JP2013518129A - 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 - Google Patents

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 Download PDF

Info

Publication number
JP2013518129A
JP2013518129A JP2012551323A JP2012551323A JP2013518129A JP 2013518129 A JP2013518129 A JP 2013518129A JP 2012551323 A JP2012551323 A JP 2012551323A JP 2012551323 A JP2012551323 A JP 2012551323A JP 2013518129 A JP2013518129 A JP 2013518129A
Authority
JP
Japan
Prior art keywords
alkyl
proteasome
usp14
compound
compound according
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.)
Pending
Application number
JP2012551323A
Other languages
English (en)
Japanese (ja)
Other versions
JP2013518129A5 (OSRAM
Inventor
フィンリー，ダニエル
ダブリュー キング，ランダール
リー，ビュン−フン
ジェ リー，ミン
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 JP2013518129A publication Critical patent/JP2013518129A/ja
Publication of JP2013518129A5 publication Critical patent/JP2013518129A5/ja
Pending legal-status Critical Current

Links

Classifications

    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/33—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/333—Radicals substituted by oxygen or sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/33—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/335—Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44—Iso-indoles; Hydrogenated iso-indoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/573—Immunoassay; Biospecific binding assay; Materials therefor for enzymes or isoenzymes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/90—Enzymes; Proenzymes
    • G01N2333/914—Hydrolases (3)
    • G01N2333/948—Hydrolases (3) acting on peptide bonds (3.4)
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • G01N2500/04—Screening involving studying the effect of compounds C directly on molecule A (e.g. C are potential ligands for a receptor A, or potential substrates for an enzyme A)

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Molecular Biology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Biochemistry (AREA)
  • Analytical Chemistry (AREA)
  • Biotechnology (AREA)
  • Cell Biology (AREA)
  • Microbiology (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Food Science & Technology (AREA)
  • Physics & Mathematics (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
JP2012551323A 2010-01-28 2011-01-28 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 Pending JP2013518129A (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US33695910P 2010-01-28 2010-01-28
US61/336,959 2010-01-28
US37340410P 2010-08-13 2010-08-13
US61/373,404 2010-08-13
PCT/US2011/022929 WO2011094545A2 (en) 2010-01-28 2011-01-28 Compositions and methods for enhancing proteasome activity

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2016060063A Division JP6371786B2 (ja) 2010-01-28 2016-03-24 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

Publications (2)

Publication Number Publication Date
JP2013518129A true JP2013518129A (ja) 2013-05-20
JP2013518129A5 JP2013518129A5 (OSRAM) 2013-12-26

Family

ID=44320152

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2012551323A Pending JP2013518129A (ja) 2010-01-28 2011-01-28 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
JP2016060063A Expired - Fee Related JP6371786B2 (ja) 2010-01-28 2016-03-24 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

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2016060063A Expired - Fee Related JP6371786B2 (ja) 2010-01-28 2016-03-24 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

Country Status (12)

Country Link
US (2) US20130045992A1 (OSRAM)
EP (1) EP2528911B1 (OSRAM)
JP (2) JP2013518129A (OSRAM)
KR (1) KR20120117905A (OSRAM)
CN (1) CN102844313B (OSRAM)
AU (1) AU2011210765A1 (OSRAM)
BR (1) BR112012018631A8 (OSRAM)
CA (1) CA2787785C (OSRAM)
MX (1) MX336731B (OSRAM)
RU (1) RU2012136451A (OSRAM)
SG (1) SG182662A1 (OSRAM)
WO (1) WO2011094545A2 (OSRAM)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2019501142A (ja) * 2015-11-30 2019-01-17 ミッション セラピューティクス リミティド Ｕｓｐ３０の阻害剤としての１−シアノピロリジン誘導体
JP2021530465A (ja) * 2018-06-27 2021-11-11 プロテオステイシス セラピューティクス， インコーポレイテッド プロテアソーム活性増強化合物
JP2022012379A (ja) * 2020-07-01 2022-01-17 国立大学法人富山大学 ユビキチン－プロテアソーム系の活性化剤、およびその利用

