CN114728071B - 用于降解tau蛋白聚集体的化合物及其用途 - Google Patents

用于降解tau蛋白聚集体的化合物及其用途 Download PDF

Info

Publication number
CN114728071B
CN114728071B CN202080078757.6A CN202080078757A CN114728071B CN 114728071 B CN114728071 B CN 114728071B CN 202080078757 A CN202080078757 A CN 202080078757A CN 114728071 B CN114728071 B CN 114728071B
Authority
CN
China
Prior art keywords
compound
alkyl
formula
alkoxy
haloalkyl
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.)
Active
Application number
CN202080078757.6A
Other languages
English (en)
Chinese (zh)
Other versions
CN114728071A (zh
Inventor
P·坦皮斯特
张明奎
林易娴
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.)
Xinxu Biotechnology Co ltd
Original Assignee
Xinxu Biotechnology Co ltd
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 Xinxu Biotechnology Co ltd filed Critical Xinxu Biotechnology Co ltd
Publication of CN114728071A publication Critical patent/CN114728071A/zh
Application granted granted Critical
Publication of CN114728071B publication Critical patent/CN114728071B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/545Heterocyclic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/55Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
CN202080078757.6A 2019-11-13 2020-11-13 用于降解tau蛋白聚集体的化合物及其用途 Active CN114728071B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962935017P 2019-11-13 2019-11-13
US62/935,017 2019-11-13
PCT/US2020/060459 WO2021097243A1 (en) 2019-11-13 2020-11-13 Compounds for degrading tau protein aggregates and uses thereof

Publications (2)

Publication Number Publication Date
CN114728071A CN114728071A (zh) 2022-07-08
CN114728071B true CN114728071B (zh) 2024-12-06

Family

ID=75912369

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202080078757.6A Active CN114728071B (zh) 2019-11-13 2020-11-13 用于降解tau蛋白聚集体的化合物及其用途

Country Status (8)

Country Link
US (5) US20220354835A1 (https=)
EP (1) EP4058065A4 (https=)
JP (1) JP7605504B2 (https=)
KR (1) KR20220100921A (https=)
CN (1) CN114728071B (https=)
CA (1) CA3161455A1 (https=)
TW (1) TWI759962B (https=)
WO (1) WO2021097243A1 (https=)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4121046A4 (en) * 2020-03-18 2024-04-24 Dana-Farber Cancer Institute, Inc. Targeted degraders of aberrant tau based on the pet tracer pbb3
IL301690A (en) * 2020-10-16 2023-05-01 Dana Farber Cancer Inst Inc Piperidinyl small molecule degraders of helios and methods of use
WO2025117551A1 (en) * 2023-11-27 2025-06-05 Amydis, Inc. Amino acid derivatives for detecting neurological disorders
WO2025129172A1 (en) * 2023-12-14 2025-06-19 The Board Of Trustees Of The Leland Stanford Junior University Crbn molecular glue degraders and uses thereof

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102438660A (zh) * 2009-03-23 2012-05-02 美国西门子医疗解决公司 用于检测神经障碍的显像剂
WO2019014429A1 (en) * 2017-07-12 2019-01-17 Dana-Farber Cancer Institute, Inc. COMPOUNDS FOR THE DEGRADATION OF TAU PROTEIN
CN110234646A (zh) * 2016-11-01 2019-09-13 阿尔维纳斯股份有限公司 靶向PROTAC的Tau蛋白及相关使用方法
WO2019214681A1 (en) * 2018-05-09 2019-11-14 Aprinoia Therapeutics Inc. Heteroaryl compounds and uses thereof

