CN101208352B - 选择性糖苷酶抑制剂、该抑制剂的制备方法和用途 - Google Patents

选择性糖苷酶抑制剂、该抑制剂的制备方法和用途 Download PDF

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Publication number
CN101208352B
CN101208352B CN2006800149950A CN200680014995A CN101208352B CN 101208352 B CN101208352 B CN 101208352B CN 2006800149950 A CN2006800149950 A CN 2006800149950A CN 200680014995 A CN200680014995 A CN 200680014995A CN 101208352 B CN101208352 B CN 101208352B
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thiazole
glucopyranosyl
dideoxy
thiazoline
tetrahydro
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CN101208352A (zh
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D·沃卡多
G·惠特沃斯
M·莫考雷
K·斯塔布斯
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Simon Fraser University
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Simon Fraser University
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Pyrane Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN2006800149950A 2005-03-01 2006-03-01 选择性糖苷酶抑制剂、该抑制剂的制备方法和用途 Expired - Fee Related CN101208352B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US65687805P 2005-03-01 2005-03-01
US60/656,878 2005-03-01
PCT/CA2006/000300 WO2006092049A1 (en) 2005-03-01 2006-03-01 Selective glycosidase inhibitors, methods of making inhibitors, and uses thereof

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CN101208352A CN101208352A (zh) 2008-06-25
CN101208352B true CN101208352B (zh) 2013-08-07

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US (1) US20080287375A1 (enExample)
EP (2) EP2436687A1 (enExample)
JP (1) JP5154954B2 (enExample)
CN (1) CN101208352B (enExample)
AU (1) AU2006220187B2 (enExample)
CA (2) CA2599843C (enExample)
WO (1) WO2006092049A1 (enExample)

