WO2009004899A1 - シアリダーゼ阻害剤 - Google Patents

シアリダーゼ阻害剤 Download PDF

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Publication number
WO2009004899A1
WO2009004899A1 PCT/JP2008/060639 JP2008060639W WO2009004899A1 WO 2009004899 A1 WO2009004899 A1 WO 2009004899A1 JP 2008060639 W JP2008060639 W JP 2008060639W WO 2009004899 A1 WO2009004899 A1 WO 2009004899A1
Authority
WO
WIPO (PCT)
Prior art keywords
sialidase
sialidase inhibitor
activity
aromatic ring
acid derivative
Prior art date
Application number
PCT/JP2008/060639
Other languages
English (en)
French (fr)
Inventor
Shin-Ichiro Nishimura
Hiroshi Hinou
Original Assignee
National University Corporation Hokkaido University
Shionogi & 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 National University Corporation Hokkaido University, Shionogi & Co., Ltd. filed Critical National University Corporation Hokkaido University
Priority to JP2009521565A priority Critical patent/JPWO2009004899A1/ja
Publication of WO2009004899A1 publication Critical patent/WO2009004899A1/ja

Links

Classifications

    • 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
    • C07H15/203—Monocyclic carbocyclic rings other than cyclohexane rings; Bicyclic carbocyclic ring systems
    • 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
    • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/7036—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
    • 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
    • A61K31/7056—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

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

Abstract

　【課題】　トリパノソーマ・クルジなどに存在するシアリダーゼの活性を阻害する新規シアリダーゼ阻害剤を提供する。　【解決手段】　９位及び２α位に芳香環を導入したＮ－アシルノイラミン酸誘導体は、強いシアリダーゼ活性の阻害効果を有する。　本発明は、Ｎ－アシルノイラミン酸誘導体　（下式、Ｒ１及びＲ2は、それぞれ独立に、芳香環を有する置換基を表す。）　又はその製薬上許容される塩から成るシアリダーゼ阻害剤である。　【化３】
PCT/JP2008/060639 2007-06-15 2008-06-11 シアリダーゼ阻害剤 WO2009004899A1 (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2009521565A JPWO2009004899A1 (ja) 2007-06-15 2008-06-11 シアリダーゼ阻害剤

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2007158635 2007-06-15
JP2007-158635 2007-06-15

Publications (1)

Publication Number Publication Date
WO2009004899A1 true WO2009004899A1 (ja) 2009-01-08

Family

ID=40225953

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2008/060639 WO2009004899A1 (ja) 2007-06-15 2008-06-11 シアリダーゼ阻害剤

Country Status (2)

Country Link
JP (1) JPWO2009004899A1 (ja)
WO (1) WO2009004899A1 (ja)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011157325A (ja) * 2010-02-03 2011-08-18 Keio Gijuku ノイラミニダーゼに対する酵素阻害剤
WO2013031239A1 (ja) 2011-09-02 2013-03-07 学校法人北里研究所 新規マングロマイシン化合物及びその製造方法
CN116003486A (zh) * 2023-03-27 2023-04-25 北京天之泰生物科技有限公司 一种先导化合物、其制备方法、以及其在制备抗流感病毒药物方面的应用

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0625209A (ja) * 1991-10-23 1994-02-01 Biota Scient Manag Pty Ltd α−Ｄ−ノイラミン酸の抗ウイルス性４−置換−２−デオキシ−２，３−ジデヒドロ誘導体
JPH10330373A (ja) * 1996-07-22 1998-12-15 Sankyo Co Ltd ノイラミン酸誘導体
JP2001131074A (ja) * 1999-08-20 2001-05-15 Inst Of Physical & Chemical Res シアル酸誘導体を有効成分として含む医薬
WO2007105094A1 (en) * 2006-03-14 2007-09-20 Universität Basel Method for the identification of new leads for drug candidates

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0625209A (ja) * 1991-10-23 1994-02-01 Biota Scient Manag Pty Ltd α−Ｄ−ノイラミン酸の抗ウイルス性４−置換−２−デオキシ−２，３−ジデヒドロ誘導体
JPH10330373A (ja) * 1996-07-22 1998-12-15 Sankyo Co Ltd ノイラミン酸誘導体
JP2001131074A (ja) * 1999-08-20 2001-05-15 Inst Of Physical & Chemical Res シアル酸誘導体を有効成分として含む医薬
WO2007105094A1 (en) * 2006-03-14 2007-09-20 Universität Basel Method for the identification of new leads for drug candidates

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
GROSS HANS JUERGEN ET AL.: "Enzymic introduction of a fluorescent sialic acid into oligosaccharide chains of glycoproteins, Fig.1.", EUROPEAN JOURNAL OF BIOCHEMISTRY, vol. 177, no. 3, 1988, pages 583 - 589, XP026265760 *
KAJIHARA YASUHIRO ET AL.: "Synthesis of CMP-9'' -modified-sialic acids as donor substrate analogues for mammalian and bacterial sialyltransferases, compounds 12 to 16", CARBOHYDRATE RESEARCH, vol. 342, no. 12-13, 5 June 2007 (2007-06-05), pages 1680 - 1688, XP029074256 *
SHELKE SACHIN V. ET AL.: "Synthesis of sialic acid derivatives as ligands for the myelin- associated glycoprotein(MAG) Tablel.", INTRODUCTION, BIOORGANIC & MEDICINAL CHEMISTRY, vol. 15, no. 14, 25 April 2007 (2007-04-25), pages 4951 - 4965, XP026265760 *

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011157325A (ja) * 2010-02-03 2011-08-18 Keio Gijuku ノイラミニダーゼに対する酵素阻害剤
WO2013031239A1 (ja) 2011-09-02 2013-03-07 学校法人北里研究所 新規マングロマイシン化合物及びその製造方法
US9000194B2 (en) 2011-09-02 2015-04-07 The Kitasato Institute Mangromicin compound and production method therefor
CN116003486A (zh) * 2023-03-27 2023-04-25 北京天之泰生物科技有限公司 一种先导化合物、其制备方法、以及其在制备抗流感病毒药物方面的应用

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Publication number Publication date
JPWO2009004899A1 (ja) 2010-08-26

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