WO2008096690A1 - ポリエチレングリコール誘導体 - Google Patents

ポリエチレングリコール誘導体 Download PDF

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Publication number
WO2008096690A1
WO2008096690A1 PCT/JP2008/051719 JP2008051719W WO2008096690A1 WO 2008096690 A1 WO2008096690 A1 WO 2008096690A1 JP 2008051719 W JP2008051719 W JP 2008051719W WO 2008096690 A1 WO2008096690 A1 WO 2008096690A1
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Prior art keywords
drug carrier
polyethylene glycol
derivative
glycol derivative
saturated
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PCT/JP2008/051719
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English (en)
French (fr)
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Satoru Sonoke
Toshihiro Ueda
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Nippon Shinyaku Co., Ltd.
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Priority to EP08704396.4A priority Critical patent/EP2119738B1/en
Priority to US12/525,570 priority patent/US8466255B2/en
Priority to JP2008557092A priority patent/JP5347510B2/ja
Publication of WO2008096690A1 publication Critical patent/WO2008096690A1/ja

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088Compounds having three or more nucleosides or nucleotides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088Compounds having three or more nucleosides or nucleotides
    • A61K31/7105Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088Compounds having three or more nucleosides or nucleotides
    • A61K31/711Natural deoxyribonucleic acids, i.e. containing only 2'-deoxyriboses attached to adenine, guanine, cytosine or thymine and having 3'-5' phosphodiester links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088Compounds having three or more nucleosides or nucleotides
    • A61K31/713Double-stranded nucleic acids or oligonucleotides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G65/00Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
    • C08G65/02Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring
    • C08G65/32Polymers modified by chemical after-treatment
    • C08G65/329Polymers modified by chemical after-treatment with organic compounds
    • C08G65/331Polymers modified by chemical after-treatment with organic compounds containing oxygen
    • C08G65/332Polymers modified by chemical after-treatment with organic compounds containing oxygen containing carboxyl groups, or halides, or esters thereof
    • C08G65/3322Polymers modified by chemical after-treatment with organic compounds containing oxygen containing carboxyl groups, or halides, or esters thereof acyclic
    • CCHEMISTRY; METALLURGY
    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G65/00Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
    • C08G65/02Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring
    • C08G65/32Polymers modified by chemical after-treatment
    • C08G65/329Polymers modified by chemical after-treatment with organic compounds
    • C08G65/333Polymers modified by chemical after-treatment with organic compounds containing nitrogen
    • C08G65/33303Polymers modified by chemical after-treatment with organic compounds containing nitrogen containing amino group
    • C08G65/33306Polymers modified by chemical after-treatment with organic compounds containing nitrogen containing amino group acyclic
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    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G2650/00Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
    • C08G2650/28Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule characterised by the polymer type
    • C08G2650/50Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule characterised by the polymer type containing nitrogen, e.g. polyetheramines or Jeffamines(r)
    • CCHEMISTRY; METALLURGY
    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08LCOMPOSITIONS OF MACROMOLECULAR COMPOUNDS
    • C08L2203/00Applications
    • C08L2203/02Applications for biomedical use

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
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  • General Health & Medical Sciences (AREA)
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  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biochemistry (AREA)
  • Polymers & Plastics (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
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  • Biomedical Technology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Polyethers (AREA)

Abstract

 本発明の目的は、主として、新規なポリエチレングリコール誘導体、当該誘導体を含有する薬物担体、及び医薬を包含する当該薬物担体を含有する医薬組成物を提供することにある。  本発明は、下記一般式(I)で表されるポリエチレングリコール誘導体、当該誘導体と2-O-(2-ジエチルアミノエチル)カルバモイル-1,3-O-ジオレオイルグリセロールとを含有する薬物担体、及び当該薬物担体と医薬(好ましくは、二本鎖RNA、二本鎖DNA、オリゴ核酸)とを含有する医薬組成物に関するものである。 式(I)中、Rは炭素数10~30の飽和若しくは不飽和の脂肪族炭化水素基、又は炭素数10~30の飽和若しくは不飽和の脂肪酸残基を表す。また、nは30~150の整数を表す。
PCT/JP2008/051719 2007-02-05 2008-02-04 ポリエチレングリコール誘導体 WO2008096690A1 (ja)

Priority Applications (3)

Application Number Priority Date Filing Date Title
EP08704396.4A EP2119738B1 (en) 2007-02-05 2008-02-04 Polyethylene glycol derivative
US12/525,570 US8466255B2 (en) 2007-02-05 2008-02-04 Polyethylene glycol derivative
JP2008557092A JP5347510B2 (ja) 2007-02-05 2008-02-04 ポリエチレングリコール誘導体

