JP2023538517A - Retの標的分解のための化合物 - Google Patents
Retの標的分解のための化合物 Download PDFInfo
- Publication number
- JP2023538517A JP2023538517A JP2023507866A JP2023507866A JP2023538517A JP 2023538517 A JP2023538517 A JP 2023538517A JP 2023507866 A JP2023507866 A JP 2023507866A JP 2023507866 A JP2023507866 A JP 2023507866A JP 2023538517 A JP2023538517 A JP 2023538517A
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- Japan
- Prior art keywords
- alkyl
- compound according
- aryl
- ret
- heterocycle
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
- 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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Anti-Oxidant Or Stabilizer Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicinal Preparation (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063061741P | 2020-08-05 | 2020-08-05 | |
| US63/061,741 | 2020-08-05 | ||
| US202163136586P | 2021-01-12 | 2021-01-12 | |
| US63/136,586 | 2021-01-12 | ||
| PCT/US2021/044838 WO2022032026A1 (en) | 2020-08-05 | 2021-08-05 | Compounds for targeted degradation of ret |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2023538517A true JP2023538517A (ja) | 2023-09-08 |
| JP2023538517A5 JP2023538517A5 (https=) | 2024-08-14 |
Family
ID=80118572
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023507866A Pending JP2023538517A (ja) | 2020-08-05 | 2021-08-05 | Retの標的分解のための化合物 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US20230233692A1 (https=) |
| EP (1) | EP4192458A4 (https=) |
| JP (1) | JP2023538517A (https=) |
| CN (1) | CN116490186B (https=) |
| CA (1) | CA3188313A1 (https=) |
| IL (1) | IL300397A (https=) |
| WO (1) | WO2022032026A1 (https=) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110769822A (zh) | 2017-06-20 | 2020-02-07 | C4医药公司 | 用于蛋白降解的n/o-连接的降解决定子和降解决定子体 |
| TW202146412A (zh) | 2020-03-05 | 2021-12-16 | 美商C4醫藥公司 | 用於標靶降解brd9之化合物 |
| WO2024030968A1 (en) * | 2022-08-03 | 2024-02-08 | Brystol-Myers Squibb Company | Compounds for modulating ret protein |
| WO2024073507A1 (en) | 2022-09-28 | 2024-04-04 | Theseus Pharmaceuticals, Inc. | Macrocyclic compounds and uses thereof |
| WO2024158759A2 (en) * | 2023-01-23 | 2024-08-02 | Purdue Research Foundation | Inhibitors of solvent front mutated ret kinase |
| KR20250145679A (ko) * | 2023-02-16 | 2025-10-13 | 브리스톨-마이어스 스큅 컴퍼니 | Ret 키나제의 분해제로서의 이소인돌리논 글루타르이미드 및 페닐 글루타르이미드 유사체 |
| TW202502750A (zh) | 2023-06-08 | 2025-01-16 | 美商新銳思生物製藥股份有限公司 | Smarca2之雙官能選擇性降解劑及其治療用途 |
| EP4735452A2 (en) | 2023-06-30 | 2026-05-06 | Merck Patent GmbH | Heterobifunctional compounds for the degradation of kras protein |
| EP4735438A2 (en) | 2023-06-30 | 2026-05-06 | Merck Patent GmbH | Heterobifunctional compounds for the degradation of kras |
| CN117003681A (zh) * | 2023-07-04 | 2023-11-07 | 苏州汉德创宏生化科技有限公司 | 一种抑制剂类中间体及其合成方法 |
| WO2025062330A1 (en) | 2023-09-20 | 2025-03-27 | Aurigene Oncology Limited | Heterocyclic compounds as cbp selective degraders |
| TW202535377A (zh) * | 2023-12-22 | 2025-09-16 | 美商C4醫藥公司 | 用於標靶降解原癌基因酪胺酸蛋白質激酶受體(ret)之化合物 |
Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2018532690A (ja) * | 2015-07-16 | 2018-11-08 | アレイ バイオファーマ、インコーポレイテッド | RETキナーゼ阻害物質としての置換ピラゾロ[1,5−a]ピリジン化合物 |
| WO2018237026A1 (en) * | 2017-06-20 | 2018-12-27 | C4 Therapeutics, Inc. | N / O-LINKED DEGRONS AND DEGRONIMERS FOR DEGRADATION OF PROTEINS |
| WO2019099868A2 (en) * | 2017-11-16 | 2019-05-23 | C4 Therapeutics, Inc. | Degraders and degrons for targeted protein degradation |
| JP2020506902A (ja) * | 2017-01-18 | 2020-03-05 | アレイ バイオファーマ、インコーポレイテッド | RETキナーゼ阻害剤としての置換ピラゾロ[1,5−a]ピラジン化合物 |
| WO2020051235A1 (en) * | 2018-09-04 | 2020-03-12 | C4 Therapeutics, Inc. | Compounds for the degradation of brd9 or mth1 |
| WO2020114487A1 (en) * | 2018-12-07 | 2020-06-11 | Sunshine Lake Pharma Co., Ltd. | Ret inhibitors, pharmaceutical compositions and uses thereof |
| WO2020132561A1 (en) * | 2018-12-20 | 2020-06-25 | C4 Therapeutics, Inc. | Targeted protein degradation |
Family Cites Families (120)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4418068A (en) | 1981-04-03 | 1983-11-29 | Eli Lilly And Company | Antiestrogenic and antiandrugenic benzothiophenes |
| TW366342B (en) | 1992-07-28 | 1999-08-11 | Lilly Co Eli | The use of 2-phenyl-3-aroylbenzothiophenes in inhibiting bone loss |
| US5478847A (en) | 1994-03-02 | 1995-12-26 | Eli Lilly And Company | Methods of use for inhibiting bone loss and lowering serum cholesterol |
| US5880137A (en) | 1996-04-19 | 1999-03-09 | American Home Products Corporation | 2-phenyl-1- 4-(amino-1-yl-alk-1-ynyl)-benzyl!-1H-indol-5-ols as estrogenic agents |
| US5780497A (en) | 1996-04-19 | 1998-07-14 | American Home Products Corporation | 2-phenyl-1- 4-(amino-1-yl-alk-1-ynyl)-benzyl!-1H-indol-5-ols as estrogenic agents |
| US5998402A (en) | 1996-04-19 | 1999-12-07 | American Home Products Corporation | 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indoles as estrogenic agents |
| TW397821B (en) | 1996-04-19 | 2000-07-11 | American Home Produits Corp | 3-[4-(2-phenyl-indole-1-ylmethyl)-phenyl]-acrylamides and 2-phenyl-1-[4-(amino-1-yl-alk-1-ynyl)-benzyl]-1H-indol-5-ol as well as pharmaceutical compositions of estrogenic agents thereof |
| HU228769B1 (en) | 1996-07-24 | 2013-05-28 | Celgene Corp | Substituted 2(2,6-dioxopiperidin-3-yl)phthalimides and -1-oxoisoindolines and their use for production of pharmaceutical compositions for mammals to reduce the level of tnf-alpha |
| US6005102A (en) | 1997-10-15 | 1999-12-21 | American Home Products Corporation | Aryloxy-alkyl-dialkylamines |
| US6326392B1 (en) | 1997-11-06 | 2001-12-04 | American Home Products Corporation | Anti-estrogen plus progestin containing oral contraceptives |
| ID24568A (id) | 1997-11-06 | 2000-07-27 | American Home Prod | Kontrasepsi oral yang mengandung anti-estrogen plus progestin |
| TR200101502T2 (tr) | 1998-03-16 | 2002-06-21 | Celgene Corporation | 2-(2,6-dioksopiperidin-3-il) izoindolin türevleri, bunların hazırlanması ve enflamatuar sitokinlerin inhibitörleri olarak kullanımı |
| US6479535B1 (en) | 1998-05-15 | 2002-11-12 | Wyeth | 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indole and estrogen formulations |
