KR20120117905A - 프로테아좀 활성을 향상시키는 조성물 및 방법 - Google Patents

프로테아좀 활성을 향상시키는 조성물 및 방법 Download PDF

Info

Publication number
KR20120117905A
KR20120117905A KR1020127022300A KR20127022300A KR20120117905A KR 20120117905 A KR20120117905 A KR 20120117905A KR 1020127022300 A KR1020127022300 A KR 1020127022300A KR 20127022300 A KR20127022300 A KR 20127022300A KR 20120117905 A KR20120117905 A KR 20120117905A
Authority
KR
South Korea
Prior art keywords
compound
alkyl
proteasome
usp14
hydrogen
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.)
Ceased
Application number
KR1020127022300A
Other languages
English (en)
Korean (ko)
Inventor
다니엘 핀리
랜달 더블유. 킹
병-훈 이
민 재 이
티모시 씨. 가흐만
Original Assignee
프레지던트 앤드 펠로우즈 오브 하바드 칼리지
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 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 filed Critical 프레지던트 앤드 펠로우즈 오브 하바드 칼리지
Publication of KR20120117905A publication Critical patent/KR20120117905A/ko
Ceased legal-status Critical Current

Links

Images

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
    • 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
    • C07D401/06—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
    • 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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Molecular Biology (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Biochemistry (AREA)
  • Food Science & Technology (AREA)
  • Analytical Chemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Biotechnology (AREA)
  • Cell Biology (AREA)
  • Microbiology (AREA)
  • Pathology (AREA)
  • Physics & Mathematics (AREA)
  • Psychology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
KR1020127022300A 2010-01-28 2011-01-28 프로테아좀 활성을 향상시키는 조성물 및 방법 Ceased KR20120117905A (ko)

Applications Claiming Priority (4)

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

Publications (1)

Publication Number Publication Date
KR20120117905A true KR20120117905A (ko) 2012-10-24

Family

ID=44320152

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020127022300A Ceased KR20120117905A (ko) 2010-01-28 2011-01-28 프로테아좀 활성을 향상시키는 조성물 및 방법

Country Status (12)

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

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022250363A1 (ko) * 2021-05-24 2022-12-01 재단법인대구경북과학기술원 아이유원 계열의 유비퀴틴 특이적 프로테아제 14 억제제를 유효성분으로 포함하는, 프로탁의 항암 효과 증진용 약학적 조성물

Families Citing this family (40)

* 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
DK2707101T3 (da) * 2011-05-12 2019-05-13 Proteostasis Therapeutics Inc Proteostaseregulatorer
ES2632786T3 (es) 2011-09-16 2017-09-15 Vivolux Ab Examen de inhibidor de desubiquitinación de proteasoma
CA2861464C (en) * 2012-01-25 2018-03-06 Proteostasis Therapeutics, Inc. Proteasome activity modulating tricyclic compounds
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
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
EP3102576B8 (en) 2014-02-03 2019-06-19 Vitae Pharmaceuticals, LLC Dihydropyrrolopyridine inhibitors of ror-gamma
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
PT3207043T (pt) 2014-10-14 2019-03-25 Vitae Pharmaceuticals Llc Inibidores de di-hidropirrolopiridina de 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
US11008340B2 (en) 2015-11-20 2021-05-18 Vitae Pharmaceuticals, Llc Modulators of ROR-gamma
GB201521109D0 (en) * 2015-11-30 2016-01-13 Mission Therapeutics Ltd Novel compounds
CN108602775B (zh) 2016-01-14 2022-04-29 贝思以色列女会吏医学中心公司 肥大细胞调节剂及其用途
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
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
EP4491236A3 (en) * 2016-05-10 2025-04-02 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
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
US9481674B1 (en) 2016-06-10 2016-11-01 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
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
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
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
EP4717317A2 (en) 2017-06-20 2026-04-01 C4 Therapeutics, Inc. N/o-linked degrons and degronimers for protein degradation
WO2019018975A1 (en) 2017-07-24 2019-01-31 Vitae Pharmaceuticals, Inc. INHIBITORS OF ROR GAMMA
JP2020528904A (ja) 2017-07-24 2020-10-01 ヴァイティー ファーマシューティカルズ，エルエルシー ＲＯＲγの阻害剤
EP3710002A4 (en) 2017-11-16 2021-07-07 C4 Therapeutics, Inc. DEGRADER AND DEGRONE FOR TARGETED PROTEIN DEGRADATION
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
CN119751456A (zh) 2018-04-16 2025-04-04 C4医药公司 螺环化合物
CN112585130A (zh) * 2018-06-27 2021-03-30 蛋白质平衡治疗股份有限公司 蛋白酶体活性增强化合物
BR112020026580A2 (pt) * 2018-06-27 2021-03-23 Proteostasis Therapeutics, Inc. (Fem) Compostos, composição farmacêutica e métodos para tratar um paciente
CN120698983A (zh) 2018-12-20 2025-09-26 C4医药公司 靶向蛋白降解
JP2023511280A (ja) * 2020-01-14 2023-03-17 ザ・トラスティーズ・オブ・コロンビア・ユニバーシティ・イン・ザ・シティ・オブ・ニューヨーク 内因性の脱ユビキチン化酵素をリダイレクトすることによる標的化されたタンパク質の安定化のための組成物及び方法
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
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

