JP2012526791A5 - - Google Patents
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- Publication number
- JP2012526791A5 JP2012526791A5 JP2012510370A JP2012510370A JP2012526791A5 JP 2012526791 A5 JP2012526791 A5 JP 2012526791A5 JP 2012510370 A JP2012510370 A JP 2012510370A JP 2012510370 A JP2012510370 A JP 2012510370A JP 2012526791 A5 JP2012526791 A5 JP 2012526791A5
- Authority
- JP
- Japan
- Prior art keywords
- acid
- derivative
- process according
- ester
- sitagliptin
- 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
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN722/KOL/2009 | 2009-05-11 | ||
| IN722KO2009 | 2009-05-11 | ||
| PCT/GB2010/050760 WO2010131025A1 (en) | 2009-05-11 | 2010-05-10 | Sitagliptin synthesis |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015174821A Division JP2016029051A (ja) | 2009-05-11 | 2015-09-04 | シタグリプチンの合成 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012526791A JP2012526791A (ja) | 2012-11-01 |
| JP2012526791A5 true JP2012526791A5 (enExample) | 2013-06-27 |
| JP6199556B2 JP6199556B2 (ja) | 2017-09-20 |
Family
ID=42312921
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012510370A Active JP6199556B2 (ja) | 2009-05-11 | 2010-05-10 | シタグリプチンの合成 |
| JP2015174821A Pending JP2016029051A (ja) | 2009-05-11 | 2015-09-04 | シタグリプチンの合成 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015174821A Pending JP2016029051A (ja) | 2009-05-11 | 2015-09-04 | シタグリプチンの合成 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US8846916B2 (enExample) |
| EP (1) | EP2430025A1 (enExample) |
| JP (2) | JP6199556B2 (enExample) |
| CN (1) | CN102574856B (enExample) |
| AU (1) | AU2010247193B2 (enExample) |
| CA (1) | CA2759077C (enExample) |
| NZ (1) | NZ596713A (enExample) |
| WO (1) | WO2010131025A1 (enExample) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2508506A1 (en) | 2011-04-08 | 2012-10-10 | LEK Pharmaceuticals d.d. | Preparation of sitagliptin intermediates |
| CN102757431B (zh) * | 2011-04-24 | 2016-03-30 | 浙江华海药业股份有限公司 | 一种合成西他列汀的新方法 |
| CA2840814A1 (en) | 2011-06-29 | 2013-01-03 | Ranbaxy Laboratories Limited | Solid dispersions of sitagliptin and processes for their preparation |
| US20150051213A1 (en) | 2011-06-30 | 2015-02-19 | Suresh Babu Jayachandra | Novel salts of sitagliptin |
| WO2013013833A1 (en) | 2011-07-27 | 2013-01-31 | Farma Grs, D.O.O. | Process for the preparation of sitagliptin and its pharmaceutically acceptable salts |
| CN102603749B (zh) * | 2011-10-27 | 2017-02-08 | 浙江华海药业股份有限公司 | 一种西他列汀中间体的合成方法 |
| EP2788352A1 (en) | 2011-12-08 | 2014-10-15 | Ranbaxy Laboratories Limited | Amorphous form of sitagliptin salts |
| CN102531937A (zh) * | 2011-12-31 | 2012-07-04 | 浙江工业大学 | 一种化学拆分法制备(r)-3-氨基-4-(2,4,5-三氟苯基)丁酸甲酯的方法 |
