CN103119047B - 三环类蛋白酶体活性增强化合物 - Google Patents

三环类蛋白酶体活性增强化合物 Download PDF

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Publication number
CN103119047B
CN103119047B CN201180045618.4A CN201180045618A CN103119047B CN 103119047 B CN103119047 B CN 103119047B CN 201180045618 A CN201180045618 A CN 201180045618A CN 103119047 B CN103119047 B CN 103119047B
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amyloidosis
disease
proteasome
alkyl
usp14
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Chinese (zh)
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CN103119047A (zh
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D·芬利
R·W·金
李秉宪
李民杰
T·C·甘曼
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Harvard University
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Harvard University
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/12Ophthalmic agents for cataracts
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Psychology (AREA)
  • Dermatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Saccharide Compounds (AREA)
CN201180045618.4A 2010-07-23 2011-07-22 三环类蛋白酶体活性增强化合物 Expired - Fee Related CN103119047B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US36717310P 2010-07-23 2010-07-23
US61/367,173 2010-07-23
PCT/US2011/044999 WO2012012712A2 (en) 2010-07-23 2011-07-22 Tricyclic proteasome activity enhancing compounds

Publications (2)

Publication Number Publication Date
CN103119047A CN103119047A (zh) 2013-05-22
CN103119047B true CN103119047B (zh) 2016-06-15

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Country Link
US (3) US8933087B2 (enExample)
EP (1) EP2595993B1 (enExample)
JP (1) JP6042331B2 (enExample)
CN (1) CN103119047B (enExample)
AU (1) AU2011281015B2 (enExample)
CA (1) CA2808432C (enExample)
WO (1) WO2012012712A2 (enExample)

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CN102844313B (zh) * 2010-01-28 2016-10-05 哈佛大学校长及研究员协会 提高蛋白酶体活性的组合物和方法
WO2012012712A2 (en) 2010-07-23 2012-01-26 President And Fellows Of Harvard College Tricyclic proteasome activity enhancing compounds
EP2663312B1 (en) 2011-01-10 2017-10-11 Nimbus Iris, Inc. Irak inhibitors and uses thereof
US9556166B2 (en) 2011-05-12 2017-01-31 Proteostasis Therapeutics, Inc. Proteostasis regulators
CN104582705A (zh) 2012-01-10 2015-04-29 林伯士艾瑞斯公司 白介素-1受体相关激酶(irak)抑制剂和其用途
WO2013112651A2 (en) 2012-01-25 2013-08-01 Proteostasis Therapeutics, Inc. Proteasome activity modulating compounds
CN104902959A (zh) 2012-07-11 2015-09-09 林伯士艾瑞斯公司 Irak抑制剂和其用途
EP2872144A4 (en) * 2012-07-11 2015-12-02 Nimbus Iris Inc IRAQ INHIBITOR AND USES THEREOF
JP2016504365A (ja) 2012-12-28 2016-02-12 アメリカ合衆国 Usp1/uaf1デユビキチナーゼ複合体阻害剤及びその使用
AU2014205577A1 (en) 2013-01-10 2015-05-28 Nimbus Iris, Inc. IRAK inhibitors and uses thereof
WO2014116228A1 (en) 2013-01-25 2014-07-31 President And Fellows Of Harvard College Usp14 inhibitors for treating or preventing viral infections
WO2014145576A2 (en) 2013-03-15 2014-09-18 Northwestern University Substituted pyrrolo(2,3-d)pyrimidines for the treatment of cancer
EP3049086A4 (en) 2013-09-27 2017-02-22 Nimbus Iris, Inc. Irak inhibitors and uses thereof
WO2015073528A1 (en) 2013-11-12 2015-05-21 Proteostasis Therapeutics, Inc. Proteasome activity enhancing compounds

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CN1522258A (zh) * 2001-04-30 2004-08-18 新的4-氨基-5,6-取代的噻吩并[2,3-d]嘧啶化合物
WO2007061764A2 (en) * 2005-11-22 2007-05-31 Merck & Co., Inc. Tricyclic compounds useful as inhibitors of kinases

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GB1570494A (en) * 1975-11-28 1980-07-02 Ici Ltd Thienopyrimidine derivatives and their use as pesticides
DD245666A1 (de) 1985-09-20 1987-05-13 Univ Halle Wittenberg Verfahren zur herstellung von 4-aminosubstituierten thieno 2,3-d-pyrimidin-2-ylessigsaeureestern
JPH01313480A (ja) 1988-06-14 1989-12-18 Nippon Soda Co Ltd ピリミジン誘導体、その製造方法及び農園芸用殺菌剤
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Also Published As

Publication number Publication date
US20160039839A1 (en) 2016-02-11
CN103119047A (zh) 2013-05-22
WO2012012712A3 (en) 2012-05-31
US20130210845A1 (en) 2013-08-15
AU2011281015A1 (en) 2013-03-07
JP6042331B2 (ja) 2016-12-14
EP2595993A2 (en) 2013-05-29
US8933087B2 (en) 2015-01-13
CA2808432C (en) 2019-06-04
AU2011281015B2 (en) 2015-09-24
CA2808432A1 (en) 2012-01-26
EP2595993A4 (en) 2014-01-08
EP2595993B1 (en) 2018-04-18
WO2012012712A2 (en) 2012-01-26
US20180265519A1 (en) 2018-09-20
US9981981B2 (en) 2018-05-29
JP2013532662A (ja) 2013-08-19

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Granted publication date: 20160615

Termination date: 20200722