Families Citing this family (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG182662A1 (en) 2010-01-28 2012-08-30 Harvard College Compositions and methods for enhancing proteasome activity
JP6042331B2 (ja) 2010-07-23 2016-12-14 プレジデント アンド フェローズ オブ ハーバード カレッジ プロテアソーム活性を向上させる三環系化合物
WO2012154967A1 (en) * 2011-05-12 2012-11-15 Proteostasis Therapeutics, Inc. Proteostasis regulators
US9856511B2 (en) 2011-09-16 2018-01-02 Vivolux Ab Protease deubiquitinating inhibitor screening
EP2806875B1 (en) * 2012-01-25 2017-07-19 Proteostasis Therapeutics, Inc. Proteasome activity modulating compounds
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
US9849135B2 (en) 2013-01-25 2017-12-26 President And Fellows Of Harvard College USP14 inhibitors for treating or preventing viral infections
US10563225B2 (en) * 2013-07-26 2020-02-18 President And Fellows Of Harvard College Genome engineering
WO2015073528A1 (en) 2013-11-12 2015-05-21 Proteostasis Therapeutics, Inc. Proteasome activity enhancing compounds
EA031804B1 (ru) 2014-02-03 2019-02-28 Вайтаи Фармасьютиклз, Инк. Дигидропирролопиридиновые ингибиторы ror-гамма
CN104844704B (zh) * 2014-02-17 2018-02-23 华东师范大学 Ub‑Nanoluc、Ub‑Ub‑GS‑Nanoluc报告基因系统及其构建和应用
SI3207043T1 (sl) 2014-10-14 2019-04-30 Vitae Pharmaceuticals, Inc. Dihidropirolopiridinovi inhibitorji za ROR-gama
US9663515B2 (en) 2014-11-05 2017-05-30 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
US9845308B2 (en) 2014-11-05 2017-12-19 Vitae Pharmaceuticals, Inc. Isoindoline inhibitors of ROR-gamma
CN104478780B (zh) * 2014-11-17 2017-04-19 华东师范大学 酰基吡咯类小分子有机化合物及其衍生物、用途及其制备方法
WO2017024018A1 (en) 2015-08-05 2017-02-09 Vitae Pharmaceuticals, Inc. Modulators of ror-gamma
CN108463458B (zh) 2015-11-20 2022-02-01 生命医药有限责任公司 ROR-γ的调节剂
CA3010615C (en) 2016-01-14 2024-02-20 Beth Israel Deaconess Medical Center, Inc. Mast-cell modulators and uses thereof
TW202220968A (zh) 2016-01-29 2022-06-01 美商維它藥物有限責任公司 ＲＯＲ－γ調節劑
CN109641874A (zh) 2016-05-10 2019-04-16 C4医药公司 用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体
CN109790143A (zh) 2016-05-10 2019-05-21 C4医药公司 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体
WO2017197055A1 (en) * 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
US9481674B1 (en) 2016-06-10 2016-11-01 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
CN106065389A (zh) * 2016-08-08 2016-11-02 山东理工大学 一种促进木瓜蛋白酶活性的方法及其在啤酒澄清中的应用
CN106281935A (zh) * 2016-08-08 2017-01-04 山东理工大学 一种促进中性蛋白酶活性的方法及其在啤酒澄清中的应用
CN107903208B (zh) * 2016-12-26 2021-09-03 杭州市西溪医院 一类联芳吡啶类去泛素化酶抑制剂、其制备方法及应用
CN110769822A (zh) 2017-06-20 2020-02-07 C4医药公司 用于蛋白降解的n/o-连接的降解决定子和降解决定子体
WO2019023207A1 (en) 2017-07-24 2019-01-31 Vitae Pharmaceuticals, Inc. Inhibitors of rorϒ
WO2019018975A1 (en) 2017-07-24 2019-01-31 Vitae Pharmaceuticals, Inc. INHIBITORS OF ROR GAMMA
CN111372585A (zh) 2017-11-16 2020-07-03 C4医药公司 用于靶蛋白降解的降解剂和降解决定子
JP2021519337A (ja) 2018-03-26 2021-08-10 シー４ セラピューティクス， インコーポレイテッド Ｉｋａｒｏｓの分解のためのセレブロン結合剤
EP3781156A4 (en) 2018-04-16 2022-05-18 C4 Therapeutics, Inc. SPIROCYCLIC COMPOUNDS
CR20200652A (es) * 2018-06-27 2021-04-28 Proteostasis Therapeutics Inc Compuestos que aumentan la actividad del proteosoma
CN120698985A (zh) 2018-12-20 2025-09-26 C4医药公司 靶向蛋白降解
WO2021146386A1 (en) * 2020-01-14 2021-07-22 The Trustees Of Columbia University In The City Of New York Compositions and methods for targeted protein stabilization by redirecting endogenous deubiquitinases
WO2022250363A1 (ko) * 2021-05-24 2022-12-01 재단법인대구경북과학기술원 아이유원 계열의 유비퀴틴 특이적 프로테아제 14 억제제를 유효성분으로 포함하는, 프로탁의 항암 효과 증진용 약학적 조성물
WO2025219559A1 (en) * 2024-04-18 2025-10-23 Booster Therapeutics Gmbh Pyrrolidine compounds as proteasome stimulators
CN119707772B (zh) * 2024-12-23 2025-09-02 浙江大学 一种usp14共价抑制剂及其制备方法和应用