| WO2013114173A1 (en) * | 2012-01-30 | 2013-08-08 | Smilax Laboratories Limited | A novel process for the preparation of sitagliptin |
| CN102702205B (zh) * | 2012-05-16 | 2014-01-15 | 苏州新凯生物医药技术有限公司 | 西他列汀的制备方法 |
| EP2674432A1 (en) | 2012-06-14 | 2013-12-18 | LEK Pharmaceuticals d.d. | New synthetic route for the preparation of ß aminobutyryl substituted 5,6,7,8-tetrahydro[1,4]diazolo[4,3-alpha]pyrazin-7-yl compounds |
| KR102157917B1 (ko) * | 2012-12-21 | 2020-09-21 | 레크 파마슈티칼스 디.디. | 키랄 γ-아릴-β-아미노부티르산 유도체의 제조를 위한 효소 경로 |
| IN2013MU00916A (enExample) * | 2013-03-20 | 2015-06-26 | Cadila Healthcare Ltd | |
| CN103497145B (zh) * | 2013-10-10 | 2016-01-27 | 南昌大学 | 一种光学纯多奈哌齐的制备工艺 |
| IN2014MU00212A (enExample) * | 2014-01-21 | 2015-08-28 | Cadila Healthcare Ltd | |
| CN104557944B (zh) * | 2014-12-31 | 2017-05-31 | 北京瑞都医药科技有限公司 | 一种降糖药物及其制备方法 |
| CN105331651B (zh) * | 2015-11-25 | 2018-11-13 | 尚科生物医药(上海)有限公司 | 西他列汀及其中间体的酶-化学制备方法 |
| CN105294479B (zh) * | 2015-12-05 | 2017-09-22 | 新发药业有限公司 | 一种3r‑氨基取代丁酰胺衍生物的制备方法 |
| JP6049923B1 (ja) | 2016-02-18 | 2016-12-21 | 三菱日立パワーシステムズ株式会社 | 部品情報検索装置、部品情報検索方法、およびプログラム |
| CN107129501B (zh) * | 2017-05-19 | 2019-05-21 | 贵州大学 | 2型糖尿病药物西他列汀制备新方法 |
| CN107669683B (zh) * | 2017-09-30 | 2020-07-03 | 杭州华东医药集团新药研究院有限公司 | 含有西格列汀与二甲双胍的药物组合物 |
| CN108586346B (zh) | 2018-05-10 | 2019-10-01 | 北京富盛嘉华医药科技有限公司 | 一种生物催化合成西他列汀及其中间体的方法 |
| CN110759914A (zh) * | 2019-02-03 | 2020-02-07 | 美华东进国际生物医药研究院有限公司 | 一种治疗糖尿病的药物的制备方法 |
| CN112300017B (zh) * | 2019-08-01 | 2023-06-09 | 浙江九洲药业股份有限公司 | 一种手性β-氨基酸及其衍生物的消旋制备方法 |
| CN112341332B (zh) * | 2020-11-11 | 2023-04-28 | 浙江昌明药业有限公司 | 一种西他列汀关键中间体降解废弃物的回收利用方法 |
| CN114644568B (zh) * | 2020-12-21 | 2024-07-19 | 浙江医药股份有限公司新昌制药厂 | 西格列汀中间体的纯化方法 |
| CN113045448A (zh) * | 2021-03-09 | 2021-06-29 | 台州市生物医化产业研究院有限公司 | 一种乙酰麦氏酸衍生物降解废弃物的回收利用方法 |
| CN115583935A (zh) * | 2022-11-03 | 2023-01-10 | 浙江工业大学 | 一种4-(2,4,5-三氟苯基)-3-氧丁酸酯的制备方法 |
| EP4630568A1 (en) | 2022-12-09 | 2025-10-15 | KRKA, D.D., Novo Mesto | Process for the preparation of sitagliptin |
| CN115819258B (zh) * | 2022-12-13 | 2024-10-18 | 浙江大学 | 一种利用含膦氧双键催化剂的西格列汀中间体的制备方法 |
| CN115960007B (zh) * | 2022-12-13 | 2025-02-07 | 浙江大学 | 一种利用含氮甲酰基催化剂的西格列汀中间体的制备方法 |
| CN117069604A (zh) * | 2023-08-22 | 2023-11-17 | 河北龙海药业有限公司 | 一种磷酸西格列汀杂质fp-e的制备方法及其检测方法 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA74912C2 (en) * | 2001-07-06 | 2006-02-15 | Merck & Co Inc | Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes |
| AR043515A1 (es) | 2003-03-19 | 2005-08-03 | Merck & Co Inc | Procedimiento para preparar derivados quirales beta aminoacidos mediante hidrogenacion asimetrica |
| WO2004085661A2 (en) | 2003-03-24 | 2004-10-07 | Merck & Co., Inc | Process to chiral beta-amino acid derivatives |
| WO2004087650A2 (en) | 2003-03-27 | 2004-10-14 | Merck & Co. Inc. | Process and intermediates for the preparation of beta-amino acid amide dipeptidyl peptidase-iv inhibitors |