Family Cites Families (122)

* 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
HU895334D0 (en) 1986-07-30 1990-01-28 Sandoz Ag Process for the preparation of nasal pharmaceutical compositions
TW226019B (https=) 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¶
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
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
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¶
ES2185693T3 (es) 1994-01-19 2003-05-01 Sankyo Co Derivado de pirrolopiridacina.
AU701025B2 (en) 1995-02-01 1999-01-21 University College Cardiff Consultants Limited Heterocyclic compounds
WO1997036881A1 (en) 1996-04-03 1997-10-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5859035A (en) 1996-04-03 1999-01-12 Merck & Co., Inc. Arylheteroaryl 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
ATE255090T1 (de) 1996-08-01 2003-12-15 Merckle Gmbh Acylpyrroldicarbonsäuren und acylindoldicarbonsäuren sowie ihre derivate als hemmstoffe der cytosolischen phospholipase a2
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
EP1062216A1 (en) 1998-02-25 2000-12-27 Genetics Institute, Inc. Inhibitors of phospholipase a2
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
AU2252101A (en) 1999-12-16 2001-06-25 Eli Lilly And Company New synthesis of SPLA2 inhibitors
CN1249051C (zh) 2000-04-28 2006-04-05 阿卡蒂亚药品公司 毒蕈碱性激动剂
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.
US6951848B2 (en) 2001-03-12 2005-10-04 Millennium Pharmaceuticals, Inc., Functionalized heterocycles as modulators of chemokine receptor function and methods of use therefor
TR200401028T2 (tr) 2001-11-09 2004-11-22 Scios Inc. Kistik fibrozun tedavisine yönelik metot
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
WO2004020408A1 (en) 2002-08-29 2004-03-11 Merck & Co., Inc. Indoles having anti-diabetic activity
PT1636236E (pt) * 2003-05-22 2013-12-16 Nerviano Medical Sciences Srl Derivados de pirazol-quinazolina, processo para sua preparação e sua utilização como inibidores de cinase
ATE556051T1 (de) 2003-07-15 2012-05-15 Dainippon Sumitomo Pharma Co Neues heteroarylderivat
US7576206B2 (en) * 2003-08-14 2009-08-18 Cephalon, Inc. Proteasome inhibitors and methods of using the same
US7767817B2 (en) 2003-09-05 2010-08-03 Binghe Wang Water soluble boronic acid fluorescent reporter compounds and methods of use thereof
US20050203063A1 (en) * 2003-09-12 2005-09-15 Raymond Deshaies Proteasome pathway inhibitors and related methods
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
WO2006060535A2 (en) 2004-11-30 2006-06-08 Plexxikon, Inc. Indole derivatives for use as ppar active compounds
GB0500492D0 (en) 2005-01-11 2005-02-16 Cyclacel Ltd Compound
JPWO2006075638A1 (ja) 2005-01-14 2008-06-12 大日本住友製薬株式会社 新規ヘテロアリール誘導体
EP1874734A1 (en) 2005-02-16 2008-01-09 Solvay Pharmaceuticals B.V. 1h-imidiazole derivatives as cannabinoid cb2 receptor modulators
EP1893576A4 (en) 2005-05-27 2010-03-17 Univ Kingston TREATMENT OF PROTEIN DISORDERING
EP1924557A2 (en) 2005-09-16 2008-05-28 Serenex, Inc. Carbazole derivatives
EP1783114A1 (en) 2005-11-03 2007-05-09 Novartis AG N-(hetero)aryl indole derivatives as pesticides