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005025515A2 (en) * 2003-09-12 2005-03-24 California Institute Of Technology Proteasome pathway inhibitors and related methods
JP2007502304A (ja) * 2003-08-14 2007-02-08 セファロン、インク． プロテアソーム阻害剤及びそれらを使用する方法
JP2007502851A (ja) * 2003-05-22 2007-02-15 ファルマシア・イタリア・エス・ピー・エー ピラゾロ−キナゾリン誘導体、その製造方法、およびキナーゼ阻害剤としてのその使用
WO2008147536A1 (en) * 2007-05-24 2008-12-04 President And Fellows For Harvard College Methods and compositions for enhancing proteasome activity
WO2009086303A2 (en) * 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
WO2009118292A1 (en) * 2008-03-24 2009-10-01 Novartis Ag Arylsulfonamide-based matrix metalloprotease inhibitors
JP2013532662A (ja) * 2010-07-23 2013-08-19 プレジデント アンド フェロウズ オブ ハーバード カレッジ プロテアソーム活性を向上させる三環系化合物

Family Cites Families (115)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2557341A1 (de) * 1975-12-19 1977-06-30 Hoechst Ag Basisch substituierte indolderivate und verfahren zu ihrer herstellung
AU531214B2 (en) 1979-06-28 1983-08-11 Ciba-Geigy Ag Stabilizers for chlorinated thermoplast
NL8701682A (nl) 1986-07-30 1988-02-16 Sandoz Ag Werkwijze voor het therapeutisch toepassen van serotonine antagonisten, aktieve verbindingen en farmaceutische preparaten die deze verbindingen bevatten.
TW226019B (OSRAM) 1992-03-23 1994-07-01 Sankyo Co
DE4325204C2 (de) 1993-07-27 2002-11-28 Matthias Lehr Acylpyrrolalkansäuren und ihre Derivate als Hemmstoffe der Phospholipase A¶2¶
US5852046A (en) 1993-08-03 1998-12-22 Hoechst Aktiengesellschaft Benzo-fused heterocyclic compounds having a 5-membered ring processes for their preparation their use as medicaments their use as diagnostic agents and medicaments containing them
EP0639573A1 (de) 1993-08-03 1995-02-22 Hoechst Aktiengesellschaft Benzokondensierte 5-Ringheterocyclen, Verfahren zu ihrer Herstellung, ihre Verwendung als Medikament, ihre Verwendung als Diagnostikum, sowie sie enthaltendes Medikament
JPH07133274A (ja) 1993-11-09 1995-05-23 Sankyo Co Ltd ピロール誘導体
DE4338770A1 (de) 1993-11-12 1995-05-18 Matthias Dr Lehr Indol-2-alkansäuren und ihre Derivate als Hemmstoffe der Phospholipase A¶2¶
PT742218E (pt) 1994-01-19 2003-02-28 Sankyo Co Derivados de pirrolopiridazina
JPH11501004A (ja) 1995-02-01 1999-01-26 ユニヴァーシティー・カレッジ・カーディフ・コンサルタンツ・リミテッド 三環系誘導体及びそれらの抗ガン剤としての使用
US5859035A (en) 1996-04-03 1999-01-12 Merck & Co., Inc. Arylheteroaryl inhibitors of farnesyl-protein transferase
WO1997036881A1 (en) 1996-04-03 1997-10-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
DE19622222A1 (de) 1996-06-03 1997-12-04 Hoechst Ag Verwendung von Inhibitoren des zellulären Na·+·/H·+·-Exchangers (NHE) zur Herstellung eines Medikament zur Normalisierung der Serumlipide
US20040122096A1 (en) 1996-06-03 2004-06-24 Hoechst Aktiengesellschaft Use of inhibitors of the cellular Na+/H+ exchanger (NHE) for preparing a medicament for normalizing serum lipids
JP2000515529A (ja) 1996-08-01 2000-11-21 メルクル・ゲーエムベーハー 細胞質ホスホリパーゼａ▲下２▼の阻害剤としてのアシルピロリドンジカルボン酸およびアシルインドールジカルボン酸ならびにその誘導体
US5998462A (en) 1996-12-16 1999-12-07 Allelix Biopharmaceuticals Inc. 5-alkyl indole compounds
US6828344B1 (en) 1998-02-25 2004-12-07 Genetics Institute, Llc Inhibitors of phospholipase enzymes
HUP0100156A3 (en) 1998-02-25 2002-12-28 Genetics Inst Inc Cambridge Indole derivatives as inhibitors of phospholipase a2 and use of them for producing pharmaceutical compositions
US6500853B1 (en) 1998-02-28 2002-12-31 Genetics Institute, Llc Inhibitors of phospholipase enzymes
US6589954B1 (en) 1998-05-22 2003-07-08 Scios, Inc. Compounds and methods to treat cardiac failure and other disorders
US6867209B1 (en) 1998-05-22 2005-03-15 Scios, Inc. Indole-type derivatives as inhibitors of p38 kinase
