AU2018338314B2 - Protein degraders and uses thereof - Google Patents
Protein degraders and uses thereof Download PDFInfo
- Publication number
- AU2018338314B2 AU2018338314B2 AU2018338314A AU2018338314A AU2018338314B2 AU 2018338314 B2 AU2018338314 B2 AU 2018338314B2 AU 2018338314 A AU2018338314 A AU 2018338314A AU 2018338314 A AU2018338314 A AU 2018338314A AU 2018338314 B2 AU2018338314 B2 AU 2018338314B2
- Authority
- AU
- Australia
- Prior art keywords
- agent
- nitrogen
- treatment
- ring
- sulfur
- 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
Links
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/08—Solutions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
- A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
- A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
- A61K9/1075—Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- 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
-
- 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
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D495/14—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Dispersion Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Molecular Biology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Dermatology (AREA)
- Biophysics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Peptides Or Proteins (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU2025201796A AU2025201796A1 (en) | 2017-09-22 | 2025-03-12 | Protein degraders and uses thereof |
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762562206P | 2017-09-22 | 2017-09-22 | |
| US62/562,206 | 2017-09-22 | ||
| US201762610403P | 2017-12-26 | 2017-12-26 | |
| US62/610,403 | 2017-12-26 | ||
| US201862714527P | 2018-08-03 | 2018-08-03 | |
| US62/714,527 | 2018-08-03 | ||
| PCT/US2018/052242 WO2019060742A1 (en) | 2017-09-22 | 2018-09-21 | AGENTS FOR DEGRADING PROTEINS AND USES THEREOF |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2025201796A Division AU2025201796A1 (en) | 2017-09-22 | 2025-03-12 | Protein degraders and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2018338314A1 AU2018338314A1 (en) | 2020-04-09 |
| AU2018338314B2 true AU2018338314B2 (en) | 2024-12-12 |
Family
ID=65810510
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2018338314A Active AU2018338314B2 (en) | 2017-09-22 | 2018-09-21 | Protein degraders and uses thereof |
| AU2025201796A Abandoned AU2025201796A1 (en) | 2017-09-22 | 2025-03-12 | Protein degraders and uses thereof |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2025201796A Abandoned AU2025201796A1 (en) | 2017-09-22 | 2025-03-12 | Protein degraders and uses thereof |
Country Status (8)
| Country | Link |
|---|---|
| US (3) | US11623932B2 (https=) |
| EP (2) | EP4624467A3 (https=) |
| JP (3) | JP7366031B2 (https=) |
| AU (2) | AU2018338314B2 (https=) |
| CA (2) | CA3283159A1 (https=) |
| IL (4) | IL273432B (https=) |
| MX (3) | MX2020003190A (https=) |
| WO (1) | WO2019060742A1 (https=) |
Families Citing this family (106)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102674902B1 (ko) | 2016-12-01 | 2024-06-14 | 아비나스 오퍼레이션스, 인코포레이티드 | 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 및 테트라히드로이소퀴놀린 유도체 |
