛОКСИ)БЕНЗИЛ]БЕНЗОЛА |
| UY32919A (es) | 2009-10-02 | 2011-04-29 | Boehringer Ingelheim Int | Composición farmacéutica, forma de dosificación farmacéutica, procedimiento para su preparación, mé todos para su tratamiento y sus usos |
| CN105541849B (zh) | 2010-08-12 | 2018-03-23 | 勃林格殷格翰国际有限公司 | 6‑环烷基‑1,5‑二氢‑吡唑并[3,4‑d]嘧啶‑4‑酮衍生物及其作为PDE9A抑制剂的用途 |
| US8809345B2 (en) | 2011-02-15 | 2014-08-19 | Boehringer Ingelheim International Gmbh | 6-cycloalkyl-pyrazolopyrimidinones for the treatment of CNS disorders |
| AR085689A1 (es) | 2011-03-07 | 2013-10-23 | Boehringer Ingelheim Int | Composiciones farmaceuticas de metformina, linagliptina y un inhibidor de sglt-2 |
| BR112013031032A2 (pt) | 2011-06-03 | 2016-11-29 | Boehringer Ingelheim Int | inibidores de sglt-2 para o tratamento de distúrbios metabólicos em pacientes tratados com agentes neurolépticos |
| US20130035298A1 (en) | 2011-07-08 | 2013-02-07 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
| US9555001B2 (en) | 2012-03-07 | 2017-01-31 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition and uses thereof |
| US9192617B2 (en) | 2012-03-20 | 2015-11-24 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
| US9193751B2 (en) | 2012-04-10 | 2015-11-24 | Theracos, Inc. | Process for the preparation of benzylbenzene SGLT2 inhibitors |
| WO2013152476A1 (en) * | 2012-04-10 | 2013-10-17 | Theracos, Inc. | Process for the preparation of benzylbenzene sglt2 inhibitors |
| EP2981269B9 (en) | 2013-04-04 | 2023-12-06 | Boehringer Ingelheim Vetmedica GmbH | Treatment of metabolic disorders in equine animals |
| CA2812519A1 (en) | 2013-04-05 | 2014-10-05 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
| US11813275B2 (en) | 2013-04-05 | 2023-11-14 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
| 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 |
| HRP20190101T1 (hr) | 2013-04-05 | 2019-03-08 | Boehringer Ingelheim International Gmbh | Terapeutske uporabe empagliflozina |
| HK1215378A1 (zh) | 2013-04-18 | 2016-08-26 | 勃林格殷格翰国际有限公司 | 药物组合物、治疗方法及其用途 |
| ES2605886T3 (es) | 2013-09-27 | 2017-03-16 | Sunshine Lake Pharma Co., Ltd. | Derivados de glucopiranosilo y sus usos en medicina |
| SI3862003T1 (sl) | 2013-12-17 | 2024-02-29 | Boehringer Ingelheim Vetmedica Gmbh | Inhibitor SGLT-2 za uporabo pri zdravljenju metabolične motnje pri mačjih živalih |
| US9902751B2 (en) | 2013-12-30 | 2018-02-27 | Mylan Laboratories Limited | Process for the preparation of empagliflozin |
| CN105960242A (zh) | 2014-01-23 | 2016-09-21 | 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 |
| PL3125882T3 (pl) | 2014-04-01 | 2020-10-19 | Boehringer Ingelheim Vetmedica Gmbh | Leczenie zaburzeń metabolicznych u zwierząt koniowatych |
| PL3197429T3 (pl) | 2014-09-25 | 2024-09-30 | Boehringer Ingelheim Vetmedica Gmbh | Leczenie skojarzone inhibitorami sglt2 i agonistami dopaminy do profilaktyki zaburzeń metabolicznych u zwierząt koniowatych |
| WO2017120249A1 (en) | 2016-01-04 | 2017-07-13 | Sandia Corporation | Poly (phenylene)-based anion exchange polymers and methods thereof |
| US10294325B2 (en) | 2016-01-04 | 2019-05-21 | National Technology & Engineering Solutions Of Sandia, Llc | Halo-containing anion exchange membranes and methods thereof |
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| WO2018069243A1 (en) * | 2016-10-13 | 2018-04-19 | Boehringer Ingelheim International Gmbh | Process for preparing glucopyranosyl-substituted benzyl-benzene derivatives |
| BR112019005930A2 (pt) | 2016-10-19 | 2019-06-11 | Boehringer Ingelheim Int | combinações compreendendo um inibidor de ssao/vap-1 e um inibidor de sglt2, e usos das mesmas |
