JP2018528948A5 - - Google Patents
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- Publication number
- JP2018528948A5 JP2018528948A5 JP2018510724A JP2018510724A JP2018528948A5 JP 2018528948 A5 JP2018528948 A5 JP 2018528948A5 JP 2018510724 A JP2018510724 A JP 2018510724A JP 2018510724 A JP2018510724 A JP 2018510724A JP 2018528948 A5 JP2018528948 A5 JP 2018528948A5
- Authority
- JP
- Japan
- Prior art keywords
- apremilast
- toluene
- mixture
- acetic acid
- isolated
- 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.)
- Pending
Links
- 238000000034 method Methods 0.000 claims 10
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 9
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 claims 9
- IMOZEMNVLZVGJZ-QGZVFWFLSA-N apremilast Chemical compound C1=C(OC)C(OCC)=CC([C@@H](CS(C)(=O)=O)N2C(C3=C(NC(C)=O)C=CC=C3C2=O)=O)=C1 IMOZEMNVLZVGJZ-QGZVFWFLSA-N 0.000 claims 4
- 229960001164 apremilast Drugs 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 3
- BXUJVINGXQGNFD-SNVBAGLBSA-N (1s)-1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethanamine Chemical compound CCOC1=CC([C@H](N)CS(C)(=O)=O)=CC=C1OC BXUJVINGXQGNFD-SNVBAGLBSA-N 0.000 claims 1
- 238000001914 filtration Methods 0.000 claims 1
- 238000002955 isolation Methods 0.000 claims 1
- PAUAJOABXCGLCN-UHFFFAOYSA-N n-(1,3-dioxo-2-benzofuran-4-yl)acetamide Chemical compound CC(=O)NC1=CC=CC2=C1C(=O)OC2=O PAUAJOABXCGLCN-UHFFFAOYSA-N 0.000 claims 1
- 230000000630 rising effect Effects 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562211280P | 2015-08-28 | 2015-08-28 | |
| US62/211,280 | 2015-08-28 | ||
| US201662279147P | 2016-01-15 | 2016-01-15 | |
| US62/279,147 | 2016-01-15 | ||
| PCT/SG2016/050413 WO2017039537A1 (en) | 2015-08-28 | 2016-08-25 | Novel forms of apremilast and the process of making the same |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2018528948A JP2018528948A (ja) | 2018-10-04 |
| JP2018528948A5 true JP2018528948A5 (OSRAM) | 2019-08-29 |
Family
ID=58097541
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018510724A Pending JP2018528948A (ja) | 2015-08-28 | 2016-08-25 | アプレミラストの新規形態及びその作成方法 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US9765026B2 (OSRAM) |
| EP (1) | EP3341360A4 (OSRAM) |
| JP (1) | JP2018528948A (OSRAM) |
| KR (1) | KR20180036791A (OSRAM) |
| CN (1) | CN107922332A (OSRAM) |
| CA (1) | CA2994217A1 (OSRAM) |
| IL (1) | IL257195A (OSRAM) |
| TW (1) | TWI613191B (OSRAM) |
| WO (1) | WO2017039537A1 (OSRAM) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10370329B2 (en) * | 2015-04-27 | 2019-08-06 | Mylan Laboratories Limited | Process for the enantiomeric resolution of apremilast intermediates |
| WO2017033206A2 (en) * | 2015-08-27 | 2017-03-02 | Msn Laboratories Private Limited | Solid state forms of n-[2-[(1 s)-1 -(3-ethoxy-4-methoxyphenyl)-2-(methyl sulfonyl)ethyl]-2,3-dihydro-1,3-dioxo-l h-isoindol-4-yl]acetamide and process for preparation thereof |
| CN106977444B (zh) * | 2016-01-18 | 2021-10-08 | 重庆医药工业研究院有限责任公司 | 一种阿普斯特无定型的制备方法 |