BRPI0707873A2 (pt) 2006-02-15 2011-05-10 Allergan Inc compostos amida, Éster, tioamida e tiol Éster do Ácido indol-3-carboxÍlico carregando grupos arila ou heteroarila tendo atividade biolàgica antagonista de recptor de esfingosina-1-fosfato (s1p)
WO2007112322A2 (en) 2006-03-28 2007-10-04 Allergan, Inc. Indole compounds having sphingosine-1-phosphate (s1p) receptor agonist and/or antagonist biological activity
ES2614931T3 (es) 2006-08-04 2017-06-02 Beth Israel Deaconess Medical Center Inhibidores de la piruvato cinasa y métodos de tratamiento de enfermedad
US8884020B2 (en) 2006-08-07 2014-11-11 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
EP2089359A2 (en) 2006-10-31 2009-08-19 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
CN101687789A (zh) 2007-02-12 2010-03-31 因特蒙公司 C型肝炎病毒复制的新颖抑制剂
EP2134704B1 (en) 2007-03-08 2010-09-22 Irm Llc Compounds and compositions as modulators of gpr119 activity
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
CN101679248A (zh) 2007-03-29 2010-03-24 阿斯比奥制药株式会社 具有cPLA2抑制活性的吲哚衍生物及其用途以及制备方法
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
WO2008133867A1 (en) 2007-04-26 2008-11-06 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
WO2008147536A1 (en) * 2007-05-24 2008-12-04 President And Fellows For Harvard College Methods and compositions for enhancing proteasome activity
TW200914437A (en) 2007-06-20 2009-04-01 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
EP2020230B1 (en) 2007-08-01 2011-01-19 Laboratorios del Dr. Esteve S.A. Combination of at least two 5-HT6-Ligands
US20100331297A1 (en) 2007-11-07 2010-12-30 Foldrx Pharmaceuticals, Inc. Modulation of protein trafficking
JP5583592B2 (ja) 2007-11-30 2014-09-03 ニューリンク ジェネティクス コーポレイション Ｉｄｏ阻害剤
KR101237576B1 (ko) 2007-12-04 2013-03-04 에프. 호프만-라 로슈 아게 아이속사졸로-피리딘 유도체
GB0723815D0 (en) 2007-12-05 2008-01-16 Glaxo Group Ltd Compounds
CA2709784A1 (en) * 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
JP2009179589A (ja) 2008-01-30 2009-08-13 Pharma Ip 抗ウイルス剤
EP2259679A4 (en) 2008-01-31 2011-09-14 Joslin Diabetes Ct METHODS OF TREATING KALLIKREIN RELATED DISORDERS
WO2009108551A2 (en) 2008-02-25 2009-09-03 H. Lundbeck A/S Heteroaryl amide analogues
JP5368485B2 (ja) 2008-02-25 2013-12-18 エフ．ホフマン−ラ ロシュ アーゲー ピロロピラジンキナーゼインヒビター
WO2009117335A2 (en) 2008-03-17 2009-09-24 Allergan, Inc. S1p3 receptor inhibitors for treating inflammation
BRPI0909183A2 (pt) 2008-03-20 2015-08-25 Forest Lab Holdings Ltd Composto, composição farmacêutica e método de tratamento de condição que responde a inibidor de estearoil-coa dessaturase
WO2009118292A1 (en) * 2008-03-24 2009-10-01 Novartis Ag Arylsulfonamide-based matrix metalloprotease inhibitors
US20110098483A1 (en) 2008-03-27 2011-04-28 University Of Southern California Substituted Nitrogen Heterocycles and Synthesis and Uses Thereof
AU2009237657B2 (en) 2008-04-16 2013-04-04 Oasmia Pharmaceutical Ab Novel estrogen receptor ligands
DK2626361T3 (en) 2008-04-24 2015-01-19 F2G Ltd Pyrrol-Antimycotics
GB0808282D0 (en) 2008-05-07 2008-06-11 Medical Res Council Compounds for use in stabilizing p53 mutants
EP2306825A4 (en) 2008-06-26 2011-12-28 Glaxosmithkline Llc HAMMER OF ACT ACTIVITY
AU2009263037B2 (en) 2008-06-26 2011-10-06 Amgen Inc. Alkynyl alcohols as kinase inhibitors