| US20180125813A1 (en) | 2016-11-10 | 2018-05-10 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
| CN108794548B (zh) * | 2017-04-28 | 2023-06-16 | 正大天晴药业集团股份有限公司 | 制备恩格列净及其中间体的方法 |
| US11046676B2 (en) | 2017-06-05 | 2021-06-29 | Laurus Labs Limited | Process for preparation of empagliflozin or its co-crystals, solvates and their polymorphs thereof |
| CN107163033A (zh) * | 2017-06-15 | 2017-09-15 | 扬子江药业集团北京海燕药业有限公司 | 一种高纯度依帕列净的制备方法 |
| CN109988161A (zh) * | 2017-12-29 | 2019-07-09 | 徐州万邦金桥制药有限公司 | 一种适合工业化生产恩格列净的制备方法 |
| CN108178751A (zh) * | 2018-01-30 | 2018-06-19 | 扬州工业职业技术学院 | 一种恩格列净中间体的合成方法 |
| US10479866B1 (en) | 2018-02-28 | 2019-11-19 | National Technology & Engineering Solutions Of Sandia, Llc | Block copolymers including poly(phenylene) and methods thereof |
| JP2021520394A (ja) | 2018-04-17 | 2021-08-19 | 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 | 医薬組成物、処置方法及びその使用 |
| US20210275558A1 (en) | 2018-07-25 | 2021-09-09 | Boehringer Ingelheim International Gmbh | Methods for treating, pharmaceutical compositions and uses thereof |
| WO2020039394A1 (en) | 2018-08-24 | 2020-02-27 | Novartis Ag | New drug combinations |
| CN109456314A (zh) * | 2018-10-19 | 2019-03-12 | 威海迪素制药有限公司 | 一种恩格列净的制备方法 |
| US12213970B2 (en) | 2018-10-29 | 2025-02-04 | Boehringer Ingelheim International Gmbh | Pyridinyl sulfonamide derivatives, pharmaceutical compositions and uses thereof |
| ES2967359T3 (es) | 2018-10-29 | 2024-04-29 | Boehringer Ingelheim Int | Derivados piridinil-sulfonamida, composiciones farmacéuticas y usos de los mismos |
| CN111233915B (zh) * | 2018-11-28 | 2023-09-22 | 上海科胜药物研发有限公司 | 一种2,3,4,6-四-o-三甲基硅基-d-葡萄糖酸内酯的制备方法 |
| CN110655511B (zh) * | 2019-05-31 | 2020-10-16 | 北京莱瑞森医药科技有限公司 | 一种高纯度恩格列净的制备和精制方法 |
| CN112812107B (zh) * | 2019-11-18 | 2024-03-15 | 上海启讯医药科技有限公司 | 一种sglt-2抑制剂及中间体的制备方法 |
| JP7441946B2 (ja) | 2019-11-28 | 2024-03-01 | 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 | 非ヒト動物の乾乳におけるｓｇｌｔ－２阻害剤の使用 |
| CN110759941B (zh) * | 2019-11-29 | 2022-08-30 | 上海网义化工有限公司 | 一种D-葡萄糖酸-γ-内酯及其中间体的制备方法 |
| CN110872216A (zh) * | 2019-12-06 | 2020-03-10 | 南京恒道医药科技有限公司 | 一种反应分离耦合生产(2-氯-5-碘苯基)-4-氟苯甲基酮的方法及装置 |
| CN110903315A (zh) * | 2019-12-16 | 2020-03-24 | 上海网义化工有限公司 | 一种D-葡萄糖酸-γ-内酯中间体的制备方法 |
| CN115087441B (zh) | 2020-02-17 | 2024-07-12 | 勃林格殷格翰动物保健有限公司 | Sglt-2抑制剂用于预防和/或治疗猫科动物的心脏疾病的用途 |
| CN115397434A (zh) | 2020-04-07 | 2022-11-25 | 勃林格殷格翰国际有限公司 | 治疗头痛障碍的方法 |
| CN111410639B (zh) * | 2020-04-14 | 2021-02-26 | 天津法莫西医药科技有限公司 | 一种恩格列净中间体杂质的制备方法 |
| CN112194655B (zh) * | 2020-10-15 | 2022-08-09 | 通化东宝药业股份有限公司 | 一种恩格列净的制备方法 |
| KR20220068805A (ko) | 2020-11-19 | 2022-05-26 | 한미약품 주식회사 | 신규한 글루코스 유도체 |
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| 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. |
| WO2023006718A1 (en) | 2021-07-28 | 2023-02-02 | Boehringer Ingelheim Vetmedica Gmbh | Use of sglt-2 inhibitors for the prevention and/or treatment of cardiac diseases in non-human mammals excluding felines, in particular canines |
| US20240269105A1 (en) | 2021-07-28 | 2024-08-15 | Boehringer Ingelheim Vetmedica Gmbh | Use of sglt-2 inhibitors for the prevention and/or treatment of hypertension in non-human mammals |
| CN114716425B (zh) * | 2022-04-11 | 2023-09-01 | 沧州那瑞化学科技有限公司 | 芳香杂环取代亚甲基的化合物的合成方法 |
| AU2023277704A1 (en) | 2022-05-25 | 2024-12-05 | Boehringer Ingelheim Vetmedica Gmbh | Aqueous pharmaceutical compositions comprising sglt-2 inhibitors |
| CN115231992B (zh) * | 2022-06-30 | 2024-08-27 | 济南鼎皓医药科技有限公司 | 一种(2-氯-5-碘苯基)(4-氟苯基)甲酮的制备方法 |
| CN115232179A (zh) * | 2022-08-15 | 2022-10-25 | 江西天戌药业有限公司 | 一种恩格列净中间体杂质的制备方法 |
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