| AU2018211975B2 (en) | 2017-01-26 | 2022-05-26 | Arvinas Operations, Inc. | Modulators of estrogen receptor proteolysis and associated methods of use |
| EP4717317A2 (en) | 2017-06-20 | 2026-04-01 | C4 Therapeutics, Inc. | N/o-linked degrons and degronimers for protein degradation |
| WO2019060693A1 (en) | 2017-09-22 | 2019-03-28 | Kymera Therapeutics, Inc. | CRBN LIGANDS AND USES THEREOF |
| EP3710002A4 (en) | 2017-11-16 | 2021-07-07 | C4 Therapeutics, Inc. | DEGRADER AND DEGRONE FOR TARGETED PROTEIN DEGRADATION |
| LT3728207T (lt) | 2017-12-21 | 2023-05-25 | Ribon Therapeutics Inc. | Chinazolinonai kaip parp14 inhibitoriai |
| IL315310A (en) | 2017-12-26 | 2024-10-01 | Kymera Therapeutics Inc | Irak degraders and uses thereof |
| WO2019140380A1 (en) | 2018-01-12 | 2019-07-18 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| WO2019140387A1 (en) | 2018-01-12 | 2019-07-18 | Kymera Therapeutics, Inc. | Crbn ligands and uses thereof |
| 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 |
| US12539292B2 (en) | 2018-04-01 | 2026-02-03 | Arvinas Operations, Inc. | BRM targeting compounds and associated methods of use |
| KR20210006356A (ko) | 2018-04-04 | 2021-01-18 | 아비나스 오퍼레이션스, 인코포레이티드 | 단백질분해 조절제 및 연관된 사용 방법 |
| CN119751456A (zh) | 2018-04-16 | 2025-04-04 | C4医药公司 | 螺环化合物 |
| US11292792B2 (en) | 2018-07-06 | 2022-04-05 | Kymera Therapeutics, Inc. | Tricyclic CRBN ligands and uses thereof |
| WO2020010227A1 (en) | 2018-07-06 | 2020-01-09 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| WO2020027225A1 (ja) | 2018-07-31 | 2020-02-06 | ファイメクス株式会社 | 複素環化合物 |
| JP7640458B2 (ja) | 2018-10-05 | 2025-03-05 | アンナプルナ バイオ インコーポレイテッド | Ａｐｊ受容体活性に関連する状態を処置するための化合物および組成物 |
| JP7623943B2 (ja) | 2018-11-30 | 2025-01-29 | カイメラ セラピューティクス， インコーポレイテッド | Ｉｒａｋ分解剤およびそれらの使用 |
| CN120698983A (zh) | 2018-12-20 | 2025-09-26 | C4医药公司 | 靶向蛋白降解 |
| TWI875749B (zh) | 2019-04-05 | 2025-03-11 | 美商凱麥拉醫療公司 | Stat降解劑及其用途 |
| CN120172958A (zh) | 2019-04-12 | 2025-06-20 | C4医药公司 | Ikaros和aiolos的三环降解物 |
| CN110058014B (zh) * | 2019-04-25 | 2021-06-04 | 中国科学院化学研究所 | 用于筛选lrpprc调控剂的产品及鉴定lrpprc调控剂的方法 |
| JP7289510B2 (ja) * | 2019-05-08 | 2023-06-12 | 国立大学法人高知大学 | 認知症治療薬のスクリーニング方法 |
| US12528808B2 (en) | 2019-05-20 | 2026-01-20 | University Of Pittsburgh Of The Commonwealth System Of Higher Education | Therapy for erythropoietic protoporphyria (EPP) and X-linked protoporphyria (XLP) |
| WO2020251972A1 (en) | 2019-06-10 | 2020-12-17 | Kymera Therapeutics, Inc. | Smarca degraders and uses thereof |
| AU2020295399B2 (en) * | 2019-06-18 | 2025-10-16 | Dana-Farber Cancer Institute, Inc. | Small molecule target bromo/acetyl proteins and uses thereof |
| BR112021026517A2 (pt) | 2019-06-28 | 2022-05-10 | Kymera Therapeutics Inc | Degradadores de irak e usos dos mesmos |
| CN119954801A (zh) | 2019-07-17 | 2025-05-09 | 阿尔维纳斯运营股份有限公司 | Tau蛋白靶向化合物及相关使用方法 |
| WO2021011868A1 (en) | 2019-07-17 | 2021-01-21 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| IL320609A (en) | 2019-08-26 | 2025-07-01 | Arvinas Operations Inc | Methods for treating breast cancer with a history of tetrahydronaphthalene as estrogen receptor-disrupting agents |
