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 PDFInfo
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- 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
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- 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
- A61K31/41—Heterocyclic 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
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
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- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 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
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- 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
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- 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
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non 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
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- 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
- A61K31/495—Heterocyclic 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- A—HUMAN NECESSITIES
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- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal 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
- A61K47/51—Medicinal 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
- A61K47/54—Medicinal 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
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- A61K47/50—Medicinal 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
- A61K47/51—Medicinal 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
- A61K47/54—Medicinal 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
- A61K47/545—Heterocyclic compounds
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K47/50—Medicinal 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
- A61K47/51—Medicinal 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
- A61K47/54—Medicinal 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
- A61K47/55—Medicinal 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
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- 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
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic 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
- C07D417/14—Heterocyclic 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
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- 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
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- 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)
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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)
| 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)
| 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)
| 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 |
-
2020
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- 2020-11-13 JP JP2022527685A patent/JP7605504B2/ja active Active
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Patent Citations (4)
| 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)
| 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 * |
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| US20220280650A1 (en) | 2022-09-08 |
| US20220267316A1 (en) | 2022-08-25 |
| EP4058065A4 (en) | 2023-05-03 |
| EP4058065A1 (en) | 2022-09-21 |
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| AU2020383593A1 (en) | 2022-06-09 |
| US20220354835A1 (en) | 2022-11-10 |
| US12377152B2 (en) | 2025-08-05 |
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| US11642413B2 (en) | 2023-05-09 |
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| TWI759962B (zh) | 2022-04-01 |
| CN114728071A (zh) | 2022-07-08 |
| JP2023502605A (ja) | 2023-01-25 |
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