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
JP2007024992 2007-02-05
JP2007-024992 2007-02-05
JP2007-176827 2007-07-05
JP2007176827 2007-07-05

Publications (1)

Publication Number Publication Date
WO2008096690A1 true WO2008096690A1 (ja) 2008-08-14

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Family Applications (1)

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PCT/JP2008/051719 WO2008096690A1 (ja) 2007-02-05 2008-02-04 ポリエチレングリコール誘導体

Country Status (4)

Country Link
US (1) US8466255B2 (ja)
EP (1) EP2119738B1 (ja)
JP (1) JP5347510B2 (ja)
WO (1) WO2008096690A1 (ja)

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011164093A (ja) * 2010-01-18 2011-08-25 Seiko Epson Corp 吐出用液体、生体試料の吐出方法、及び化合物
WO2012029986A1 (ja) 2010-09-01 2012-03-08 日本新薬株式会社 アンチセンス核酸
WO2013100190A1 (ja) 2011-12-28 2013-07-04 日本新薬株式会社 アンチセンス核酸
JP2014505145A (ja) * 2011-01-11 2014-02-27 アルニラム・ファーマシューティカルズ・インコーポレーテッド Peg化脂質および薬剤送達のためのそれらの使用
US20140309277A1 (en) * 2009-12-23 2014-10-16 Novartis Ag Lipids, lipid compositions, and methods of using them
EP3514234A1 (en) 2014-03-12 2019-07-24 Nippon Shinyaku Co., Ltd. Antisense nucleic acid
WO2020138509A1 (en) 2018-12-28 2020-07-02 Nippon Shinyaku Co., Ltd. Myostatin signal inhibitor
EP3778895A1 (en) 2015-09-15 2021-02-17 Nippon Shinyaku Co., Ltd. Antisense nucleic acid

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2119738B1 (en) 2007-02-05 2014-04-16 Nippon Shinyaku Co., Ltd. Polyethylene glycol derivative
US10342761B2 (en) 2014-07-16 2019-07-09 Novartis Ag Method of encapsulating a nucleic acid in a lipid nanoparticle host
CN107200841B (zh) * 2016-03-17 2019-02-01 华东师范大学 一种培化二酰甘油的合成方法
EP3668915B1 (en) 2017-08-17 2023-03-08 SABIC Global Technologies B.V. Method of preparing fatty acid monoester of polyoxyethylene, ester made therewith, and uses thereof
WO2024105069A1 (en) * 2022-11-15 2024-05-23 Evonik Operations Gmbh Polyoxyalkylene-n,n-ditetradecylacetamid compounds, wherein the polyoxyalkylene is a poly(ethylene oxide) having c1 to c3-alkyloxymethyl side chains
EP4372027A1 (en) * 2022-11-15 2024-05-22 Johannes Gutenberg-Universität Mainz Use of polyethylenoxide polymers for the preparation of lipids conjugated with poly(ethylene oxide) having c1 to c3-alkyloxymethyl side chains
WO2024105068A1 (en) * 2022-11-15 2024-05-23 Evonik Operations Gmbh Lipids conjugated with poly(ethylene oxide) having c1 to c3-alkyloxymethyl side chains

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1994019314A1 (en) 1993-02-19 1994-09-01 Nippon Shinyaku Co., Ltd. Glycerol derivative, device and pharmaceutical composition
WO1997048712A1 (fr) * 1996-06-17 1997-12-24 Nippon Shinyaku Co., Ltd. Derives asialotrisaccharide moranoline et medicaments
WO1999020283A1 (fr) 1997-10-16 1999-04-29 Nippon Shinyaku Co., Ltd. Activateur de nuclease de cellules intracancereuses
WO1999048531A1 (fr) 1998-03-24 1999-09-30 Nippon Shinyaku Co., Ltd. Nouveaux remedes contre l'hepatite
JP2000281569A (ja) * 1999-03-25 2000-10-10 Nippon Shinyaku Co Ltd 脊髄障害治療剤
JP2003505401A (ja) * 1999-07-14 2003-02-12 アルザ・コーポレーション 中性リポポリマーとそれを含有するリポソーム組成物
WO2005030835A1 (ja) * 2003-09-25 2005-04-07 Terumo Kabushiki Kaisha ポリエチレングリコール誘導体及びこれを膜構成成分とする薬物担体
JP2007505954A (ja) * 2003-09-15 2007-03-15 プロチバ バイオセラピューティクス インコーポレイティッド ポリエチレングリコール修飾脂質化合物およびその使用