| WO2021041942A1 (en) | 2019-08-28 | 2021-03-04 | University Of Kentucky Research Foundation | Collagen p4h1 inhibitor and its use |
| CN110596403B (zh) * | 2019-09-17 | 2022-12-16 | 中山大学附属第一医院 | 用于卵巢癌诊断的特异性蛋白标记物及制备方法 |
| CN115397821B (zh) | 2019-10-17 | 2024-09-03 | 阿尔维纳斯运营股份有限公司 | 含有与bcl6靶向部分连接的e3泛素连接酶结合部分的双官能分子 |
| CN110749733B (zh) * | 2019-12-06 | 2021-08-27 | 四川大学华西医院 | Tgif2ly自身抗体检测试剂在制备肺癌筛查试剂盒中的用途 |
| US12551564B2 (en) | 2019-12-10 | 2026-02-17 | Kymera Therapeutics, Inc. | IRAK degraders and uses thereof |
| WO2021127283A2 (en) | 2019-12-17 | 2021-06-24 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| JP2023507172A (ja) * | 2019-12-17 | 2023-02-21 | オリオニス バイオサイエンシズ，インコーポレイテッド | タンパク質分解の調節 |
| WO2021127190A1 (en) | 2019-12-17 | 2021-06-24 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| US20240383886A1 (en) * | 2019-12-20 | 2024-11-21 | Calico Life Sciences Llc | Protein Tyrosine Phosphatase Degraders and Methods of Use Thereof |
| BR112022011827A2 (pt) | 2019-12-20 | 2022-08-30 | C4 Therapeutics Inc | Composto, composição farmacêutica, uso de um composto, métodos para tratamento ou profilaxia de câncer e para tratar um paciente com um distúrbio mediado por receptor do fator de crescimento epidérmico, e, invenção |
| BR112022012410A2 (pt) | 2019-12-23 | 2022-08-30 | Kymera Therapeutics Inc | Degradadores smarca e usos dos mesmos |
| WO2021162493A1 (ko) * | 2020-02-14 | 2021-08-19 | 보로노이 주식회사 | 단백질 키나아제 분해 유도 화합물 및 이의 용도 |
| CN111214664B (zh) * | 2020-02-24 | 2022-02-11 | 大连医科大学 | USP2和HSP90抑制剂联合使用抑制ErbB2阳性乳腺癌生长的应用 |
| AU2021231898A1 (en) | 2020-03-05 | 2022-10-27 | C4 Therapeutics, Inc. | Compounds for targeted degradation of BRD9 |
| EP3878847A1 (en) * | 2020-03-13 | 2021-09-15 | Centre Régional de Lutte contre le Cancer - Centre François Baclesse | Bcl-2 family proteins modulating compounds for cancer treatment |
| IL296334A (en) * | 2020-03-17 | 2022-11-01 | Kymera Therapeutics Inc | Stat degraders and uses thereof |
| WO2021185291A1 (zh) * | 2020-03-17 | 2021-09-23 | 南京明德新药研发有限公司 | 蛋白降解调节剂与其使用方法 |
| US12528785B2 (en) | 2020-03-19 | 2026-01-20 | Kymera Therapeutics, Inc. | MDM2 degraders and uses thereof |
| KR20230004511A (ko) | 2020-03-21 | 2023-01-06 | 아비나스 오퍼레이션스, 인코포레이티드 | 인다졸계 화합물 및 관련된 사용 방법 |
| AU2021275146A1 (en) * | 2020-05-21 | 2022-09-29 | Dana-Farber Cancer Institute, Inc. | Piperidine-2,6-diones as small molecule degraders of Helios and methods of use |
| TW202210483A (zh) | 2020-06-03 | 2022-03-16 | 美商凱麥拉醫療公司 | Irak降解劑之結晶型 |
| WO2021255212A1 (en) | 2020-06-19 | 2021-12-23 | F. Hoffmann-La Roche Ag | Braf degraders |
| KR102654220B1 (ko) * | 2020-07-07 | 2024-04-04 | 한국식품연구원 | Cmip 억제제를 포함하는 지방간 질환의 예방 또는 치료용 약학적 조성물 |
| WO2022012623A1 (en) * | 2020-07-16 | 2022-01-20 | Beigene, Ltd. | Degradation of (egfr) by conjugation of egfr inhibitors with e3 ligase ligand and methods of use |
| JP7692128B2 (ja) * | 2020-07-17 | 2025-06-13 | 国立医薬品食品衛生研究所長 | 新規化合物及び医薬組成物 |
| JP2023545730A (ja) * | 2020-10-07 | 2023-10-31 | カイメラ セラピューティクス， インコーポレイテッド | Ｓｔａｔ分解剤およびそれらの使用 |
| CA3199652A1 (en) * | 2020-11-20 | 2022-05-27 | Matthew Netherton | Compounds and uses thereof |
