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WO2008108384A1 - 安定性が改善されたクロロメチルフォスフェイト誘導体を含む組成物及びその製造方法 - Google Patents

安定性が改善されたクロロメチルフォスフェイト誘導体を含む組成物及びその製造方法 Download PDF

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Publication number
WO2008108384A1
WO2008108384A1 PCT/JP2008/053905 JP2008053905W WO2008108384A1 WO 2008108384 A1 WO2008108384 A1 WO 2008108384A1 JP 2008053905 W JP2008053905 W JP 2008053905W WO 2008108384 A1 WO2008108384 A1 WO 2008108384A1
Authority
WO
WIPO (PCT)
Prior art keywords
producing
composition containing
same
phosphate derivative
formula
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.)
Ceased
Application number
PCT/JP2008/053905
Other languages
English (en)
French (fr)
Inventor
Keizo Sato
Shinya Abe
Kazuhiro Yoshizawa
Kazunori Wakasugi
Shigeto Negi
Mamoru Miyazawa
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Eisai R&D Management Co Ltd
Original Assignee
Eisai R&D Management Co Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Eisai R&D Management Co Ltd filed Critical Eisai R&D Management Co Ltd
Priority to US12/526,905 priority Critical patent/US20100094001A1/en
Priority to CN200880007043.5A priority patent/CN101622263B/zh
Priority to EP08721325A priority patent/EP2133355A4/en
Priority to JP2009502595A priority patent/JP5221514B2/ja
Publication of WO2008108384A1 publication Critical patent/WO2008108384A1/ja
Priority to IL200218A priority patent/IL200218A0/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/025Purification; Separation; Stabilisation; Desodorisation of organo-phosphorus compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/06Phosphorus compounds without P—C bonds
    • C07F9/08Esters of oxyacids of phosphorus
    • C07F9/09Esters of phosphoric acids
    • C07F9/091Esters of phosphoric acids with hydroxyalkyl compounds with further substituents on alkyl

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

 本発明は、水溶性プロドラッグの製造のために有用なクロロメチルフォスフェイト誘導体の製造方法であって、作業性、操作性及び省エネルギー性の観点から優れる製造方法等を提供することである。本発明によれば、下記式(I)で表される化合物に、1気圧における沸点が150°C以上を有する三級アミンを添加する工程を含む、 【化1】 (式中、R1及びR2は、同一又は相異なって、C1-C6アルキル基、C2-C6アルケニル基又は置換基を有してもよいC6-C14アリールC1-C6アルキル基を示し、R1とR2とは一緒になって環を形成してもよい。)、前記式(I)で表される化合物と前記三級アミンとを含む組成物の製造方法を提供する。
PCT/JP2008/053905 2007-03-06 2008-03-05 安定性が改善されたクロロメチルフォスフェイト誘導体を含む組成物及びその製造方法 Ceased WO2008108384A1 (ja)

Priority Applications (5)

Application Number Priority Date Filing Date Title
US12/526,905 US20100094001A1 (en) 2007-03-06 2008-03-05 Composition containing stability-improved chloromethyl phosphate derivative and process for producing same
CN200880007043.5A CN101622263B (zh) 2007-03-06 2008-03-05 稳定性被改善的含有磷酸氯甲酯衍生物的组合物及其制备方法
EP08721325A EP2133355A4 (en) 2007-03-06 2008-03-05 COMPOSITION WITH A CHLOROMETHYPHOSPHATE DERIVATIVE WITH INCREASED STABILITY AND METHOD FOR THE PRODUCTION THEREOF
JP2009502595A JP5221514B2 (ja) 2007-03-06 2008-03-05 安定性が改善されたクロロメチルフォスフェイト誘導体を含む組成物及びその製造方法
IL200218A IL200218A0 (en) 2007-03-06 2009-08-03 Composition containing stability-improved chloromethyl phosphate derivative and process for producing same

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2007-056003 2007-03-06
JP2007056003 2007-03-06

Publications (1)

Publication Number Publication Date
WO2008108384A1 true WO2008108384A1 (ja) 2008-09-12

Family

ID=39738257

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2008/053905 Ceased WO2008108384A1 (ja) 2007-03-06 2008-03-05 安定性が改善されたクロロメチルフォスフェイト誘導体を含む組成物及びその製造方法

Country Status (6)

Country Link
US (1) US20100094001A1 (ja)
EP (1) EP2133355A4 (ja)
JP (1) JP5221514B2 (ja)
CN (1) CN101622263B (ja)
IL (1) IL200218A0 (ja)
WO (1) WO2008108384A1 (ja)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102596977A (zh) * 2009-05-07 2012-07-18 明尼苏达大学评议会 新的雷公藤内酯前药
US9150600B2 (en) 2009-05-07 2015-10-06 Regents Of The University Of Minnesota Triptolide prodrugs