| BR112018070155B1 (pt) * | 2016-03-30 | 2023-10-24 | Sarudbhava Formulations Private Limited | Composições farmacêuticas de apremilast |
| CN107686461A (zh) * | 2016-08-04 | 2018-02-13 | 广东东阳光药业有限公司 | 阿普斯特的溶剂化物及其制备方法和用途 |
| WO2019021303A1 (en) * | 2017-07-23 | 2019-01-31 | Alkem Laboratories Limited | NOVEL PROCESS FOR THE PREPARATION OF APREMILAST IN AMORPHOUS FORM |
| CN108440381A (zh) * | 2018-03-15 | 2018-08-24 | 威海迪素制药有限公司 | 一种阿普斯特新晶型h及其制备方法 |
| AR125097A1 (es) | 2021-04-26 | 2023-06-07 | Amgen Inc | Proceso para la síntesis de apremilast |
| JPWO2023120466A1 (OSRAM) * | 2021-12-23 | 2023-06-29 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8093293B2 (en) | 1998-07-06 | 2012-01-10 | Johnson & Johnson Consumer Companies, Inc. | Methods for treating skin conditions |
| US6962940B2 (en) | 2002-03-20 | 2005-11-08 | Celgene Corporation | (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione: methods of using and compositions thereof |
| US7893101B2 (en) | 2002-03-20 | 2011-02-22 | Celgene Corporation | Solid forms comprising (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, compositions thereof, and uses thereof |
| US8796313B2 (en) * | 2005-11-01 | 2014-08-05 | Janssen Pharmaceutica N.V. | Substituted dihydroisoindolones as allosteric modulators of glucokinase |
| KR20150038547A (ko) * | 2008-03-27 | 2015-04-08 | 셀진 코포레이션 | (+)-2-[1-(3-에톡시-4-메톡시페닐)-2-메틸설포닐에틸]-4-아세틸아미노이소인돌린-1,3-디온을 포함하는 고체 형태, 이의 조성물, 및 이의 용도 |
| WO2010130224A1 (zh) | 2009-05-14 | 2010-11-18 | 天津和美生物技术有限公司 | 噻吩衍生物 |
| WO2012177893A2 (en) * | 2011-06-24 | 2012-12-27 | Amgen Inc. | Trpm8 antagonists and their use in treatments |
| US8981117B2 (en) | 2012-09-14 | 2015-03-17 | Celgene Corporation | Processes for the preparation of isoindole compounds and isotopologues thereof |
| UY35103A (es) * | 2012-10-29 | 2014-05-30 | Glaxo Group Ltd | Compuestos de cefem 2-sustituidos |
| EP2730278A1 (en) | 2012-11-08 | 2014-05-14 | Ratiopharm GmbH | Composition melt |
| IN2014MU01283A (OSRAM) | 2014-04-04 | 2015-10-09 | Cadila Healthcare Ltd | |
| CN104447445B (zh) | 2014-12-05 | 2016-07-06 | 新发药业有限公司 | 一种合成阿普斯特中间体的制备方法 |
| MX2017015151A (es) | 2015-05-26 | 2018-08-15 | Lupin Ltd | Un proceso mejorado para la preparación de apremilast y novedosos polimorfos del mismo. |
| US20180334429A1 (en) * | 2015-06-09 | 2018-11-22 | Dr. Reddy's Laboratories Limited | Process for preparation of apremilast and its intermediates |
-
2016
- 2016-08-24 US US15/246,392 patent/US9765026B2/en active Active
- 2016-08-25 WO PCT/SG2016/050413 patent/WO2017039537A1/en not_active Ceased
- 2016-08-25 CA CA2994217A patent/CA2994217A1/en not_active Abandoned
- 2016-08-25 CN CN201680050410.4A patent/CN107922332A/zh active Pending
- 2016-08-25 JP JP2018510724A patent/JP2018528948A/ja active Pending
- 2016-08-25 KR KR1020187008651A patent/KR20180036791A/ko not_active Ceased
- 2016-08-25 EP EP16842429.9A patent/EP3341360A4/en not_active Withdrawn
- 2016-08-26 TW TW105127548A patent/TWI613191B/zh active
-
2018
- 2018-01-28 IL IL257195A patent/IL257195A/en unknown
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