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CN107253970A (zh) * 2006-08-31 2017-10-17 西蒙·弗雷瑟大学 选择性糖苷酶抑制剂及其用途
EP2057171A4 (en) * 2006-08-31 2010-04-21 Univ Fraser Simon SELECTIVE GLYCOSIDASE INHIBITORS AND APPLICATIONS THEREOF
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US8518903B2 (en) 2007-04-19 2013-08-27 University of Pittsburgh—of the Commonwealth System of Higher Education Use of toll-like receptor-9 agonists
AU2009276222B2 (en) 2008-08-01 2015-03-05 Simon Fraser University Selective glycosidase inhibitors and uses thereof
JP5687194B2 (ja) * 2008-08-01 2015-03-18 サイモン フレイザー ユニバーシティ 選択的グリコシダーゼインヒビターおよびその使用
EP2344452A4 (en) * 2008-09-16 2012-03-14 Univ Fraser Simon SELECTIVE GLYCOSIDASE HEMMER AND ITS USE
US9120781B2 (en) 2010-05-11 2015-09-01 Simon Fraser University Selective glycosidase inhibitors and uses thereof
US10668092B2 (en) 2010-09-24 2020-06-02 The John Hopkins University Compositions and methods for treatment of inflammatory disorders
US9072760B2 (en) 2010-09-24 2015-07-07 University of Pittsburgh—of the Commonwealth System of Higher Education TLR4 inhibitors for the treatment of human infectious and inflammatory disorders
WO2012040719A2 (en) * 2010-09-24 2012-03-29 University Of Pittsburgh - Of The Commonwealth System Of Higher Education Novel tlr4 inhibitors for the treatment of human infectious and inflammatory disorders
WO2012061972A1 (en) * 2010-11-08 2012-05-18 Alectos Therapeutics Inc. Selective glycosidase inhibitors and uses thereof
US8901087B2 (en) * 2010-11-08 2014-12-02 Merck Sharp & Dohme Corp. Selective glycosidase inhibitors and uses thereof
US8933040B2 (en) 2010-11-08 2015-01-13 Craig A. Coburn Selective glycosidase inhibitors and uses thereof
TW201249848A (en) 2010-11-08 2012-12-16 Merck Sharp & Dohme Selective glycosidase inhibitors and uses thereof
WO2012088425A2 (en) 2010-12-22 2012-06-28 University Of Pittsburgh - Of The Commonwealth System Of Higher Education Gap junction-enhancing agents for treatment of necrotizing enterocolitis and inflammatory bowel disease
LT2655388T (lt) 2010-12-23 2016-11-10 Alectos Therapeutics Inc. Selektyvieji glikozidazės inhibitoriai ir jų panaudojimas
US8927507B2 (en) * 2011-03-24 2015-01-06 Ernest J. McEachern Selective glycosidase inhibitors and uses thereof
US9718854B2 (en) 2011-03-31 2017-08-01 Alectos Therapeutics Inc. Selective glycosidase inhibitors and uses thereof
WO2012129802A1 (en) * 2011-03-31 2012-10-04 Alectos Therapeutics Inc. Pyrano[3,2-d]thiazol derivatives and uses as selective glycosidase inhibitors thereof
WO2013000084A1 (en) 2011-06-27 2013-01-03 Alectos Therapeutics Inc. Selective glycosidase inhibitors and uses thereof
US9199949B2 (en) 2011-06-27 2015-12-01 Alectos Therapeutics Inc. Selective glycosidase inhibitors and uses thereof
US9701693B2 (en) 2011-06-27 2017-07-11 Alectos Therapeutics Inc. Selective glycosidase inhibitors and uses thereof
EP2744338B1 (en) 2011-08-18 2016-04-27 Merck Sharp & Dohme Corp. Selective glycosidase inhibitors and uses thereof
HRP20160334T1 (hr) * 2011-08-25 2016-05-06 Merck Patent Gmbh Pirano [3, 2 - d][1, 3]tiazol kao inhibitori glikozidaze
KR102108586B1 (ko) * 2012-05-08 2020-05-07 머크 샤프 앤드 돔 코포레이션 투과성 글리코시다제 억제제 및 그의 용도
WO2014032185A1 (en) 2012-08-31 2014-03-06 Alectos Therapeutics Inc. Glycosidase inhibitors and uses thereof
WO2014032188A1 (en) 2012-08-31 2014-03-06 Alectos Therapeutics Inc. Glycosidase inhibitors and uses thereof
WO2014052453A1 (en) 2012-09-25 2014-04-03 University Of Pittsburgh - Of The Commonwealth System Of Higher Education Oral therapy of necrotizing enterocolitis
CA2890115A1 (en) * 2012-10-31 2014-05-08 Alectos Therapeutics Inc. Glycosidase inhibitors and uses thereof
WO2014100934A1 (en) 2012-12-24 2014-07-03 Merck Sharp & Dohme Corp. Glycosidase inhibitors and uses thereof
WO2014171206A1 (ja) * 2013-04-17 2014-10-23 Yuasa Tomoyuki 糖尿病治療薬の新規なスクリーニング方法
BR112017003658B1 (pt) 2014-08-28 2022-12-06 Asceneuron Sa Composto, mistura, método para inibição de uma glicosidase, e, composição farmacêutica
US11612599B2 (en) 2016-02-25 2023-03-28 Asceneuron Sa Glycosidase inhibitors
EP3419976B1 (en) 2016-02-25 2021-04-07 Asceneuron SA Acid addition salts of piperazine derivatives
EP3585783A2 (en) 2016-02-25 2020-01-01 Asceneuron SA Sulfoximine glycosidase inhibitors
AU2017222964B2 (en) 2016-02-25 2020-01-02 Asceneuron S. A. Glycosidase inhibitors
EP3672959A1 (en) 2017-08-24 2020-07-01 Asceneuron SA Linear glycosidase inhibitors
US11731972B2 (en) 2018-08-22 2023-08-22 Asceneuron Sa Spiro compounds as glycosidase inhibitors
EP3841093B1 (en) 2018-08-22 2023-06-21 Asceneuron SA Succinate and fumarate acid addition salts of piperazine derivatives useful as glycosidase inhibitors
US12016852B2 (en) 2018-08-22 2024-06-25 Asceneuron Sa Pyrrolidine glycosidase inhibitors
WO2020039028A1 (en) 2018-08-22 2020-02-27 Asceneuron S. A. Tetrahydro-benzoazepine glycosidase inhibitors
CN114524854B (zh) * 2022-02-25 2023-05-26 中国农业大学 一种糖基芳香环碳苷衍生物及其制备方法与应用
WO2024083820A1 (en) 2022-10-18 2024-04-25 Institut National de la Santé et de la Recherche Médicale Method and composition for determining the level of o-glcnacylation in horses
CN116376875B (zh) * 2023-03-03 2024-02-23 云南师范大学 耐热性提高的n-乙酰氨基葡萄糖苷酶突变体及其应用
CN116555229B (zh) * 2023-05-25 2024-09-20 云南师范大学 N-乙酰氨基葡萄糖苷酶突变体、重组表达载体及菌和应用
CN118086249B (zh) * 2024-01-24 2024-12-06 云南师范大学 一种协同提高酶活和热稳定性的n-乙酰氨基葡萄糖苷酶突变体及其制备与应用

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AU2009276222B2 (en) * 2008-08-01 2015-03-05 Simon Fraser University Selective glycosidase inhibitors and uses thereof
JP5687194B2 (ja) * 2008-08-01 2015-03-18 サイモン フレイザー ユニバーシティ 選択的グリコシダーゼインヒビターおよびその使用
EP2344452A4 (en) * 2008-09-16 2012-03-14 Univ Fraser Simon SELECTIVE GLYCOSIDASE HEMMER AND ITS USE
US9120781B2 (en) * 2010-05-11 2015-09-01 Simon Fraser University Selective glycosidase inhibitors and uses thereof
US8933040B2 (en) * 2010-11-08 2015-01-13 Craig A. Coburn Selective glycosidase inhibitors and uses thereof
LT2655388T (lt) * 2010-12-23 2016-11-10 Alectos Therapeutics Inc. Selektyvieji glikozidazės inhibitoriai ir jų panaudojimas
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Publication number Publication date
EP1869060A4 (en) 2009-08-12
CA2599843A1 (en) 2006-09-08
EP2436687A1 (en) 2012-04-04
CA2599843C (en) 2013-08-27
EP1869060A1 (en) 2007-12-26
US20080287375A1 (en) 2008-11-20
EP1869060B1 (en) 2012-08-15
JP2008531604A (ja) 2008-08-14
WO2006092049A1 (en) 2006-09-08
AU2006220187A1 (en) 2006-09-08
JP5154954B2 (ja) 2013-02-27
CA2819464A1 (en) 2006-09-08
CN101208352A (zh) 2008-06-25
AU2006220187B2 (en) 2012-11-08

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