AUPP433398A0 (en) 1998-06-25 1998-07-16 Australian National University, The Compounds and processes
JP2000063354A (ja) 1998-08-21 2000-02-29 Sumitomo Pharmaceut Co Ltd ピロール誘導体
JP2001151771A (ja) 1999-09-10 2001-06-05 Kyowa Hakko Kogyo Co Ltd 含窒素芳香族複素環誘導体
WO2001044182A2 (en) 1999-12-16 2001-06-21 Eli Lilly And Company New synthesis of spla2 inhibitors
BR0110420A (pt) 2000-04-28 2003-07-01 Acadia Pharm Inc Agonistas muscarìnicos
ES2172415B2 (es) 2000-07-28 2003-11-16 Univ Madrid Complutense Tratamiento del glaucoma y la hipertension ocular por medio de un analogo de la melatonina.
EP1377549A1 (en) 2001-03-12 2004-01-07 Millennium Pharmaceuticals, Inc. Functionalized heterocycles as modulators of chemokine receptor function and methods of use therefor
CA2466665A1 (en) 2001-11-09 2003-05-22 Scios Inc. Method to treat cystic fibrosis
US7528165B2 (en) 2001-12-13 2009-05-05 National Health Research Institutes Indole compounds
US7632955B2 (en) 2001-12-13 2009-12-15 National Health Research Institutes Indole compounds
HRP20050181A2 (en) 2002-08-29 2006-03-31 Merck & Co. Inc. Indoles having anti-diabetic activity
MXPA06000539A (es) 2003-07-15 2006-03-30 Dainippon Sumitomo Pharma Co Derivado novedoso de heteroarilo.
WO2005024416A1 (en) 2003-09-05 2005-03-17 Binghe Wang Water soluble boronic acid fluorescent reporter compounds and methods of use thereof
TW200522944A (en) 2003-12-23 2005-07-16 Lilly Co Eli CB1 modulator compounds
US7417063B2 (en) 2004-04-13 2008-08-26 Bristol-Myers Squibb Company Bicyclic heterocycles useful as serine protease inhibitors
WO2005121175A2 (en) 2004-06-08 2005-12-22 Novartis Vaccines And Diagnostics Inc. Env polypeptide complexes and methods of use
ES2246721B1 (es) 2004-08-10 2007-03-16 Laboratorios Del Dr. Esteve, S.A. Compuestos indolicos sustituidos, su preparacion y su uso como medicamentos.
US20090264384A1 (en) 2004-11-01 2009-10-22 Nuada, Inc. Indole, benzimidazole, and benzolactam boronic acid compounds, analogs thereof and methods of use thereof
EP1833787A2 (en) 2004-11-30 2007-09-19 Plexxikon, Inc. Indole derivatives for use as ppar active compounds
GB0500492D0 (en) 2005-01-11 2005-02-16 Cyclacel Ltd Compound
EP1837329A4 (en) 2005-01-14 2009-08-05 Dainippon Sumitomo Pharma Co NEW HETEROARYL DERIVATIVE
CA2597896A1 (en) 2005-02-16 2006-08-24 Solvay Pharmaceuticals B.V. 1h-imidazole derivatives as cannabinoid cb2 receptor modulators
CA2609980C (en) 2005-05-27 2015-10-13 Queen's University At Kingston Treatment of protein folding disorders
AU2006292429A1 (en) 2005-09-16 2007-03-29 Serenex, Inc. Carbazole derivatives
EP1783114A1 (en) 2005-11-03 2007-05-09 Novartis AG N-(hetero)aryl indole derivatives as pesticides
AU2007214434B2 (en) 2006-02-15 2012-06-14 Allergan, Inc. Indole-3-carboxylic acid amide, ester, thioamide and thiol ester compounds bearing aryl or heteroaryl groups having sphingosine-1-phosphate (S1P) receptor antagonist biological activity
US8097644B2 (en) 2006-03-28 2012-01-17 Allergan, Inc. Indole compounds having sphingosine-1-phosphate (S1P) receptor antagonist
US8877791B2 (en) 2006-08-04 2014-11-04 Beth Israel Deaconess Medical Center, Inc. Inhibitors of pyruvate kinase and methods of treating disease
SG176477A1 (en) 2006-08-07 2011-12-29 Ironwood Pharmaceuticals Inc Indole compounds
US20080119457A1 (en) 2006-08-24 2008-05-22 Serenex, Inc. Benzene, Pyridine, and Pyridazine Derivatives
EP1902733A1 (en) 2006-09-19 2008-03-26 Laboratorios Del Dr. Esteve, S.A. Combination of a NMDA-receptor ligand and a compound with 5-HT6 receptor affinity
US7943659B2 (en) 2006-10-31 2011-05-17 Takeda Pharmaceutical Company Limited MAPK/ERK kinase inhibitors