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US20060211642A1 (en) * 2001-05-18 2006-09-21 Sirna Therapeutics, Inc. RNA inteference mediated inhibition of hepatitis C virus (HVC) gene expression using short interfering nucleic acid (siNA)
US20040213835A1 (en) 2003-02-28 2004-10-28 Samuel Zalipsky Method to reduce liposome-induced complement activation
CN1747748B (zh) 2003-05-23 2011-01-19 尼克塔治疗公司 具有特定原子排列的聚合物衍生物
WO2004105774A1 (ja) * 2003-05-30 2004-12-09 Nippon Shinyaku Co., Ltd. オリゴ核酸担持複合体、当該複合体を含有する医薬組成物
WO2006022325A1 (ja) 2004-08-26 2006-03-02 Nippon Shinyaku Co., Ltd. ガラクトース誘導体、薬物担体及び医薬組成物
EP2119738B1 (en) 2007-02-05 2014-04-16 Nippon Shinyaku Co., Ltd. Polyethylene glycol derivative

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1994019314A1 (en) 1993-02-19 1994-09-01 Nippon Shinyaku Co., Ltd. Glycerol derivative, device and pharmaceutical composition
WO1997048712A1 (fr) * 1996-06-17 1997-12-24 Nippon Shinyaku Co., Ltd. Derives asialotrisaccharide moranoline et medicaments
WO1999020283A1 (fr) 1997-10-16 1999-04-29 Nippon Shinyaku Co., Ltd. Activateur de nuclease de cellules intracancereuses
WO1999048531A1 (fr) 1998-03-24 1999-09-30 Nippon Shinyaku Co., Ltd. Nouveaux remedes contre l'hepatite
JP2000281569A (ja) * 1999-03-25 2000-10-10 Nippon Shinyaku Co Ltd 脊髄障害治療剤
JP2003505401A (ja) * 1999-07-14 2003-02-12 アルザ・コーポレーション 中性リポポリマーとそれを含有するリポソーム組成物
JP2007505954A (ja) * 2003-09-15 2007-03-15 プロチバ バイオセラピューティクス インコーポレイティッド ポリエチレングリコール修飾脂質化合物およびその使用
WO2005030835A1 (ja) * 2003-09-25 2005-04-07 Terumo Kabushiki Kaisha ポリエチレングリコール誘導体及びこれを膜構成成分とする薬物担体

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Title
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, vol. 314, 2004, pages 283 - 291
JOURNAL OF CONTROLLED RELEASE, vol. 70, 2001, pages 295 - 307
KAZUKO HIRABAYASHI ET AL., CANCER RESEARCH, vol. 59, 1999, pages 4325 - 4333
KAZUKO HIRABAYASHI ET AL., ONCOLOGY RESEARCH, vol. 11, 1999, pages 497 - 504
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See also references of EP2119738A4
THE JOURNAL OF ORGANIC CHEMISTRY, vol. 35, 1970, pages 2082 - 2083

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20140309277A1 (en) * 2009-12-23 2014-10-16 Novartis Ag Lipids, lipid compositions, and methods of using them
US9301923B2 (en) * 2009-12-23 2016-04-05 Novartis Ag Lipids, lipid compositions, and methods of using them
JP2020007562A (ja) * 2009-12-23 2020-01-16 ノバルティス アーゲー 脂質、脂質組成物およびそれらの使用方法
JP2011164093A (ja) * 2010-01-18 2011-08-25 Seiko Epson Corp 吐出用液体、生体試料の吐出方法、及び化合物
WO2012029986A1 (ja) 2010-09-01 2012-03-08 日本新薬株式会社 アンチセンス核酸
JP2014505145A (ja) * 2011-01-11 2014-02-27 アルニラム・ファーマシューティカルズ・インコーポレーテッド Peg化脂質および薬剤送達のためのそれらの使用
WO2013100190A1 (ja) 2011-12-28 2013-07-04 日本新薬株式会社 アンチセンス核酸
EP3514234A1 (en) 2014-03-12 2019-07-24 Nippon Shinyaku Co., Ltd. Antisense nucleic acid
EP3778895A1 (en) 2015-09-15 2021-02-17 Nippon Shinyaku Co., Ltd. Antisense nucleic acid
WO2020138509A1 (en) 2018-12-28 2020-07-02 Nippon Shinyaku Co., Ltd. Myostatin signal inhibitor

Also Published As

Publication number Publication date
US20100074880A1 (en) 2010-03-25
JPWO2008096690A1 (ja) 2010-05-20
JP5347510B2 (ja) 2013-11-20
EP2119738A4 (en) 2011-08-17
EP2119738B1 (en) 2014-04-16
EP2119738A1 (en) 2009-11-18
US8466255B2 (en) 2013-06-18

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