| US6583170B1 (en) | 1998-05-15 | 2003-06-24 | Wyeth | 2-Phenyl-1-[4-(amino-1-yl-alk-1-ynyl)-benzyl]-1H-indol-5-ol and estrogen formulations |
| US6045501A (en) | 1998-08-28 | 2000-04-04 | Celgene Corporation | Methods for delivering a drug to a patient while preventing the exposure of a foetus or other contraindicated individual to the drug |
| US6306663B1 (en) | 1999-02-12 | 2001-10-23 | Proteinex, Inc. | Controlling protein levels in eucaryotic organisms |
| CO5271697A1 (es) | 2000-01-12 | 2003-04-30 | Pfizer Prod Inc | Composiciones y procedimientos para el tratamiento de afecciones que responden a un aumento de testosterona |
| CO5271709A1 (es) | 2000-01-12 | 2003-04-30 | Pfizer Prod Inc | Composiciones y procedimientos para el y tratamiento de afecciones que responden a estrogenos |
| CO5271696A1 (es) | 2000-01-12 | 2003-04-30 | Pfizer Prod Inc | Procedimiento para reducir la morbilidad y el riesgo de mortalidad |
| CO5251465A1 (es) | 2000-01-26 | 2003-02-28 | Pfizer Prod Inc | Composiciones y procedimientos para tratar la osteoporosis y reducir el colesterol |
| US20020013327A1 (en) | 2000-04-18 | 2002-01-31 | Lee Andrew G. | Compositions and methods for treating female sexual dysfunction |
| WO2002003986A2 (en) | 2000-07-06 | 2002-01-17 | Wyeth | Use of substituted indole compounds for treating breast disorders |
| WO2002003989A2 (en) | 2000-07-06 | 2002-01-17 | Wyeth | Use of substituted indole compounds for treating sphincter incontinence |
| AU7178301A (en) | 2000-07-06 | 2002-01-21 | American Home Prod | Methods for increasing nitric oxide synthase activity |
| AU2001273144A1 (en) | 2000-07-06 | 2002-01-21 | Wyeth | Use of substituted indole compounds for treating neuropeptide y-related conditions |
| MXPA03000170A (es) | 2000-07-06 | 2003-05-27 | Wyeth Corp | Combinaciones de un inhibidor de recaptacion de serotonina selectivo y agentes estrogenicos. |
| AU2001271784A1 (en) | 2000-07-06 | 2002-01-21 | Wyeth | Therapy for prosthesis-related bone degeneration |
| WO2002003990A2 (en) | 2000-07-06 | 2002-01-17 | Wyeth | Use of substituted insole compounds for treating excessive intraocular pressure |
| AU2001271785A1 (en) | 2000-07-06 | 2002-01-21 | American Home Products Corporation | Combinations of statins, estrogenic agents and optionally estrogens |
| AU2001273125A1 (en) | 2000-07-06 | 2002-01-21 | American Home Products Corporation | Combinations of bisphosphonates, estrogenic agents and optionally estrogens |
| AR030064A1 (es) | 2000-07-06 | 2003-08-13 | Wyeth Corp | Metodos para inhibir los efectos uterotroficos de los agentes estrogenicos |
| EP1177787A3 (en) | 2000-07-28 | 2003-09-10 | Pfizer Products Inc. | Use of an estrogen agonist/antagonist for treating cataracts |
| JP2004507465A (ja) | 2000-08-11 | 2004-03-11 | ワイス | エストロゲン受容体陽性癌腫の治療方法 |
| EP1192945A3 (en) | 2000-09-21 | 2004-03-03 | Pfizer Products Inc. | Use of an estrogen agonist/antagonist for treating osteoarthritis |
| IL145838A (en) | 2000-10-16 | 2008-11-03 | Pfizer Prod Inc | Use of an estrogen agonist/antagonist for the manufacture of a medicament for treating vaginitis |
