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

Info

Publication number
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
Authority
JP
Japan
Prior art keywords
disease
amyloidosis
usp14
proteasome
acid
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
JP2013520880A
Other languages
English (en)
Japanese (ja)
Other versions
JP2013532662A5 (enExample
JP2013532662A (ja
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
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Harvard University
Original Assignee
Harvard University
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Harvard University filed Critical Harvard University
Publication of JP2013532662A publication Critical patent/JP2013532662A/ja
Publication of JP2013532662A5 publication Critical patent/JP2013532662A5/ja
Application granted granted Critical
Publication of JP6042331B2 publication Critical patent/JP6042331B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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

Landscapes

  • 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)
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 (enExample) 2014-08-28
JP6042331B2 true JP6042331B2 (ja) 2016-12-14

Family

ID=45497483

Family Applications (1)

Application Number Title Priority Date Filing Date
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 (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)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

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
AU7890598A (en) * 1996-12-27 1998-07-31 Yoshitomi Pharmaceutical Industries, Ltd. Fused pyrimidine compounds and medicinal use thereof
KR20010105399A (ko) 1999-03-30 2001-11-28 쓰끼하시 다미까따 티에노피리미딘 화합물 및 그의 염, 및 그들의 제조 방법
EP1175421A1 (en) 1999-04-30 2002-01-30 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
JP2004517940A (ja) 2001-01-31 2004-06-17 メルク　パテント　ゲゼルシャフト　ミット　ベシュレンクテル　ハフトング ピラゾロ［４，３−ｄ］ピリミジンおよびニトレートまたはチエノピリミジンおよびニトレートを含む医薬製剤
EP1401840A4 (en) 2001-04-30 2007-05-16 Bayer Corp NEW 4-AMINO-5,6-SUBSTITUTED THIOPHENO 2,3 D | PYRIMIDINE
DE10148883A1 (de) 2001-10-04 2003-04-10 Merck Patent Gmbh Pyrimidinderivate
WO2003037898A1 (en) * 2001-10-31 2003-05-08 Bayer Healthcare Ag Pyrimido [4,5-b] indole derivatives
JP2003137886A (ja) * 2001-10-31 2003-05-14 Bayer Ag ピリミド［４，５−ｂ］インドール
US7199119B2 (en) 2002-10-31 2007-04-03 Amgen Inc. Antiinflammation agents
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
JP5249772B2 (ja) * 2005-11-22 2013-07-31 メルク・シャープ・アンド・ドーム・コーポレーション キナーゼの阻害剤として有用な三環式化合物
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
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
WO2009033581A1 (en) 2007-09-14 2009-03-19 Bayer Schering Pharma Aktiengesellschaft Substituted tricyclic compounds and methods of use thereof
US20100227853A1 (en) 2008-04-18 2010-09-09 Trustees Of Boston College Inhibitors of cyclic amp phosphodiesterases
US8507502B2 (en) 2008-11-10 2013-08-13 National Health Research Institutes Fused bicyclic and tricyclic pyrimidine compounds as tyrosine kinase inhibitors
KR20110136819A (ko) 2009-02-27 2011-12-21 시가 테크놀로지스, 인크. 뎅기 바이러스 감염의 치료 및 예방을 위한 티에노피리딘 유도체
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
TW201219401A (en) 2010-09-14 2012-05-16 Lexicon Pharmaceuticals Inc Bicyclic inhibitors of Notum Pectinacetylesterase and methods of their use
CN103261205B (zh) 2010-11-12 2015-08-19 姚雪彪 动点马达蛋白cenp-e小分子抑制剂syntelin及其应用
EP2663312B1 (en) 2011-01-10 2017-10-11 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
US20160039839A1 (en) 2016-02-11
CN103119047A (zh) 2013-05-22
CN103119047B (zh) 2016-06-15
WO2012012712A3 (en) 2012-05-31
US20130210845A1 (en) 2013-08-15
AU2011281015A1 (en) 2013-03-07
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

Similar Documents

Publication Publication Date Title
JP6371786B2 (ja) プロテアソーム活性を向上させるための組成物および方法
JP6042331B2 (ja) プロテアソーム活性を向上させる三環系化合物
US20250188074A1 (en) Ptpn11 inhibitors
US9643977B2 (en) Necroptosis inhibitors and methods of use therefor
US20090291950A1 (en) Bicyclic heteroaryl inhibitors of pde4
CA3165382A1 (en) Combinations
JP2021503442A (ja) 中枢および末梢神経系障害の治療のためのキナーゼ阻害剤
CN109602734A (zh) 用于治疗白血病的化合物和方法
CN110753691A (zh) 化合物
US20230159439A1 (en) Arylamides and methods of use thereof
AU2017204046A1 (en) Compositions and methods for enhancing proteasome activity
CA2957566A1 (en) Indoline sulfonamide inhibitors of dape and ndm-1 and use of the same

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20140710

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20140710

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20150528

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20150616

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20150915

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20151215

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20160531

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20160830

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20161011

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20161109

R150 Certificate of patent or registration of utility model

Ref document number: 6042331

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

LAPS Cancellation because of no payment of annual fees