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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic 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
    • C07D495/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/12—Ophthalmic agents for cataracts
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Endocrinology (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (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 (https=)
EP (1) EP2595993B1 (https=)
JP (1) JP6042331B2 (https=)
CN (1) CN103119047B (https=)
AU (1) AU2011281015B2 (https=)
CA (1) CA2808432C (https=)
WO (1) WO2012012712A2 (https=)

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KR20120117905A (ko) * 2010-01-28 2012-10-24 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 프로테아좀 활성을 향상시키는 조성물 및 방법
EP2595993B1 (en) 2010-07-23 2018-04-18 President and Fellows of Harvard College Tricyclic proteasome activity enhancing compounds
WO2012097013A1 (en) 2011-01-10 2012-07-19 Nimbus Iris, Inc. Irak inhibitors and uses thereof
HUE044867T2 (hu) 2011-05-12 2019-11-28 Proteostasis Therapeutics Inc Proteosztázis szabályzók
JP6126131B2 (ja) 2012-01-10 2017-05-10 ニンバス アイリス， インコーポレイテッド Ｉｒａｋ阻害剤およびその使用
EP2806875B1 (en) * 2012-01-25 2017-07-19 Proteostasis Therapeutics, Inc. Proteasome activity modulating compounds
WO2014011906A2 (en) 2012-07-11 2014-01-16 Nimbus Iris, Inc. Irak inhibitors and uses thereof
WO2014011902A1 (en) 2012-07-11 2014-01-16 Nimbus Iris, Inc. Irak inhibitors and uses thereof
EP2938610A2 (en) 2012-12-28 2015-11-04 The U.S.A. as represented by the Secretary, Department of Health and Human Services Inhibitors of the usp1/uaf1 deubiquitinase complex and uses thereof
CA2890911A1 (en) 2013-01-10 2014-07-17 Nimbus Iris, Inc. Irak inhibitors and uses thereof
US9849135B2 (en) 2013-01-25 2017-12-26 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
CN106232122A (zh) 2013-09-27 2016-12-14 林伯士艾瑞斯公司 Irak抑制剂和其用途
WO2015073528A1 (en) 2013-11-12 2015-05-21 Proteostasis Therapeutics, Inc. Proteasome activity enhancing compounds

Citations (3)

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

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Granted publication date: 20160615

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CF01 Termination of patent right due to non-payment of annual fee