| US6315720B1 (en) | 2000-10-23 | 2001-11-13 | Celgene Corporation | Methods for delivering a drug to a patient while avoiding the occurrence of an adverse side effect known or suspected of being caused by the drug |
| AU781168B2 (en) | 2001-01-26 | 2005-05-12 | Pfizer Products Inc. | Method of treating certain cancers using an estrogen agonist/antagonist |
| US7968569B2 (en) | 2002-05-17 | 2011-06-28 | Celgene Corporation | Methods for treatment of multiple myeloma using 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione |
| US8404716B2 (en) | 2002-10-15 | 2013-03-26 | Celgene Corporation | Methods of treating myelodysplastic syndromes with a combination therapy using lenalidomide and azacitidine |
| US7230012B2 (en) | 2002-11-14 | 2007-06-12 | Celgene Corporation | Pharmaceutical compositions and dosage forms of thalidomide |
| AU2006206446A1 (en) | 2005-01-21 | 2006-07-27 | Janssen Pharmaceutica N.V. | Novel heterocyclic benzo[c]chromene derivatives useful as modulators of the estrogen receptors |
| JP5315060B2 (ja) | 2006-02-03 | 2013-10-16 | バイオノミックス リミテッド | 置換ベンゾフラン、ベンゾチオフェン、ベンゾセレノフェンおよびインドールおよびそれらのチューブリン重合阻害剤としての使用 |
| CL2007002218A1 (es) | 2006-08-03 | 2008-03-14 | Celgene Corp Soc Organizada Ba | Uso de 3-(4-amino-1-oxo-1,3-dihidro-isoindol-2-il)-piperidina 2,6-diona para la preparacion de un medicamento util para el tratamiento de linfoma de celula de capa. |
| BRPI1007855B1 (pt) | 2009-05-19 | 2020-03-10 | Celgene Corporation | Formas de dosagem oral compreendendo 4-amino-2-(2,6-dioxopiperidina-3-il)isoindolina-1,3-diona |
| US9556426B2 (en) | 2009-09-16 | 2017-01-31 | Celgene Avilomics Research, Inc. | Protein kinase conjugates and inhibitors |
| RS56042B1 (sr) | 2010-06-10 | 2017-09-29 | Seragon Pharmaceuticals Inc | Modulatori estrogenih receptora i njihove upotrebe |
| US8853423B2 (en) | 2010-06-17 | 2014-10-07 | Seragon Pharmaceuticals, Inc. | Indane estrogen receptor modulators and uses thereof |
| GB2483736B (en) | 2010-09-16 | 2012-08-29 | Aragon Pharmaceuticals Inc | Estrogen receptor modulators and uses thereof |
| US10005750B2 (en) | 2010-10-06 | 2018-06-26 | J-Pharma Co., Ltd. | Developing potent urate transporter inhibitors: compounds designed for their uricosuric action |
| CA2819299A1 (en) | 2010-12-24 | 2012-06-28 | Merck Sharp & Dohme B.V. | N-substituted azetidine derivatives |
| WO2013090829A1 (en) | 2011-12-14 | 2013-06-20 | Aragon Pharmaceuticals, Inc. | Estrogen receptor modulators and uses thereof |
| EP2791128A4 (en) | 2011-12-16 | 2015-04-22 | Olema Pharmaceuticals Inc | NOVEL BENZOPYRAN COMPOUNDS, COMPOSITIONS AND USES THEREOF |
| ES2872967T3 (es) | 2012-06-29 | 2021-11-03 | Celgene Corp | Métodos para determinar la eficacia de fármacos usando IKZF3 (AIOLOS) |
| WO2014019176A1 (zh) | 2012-08-01 | 2014-02-06 | 华为技术有限公司 | 用于同步的方法、装置及系统 |
| US9587281B2 (en) | 2012-08-14 | 2017-03-07 | Celgene Corporation | Cereblon isoforms and their use as biomarkers for therapeutic treatment |
| UY35590A (es) | 2013-05-28 | 2014-11-28 | Astrazeneca Ab | Nuevos compuestos para el tratamiento del cáncer |
| WO2014203129A1 (en) | 2013-06-19 | 2014-12-24 | Olema Pharmaceuticals, Inc. | Combinations of benzopyran compounds, compositions and uses thereof |