EP2141163A1 (de) 2008-07-02 2010-01-06 Bayer Schering Pharma AG Substituierte Thiazolidinone, deren Herstellung und Verwendung als Arzneimittel
EP2323652A2 (en) 2008-08-06 2011-05-25 Summit Corporation Plc Treatment of lysosomal storage disorders and other proteostatic diseases
US8426598B2 (en) 2008-08-12 2013-04-23 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
TW201026695A (en) 2008-12-12 2010-07-16 Astrazeneca Ab Piperidine compounds and uses thereof-596
US20120022057A1 (en) 2009-03-18 2012-01-26 Schering Corporation Bicyclic compounds as inhibitors of diacyglycerol acyltransferase
US20120071448A1 (en) 2009-05-05 2012-03-22 Allergan, Inc. S1P3 Receptor Inhibitors for Treating Conditions of the Eye
EP2464227A4 (en) 2009-08-10 2013-02-20 Galenea Corp COMPOUNDS AND METHODS OF USE
WO2011038579A1 (en) 2009-09-30 2011-04-07 Zhejiang Beta Pharma Inc. Compounds and compositions as protein kinase inhibitors
BR112012009215A2 (pt) 2009-10-19 2019-09-24 Synta Pharmaceuticals Corp "terapia combinada contra o cancer com compostos inibidores de hsp90"
MX336731B (es) 2010-01-28 2016-01-28 Harvard College Composiciones y metodos para potenciar la actividad de proteasoma.
WO2011127333A2 (en) 2010-04-09 2011-10-13 University Of Louisville Research Foundation, Inc. Compounds for treating disease, for administering, and for pharmaceutical compositions
EP2560641A2 (en) 2010-04-19 2013-02-27 Synta Pharmaceuticals Corp. Cancer therapy using a combination of a hsp90 inhibitory compounds and a vegf inhibitor
US9205086B2 (en) 2010-04-19 2015-12-08 Synta Pharmaceuticals Corp. Cancer therapy using a combination of a Hsp90 inhibitory compounds and a EGFR inhibitor
US20120064175A1 (en) 2010-05-20 2012-03-15 Synta Pharmaceuticals Corp. HSP90 Inhibitors for Treating Non-Small Cell Lung Cancer in Wild-Type EGFR and/or KRAS Patients
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
AU2011281015B2 (en) * 2010-07-23 2015-09-24 President And Fellows Of Harvard College Tricyclic proteasome activity enhancing compounds
US20140005145A1 (en) 2010-12-08 2014-01-02 Synta Pharmaceuticals Corp. Combination breast cancer therapy with hsp90 inhibitory compounds
EP2663305A1 (en) 2011-01-11 2013-11-20 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
US20140051665A1 (en) 2011-02-24 2014-02-20 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
DK2707101T3 (da) 2011-05-12 2019-05-13 Proteostasis Therapeutics Inc Proteostaseregulatorer
WO2012162293A1 (en) 2011-05-23 2012-11-29 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
US9260416B2 (en) 2011-05-27 2016-02-16 Amira Pharmaceuticals, Inc. Heterocyclic autotaxin inhibitors and uses thereof
JP2014520808A (ja) 2011-07-07 2014-08-25 シンタ ファーマシューティカルズ コーポレーション Ｈｓｐ９０阻害化合物を用いた癌の治療
EP2548865B1 (en) 2011-07-22 2014-03-05 Université Joseph Fourier Novel bis-indolic derivatives, their uses in particular as antibacterials
EP2773345A1 (en) 2011-11-02 2014-09-10 Synta Pharmaceuticals Corp. Cancer therapy using a combination of hsp90 inhibitors with topoisomerase i inhibitors
AU2012332424A1 (en) 2011-11-02 2014-06-05 Synta Pharmaceuticals Corp. Combination therapy of Hsp90 inhibitors with platinum-containing agents
WO2013074594A1 (en) 2011-11-14 2013-05-23 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

