JP6042331B2 - プロテアソーム活性を向上させる三環系化合物 - Google Patents

プロテアソーム活性を向上させる三環系化合物 Download PDF

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JP6042331B2
JP6042331B2 JP2013520880A JP2013520880A JP6042331B2 JP 6042331 B2 JP6042331 B2 JP 6042331B2 JP 2013520880 A JP2013520880 A JP 2013520880A JP 2013520880 A JP2013520880 A JP 2013520880A JP 6042331 B2 JP6042331 B2 JP 6042331B2
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disease
amyloidosis
usp14
proteasome
acid
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Japanese (ja)
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JP2013532662A (ja
JP2013532662A5 (https=
Inventor
フィンリー,ダニエル
ダブリュー キング,ランドール
ダブリュー キング,ランドール
リー,ビュン−ホン
ジャエ リー,ミン
ジャエ リー,ミン
シー ガーマン,ティモシー
シー ガーマン,ティモシー
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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)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Saccharide Compounds (AREA)
JP2013520880A 2010-07-23 2011-07-22 プロテアソーム活性を向上させる三環系化合物 Expired - Fee Related JP6042331B2 (ja)

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 (3)

Publication Number Publication Date
JP2013532662A JP2013532662A (ja) 2013-08-19
JP2013532662A5 JP2013532662A5 (https=) 2014-08-28
JP6042331B2 true JP6042331B2 (ja) 2016-12-14

Family

ID=45497483

Family Applications (1)

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JP2013520880A Expired - Fee Related JP6042331B2 (ja) 2010-07-23 2011-07-22 プロテアソーム活性を向上させる三環系化合物

Country Status (7)

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=)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX336731B (es) * 2010-01-28 2016-01-28 Harvard College Composiciones y metodos para potenciar la actividad de proteasoma.
AU2011281015B2 (en) 2010-07-23 2015-09-24 President And Fellows Of Harvard College Tricyclic proteasome activity enhancing compounds
US8703941B2 (en) 2011-01-10 2014-04-22 Nimbus Iris, Inc. IRAK inhibitors and uses thereof
DK2707101T3 (da) 2011-05-12 2019-05-13 Proteostasis Therapeutics Inc Proteostaseregulatorer
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
CA2861464C (en) * 2012-01-25 2018-03-06 Proteostasis Therapeutics, Inc. Proteasome activity modulating tricyclic compounds
WO2014011906A2 (en) 2012-07-11 2014-01-16 Nimbus Iris, Inc. Irak inhibitors and uses thereof
HK1210696A1 (en) * 2012-07-11 2016-05-06 Nimbus Iris, Inc. Irak inhibitors and uses thereof
CA2896731A1 (en) 2012-12-28 2014-07-03 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Inhibitors of the usp1/uaf1 deubiquitinase complex and uses thereof
JP2016505012A (ja) 2013-01-10 2016-02-18 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
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
BR112016006319A2 (pt) 2013-09-27 2017-08-01 Nimbus Iris Inc inibidores de irak e usos dos mesmos
WO2015073528A1 (en) 2013-11-12 2015-05-21 Proteostasis Therapeutics, Inc. Proteasome activity enhancing compounds