| CA2915534A1 (en) | 2013-06-19 | 2014-12-24 | Seragon Pharmaceuticals, Inc. | Azetidine estrogen receptor modulators and uses thereof |
| EA031077B1 (ru) | 2013-06-19 | 2018-11-30 | Серагон Фармасьютикалз, Инк. | Модулятор рецептора эстрогена и его применения |
| WO2014203132A1 (en) | 2013-06-19 | 2014-12-24 | Olema Pharmaceuticals, Inc. | Substituted benzopyran compounds, compositions and uses thereof |
| WO2015136016A2 (en) | 2014-03-13 | 2015-09-17 | F. Hoffmann-La Roche Ag | Therapeutic combinations with estrogen receptor modulators |
| RU2738833C9 (ru) | 2014-04-14 | 2022-02-28 | Арвинас, Оперэйшнз, Инк. | Имидные модуляторы протеолиза и способы их применения |
| EP3827836A1 (en) | 2014-06-27 | 2021-06-02 | Celgene Corporation | Compositions and methods for inducing conformational changes in cereblon and other e3 ubiquitin ligases |
| TWI874834B (zh) | 2014-12-18 | 2025-03-01 | 瑞士商赫孚孟拉羅股份公司 | 四氫-吡啶并[3,4-b]吲哚雌激素受體調節劑及其用途 |
| WO2016105518A1 (en) | 2014-12-23 | 2016-06-30 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| JP6817962B2 (ja) | 2015-01-20 | 2021-01-20 | 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. | ターゲティングされたアンドロゲン受容体分解のための化合物および方法 |
| EP3270917A4 (en) | 2015-03-18 | 2018-08-08 | Arvinas, Inc. | Compounds and methods for the enhanced degradation of targeted proteins |
| CA2988414C (en) | 2015-06-04 | 2023-09-26 | Arvinas, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| WO2016197114A1 (en) | 2015-06-05 | 2016-12-08 | Arvinas, Inc. | Tank-binding kinase-1 protacs and associated methods of use |
| WO2017007612A1 (en) | 2015-07-07 | 2017-01-12 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| EP3319944A4 (en) | 2015-07-10 | 2019-04-24 | Arvinas, Inc. | MDM2-BASED MODULATORS OF PROTEOLYSIS AND RELATED USE METHODS |
| BR112017028269A2 (pt) | 2015-07-13 | 2018-09-04 | Arvinas Inc | composto, composição farmacêutica, uso de uma quantidade efetiva de um composto, estado ou condição de doença, e, método para identificar um composto. |
| US10772962B2 (en) | 2015-08-19 | 2020-09-15 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of bromodomain-containing proteins |
| GB201516243D0 (en) | 2015-09-14 | 2015-10-28 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| US20170281784A1 (en) | 2016-04-05 | 2017-10-05 | Arvinas, Inc. | Protein-protein interaction inducing technology |
| SG11201808728QA (en) | 2016-04-06 | 2018-11-29 | Univ Michigan Regents | Mdm2 protein degraders |
| KR20180132861A (ko) | 2016-04-12 | 2018-12-12 | 더 리젠츠 오브 더 유니버시티 오브 미시간 | Bet 단백질 분해제 |
| ES2990061T3 (es) | 2016-05-10 | 2024-11-28 | C4 Therapeutics Inc | Degronímeros espirocíclicos para la degradación de proteínas diana |
| 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 |
| EP3454856B1 (en) | 2016-05-10 | 2024-09-11 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
| 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 |
| WO2017197056A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Bromodomain targeting degronimers for target protein degradation |
