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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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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  • 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)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (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 (https=)
EP (2) EP1869060B1 (https=)
JP (1) JP5154954B2 (https=)
CN (1) CN101208352B (https=)
AU (1) AU2006220187B2 (https=)
CA (2) CA2599843C (https=)
WO (1) WO2006092049A1 (https=)

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WO2011140640A1 (en) * 2010-05-11 2011-11-17 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
US8933040B2 (en) 2010-11-08 2015-01-13 Craig A. Coburn Selective glycosidase inhibitors and uses thereof
US8901087B2 (en) * 2010-11-08 2014-12-02 Merck Sharp & Dohme Corp. Selective glycosidase inhibitors and uses thereof
TW201249848A (en) 2010-11-08 2012-12-16 Merck Sharp & Dohme Selective glycosidase inhibitors and uses thereof
WO2012061972A1 (en) * 2010-11-08 2012-05-18 Alectos Therapeutics Inc. 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
RU2609210C2 (ru) * 2010-12-23 2017-01-31 Алектос Терапьютикс Инк. Селективные ингибиторы гликозидазы и их применение
EP2688899B1 (en) 2011-03-24 2017-02-22 Alectos Therapeutics Inc. Selective glycosidase inhibitors and uses thereof
EP2691407B1 (en) 2011-03-31 2017-02-22 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
US9701693B2 (en) 2011-06-27 2017-07-11 Alectos Therapeutics Inc. Selective glycosidase inhibitors and uses thereof
EP2726468B1 (en) * 2011-06-27 2017-04-12 Alectos Therapeutics Inc. Selective glycosidase inhibitors and uses thereof
BR112013033098B8 (pt) 2011-06-27 2021-03-23 Alectos Therapeutics Inc inibidores de glicosidade seletivos e usos dos mesmos
US9126957B2 (en) 2011-08-18 2015-09-08 Merck Sharp & Dohme Corp. Selective glycosidase inhibitors and uses thereof
ES2568603T3 (es) * 2011-08-25 2016-05-03 Merck Patent Gmbh Pirano[3,2-d][1,3]tiazol como inhibidores de glicosidasas
EP2847199B1 (en) 2012-05-08 2017-10-25 Merck Sharp & Dohme Corp. Permeable glycosidase inhibitors and uses thereof
EP2890675A4 (en) 2012-08-31 2016-01-13 Alectos Therapeutics Inc GLYCOSIDASE INHIBITORS AND USES THEREOF
EP2890676B1 (en) 2012-08-31 2018-12-05 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
KR20150079711A (ko) * 2012-10-31 2015-07-08 알렉토스 테라퓨틱스 인크. 글리코시다아제 저해제 및 이의 용도
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
KR102043337B1 (ko) 2014-08-28 2019-11-11 아셰뉴론 에스아 글리코시다제 저해제
US11261183B2 (en) 2016-02-25 2022-03-01 Asceneuron Sa Sulfoximine glycosidase inhibitors
CA3014572C (en) 2016-02-25 2023-10-03 Asceneuron S.A. Acid addition salts of piperazine derivatives
KR20180132629A (ko) 2016-02-25 2018-12-12 아셰뉴론 에스아 글리코시다제 저해제
AU2017222964B2 (en) 2016-02-25 2020-01-02 Asceneuron S. A. Glycosidase inhibitors
US11213525B2 (en) 2017-08-24 2022-01-04 Asceneuron Sa Linear glycosidase inhibitors
WO2020039027A1 (en) 2018-08-22 2020-02-27 Asceneuron S. A. Pyrrolidine glycosidase inhibitors
JP7407171B2 (ja) 2018-08-22 2023-12-28 エースニューロン・ソシエテ・アノニム グリコシダーゼ阻害剤として有用なピペラジン誘導体のコハク酸付加塩及びフマル酸付加塩
WO2020039029A1 (en) 2018-08-22 2020-02-27 Asceneuron S. A. Spiro compounds as 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
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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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CA2737267A1 (en) * 2008-09-16 2010-04-08 Simon Fraser University Selective glycosidase inhibitors and uses thereof
WO2011140640A1 (en) * 2010-05-11 2011-11-17 Simon Fraser University Selective glycosidase inhibitors and uses thereof
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RU2609210C2 (ru) * 2010-12-23 2017-01-31 Алектос Терапьютикс Инк. Селективные ингибиторы гликозидазы и их применение
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EP2436687A1 (en) 2012-04-04
CA2819464A1 (en) 2006-09-08
EP1869060A4 (en) 2009-08-12
US20080287375A1 (en) 2008-11-20
WO2006092049A1 (en) 2006-09-08
AU2006220187A1 (en) 2006-09-08
CA2599843C (en) 2013-08-27
JP5154954B2 (ja) 2013-02-27
CA2599843A1 (en) 2006-09-08
EP1869060A1 (en) 2007-12-26
AU2006220187B2 (en) 2012-11-08
CN101208352A (zh) 2008-06-25
JP2008531604A (ja) 2008-08-14
EP1869060B1 (en) 2012-08-15

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