Family Cites Families (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3833863A (en) 1971-12-27 1974-09-03 Eastman Kodak Co Styryl and arylbutadienyl dye lasers
JPS5553333A (en) 1978-10-16 1980-04-18 Hitachi Ltd Composite type electrophotographic plate
JPS61275836A (ja) 1985-05-31 1986-12-05 Fuji Photo Film Co Ltd ハロゲン化銀写真乳剤
GB8921116D0 (en) 1989-09-18 1989-11-01 Du Pont Improvements in or relating to radiation sensitive compositions
US5264329A (en) 1989-09-18 1993-11-23 Dupont (U.K.) Limited Radiation sensitive compositions
RU2324686C2 (ru) 2000-08-24 2008-05-20 Юнивесити Оф Питсбэг ПРОИЗВОДНЫЕ ТИОФЛАВИНА, СВЯЗЫВАЮЩИЕ АМИЛОИД, СПОСОБ ОБНАРУЖЕНИЯ in vivo ОТЛОЖЕНИЙ АМИЛОИДА И СПОСОБ РАСПОЗНАВАНИЯ БОЛЕЗНИ АЛЬЦГЕЙМЕРА
WO2003048137A1 (en) * 2001-11-30 2003-06-12 Merck & Co., Inc. Metabotropic glutamate receptor-5 modulators
MXPA05012459A (es) 2003-05-19 2006-02-22 Irm Llc Compuestos y composiciones inmunosupresoras.
WO2005016384A1 (ja) 2003-08-13 2005-02-24 Bf Research Institute, Inc. アミロイド蓄積性疾患のプローブ、アミロイド染色剤、アミロイド蓄積性疾患の治療および予防薬、ならびに神経原線維変化の診断プローブおよび染色剤
CA2500358A1 (en) 2003-08-13 2005-02-24 Bf Research Institute, Inc. Probes for diseases in which amyloid accumulates, agents for staining amyloid, drugs for treatment and prophylaxis of diseases with accumulated amyloid, and probes for diagnosis of neurofibrillary tangles and agents for staining neurofibrillary tangles
JP2007106755A (ja) 2005-09-13 2007-04-26 Japan Health Science Foundation アミロイドイメージング用プローブ
WO2007034282A2 (en) 2005-09-19 2007-03-29 Pfizer Products Inc. Diaryl-imidazole compounds condensed with a heterocycle as c3a receptor antagonists
CN101351458A (zh) 2005-12-01 2009-01-21 匹兹堡大学 作为促淀粉样变蛋白成像剂的同位素标记的苯并噻唑化合物
TW201018678A (en) 2006-01-27 2010-05-16 Astrazeneca Ab Novel heteroaryl substituted benzothiazoles
FR2906250B1 (fr) 2006-09-22 2008-10-31 Sanofi Aventis Sa Derives de 2-aryl-6phenyl-imidazo(1,2-a) pyridines, leur preparation et leur application en therapeutique
WO2008078424A1 (ja) 2006-12-25 2008-07-03 Tohoku University ベンゾキサゾール誘導体
EP2247558B2 (en) 2008-02-14 2024-07-03 Eli Lilly and Company Novel imaging agents for detecting neurological dysfunction
JP5603855B2 (ja) 2008-04-04 2014-10-08 アビッド レディオファーマシューティカルズ、インク. 神経変成疾患の放射性薬剤による画像化
JP2011529086A (ja) * 2008-07-24 2011-12-01 シーメンス メディカル ソリューションズ ユーエスエー インコーポレイテッド Ad病変を同定するために有用な造影剤
US8193363B2 (en) 2008-08-29 2012-06-05 Astrazeneca Ab Compounds suitable as precursors to compounds that are useful for imaging amyloid deposits
CA2737028C (en) 2008-09-23 2017-06-27 Wista Laboratories Ltd. Ligands for aggregated tau molecules
JP5591720B2 (ja) 2009-01-29 2014-09-17 株式会社林原 抗神経変性疾患剤
JPWO2010087315A1 (ja) 2009-01-29 2012-08-02 株式会社林原生物化学研究所 抗アルツハイマー病剤
US8691187B2 (en) 2009-03-23 2014-04-08 Eli Lilly And Company Imaging agents for detecting neurological disorders
JP2010275836A (ja) 2009-06-01 2010-12-09 Miwa Lock Co Ltd 電気錠システムの雷サージ対策アダプタ
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
US20120263646A1 (en) 2009-10-15 2012-10-18 Guerbet Imaging agents and their use for the diagnostic in vivo of neurodegenerative diseases, notably alzheimer's disease and derivative diseases
KR101116234B1 (ko) 2009-10-29 2014-03-06 (주)퓨쳐켐 (3-플루오로-2-히드록시)프로필 작용기가 도입된 아릴 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 퇴행성 뇌질환의 진단 또는 치료용 약학적 조성물