| US20180072711A1 (en) | 2016-09-15 | 2018-03-15 | Arvinas, Inc. | Indole derivatives as estrogen receptor degraders |
| TWI752098B (zh) | 2016-10-10 | 2022-01-11 | 美商亞雷生物製藥股份有限公司 | 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| CN110506039A (zh) | 2016-10-11 | 2019-11-26 | 阿尔维纳斯股份有限公司 | 用于雄激素受体靶向降解的化合物和方法 |
| MX2019005007A (es) | 2016-11-01 | 2019-07-18 | Arvinas Inc | Protac dirigidos a la proteína tau y métodos asociados de uso. |
| BR112019011200B1 (pt) | 2016-12-01 | 2021-12-28 | Arvinas Operations, Inc | Derivados de tetrahidronaftaleno e tetrahidroisoquinolina como degradadores do receptor de estrogênio |
| US10806737B2 (en) | 2016-12-23 | 2020-10-20 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of fetal liver kinase polypeptides |
| 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 |
| KR20250117470A (ko) | 2016-12-23 | 2025-08-04 | 아비나스 오퍼레이션스, 인코포레이티드 | 급속 진행성 섬유육종 폴리펩티드의 표적화 분해를 위한 화합물 및 방법 |
| US11191741B2 (en) | 2016-12-24 | 2021-12-07 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide |
| WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
| BR112019015312A2 (pt) | 2017-01-26 | 2020-03-10 | Arvinas Operations, Inc. | Moduladores da proteólise pelo receptor de estrogênio e métodos de uso associados |
| IL312367A (en) | 2017-01-31 | 2024-06-01 | Arvinas Operations Inc | Cereblon ligands and bifunctional compounds comprising the same |
| WO2018226542A1 (en) | 2017-06-09 | 2018-12-13 | Arvinas, Inc. | Modulators of proteolysis and associated methods of use |
| EP3658548A1 (en) | 2017-07-28 | 2020-06-03 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| TWI783057B (zh) | 2017-10-10 | 2022-11-11 | 美商絡速藥業公司 | 製備6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈的方法 |
| TWI876442B (zh) | 2017-10-10 | 2025-03-11 | 美商絡速藥業公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物 |
| EP3710443A1 (en) | 2017-11-17 | 2020-09-23 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of interleukin-1 receptor-associated kinase 4 polypeptides |
| LT3728271T (lt) | 2017-12-19 | 2022-12-12 | Turning Point Therapeutics, Inc. | Makrocikliniai junginiai, skirti ligų gydymui |
| US11472802B2 (en) | 2018-01-18 | 2022-10-18 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridine compounds as RET kinase inhibitors |
| JP7060694B2 (ja) | 2018-01-18 | 2022-04-26 | アレイ バイオファーマ インコーポレイテッド | Retキナーゼ阻害剤としての置換ピロロ[2,3-d]ピリミジン化合物 |
| EP3740490A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors |
| EP3773576A4 (en) | 2018-03-26 | 2021-12-29 | C4 Therapeutics, Inc. | Cereblon binders for the degradation of ikaros |
| US20190300521A1 (en) | 2018-04-01 | 2019-10-03 | Arvinas Operations, Inc. | Brm targeting compounds and associated methods of use |
| WO2019195609A2 (en) | 2018-04-04 | 2019-10-10 | Arvinas Operations, Inc. | Modulators of proteolysis and associated methods of use |
| IL302595A (en) | 2018-04-13 | 2023-07-01 | Arvinas Operations Inc | Servalon ligands and bifunctional compounds containing them |
| EP3781156A4 (en) | 2018-04-16 | 2022-05-18 | C4 Therapeutics, Inc. | SPIROCYCLIC COMPOUNDS |
| EP3578561A1 (en) | 2018-06-04 | 2019-12-11 | F. Hoffmann-La Roche AG | Spiro compounds |