US8524917B2 (en) 2007-01-11 2013-09-03 Allergan, Inc. 6-substituted indole-3-carboxylic acid amide compounds having sphingosine-1-phosphate (S1P) receptor antagonist biological activity
JP2010518025A (ja) 2007-02-05 2010-05-27 アミラ ファーマシューティカルス，インコーポレーテッド ５−リポキシゲナーゼ活性化タンパク質（ｆｌａｐ）インヒビターとしての逆インドール
MX2009008439A (es) 2007-02-12 2009-08-13 Intermune Inc Nuevos inhibidores de la replicacion del virus de hepatitis c.
BRPI0808775A2 (pt) 2007-03-08 2017-05-30 Irm Llc compostos e composições como moduladores de atividade de gpr119
CN101016294A (zh) 2007-03-13 2007-08-15 中国人民武装警察部队医学院 具有多种生物活性的取代吲哚－3－基草酰胺衍生物
BRPI0809542A8 (pt) 2007-03-29 2015-09-15 Asubio Pharma Co Ltd Compostos derivados de indol tendo atividade de inibição de cpla2, composição farmacêutica, e métodos de produção dos referidos compostos
US8091582B2 (en) 2007-04-13 2012-01-10 Cla-Val Co. System and method for hydraulically managing fluid pressure downstream from a main valve between set points
EP2150112A1 (en) 2007-04-26 2010-02-10 Merck & Co., Inc. 2-substituted indole derivatives as calcium channel blockers
US8563594B2 (en) 2007-05-08 2013-10-22 Allergan, Inc. S1P3 receptor inhibitors for treating pain
WO2008157740A2 (en) 2007-06-20 2008-12-24 Ironwood Pharmaceuticals, Inc. Faah inhibitors
EP2018861A1 (en) 2007-07-26 2009-01-28 Laboratorios del Dr. Esteve S.A. 5HT6-Ligands such as sulfonamide derivatives in drug-induced weight-gain
ATE495737T1 (de) 2007-08-01 2011-02-15 Esteve Labor Dr Kombination von mindestens zwei 5-ht6-liganden
CN101917999A (zh) 2007-11-07 2010-12-15 弗尔德里克斯制药股份有限公司 蛋白质运输的调节
EP2227233B1 (en) 2007-11-30 2013-02-13 Newlink Genetics Ido inhibitors
HUE025545T2 (en) 2007-12-04 2016-03-29 Hoffmann La Roche Isoxazole-pyridine derivatives
GB0723815D0 (en) 2007-12-05 2008-01-16 Glaxo Group Ltd Compounds
JP2009179589A (ja) 2008-01-30 2009-08-13 Pharma Ip 抗ウイルス剤
WO2009097141A1 (en) 2008-01-31 2009-08-06 Joslin Diabetes Center Methods for treatment of kallikrein-related disorders
PL2247592T3 (pl) 2008-02-25 2012-01-31 Hoffmann La Roche Pirolopirazynowe inhibitory kinazy
WO2009108551A2 (en) 2008-02-25 2009-09-03 H. Lundbeck A/S Heteroaryl amide analogues
CA2718705A1 (en) 2008-03-17 2009-09-24 Allergan, Inc. S1p3 receptor inhibitors for treating inflammation
RU2010142937A (ru) 2008-03-20 2012-04-27 Форест Лабораториес Холдингс Лимитед (Bm) НОВЫЕ ПРОИЗВОДНЫЕ ПИПЕРИДИНА В КАЧЕСТВЕ ИНГИБИТОРОВ СТЕАРОИЛ-КоА ДЕСАТУРАЗЫ
US20090247766A1 (en) 2008-03-27 2009-10-01 University Of Southern California Substituted Nitrogen Heterocycles and Synthesis and Uses Thereof
KR20160067981A (ko) 2008-04-16 2016-06-14 카로 바이오 아베 신규한 에스트로겐 수용체 리간드
AU2009239778B2 (en) 2008-04-24 2014-03-13 F2G Ltd Pyrrole antifungal agents
GB0808282D0 (en) 2008-05-07 2008-06-11 Medical Res Council Compounds for use in stabilizing p53 mutants
US20110086834A1 (en) 2008-06-26 2011-04-14 Amgen Inc. Alkynyl alcohols as kinase inhibitors
JP2011525928A (ja) 2008-06-26 2011-09-29 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー Ａｋｔ活性の阻害剤
EP2141163A1 (de) 2008-07-02 2010-01-06 Bayer Schering Pharma AG Substituierte Thiazolidinone, deren Herstellung und Verwendung als Arzneimittel
US20110237538A1 (en) 2008-08-06 2011-09-29 Summit Corporation Plc Treatment of lysosomal storage disorders and other proteostatic diseases
CA2733588A1 (en) 2008-08-12 2010-02-18 Merck Sharp & Dohme Corp. N-heterocyclic m1 receptor positive allosteric modulators
US8143269B2 (en) 2008-10-03 2012-03-27 Calcimedica, Inc. Inhibitors of store operated calcium release
US8071605B2 (en) 2008-12-12 2011-12-06 Astrazeneca Ab Piperidine compounds for use in the treatment of bacterial infections