US9133343B2 (en) 2009-11-30 2015-09-15 Enzo Biochem, Inc. Dyes and compositions, and processes for using same in analysis of protein aggregation and other applications
JP6106157B2 (ja) 2011-04-26 2017-03-29 レトロトップ、 インコーポレイテッドRetrotope, Inc. 神経変性障害および筋疾患に関与するpufa
EP2724161A1 (en) 2011-06-22 2014-04-30 F.Hoffmann-La Roche Ag A method for the identification of beta-sheet aggregated protein ligands
DK2767532T3 (en) 2012-12-21 2016-09-12 Nat Inst For Quantum And Radiological Science And Tech New connection for reproduction of tau protein heavy in the brain.
US9447054B2 (en) 2014-01-15 2016-09-20 Korea Institute Of Radiological & Medical Sciences Anticancer supplement agent including benzo[D]oxazol derivative as effective ingredient
WO2015188368A1 (en) 2014-06-13 2015-12-17 Merck Sharp & Dohme Corp. Pyrrolo[2,3-c]pyridines as imaging agents for neurofibrilary tangles
WO2016105518A1 (en) 2014-12-23 2016-06-30 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
US9694084B2 (en) 2014-12-23 2017-07-04 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
US10308871B2 (en) 2015-02-19 2019-06-04 Jnc Corporation Liquid crystal compound having benzothiophene, liquid crystal composition and liquid crystal display device
EP3270917A4 (en) 2015-03-18 2018-08-08 Arvinas, Inc. Compounds and methods for the enhanced degradation of targeted proteins
WO2017007612A1 (en) 2015-07-07 2017-01-12 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
WO2017024318A1 (en) * 2015-08-06 2017-02-09 Dana-Farber Cancer Institute, Inc. Targeted protein degradation to attenuate adoptive t-cell therapy associated adverse inflammatory responses
US10772962B2 (en) 2015-08-19 2020-09-15 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
TW201722958A (zh) * 2015-09-15 2017-07-01 葛蘭素史克智慧財產(第二)有限公司 化學化合物
TW201722957A (zh) * 2015-09-15 2017-07-01 葛蘭素史克智慧財產(第二)有限公司 化學化合物
US10300155B2 (en) 2015-12-31 2019-05-28 Washington University Alpha-synuclein ligands
US10059878B2 (en) 2016-02-17 2018-08-28 Jnc Corporation Liquid crystal composition and liquid crystal display device
JP6696312B2 (ja) 2016-06-15 2020-05-20 Jnc株式会社 液晶組成物および液晶表示素子
PH12018502613B1 (en) 2016-07-12 2023-02-01 H Lundbeck As Antibodies specific for hyperphosphorylated tau and methods of use thereof
CA3030754C (en) 2016-07-20 2022-04-26 Anahit Ghochikyan Humanized anti-tau antibodies and compositions for and methods of making and using in treatment, diagnosis and monitoring of tauopathies
KR20250117470A (ko) * 2016-12-23 2025-08-04 아비나스 오퍼레이션스, 인코포레이티드 급속 진행성 섬유육종 폴리펩티드의 표적화 분해를 위한 화합물 및 방법
JP2020505327A (ja) * 2016-12-23 2020-02-20 アルビナス・オペレーションズ・インコーポレイテッドArvinas Operations, Inc. Egfrタンパク質分解標的化キメラ分子およびその関連する使用方法
US11919902B2 (en) * 2017-12-22 2024-03-05 Hibercell, Inc. Aryl-bipyridine amine derivatives as phosphatidylinositol phosphate kinase inhibitors
AU2019294835B2 (en) 2018-06-29 2025-04-17 Dana-Farber Cancer Institute, Inc. Ligands to cereblon (CRBN)
JP7297053B2 (ja) 2018-08-20 2023-06-23 アルビナス・オペレーションズ・インコーポレイテッド 神経変性疾患を治療するためのe3ユビキチンリガーゼ結合活性を有するキメラ(protac)化合物を標的とし、アルファ-シヌクレインタンパク質を標的とするタンパク質分解
EP3999182A1 (en) 2019-07-17 2022-05-25 Arvinas Operations, Inc. Tau-protein targeting compounds and associated methods of use