| JO2625B1 (en) | 2003-06-24 | 2011-11-01 | ميرك شارب اند دوم كوربوريشن | Phosphoric acid salts of dipeptidyl betidase inhibitor 4 |
| US20060287528A1 (en) | 2003-09-02 | 2006-12-21 | Wenslow Robert M | Novel crystalline forms of a phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor |
| WO2005030127A2 (en) | 2003-09-23 | 2005-04-07 | Merck & Co., Inc. | Novel crystalline form of a phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor |
| EP1796671A4 (en) | 2004-09-15 | 2009-01-21 | Merck & Co Inc | AMORPHIC FORM OF A PHOSPHORIC ACID SALT OF A DIPEPTIDYL-PEPTIDASE IV HEMMER |
| WO2006065826A2 (en) * | 2004-12-15 | 2006-06-22 | Merck & Co., Inc. | Process to chiral beta amino acid derivatives by asymmetric hydrogenation |
| US8334385B2 (en) * | 2007-11-02 | 2012-12-18 | Glenmark Generics Limited | Process for the preparation of R-sitagliptin and its pharmaceutically acceptable salts thereof |
| WO2009064476A1 (en) | 2007-11-13 | 2009-05-22 | Teva Pharmaceutical Industries Ltd. | Preparation of sitagliptin intermediate |
| KR20100101073A (ko) | 2007-12-20 | 2010-09-16 | 닥터 레디스 레보러터리즈 리미티드 | 시타글립틴 및 약제학적으로 허용되는 그의 염의 제조 방법 |
| US20090247532A1 (en) | 2008-03-28 | 2009-10-01 | Mae De Ltd. | Crystalline polymorph of sitagliptin phosphate and its preparation |
| CN101633625B (zh) | 2008-07-23 | 2013-02-13 | 江苏恒瑞医药股份有限公司 | R-β-氨基苯丁酸衍生物的制备方法 |
| WO2010032264A2 (en) | 2008-08-27 | 2010-03-25 | Cadila Healthcare Limited | Improved process for preparation of (2r)-4-oxo-4-[3- (trifluoromethyl)-5,6-dihydro [1,2,4]-triazolo[4,3-a]pyrazin- 7(8h)-yl]-l-(2,4,5-trifluorophenyl)butan-2-amine & new impurities in preparation thereof |
| WO2010078440A1 (en) * | 2008-12-31 | 2010-07-08 | Chiral Quest, Inc. | Process and intermediates for the preparation of n-acylated-4-aryl beta-amino acid derivatives |
| WO2010131035A1 (en) | 2009-05-11 | 2010-11-18 | Generics [Uk] Limited | Novel crystalline polymorph of sitagliptin dihydrogen phosphate |
| CN101928289A (zh) * | 2009-06-19 | 2010-12-29 | 北京海步国际医药科技发展有限公司 | 制备二肽基肽酶-iv抑制剂的方法 |
-
2010
- 2010-05-10 US US13/265,087 patent/US8846916B2/en active Active
- 2010-05-10 AU AU2010247193A patent/AU2010247193B2/en not_active Ceased
- 2010-05-10 JP JP2012510370A patent/JP6199556B2/ja active Active
- 2010-05-10 NZ NZ596713A patent/NZ596713A/en not_active IP Right Cessation
- 2010-05-10 WO PCT/GB2010/050760 patent/WO2010131025A1/en not_active Ceased
- 2010-05-10 CA CA2759077A patent/CA2759077C/en active Active
- 2010-05-10 CN CN201080031317.1A patent/CN102574856B/zh not_active Expired - Fee Related
- 2010-05-10 EP EP10720189.9A patent/EP2430025A1/en not_active Withdrawn
-
2015
- 2015-09-04 JP JP2015174821A patent/JP2016029051A/ja active Pending
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