JP2012520886A (ja) 2009-03-18 2012-09-10 シェーリング コーポレイション ジアシルグリセロールアシルトランスフェラーゼの阻害剤としての二環式化合物
US20120071448A1 (en) 2009-05-05 2012-03-22 Allergan, Inc. S1P3 Receptor Inhibitors for Treating Conditions of the Eye
US8912220B2 (en) 2009-08-10 2014-12-16 Galenea Pharmaceuticals Compounds and methods of use thereof
CN102216300B (zh) 2009-09-30 2014-10-22 贝达药业股份有限公司 作为蛋白激酶抑制剂的化合物和组合物
HRP20141150T1 (hr) 2009-10-19 2015-01-30 Synta Pharmaceuticals Corp. Kombinacijska terapija raka sa hsp90 inhibitornim spojevima
SG182662A1 (en) 2010-01-28 2012-08-30 Harvard College Compositions and methods for enhancing proteasome activity
US8785490B2 (en) 2010-04-09 2014-07-22 University Of Louisville Research Foundation, Inc. Compounds for treating disease, for administering, and for pharmaceutical compositions
US20130156755A1 (en) 2010-04-19 2013-06-20 Synta Pharmaceuticals Corp. Cancer therapy using a combination of a hsp90 inhibitory compounds and a vegf inhibitor
EP2560640A1 (en) 2010-04-19 2013-02-27 Synta Pharmaceuticals Corp. Cancer therapy using a combination of a hsp90 inhibitory compounds and a egfr inhibitor
WO2011149824A1 (en) 2010-05-24 2011-12-01 Synta Pharmaceuticals Corp. Cancer therapy using a combination of a hsp90 inhibitory compound and a topoisomerase ii inhibitor
AU2011302344B2 (en) 2010-09-13 2015-01-15 Synta Pharmaceuticals Corp. HSP90 inhibitors for treating non-small cell lung cancers in wild-type EGFR and/or KRAS patients
WO2012078757A2 (en) 2010-12-08 2012-06-14 Synta Pharmaceuticals Corp. Combination breast cancer therapy with hsp90 inhibitory compounds
WO2012096919A1 (en) 2011-01-11 2012-07-19 Synta Pharmaceuticals Corp. Combination therapy of hsp90 inhibitory compounds with proteasome inhibitors
WO2012106343A2 (en) 2011-02-01 2012-08-09 The Board Of Trustees Of The University Of Illinois Hdac inhibitors and therapeutic methods using the same
WO2012116061A1 (en) 2011-02-23 2012-08-30 Synta Pharmaceuticals Corp. Combination therapy of hsp90 inhibitory compounds with radiotherapy
EP2678014A2 (en) 2011-02-24 2014-01-01 Synta Pharmaceuticals Corp. Prostate cancer therapy with hsp90 inhibitory compounds
US20140045908A1 (en) 2011-02-25 2014-02-13 Synta Pharmaceuticals Corp. Hsp90 inhibitory compounds in treating jak/stat signaling-mediated cancers
WO2012154967A1 (en) 2011-05-12 2012-11-15 Proteostasis Therapeutics, Inc. Proteostasis regulators
EP2714039A1 (en) 2011-05-23 2014-04-09 Synta Pharmaceuticals Corp. Combination therapy of hsp90 inhibitory compounds with mek inhibitors
WO2012162372A1 (en) 2011-05-24 2012-11-29 Synta Pharmaceuticals Corp. Combination therapy of hsp90 inhibitory compounds with mtor/p13k inhibitors
EP2714033A1 (en) 2011-05-26 2014-04-09 Synta Pharmaceuticals Corp. Combination therapy of hsp90 inhibitory compounds with chk inhibitors
WO2012166415A1 (en) 2011-05-27 2012-12-06 Amira Pharmaceuticals, Inc. Heterocyclic autotaxin inhibitors and uses thereof
EP2729144A2 (en) 2011-07-07 2014-05-14 Synta Pharmaceuticals Corp. Treating cancer with hsp90 inhibitory compounds
EP2548865B1 (en) 2011-07-22 2014-03-05 Université Joseph Fourier Novel bis-indolic derivatives, their uses in particular as antibacterials
JP2014532712A (ja) 2011-11-02 2014-12-08 シンタ ファーマシューティカルズ コーポレーション トポイソメラーゼｉ阻害剤とｈｓｐ９０阻害剤の組合せを使用する癌療法
JP2014534228A (ja) 2011-11-02 2014-12-18 シンタ ファーマシューティカルズ コーポレーション 白金含有剤とｈｓｐ９０阻害剤の組合せ療法
AU2012339679A1 (en) 2011-11-14 2014-06-12 Synta Pharmaceuticals Corp. Combination therapy of Hsp90 inhibitors with BRAF inhibitors
US9849135B2 (en) 2013-01-25 2017-12-26 President And Fellows Of Harvard College USP14 inhibitors for treating or preventing viral infections

