JP2012524113A - ゲムシタビン構造に基づくプロドラッグおよびその合成方法と応用 - Google Patents

ゲムシタビン構造に基づくプロドラッグおよびその合成方法と応用 Download PDF

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JP2012524113A
JP2012524113A JP2012506308A JP2012506308A JP2012524113A JP 2012524113 A JP2012524113 A JP 2012524113A JP 2012506308 A JP2012506308 A JP 2012506308A JP 2012506308 A JP2012506308 A JP 2012506308A JP 2012524113 A JP2012524113 A JP 2012524113A
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dicarboxylic acid
gemcitabine
acid
anhydride
dicarboxylic
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JP2012524113A5 (enExample
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シュー，シャオシャ
リ，ガン
スン，チャンジュン
リ，ウェンバオ
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サンルゲン ファーマテック リミテッド
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Publication of JP2012524113A publication Critical patent/JP2012524113A/ja
Publication of JP2012524113A5 publication Critical patent/JP2012524113A5/ja
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    • 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
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
JP2012506308A 2009-04-21 2010-03-25 ゲムシタビン構造に基づくプロドラッグおよびその合成方法と応用 Pending JP2012524113A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN200910020716.7 2009-04-21
CN2009100207167A CN101525361B (zh) 2009-04-21 2009-04-21 基于吉西他滨结构的前药及其合成方法及应用
PCT/CN2010/000372 WO2010121486A1 (zh) 2009-04-21 2010-03-25 基于吉西他滨结构的前药及其合成方法及应用

Publications (2)

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JP2012524113A true JP2012524113A (ja) 2012-10-11
JP2012524113A5 JP2012524113A5 (enExample) 2013-05-09

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JP2012506308A Pending JP2012524113A (ja) 2009-04-21 2010-03-25 ゲムシタビン構造に基づくプロドラッグおよびその合成方法と応用

Country Status (7)

Country Link
US (1) US8653048B2 (enExample)
EP (1) EP2423215A4 (enExample)
JP (1) JP2012524113A (enExample)
CN (2) CN101525361B (enExample)
CA (1) CA2759474A1 (enExample)
IL (1) IL215792A0 (enExample)
WO (1) WO2010121486A1 (enExample)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015536954A (ja) * 2012-11-07 2015-12-24 ズカイ スオ 置換ゲムシタビンアリールアミド類似体
JP2016539956A (ja) * 2013-12-04 2016-12-22 杭州民生▲薬▼物研究院有限公司 ゲムシタビン誘導体、該誘導体を含む組成物及び該誘導体の製薬用途
JP2019508505A (ja) * 2016-03-14 2019-03-28 スフェラ ファーマ ピーブイティー リミテッドＳｐｈａｅｒａ Ｐｈａｒｍａ Ｐｖｔ． Ｌｔｄ． トリゴネリンベースの化合物

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* Cited by examiner, † Cited by third party
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CN101525361B (zh) 2009-04-21 2010-11-17 济南圣鲁金药物技术开发有限公司 基于吉西他滨结构的前药及其合成方法及应用
CN102115485A (zh) * 2009-12-30 2011-07-06 济南圣鲁金药物技术开发有限公司 基于阿糖胞苷结构的前药及其合成方法及应用
CN102432654A (zh) * 2011-09-26 2012-05-02 宋云龙 吉西他滨酰胺衍生物及其制备方法和用途
KR20150082606A (ko) 2012-11-13 2015-07-15 보옌 테라퓨틱스, 인크. 겜시타빈 전구약물 및 그의 용도
WO2014145207A1 (en) * 2013-03-15 2014-09-18 Ohio State Innovation Foundation Substituted gemcitabine bicyclic amide analogs and treatment methods using same
US10463684B2 (en) 2014-01-29 2019-11-05 Board Of Regents, The Uneversety Of Texas System Nucleobase analogue derivatives and their applications
US10059733B2 (en) * 2014-03-03 2018-08-28 Nucorion Pharmaceuticals, Inc. Gemcitabine analogs
CN105001291B (zh) * 2014-04-15 2018-12-04 上海知萌生物医药科技有限公司 吉西他滨化学传递前药及其制备方法和应用
CN104910024B (zh) * 2015-05-12 2017-02-22 四川理工学院 一种驱油用表面活性剂
US10435429B2 (en) 2017-10-03 2019-10-08 Nucorion Pharmaceuticals, Inc. 5-fluorouridine monophosphate cyclic triester compounds
AU2019207626B2 (en) 2018-01-10 2023-10-05 Nucorion Pharmaceuticals, Inc. Phosphor(n)amidatacetal and phosph(on)atalcetal compounds
US11427550B2 (en) 2018-01-19 2022-08-30 Nucorion Pharmaceuticals, Inc. 5-fluorouracil compounds
CN108329371B (zh) * 2018-03-06 2021-04-09 沈阳药科大学 白蛋白结合型吉西他滨前药及其合成和应用
CN113166189A (zh) * 2018-04-26 2021-07-23 纳米医学控股有限公司 吉西他滨两亲性前体药物
MX2022000573A (es) 2019-07-17 2022-02-10 Nucorion Pharmaceuticals Inc Compuestos ciclicos de desoxirribonucleotido.
CN110845560B (zh) * 2019-11-21 2021-08-24 广东中科药物研究有限公司 苯丙氨酸酰胺化的核苷酸衍生物及其制备方法与应用
CN111298132B (zh) * 2020-02-22 2022-06-24 新乡医学院 一种树状分子吉西他滨自组装纳米前药及其制备方法和应用
CN115605492B (zh) 2020-04-21 2025-09-16 配体制药股份有限公司 核苷酸前药化合物