Family Cites Families (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3577420A (en) 1968-01-05 1971-05-04 Pfizer Certain 4-aminofuro(2,3-d)pyrimidines
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
WO1998029397A1 (en) * 1996-12-27 1998-07-09 Yoshitomi Pharmaceutical Industries, Ltd. Fused pyrimidine compounds and medicinal use thereof
EP1167367A4 (en) 1999-03-30 2002-04-24 Nippon Soda Co THIENOPYRIMIDINE COMPOUNDS AND SALTS THEREOF, AND PROCESS FOR THE PREPARATION THEREOF
WO2000066585A1 (en) 1999-04-30 2000-11-09 Neurogen Corporation 9H-PYRIMIDO[4,5-b]INDOLE DERIVATIVES: CRF1 SPECIFIC LIGANDS
JP2002105082A (ja) 2000-09-29 2002-04-10 Nippon Soda Co Ltd 縮合チエノピリミジン化合物、その塩及び製造法
DE10064994A1 (de) 2000-12-23 2002-07-04 Merck Patent Gmbh Sulfamidothienopyrimidine
CZ20032339A3 (cs) 2001-01-31 2004-09-15 Merck Patent Gmbh Farmaceutický prostředek obsahující parazolo [4,3-d]pyrimidiny a nitráty nebo thienopyrimidiny a nitráty
US6849638B2 (en) 2001-04-30 2005-02-01 Bayer Pharmaceuticals Corporation 4-amino-5,6-substituted thiopheno [2,3-d] pyrimidines, pharmaceutical compositions containing the same, and their use in the treatment or prevention of pde7b-mediated diseases and conditions
DE10148883A1 (de) 2001-10-04 2003-04-10 Merck Patent Gmbh Pyrimidinderivate
JP2003137886A (ja) * 2001-10-31 2003-05-14 Bayer Ag ピリミド[4,5−b]インドール
EP1442039A1 (en) * 2001-10-31 2004-08-04 Bayer HealthCare AG Pyrimido (4,5-b) indole derivatives
JP2006512313A (ja) 2002-10-31 2006-04-13 アムジェン インコーポレイテッド 抗炎症剤
ES2217956B1 (es) 2003-01-23 2006-04-01 Almirall Prodesfarma, S.A. Nuevos derivados de 4-aminotieno(2,3-d)pirimidin-6-carbonitrilo.
JP4677518B2 (ja) 2003-03-31 2011-04-27 エピックス デラウェア, インコーポレイテッド 新規ピペリジニルアミノ−チエノ[2,3−d]ピリミジン化合物
US7612078B2 (en) 2003-03-31 2009-11-03 Epix Delaware, Inc. Piperidinylamino-thieno[2,3-D] pyrimidine compounds
US8518964B2 (en) * 2005-11-22 2013-08-27 Merck Sharp & Dohme Corp. Tricyclic compounds useful as inhibitors of kinases
US7982035B2 (en) 2007-08-27 2011-07-19 Duquesne University Of The Holy Spirit Tricyclic compounds having antimitotic and/or antitumor activity and methods of use thereof
US7960400B2 (en) 2007-08-27 2011-06-14 Duquesne University Of The Holy Ghost Tricyclic compounds having cytostatic and/or cytotoxic activity and methods of use thereof
JP5461402B2 (ja) 2007-09-14 2014-04-02 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング 置換三環式化合物およびその使用方法
US20100227853A1 (en) 2008-04-18 2010-09-09 Trustees Of Boston College Inhibitors of cyclic amp phosphodiesterases
KR101703941B1 (ko) 2008-11-10 2017-02-07 내셔날 헬스 리서치 인스티튜트 티로신 키나아제 억제제로서의 접합 이환 및 삼환 피리미딘 화합물
MX2011008988A (es) 2009-02-27 2011-12-16 Siga Technologies Inc Derivados de tienopiridina para el tratamiento y prevencion de infecciones por el virus del dengue.
MX336731B (es) 2010-01-28 2016-01-28 Harvard College Composiciones y metodos para potenciar la actividad de proteasoma.
AU2011281015B2 (en) 2010-07-23 2015-09-24 President And Fellows Of Harvard College Tricyclic proteasome activity enhancing compounds
TW201219401A (en) 2010-09-14 2012-05-16 Lexicon Pharmaceuticals Inc Bicyclic inhibitors of Notum Pectinacetylesterase and methods of their use
WO2012062044A1 (zh) 2010-11-12 2012-05-18 Yao Xuebiao 动点马达蛋白cenp-e小分子抑制剂syntelin及其应用
US8703941B2 (en) 2011-01-10 2014-04-22 Nimbus Iris, Inc. IRAK inhibitors and uses thereof
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

Also Published As

Publication number Publication date
US8933087B2 (en) 2015-01-13
JP2013532662A (ja) 2013-08-19
EP2595993A4 (en) 2014-01-08
AU2011281015A1 (en) 2013-03-07
US20160039839A1 (en) 2016-02-11
US9981981B2 (en) 2018-05-29
CA2808432C (en) 2019-06-04
WO2012012712A3 (en) 2012-05-31
EP2595993A2 (en) 2013-05-29
CA2808432A1 (en) 2012-01-26
CN103119047A (zh) 2013-05-22
US20130210845A1 (en) 2013-08-15
US20180265519A1 (en) 2018-09-20
CN103119047B (zh) 2016-06-15
AU2011281015B2 (en) 2015-09-24
EP2595993B1 (en) 2018-04-18
WO2012012712A2 (en) 2012-01-26

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