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007502851A (ja) * 2003-05-22 2007-02-15 ファルマシア・イタリア・エス・ピー・エー ピラゾロ−キナゾリン誘導体、その製造方法、およびキナーゼ阻害剤としてのその使用
JP2007502304A (ja) * 2003-08-14 2007-02-08 セファロン、インク． プロテアソーム阻害剤及びそれらを使用する方法
WO2005025515A2 (en) * 2003-09-12 2005-03-24 California Institute Of Technology Proteasome pathway inhibitors and related methods
WO2008147536A1 (en) * 2007-05-24 2008-12-04 President And Fellows For Harvard College Methods and compositions for enhancing proteasome activity
WO2009086303A2 (en) * 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
WO2009118292A1 (en) * 2008-03-24 2009-10-01 Novartis Ag Arylsulfonamide-based matrix metalloprotease inhibitors
JP2013532662A (ja) * 2010-07-23 2013-08-19 プレジデント アンド フェロウズ オブ ハーバード カレッジ プロテアソーム活性を向上させる三環系化合物

Non-Patent Citations (9)

* Cited by examiner, † Cited by third party
Title
JPN6014047718; Ｇａｄａｇｉｎａｍａｔｈ，　Ｇｕｒｕ　Ｓ．；　Ｋａｍａｔ，　Ａｎａｎｄ　Ｇ．；　Ｐｕｊａｒ，　Ｂａｓａｙｙａ　Ｇ．: 'Ｓｙｎｔｈｅｓｉｓ　ａｎｄ　ａｎｔｉｍｉｃｒｏｂｉａｌ　ａｃｔｉｖｉｔｙ　ｏｆ　４-ｉｓｏｇｒａｍｉｎｅｓ，　４-ａｒｙｌｔｈｉｏｍｅｔｈｙｌ　ａｎｄ　３-ａｍｉｎｏａｃｅｔｙｌ　ｄｅｒｉｖａｔｉｖｅ' Ｒｅｖｕｅ　Ｒｏｕｍａｉｎｅ　ｄｅ　Ｃｈｉｍｉｅ ４０（３）, 1995, ２６５-７３ *
JPN6014047720; Ｇａｄａｇｉｎａｍａｔｈ， Ｇ． Ｓ．； Ｋａｖａｌｉ， Ｒ． Ｒ．； Ｓｈｙａｄｌｉｇｅｒｉ， Ａ． Ｓ．； Ｄｏｄｄａｍａｎｉ， Ｈ． Ｐ．: 'Ｓｙｎｔｈｅｓｉｓ ａｎｄ ａｎｔｉｍｉｃｒｏｂｉａｌ ａｃｔｉｖｉｔｙ ｏｆ ｎｏｖｅｌ ３-ｔｈｉａｚｏｌｙｌ／ｉｍｉｄａｚｏ［２，１-ｂ］-１，３，４-ｔｈｉａｄｉａｚｏｌｙｌ／ａｎｉｌｉｎｏ' Ｉｎｄｉａｎ Ｊｏｕｒｎａｌ ｏｆ Ｈｅｔｅｒｏｃｙｃｌｉｃ Ｃｈｅｍｉｓｔｒｙ ９（１）, 1999, ３３-３８ *
JPN6014047722; Ｋａｎｇ， Ｊｅｏｎｇｈｗａ； Ｌｅｅ， Ｄｏｎｇ-Ｋｅｕｎ； Ｌｅｅ， Ｃｈｕｌ-Ｈｏｏｎ: 'Ｃｅｌｌ ｃｙｃｌｅ ａｒｒｅｓｔ ａｎｄ ｃｙｔｏｃｈｒｏｍｅ ｃ-ｍｅｄｉａｔｅｄ ａｐｏｐｔｏｔｉｃ ｉｎｄｕｃｔｉｏｎ ｉｎ Ａ５４９ ｈｕｍａｎ ｌｕｎｇ ｃａｎｃｅｒ ｃｅｌｌｓ ｂｙ' Ｊｏｕｒｎａｌ ｏｆ Ｍｉｃｒｏｂｉｏｌｏｇｙ ａｎｄ Ｂｉｏｔｅｃｈｎｏｌｏｇｙ ２０（２）, 2010, ４２８-４３２ *
JPN6014047724; ＲＥＧＩＳＴＲＹ（ＳＴＮ）　［ｏｎｌｉｎｅ］ *
JPN6014047725; ＲＥＧＩＳＴＲＹ（ＳＴＮ）　［ｏｎｌｉｎｅ］ *
JPN6014047727; ＲＥＧＩＳＴＲＹ（ＳＴＮ）　［ｏｎｌｉｎｅ］ *
JPN6014047729; ＲＥＧＩＳＴＲＹ（ＳＴＮ）　［ｏｎｌｉｎｅ］ *
JPN6014047731; ＲＥＧＩＳＴＲＹ（ＳＴＮ）　［ｏｎｌｉｎｅ］ *
JPN6014047733; Ｉｗａｋｉ， Ｔａｋａｋｏ； Ｆｕｊｉｔａ， Ｙａｓｕａｋｉ； Ｙａｍａｄａ， Ｆｕｍｉｏ； Ｓｏｍｅｉ， Ｍａｓａｎｏｒｉ: 'Ｗａｔｅｒ-ｓｏｌｕｂｌｅ ｍｅｌａｔｏｎｉｎｓ： Ｓｙｎｔｈｅｓｅｓ ｏｆ ｍｅｌａｔｏｎｉｎｓ ｃａｒｒｙｉｎｇ ａ ｇｌｙｃｏｓｙｌ ｇｒｏｕｐ ａｔ ｔｈｅ １-ｐｏｓｉｔｉｏｎ．' Ｈｅｔｅｒｏｃｙｃｌｅｓ ６０（６）, 2003, １４１１-１４１８ *