Citations (2)

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Publication number Priority date Publication date Assignee Title
WO2004041203A2 (en) * 2002-11-04 2004-05-21 Xenoport, Inc. Gemcitabine prodrugs, pharmaceutical compositions and uses thereof
CN101525361A (zh) * 2009-04-21 2009-09-09 济南圣鲁金药物技术开发有限公司 基于吉西他滨结构的前药及其合成方法及应用

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US5637688A (en) * 1994-12-13 1997-06-10 Eli Lilly And Company Process for preparing 1-(2'-deoxy-2'-difluoro-d-ribofuranosyl)-4-aminopyrimidin-2-one hydrochloride
ATE236188T1 (de) 1997-01-24 2003-04-15 Conpharma As Gemcitabin-derivate
AU7361400A (en) 1999-09-08 2001-04-10 Metabasis Therapeutics, Inc. Prodrugs for liver specific drug delivery
GB0321613D0 (en) 2003-09-15 2003-10-15 Drug Discovery Lab As Compounds
US20050137141A1 (en) * 2003-10-24 2005-06-23 John Hilfinger Prodrug composition
EP1804838A2 (en) 2004-09-15 2007-07-11 Drug Discovery Laboratory AS Drug conjugates of long chain fatty acid or ester moieties as protein binding prodrugs
US7691827B2 (en) * 2004-12-17 2010-04-06 Eli Lilly And Company Amide prodrug of gemcitabine, compositions and use thereof
NO322682B1 (no) 2005-03-18 2006-11-27 Clavis Pharma Asa Anvendelse av gemcitabinderivater for fremstilling av orale doseringsformer ved kreftbehandling, samt slike orale doseringsformer
US20070225248A1 (en) 2006-03-21 2007-09-27 Clavis Pharma As Oral dosage forms of gemcitabine derivatives
CA2652633C (en) * 2006-06-21 2014-03-25 Eli Lilly And Company Crystalline forms of gemcitabine amide prodrug, compositions and use thereof
US20090068286A1 (en) * 2007-09-11 2009-03-12 Resprotect, Gmbh Method of treating cancer by administration of 5-substituted nucleosides
FR2922551B1 (fr) 2007-10-17 2009-12-25 Univ Claude Bernard Lyon Prodrogues phosphoesters de la gemcitabine comme agents anticancereux

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004041203A2 (en) * 2002-11-04 2004-05-21 Xenoport, Inc. Gemcitabine prodrugs, pharmaceutical compositions and uses thereof
CN101525361A (zh) * 2009-04-21 2009-09-09 济南圣鲁金药物技术开发有限公司 基于吉西他滨结构的前药及其合成方法及应用

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015536954A (ja) * 2012-11-07 2015-12-24 ズカイ スオ 置換ゲムシタビンアリールアミド類似体
JP2016539956A (ja) * 2013-12-04 2016-12-22 杭州民生▲薬▼物研究院有限公司 ゲムシタビン誘導体、該誘導体を含む組成物及び該誘導体の製薬用途
JP2019508505A (ja) * 2016-03-14 2019-03-28 スフェラ ファーマ ピーブイティー リミテッドＳｐｈａｅｒａ Ｐｈａｒｍａ Ｐｖｔ． Ｌｔｄ． トリゴネリンベースの化合物

Also Published As

Publication number Publication date
EP2423215A4 (en) 2013-05-22
CN101525361A (zh) 2009-09-09
CA2759474A1 (en) 2010-10-28
CN102428093A (zh) 2012-04-25
IL215792A0 (en) 2012-01-31
US20120088908A1 (en) 2012-04-12
WO2010121486A1 (zh) 2010-10-28
US8653048B2 (en) 2014-02-18
CN101525361B (zh) 2010-11-17
EP2423215A1 (en) 2012-02-29

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