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022250363A1 (ko) * 2021-05-24 2022-12-01 재단법인대구경북과학기술원 아이유원 계열의 유비퀴틴 특이적 프로테아제 14 억제제를 유효성분으로 포함하는, 프로탁의 항암 효과 증진용 약학적 조성물

Also Published As

Publication number Publication date
EP2528911B1 (en) 2017-10-25
CA2787785A1 (en) 2011-08-04
US20160214989A1 (en) 2016-07-28
WO2011094545A3 (en) 2012-01-05
RU2012136451A (ru) 2014-03-10
CN102844313B (zh) 2016-10-05
US20130045992A1 (en) 2013-02-21
CA2787785C (en) 2018-03-06
JP2016147893A (ja) 2016-08-18
AU2011210765A1 (en) 2012-09-13
JP6371786B2 (ja) 2018-08-08
CN102844313A (zh) 2012-12-26
BR112012018631A2 (pt) 2016-04-05
EP2528911A2 (en) 2012-12-05
WO2011094545A2 (en) 2011-08-04
EP2528911A4 (en) 2014-08-06
MX336731B (es) 2016-01-28
BR112012018631A8 (pt) 2017-12-19
MX2012008626A (es) 2012-08-15
US10351568B2 (en) 2019-07-16
SG182662A1 (en) 2012-08-30
JP2013518129A (ja) 2013-05-20

Similar Documents

Publication Publication Date Title
KR20120117905A (ko) 프로테아좀 활성을 향상시키는 조성물 및 방법
CA2808432C (en) Tricyclic proteasome activity enhancing compounds with thieno[2,3-d]pyrimidine core
RU2720488C2 (ru) Замещенные амино шестичленные насыщенные гетероалициклы в качестве ингибиторов dpp-iv длительного действия
JPWO2007043568A1 (ja) Ｓ１ｐ３受容体拮抗剤
HUE025731T2 (en) Chromone derivatives useful in the treatment of diseases mediated by TCR-NCK interaction
EP3242881B1 (en) Furoquinolinediones as inhibitors of tdp2
KR20190110106A (ko) 신경퇴행성 질환의 치료를 위한 중성 스핑고미엘리나제 2(nSMAse2)의 저분자 억제제
US8314092B2 (en) Substituted [(5H-pyrrolo[2,1-c][1,4]benzodiazepin-11-yl)piperazin-1-yl]-2,2-dimethylpropanoic acid compounds as dual activity H1 inverse agonists/5-HT2A antagonists
Liu et al. Design and synthesis of 2-phenyl-1 H-benzo [d] imidazole derivatives as 17β-HSD10 inhibitors for the treatment of Alzheimer's disease
US20250129080A1 (en) Compositions and methods of using the same for treatment of neurodegenerative and mitochondrial disease
US6602865B1 (en) Pyridazino(4,5-b)(1,5)oxazepinone, -thiazepinone and -diazepinone compounds
JP2021522290A (ja) １−イミダゾチアジアゾロ−２ｈ−ピロール−５−オン誘導体
EP2980087B1 (en) Prodrugs of bicyclic substituted pyrimidine type pde-5 inhibitors
WO2021189036A1 (en) Taf1 inhibitors
AU2017204046A1 (en) Compositions and methods for enhancing proteasome activity
WO2025214437A1 (zh) 咪唑稠环类化合物、药物组合物及其制备方法和应用
CN120936595A (zh) 作为phd抑制剂的吡唑衍生物

Legal Events

Date Code Title Description
PA0105 International application

Patent event date: 20120824

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
A201 Request for examination
PA0201 Request for examination

Patent event code: PA02012R01D

Patent event date: 20160128

Comment text: Request for Examination of Application

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

Comment text: Notification of reason for refusal

Patent event date: 20160928

Patent event code: PE09021S01D

E601 Decision to refuse application
PE0601 Decision on rejection of patent

Patent event date: 20170531

Comment text: Decision to Refuse Application

Patent event code: PE06012S01D

Patent event date: 20160928

Comment text: Notification of reason for refusal

Patent event code: PE06011S01I