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2018265584B2 (en) 2017-05-12 2023-09-28 Ludwig-Maximilians-Universität München Phenyl-heterocycle-phenyl derivatives for use in the treatment or prevention of melanoma
CN116399983B (zh) * 2023-06-09 2023-08-15 天津辰欣药物研究有限公司 一种利用gc-ms法检测二叔丁基氯甲基磷酸酯残留量的方法
CN119176987B (zh) * 2024-11-26 2025-03-14 合肥科拜尔新材料股份有限公司 一种冰箱内胆用pp复合材料及其制备方法

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH07258238A (ja) * 1994-02-04 1995-10-09 Santen Pharmaceut Co Ltd 新規チアジンまたはチオモルフォリン誘導体
US5648372A (en) 1994-02-07 1997-07-15 Eisai Co., Ltd. Antifungal agents, and compositions
JP2001527083A (ja) * 1997-12-31 2001-12-25 ザ・ユニバーシティ・オブ・カンザス 第二級および第三級アミン含有薬剤の水溶性プロドラッグおよびその製造方法
JP2004518640A (ja) 2000-11-20 2004-06-24 ブリストル−マイヤーズ スクイブ カンパニー 水溶性アゾール化合物の改良された方法
WO2007032263A1 (ja) * 2005-09-13 2007-03-22 Eisai R & D Management Co., Ltd. 安定性が改善されたクロロメチルフォスフェイト誘導体を含む組成物およびその製造方法
WO2007097386A1 (ja) * 2006-02-22 2007-08-30 Eisai R & D Management Co., Ltd. 安定化医薬組成物

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6235728B1 (en) * 1999-02-19 2001-05-22 Bristol-Myers Squibb Company Water-soluble prodrugs of azole compounds
CN101678120A (zh) * 2006-12-05 2010-03-24 纽罗吉斯克斯公司 前药及其制备和使用方法

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH07258238A (ja) * 1994-02-04 1995-10-09 Santen Pharmaceut Co Ltd 新規チアジンまたはチオモルフォリン誘導体
US5648372A (en) 1994-02-07 1997-07-15 Eisai Co., Ltd. Antifungal agents, and compositions
JP2001527083A (ja) * 1997-12-31 2001-12-25 ザ・ユニバーシティ・オブ・カンザス 第二級および第三級アミン含有薬剤の水溶性プロドラッグおよびその製造方法
JP2004518640A (ja) 2000-11-20 2004-06-24 ブリストル−マイヤーズ スクイブ カンパニー 水溶性アゾール化合物の改良された方法
WO2007032263A1 (ja) * 2005-09-13 2007-03-22 Eisai R & D Management Co., Ltd. 安定性が改善されたクロロメチルフォスフェイト誘導体を含む組成物およびその製造方法
WO2007097386A1 (ja) * 2006-02-22 2007-08-30 Eisai R & D Management Co., Ltd. 安定化医薬組成物

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
ANTTI MANTYLA ET AL., TETRAHEDRON LETTERS, vol. 43, 2002, pages 3793 - 3794
MULLER, E.: "Methoden Der Organischen Chemie", vol. 12/2, 1964, GEORG THIEME, pages: 286 - 90
See also references of EP2133355A4
ZWIERZAK, A.; KLUBA, M., TETRAHERDON, vol. 27, 1971, pages 3163 - 3170

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102596977A (zh) * 2009-05-07 2012-07-18 明尼苏达大学评议会 新的雷公藤内酯前药
US9150600B2 (en) 2009-05-07 2015-10-06 Regents Of The University Of Minnesota Triptolide prodrugs
CN102596977B (zh) * 2009-05-07 2016-06-29 明尼苏达大学评议会 雷公藤内酯前药
US9623035B2 (en) 2009-05-07 2017-04-18 Regents Of The University Of Minnesota Triptolide prodrugs
US10183033B2 (en) 2009-05-07 2019-01-22 Regents Of The University Of Minnesota Triptolide prodrugs

Also Published As

Publication number Publication date
EP2133355A1 (en) 2009-12-16
CN101622263B (zh) 2013-05-29
JP5221514B2 (ja) 2013-06-26
JPWO2008108384A1 (ja) 2010-06-17
CN101622263A (zh) 2010-01-06
EP2133355A4 (en) 2011-12-28
US20100094001A1 (en) 2010-04-15
IL200218A0 (en) 2010-04-29

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