WO2015178265A1 - Nouveau dérivé d'acide glutamique et utilisation associée - Google Patents

Nouveau dérivé d'acide glutamique et utilisation associée Download PDF

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Publication number
WO2015178265A1
WO2015178265A1 PCT/JP2015/063736 JP2015063736W WO2015178265A1 WO 2015178265 A1 WO2015178265 A1 WO 2015178265A1 JP 2015063736 W JP2015063736 W JP 2015063736W WO 2015178265 A1 WO2015178265 A1 WO 2015178265A1
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WO
WIPO (PCT)
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group
active substance
physiologically active
amino
glutamic acid
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PCT/JP2015/063736
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English (en)
Japanese (ja)
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米田　靖
啓子 関根
節子 新妻
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日本化薬株式会社
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Publication of WO2015178265A1 publication Critical patent/WO2015178265A1/fr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/20—Carbocyclic rings
    • C07H15/24—Condensed ring systems having three or more rings
    • C07H15/252—Naphthacene radicals, e.g. daunomycins, adriamycins
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06—Pyrimidine radicals
    • C07H19/067—Pyrimidine radicals with ribosyl as the saccharide radical

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Selon l'invention, il a été établi que l'interposition d'un coupleur d'amidation aromatique approprié dans la fabrication d'un promédicament destiné à servir de médicament à γ-glutamylation permet d'obtenir une stabilité même dans un environnement proche de l'environnement physiologique, une reconnaissance par GGT, ainsi qu'une libération rapide du principe pharmacologiquement actif. L'invention concerne plus particulièrement un médicament représenté par la formule générale (1), auquel un amide aromatique de γ-glutamyle a été lié, qui libère rapidement le principe pharmacologiquement actif dans des tissus en exprimant un niveau élevé de GGT. Le médicament selon l'invention peut devenir un médicament doté d'un effet thérapeutique élevé.
PCT/JP2015/063736 2014-05-23 2015-05-13 Nouveau dérivé d'acide glutamique et utilisation associée WO2015178265A1 (fr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
JP2014-106915 2014-05-23
JP2014106915 2014-05-23
JP2014238414 2014-11-26
JP2014-238414 2014-11-26

Publications (1)

Publication Number Publication Date
WO2015178265A1 true WO2015178265A1 (fr) 2015-11-26

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PCT/JP2015/063736 WO2015178265A1 (fr) 2014-05-23 2015-05-13 Nouveau dérivé d'acide glutamique et utilisation associée

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TW (1) TW201625313A (fr)
WO (1) WO2015178265A1 (fr)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017086392A1 (fr) * 2015-11-18 2017-05-26 日本化薬株式会社 Composition comprenant un nouveau dérivé de l'acide glutamique et un copolymère à blocs, et utilisation de cette dernière
WO2017094011A1 (fr) * 2015-12-03 2017-06-08 Biosight Ltd. Sels de conjugués en cancéro-thérapie
CN108431017A (zh) * 2015-12-03 2018-08-21 拜欧赛特有限公司 用于癌症疗法的缀合物的盐
WO2019172210A1 (fr) * 2018-03-03 2019-09-12 国立大学法人 東京大学 Agent anticancéreux de type promédicament utilisant une activité enzymatique spécifique du cancer
WO2021005583A1 (fr) 2019-07-11 2021-01-14 Sun Pharma Advanced Research Company Ltd. Dérivés de camptothécine ayant une fraction disulfure et une fraction pipérazine
US11058701B2 (en) 2015-12-03 2021-07-13 Biosight Ltd. Cytarabine conjugates for cancer therapy
CN114539353A (zh) * 2020-11-26 2022-05-27 南京碳硅人工智能生物医药技术研究院有限公司 培美曲塞多谷氨酸化代谢物及其制备方法

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005514359A (ja) * 2001-11-23 2005-05-19 中外製薬株式会社 腫瘍を標的とする酵素の同定法

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005514359A (ja) * 2001-11-23 2005-05-19 中外製薬株式会社 腫瘍を標的とする酵素の同定法