| WO2020023851A1 (en) | 2018-07-26 | 2020-01-30 | Yale University | Bifunctional substitued pyrimidines as modulators of fak proteolyse |
| 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 |
| IL281188B2 (en) | 2018-09-07 | 2025-08-01 | Arvinas Operations Inc | Polycyclic compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides |
| CN112996794A (zh) | 2018-09-10 | 2021-06-18 | 阿雷生物药品公司 | 作为ret激酶抑制剂的稠合杂环化合物 |
| ES2995214T3 (en) | 2019-03-06 | 2025-02-07 | C4 Therapeutics Inc | Heterocyclic compounds for medical treatment |
| WO2020210630A1 (en) | 2019-04-12 | 2020-10-15 | C4 Therapeutics, Inc. | Tricyclic degraders of ikaros and aiolos |
| JP2023511471A (ja) | 2019-10-28 | 2023-03-20 | エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト | 二官能性化合物 |
| JP2023511472A (ja) | 2019-10-29 | 2023-03-20 | エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト | がんの治療のための二官能性化合物 |
| KR20220119415A (ko) | 2019-12-20 | 2022-08-29 | 씨4 테라퓨틱스, 인코포레이티드 | Egfr 분해를 위한 이소인돌리논 및 인다졸 화합물 |
-
2021
- 2021-08-05 IL IL300397A patent/IL300397A/en unknown
- 2021-08-05 CN CN202180068438.1A patent/CN116490186B/zh active Active
- 2021-08-05 JP JP2023507866A patent/JP2023538517A/ja active Pending
- 2021-08-05 EP EP21854440.1A patent/EP4192458A4/en active Pending
- 2021-08-05 WO PCT/US2021/044838 patent/WO2022032026A1/en not_active Ceased
- 2021-08-05 CA CA3188313A patent/CA3188313A1/en active Pending
-
2023
- 2023-02-03 US US18/105,735 patent/US20230233692A1/en active Pending
Patent Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2018532690A (ja) * | 2015-07-16 | 2018-11-08 | アレイ バイオファーマ、インコーポレイテッド | RETキナーゼ阻害物質としての置換ピラゾロ[1,5−a]ピリジン化合物 |
| JP2020506902A (ja) * | 2017-01-18 | 2020-03-05 | アレイ バイオファーマ、インコーポレイテッド | RETキナーゼ阻害剤としての置換ピラゾロ[1,5−a]ピラジン化合物 |
| WO2018237026A1 (en) * | 2017-06-20 | 2018-12-27 | C4 Therapeutics, Inc. | N / O-LINKED DEGRONS AND DEGRONIMERS FOR DEGRADATION OF PROTEINS |
| WO2019099868A2 (en) * | 2017-11-16 | 2019-05-23 | C4 Therapeutics, Inc. | Degraders and degrons for targeted protein degradation |
| WO2020051235A1 (en) * | 2018-09-04 | 2020-03-12 | C4 Therapeutics, Inc. | Compounds for the degradation of brd9 or mth1 |
| WO2020114487A1 (en) * | 2018-12-07 | 2020-06-11 | Sunshine Lake Pharma Co., Ltd. | Ret inhibitors, pharmaceutical compositions and uses thereof |
| WO2020132561A1 (en) * | 2018-12-20 | 2020-06-25 | C4 Therapeutics, Inc. | Targeted protein degradation |
Non-Patent Citations (2)
| Title |
|---|
| 大岡 伸通 他: "新しい低分子薬の創薬モダリティPROTAC", ファルマシア, vol. 第56巻, 第1号, JPN6023042753, 1 January 2020 (2020-01-01), pages 41 - 45, ISSN: 0005749029 * |
| 天児 由佳: "PROTACs−ユビキチンリガーゼをハイジャックしてタンパク質を分解するキメラ分子−", 有機合成化学協会誌, vol. 第76巻, 第4号, JPN6024006694, 1 April 2018 (2018-04-01), pages 358 - 359, ISSN: 0005749030 * |
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| US20230233692A1 (en) | 2023-07-27 |
| EP4192458A4 (en) | 2024-09-04 |
| CN116490186B (zh) | 2025-10-31 |
| CA3188313A1 (en) | 2022-02-10 |
| CN116490186A (zh) | 2023-07-25 |
| EP4192458A1 (en) | 2023-06-14 |
| WO2022032026A1 (en) | 2022-02-10 |
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