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2019501142A (ja) * 2015-11-30 2019-01-17 ミッション セラピューティクス リミティド Ｕｓｐ３０の阻害剤としての１−シアノピロリジン誘導体
JP2021530465A (ja) * 2018-06-27 2021-11-11 プロテオステイシス セラピューティクス， インコーポレイテッド プロテアソーム活性増強化合物
JP7551087B2 (ja) 2018-06-27 2024-09-17 キネタ， インコーポレイテッド プロテアソーム活性増強化合物
JP2022012379A (ja) * 2020-07-01 2022-01-17 国立大学法人富山大学 ユビキチン－プロテアソーム系の活性化剤、およびその利用

Also Published As

Publication number Publication date
EP2528911B1 (en) 2017-10-25
SG182662A1 (en) 2012-08-30
CN102844313B (zh) 2016-10-05
US20160214989A1 (en) 2016-07-28
AU2011210765A1 (en) 2012-09-13
JP2016147893A (ja) 2016-08-18
EP2528911A4 (en) 2014-08-06
CA2787785A1 (en) 2011-08-04
US20130045992A1 (en) 2013-02-21
WO2011094545A3 (en) 2012-01-05
US10351568B2 (en) 2019-07-16
WO2011094545A2 (en) 2011-08-04
JP6371786B2 (ja) 2018-08-08
MX336731B (es) 2016-01-28
MX2012008626A (es) 2012-08-15
RU2012136451A (ru) 2014-03-10
EP2528911A2 (en) 2012-12-05
BR112012018631A8 (pt) 2017-12-19
BR112012018631A2 (pt) 2016-04-05
KR20120117905A (ko) 2012-10-24
CN102844313A (zh) 2012-12-26
CA2787785C (en) 2018-03-06

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
US10519118B2 (en) KDM1A inhibitors for the treatment of disease
AU2016336437B2 (en) Compounds, compositions, and methods for modulating CFTR
AU2017248253B2 (en) Silicone atoms containing ivacaftor analogues
CA3041676A1 (en) Pyridazine derivatives, compositions and methods for modulating cftr
CA2971855A1 (en) Derivatives of 5-(hetero)arylpyrazol-3-carboxylic amide or 1-(hetero)aryltriazol-4-carboxylic amide useful for the treatment of inter alia cystic fibrosis
WO2019071078A1 (en) COMPOUNDS, COMPOSITIONS AND METHODS FOR INCREASING CFTR ACTIVITY
WO2016105468A1 (en) Derivatives of 3-heteroarylisoxazol-5-carboxylic amide useful for the treatment of inter alia cystic fibrosis
KR20210049778A (ko) 질병 상태 및 병태를 치료하는데 사용하기 위한 거울상 이성질체적으로 정제된 gper 작용제
AU2017204046A1 (en) Compositions and methods for enhancing proteasome activity
WO2014181101A1 (en) 2-acyl-4-oxy-1,2-dihydropyrrol-5-one compounds for improving memory and cognitive function
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: 20131108

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20140127

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20141030

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20141111

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20150206

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20150508

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20151124