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102438660A (zh) * 2009-03-23 2012-05-02 美国西门子医疗解决公司 用于检测神经障碍的显像剂
CN110234646A (zh) * 2016-11-01 2019-09-13 阿尔维纳斯股份有限公司 靶向PROTAC的Tau蛋白及相关使用方法
WO2019014429A1 (en) * 2017-07-12 2019-01-17 Dana-Farber Cancer Institute, Inc. COMPOUNDS FOR THE DEGRADATION OF TAU PROTEIN
WO2019214681A1 (en) * 2018-05-09 2019-11-14 Aprinoia Therapeutics Inc. Heteroaryl compounds and uses thereof

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Targeted degradation of aberrant tau in frontotemporal dementia patient-derived neuronal cell models;M Catarina Silva et al.;《elife》;第8卷;摘要, 图1 *

Also Published As

Publication number Publication date
US20220280650A1 (en) 2022-09-08
US20220267316A1 (en) 2022-08-25
EP4058065A4 (en) 2023-05-03
EP4058065A1 (en) 2022-09-21
JP7605504B2 (ja) 2024-12-24
WO2021097243A1 (en) 2021-05-20
TW202128657A (zh) 2021-08-01
AU2020383593A1 (en) 2022-06-09
US20220354835A1 (en) 2022-11-10
US12377152B2 (en) 2025-08-05
US11291732B1 (en) 2022-04-05
KR20220100921A (ko) 2022-07-18
CA3161455A1 (en) 2021-05-20
US11642413B2 (en) 2023-05-09
US20230346955A1 (en) 2023-11-02
TWI759962B (zh) 2022-04-01
CN114728071A (zh) 2022-07-08
JP2023502605A (ja) 2023-01-25

Similar Documents

Publication Publication Date Title
CN114728071B (zh) 用于降解tau蛋白聚集体的化合物及其用途
JP7490781B2 (ja) Sarm1の阻害剤
CN112313231B (zh) Oga抑制剂化合物
JP2020503300A (ja) 二環式oga阻害剤化合物
WO2018154133A1 (en) [1,2,4]-triazolo [1,5-a]-pyrimidinyl derivatives substituted with piperidine, morpholine or piperazine as oga inhibitors
US20070203135A1 (en) Novel Fused Pyrrolocarbazoles
CN110267961A (zh) Oga抑制剂化合物
US7169802B2 (en) Fused pyrrolocarbazoles
CN117377496A (zh) 用于降解α-突触核蛋白聚集体的化合物及其用途
US20210277015A1 (en) Oga inhibitor compounds
AU2020383593B2 (en) Compounds for degrading Tau protein aggregates and uses thereof
HK40069557A (en) Compounds for degrading tau protein aggregates and uses thereof
CN112334462A (zh) Oga抑制剂化合物
HK40069557B (zh) 用於降解tau蛋白聚集体的化合物及其用途
US20210261527A1 (en) Oga inhibitor compounds

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 40069557

Country of ref document: HK

GR01 Patent grant
GR01 Patent grant
PP01 Preservation of patent right

Effective date of registration: 20250611

Granted publication date: 20241206

PP01 Preservation of patent right