JP2018528948A - アプレミラストの新規形態及びその作成方法 - Google Patents

アプレミラストの新規形態及びその作成方法 Download PDF

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Publication number
JP2018528948A
JP2018528948A JP2018510724A JP2018510724A JP2018528948A JP 2018528948 A JP2018528948 A JP 2018528948A JP 2018510724 A JP2018510724 A JP 2018510724A JP 2018510724 A JP2018510724 A JP 2018510724A JP 2018528948 A JP2018528948 A JP 2018528948A
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Japan
Prior art keywords
apremilast
suspension
temperature
amorphous
process according
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JP2018510724A
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English (en)
Japanese (ja)
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JP2018528948A5 (OSRAM
Inventor
シャオ−ピン ファン
シャオ−ピン ファン
ウェイ−シュオ ロー
ウェイ−シュオ ロー
クアン シュン ワン
クアン シュン ワン
ユイ−ション リン
ユイ−ション リン
ツン−チョン フー
ツン−チョン フー
ユアンチャン ホアン
ユアンチャン ホアン
Original Assignee
サイノファーム タイワン，リミティド
サイノファーム タイワン，リミティド
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Application filed by サイノファーム タイワン，リミティド, サイノファーム タイワン，リミティド filed Critical サイノファーム タイワン，リミティド
Publication of JP2018528948A publication Critical patent/JP2018528948A/ja
Publication of JP2018528948A5 publication Critical patent/JP2018528948A5/ja
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44—Iso-indoles; Hydrogenated iso-indoles
    • C07D209/50—Iso-indoles; Hydrogenated iso-indoles with oxygen and nitrogen atoms in positions 1 and 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44—Iso-indoles; Hydrogenated iso-indoles
    • C07D209/48—Iso-indoles; Hydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/4035—Isoindoles, e.g. phthalimide
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Indole Compounds (AREA)
JP2018510724A 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 Pending JP2018528948A (ja)

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 true JP2018528948A (ja) 2018-10-04
JP2018528948A5 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)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023120466A1 (ja) * 2021-12-23 2023-06-29 沢井製薬株式会社 アプレミラスト水和物含有製剤

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016174685A1 (en) * 2015-04-27 2016-11-03 Mylan Laboratories Limited Process for the enantiomeric resolution of apremilast intermediates
US10544097B2 (en) * 2015-08-27 2020-01-28 Msn Laboratories Private Limited Solid state forms of N-[2-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-2,3-dihydro-1,3-dioxo-1H-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
EA038882B1 (ru) * 2016-03-30 2021-11-02 Сарудбхава Формулатионс Приват Лимитед Фармацевтическая композиция апремиласта
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
CA3216107A1 (en) * 2021-04-26 2022-11-03 Amgen Inc. Process for synthesizing apremilast

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009513704A (ja) * 2005-11-01 2009-04-02 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ グルコキナーゼのアロステリックモジュレーターとしての置換ジヒドロイソインドロン
JP2011515463A (ja) * 2008-03-27 2011-05-19 セルジーン コーポレイション （＋）−２−［１−（３−エトキシ−４−メトキシフェニル）−２−メチルスルホニルエチル］−４−アセチルアミノイソインドリン−１，３−ジオンを含む固形物形態、その組成物およびその使用
WO2014068388A1 (en) * 2012-10-29 2014-05-08 Glaxo Group Limited 2 substituted cephem compounds
JP2014527511A (ja) * 2011-06-24 2014-10-16 アムジエン・インコーポレーテツド Ｔｒｐｍ８拮抗剤及び治療におけるそれらの使用
WO2016199031A1 (en) * 2015-06-09 2016-12-15 Dr. Reddy’S Laboratories Limited Process for preparation of apremilast and its intermediates

Family Cites Families (9)

* Cited by examiner, † Cited by third party
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
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
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
AU2010246749B8 (en) * 2009-05-14 2014-03-20 Ganzhou Hemay Pharmaceutical Co., Ltd Thiophene derivatives
US8981117B2 (en) 2012-09-14 2015-03-17 Celgene Corporation Processes for the preparation of isoindole compounds and isotopologues thereof
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
WO2016189486A1 (en) 2015-05-26 2016-12-01 Lupin Limited An improved process for preparation of apremilast and novel polymorphs thereof

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009513704A (ja) * 2005-11-01 2009-04-02 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ グルコキナーゼのアロステリックモジュレーターとしての置換ジヒドロイソインドロン
JP2011515463A (ja) * 2008-03-27 2011-05-19 セルジーン コーポレイション （＋）−２−［１−（３−エトキシ−４−メトキシフェニル）−２−メチルスルホニルエチル］−４−アセチルアミノイソインドリン−１，３−ジオンを含む固形物形態、その組成物およびその使用
JP2014527511A (ja) * 2011-06-24 2014-10-16 アムジエン・インコーポレーテツド Ｔｒｐｍ８拮抗剤及び治療におけるそれらの使用
WO2014068388A1 (en) * 2012-10-29 2014-05-08 Glaxo Group Limited 2 substituted cephem compounds
WO2016199031A1 (en) * 2015-06-09 2016-12-15 Dr. Reddy’S Laboratories Limited Process for preparation of apremilast and its intermediates

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023120466A1 (ja) * 2021-12-23 2023-06-29 沢井製薬株式会社 アプレミラスト水和物含有製剤

Also Published As

Publication number Publication date
CN107922332A (zh) 2018-04-17
WO2017039537A1 (en) 2017-03-09
KR20180036791A (ko) 2018-04-09
US20170057916A1 (en) 2017-03-02
IL257195A (en) 2018-03-29
TWI613191B (zh) 2018-02-01
US9765026B2 (en) 2017-09-19
EP3341360A1 (en) 2018-07-04
EP3341360A4 (en) 2019-01-23
CA2994217A1 (en) 2017-03-09
TW201718485A (zh) 2017-06-01

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