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
R KEREN ET AL.: "y-Glutamyl transpeptidase- dependent mutagenicity and cytotoxicity of y- glutamyl derivatives: A model for biochemical targeting of chemotherapeutic agents", ENVIRONMENTAL AND MOLECULAR MUTAGENESIS, vol. 32, no. 4, 1998, pages 377 - 386, XP055237992 *
ZHANG,Q. ET AL.: "A new class of NO -donor pro- drugs triggered by y-glutamyl transpeptidase with potential for reno-selective vasodilatation", CHEMICAL COMMUNICATIONS, vol. 49, no. 14, 2013, Cambridge, United Kingdom, pages 1389 - 1391 *
ZHANG,Q. ET AL.: "Development and Characterization of Glutamyl-Protected N- Hydroxyguanidines as Reno-Active Nitric Oxide Donor Drugs with Therapeutic Potential in Acute Renal Failure", JOURNAL OF MEDICINAL CHEMISTRY, vol. 56, no. 13, 2013, pages 5321 - 5334, XP055237991, ISSN: 0022-2623 *

Cited By (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPWO2017086392A1 (ja) * 2015-11-18 2018-09-06 日本化薬株式会社 新規なグルタミン酸誘導体とブロック共重合体を含有する組成物及びその用途
WO2017086392A1 (fr) * 2015-11-18 2017-05-26 日本化薬株式会社 Composition comprenant un nouveau dérivé de l'acide glutamique et un copolymère à blocs, et utilisation de cette dernière
EP3378495A4 (fr) * 2015-11-18 2019-09-04 Nippon Kayaku Kabushiki Kaisha Composition comprenant un nouveau dérivé de l'acide glutamique et un copolymère à blocs, et utilisation de cette dernière
CN108431017B (zh) * 2015-12-03 2021-12-21 拜欧赛特有限公司 用于癌症疗法的缀合物的盐
JP2022000463A (ja) * 2015-12-03 2022-01-04 バイオサイト リミテッド 癌療法のためのコンジュゲートの塩
CN108431017A (zh) * 2015-12-03 2018-08-21 拜欧赛特有限公司 用于癌症疗法的缀合物的盐
IL259569B2 (en) * 2015-12-03 2024-03-01 Biosight Ltd Salts of cytarabine-amino acid conjugate
IL259569B1 (en) * 2015-12-03 2023-11-01 Biosight Ltd Salts of cytarabine-amino acid conjugate
JP2018535987A (ja) * 2015-12-03 2018-12-06 バイオサイト リミテッド 癌療法のためのコンジュゲートの塩
WO2017094011A1 (fr) * 2015-12-03 2017-06-08 Biosight Ltd. Sels de conjugués en cancéro-thérapie
US11058701B2 (en) 2015-12-03 2021-07-13 Biosight Ltd. Cytarabine conjugates for cancer therapy
US11104698B2 (en) 2015-12-03 2021-08-31 Biosight Ltd. Salts of conjugates for cancer therapy
JPWO2019172210A1 (ja) * 2018-03-03 2021-02-25 国立大学法人 東京大学 がん特異的酵素活性を利用したプロドラッグ型抗がん剤
US11655269B2 (en) 2018-03-03 2023-05-23 The University Of Tokyo Prodrug-type anticancer agent using cancer-specific enzymatic activity
CN111801315A (zh) * 2018-03-03 2020-10-20 国立大学法人东京大学 利用癌特异性酶活性的前药型抗癌剂
WO2019172210A1 (fr) * 2018-03-03 2019-09-12 国立大学法人 東京大学 Agent anticancéreux de type promédicament utilisant une activité enzymatique spécifique du cancer
JP7442192B2 (ja) 2018-03-03 2024-03-04 国立大学法人 東京大学 がん特異的酵素活性を利用したプロドラッグ型抗がん剤
WO2021005583A1 (fr) 2019-07-11 2021-01-14 Sun Pharma Advanced Research Company Ltd. Dérivés de camptothécine ayant une fraction disulfure et une fraction pipérazine
CN114539353A (zh) * 2020-11-26 2022-05-27 南京碳硅人工智能生物医药技术研究院有限公司 培美曲塞多谷氨酸化代谢物及其制备方法

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