| EP4259144A4 (en) | 2020-12-09 | 2025-08-20 | Kymera Therapeutics Inc | SMARCA DEGRADING AGENTS AND THEIR USES |
| PH12023500015A1 (en) | 2020-12-30 | 2024-03-11 | Kymera Therapeutics Inc | Irak degraders and uses thereof |
| CN112899351B (zh) * | 2021-02-03 | 2022-08-26 | 东华大学 | 一种双重荧光定量pcr检测pdx模型小鼠细胞浸润状态试剂盒 |
| WO2022174268A1 (en) | 2021-02-15 | 2022-08-18 | Kymera Therapeutics, Inc. | Irak4 degraders and uses thereof |
| CN116867494A (zh) | 2021-02-15 | 2023-10-10 | 凯麦拉医疗公司 | Irak4降解剂和其用途 |
| WO2022198112A1 (en) | 2021-03-19 | 2022-09-22 | Arvinas Operations, Inc. | Indazole based compounds and associated methods of use |
| WO2022216675A1 (en) * | 2021-04-06 | 2022-10-13 | Believe In A Cure, Inc. | [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)- amino]-acetic acid for use in increasing foxg1 expression |
| CN117279910A (zh) | 2021-04-16 | 2023-12-22 | 阿尔维纳斯运营股份有限公司 | Bcl6蛋白水解的调节剂和其相关使用方法 |
| AU2022271290A1 (en) | 2021-05-07 | 2023-11-23 | Kymera Therapeutics, Inc. | Cdk2 degraders and uses thereof |
| CN113186273B (zh) * | 2021-05-13 | 2023-02-21 | 中国人民解放军总医院第一医学中心 | 一种用于预测P2Y12受体拮抗剂抗血小板疗效的circRNA检测试剂盒及其应用 |
| WO2022261250A1 (en) | 2021-06-08 | 2022-12-15 | C4 Therapeutics, Inc. | Therapeutics for the degradation of mutant braf |
| AU2022292649A1 (en) * | 2021-06-16 | 2024-01-04 | Biotheryx, Inc. | Sos1 protein degraders, pharmaceutical compositions thereof, and their therapeutic applications |
| WO2022271727A1 (en) * | 2021-06-21 | 2022-12-29 | Calico Life Sciences Llc | Degrader compounds and uses thereof |
| US20250129047A1 (en) | 2021-07-04 | 2025-04-24 | Newave Pharmaceutical Inc. | Isoquinoline derivatives as mutant egfr modulators and uses thereof |
| CN113637750A (zh) * | 2021-07-16 | 2021-11-12 | 宁波市第一医院 | 急性髓系白血病的辅助诊断、预后诊断或危险度分层标记物及其应用 |
| CN113817818B (zh) * | 2021-10-22 | 2023-04-28 | 常州市第二人民医院 | 用于诊断过敏性气道炎症的工具 |
| CN113817833B (zh) * | 2021-10-26 | 2022-09-30 | 常州国药医学检验实验室有限公司 | 一种基于荧光定量pcr技术的检测宫颈细胞基因甲基化的试剂盒与应用 |
| US12187744B2 (en) | 2021-10-29 | 2025-01-07 | Kymera Therapeutics, Inc. | IRAK4 degraders and synthesis thereof |
| JP2024545125A (ja) * | 2021-12-11 | 2024-12-05 | カイメラ セラピューティクス， インコーポレイテッド | Ｓｔａｔ３分解剤およびその使用 |
| KR20230091052A (ko) * | 2021-12-14 | 2023-06-22 | (주)프레이저테라퓨틱스 | 폴리유비퀴틴화에 의한 표적 단백질 또는 폴리펩티드의 분해용 신규 화합물 |
| EP4472967A4 (en) | 2022-01-31 | 2026-04-15 | Kymera Therapeutics Inc | Iraqi Degradation Agents and Their Uses |
| CN114656509B (zh) * | 2022-04-08 | 2024-05-24 | 国科温州研究院(温州生物材料与工程研究所) | 一种氮杂环卡宾-金钯合金纳米粒子及其制备方法和应用 |
| US20250333733A1 (en) * | 2022-05-19 | 2025-10-30 | University Of Puerto Rico | Novel targets against ovarian cancer |
| KR20250020448A (ko) | 2022-06-02 | 2025-02-11 | 시젱 하이스코 파마수티칼 씨오., 엘티디. | Bcl6을 억제하거나 분해하는 화합물 및 의약학에서의 응용 |
| JP2025523393A (ja) | 2022-06-06 | 2025-07-23 | シーフォー セラピューティクス， インコーポレイテッド | 二環式置換グルタルイミドセレブロンバインダー |
| WO2023250058A1 (en) * | 2022-06-22 | 2023-12-28 | Kymera Therapeutics, Inc. | Stat degraders and uses thereof |
| WO2024006776A1 (en) | 2022-06-27 | 2024-01-04 | Relay Therapeutics, Inc. | Estrogen receptor alpha degraders and medical use thereof |
| TW202417425A (zh) | 2022-06-27 | 2024-05-01 | 美商傳達治療有限公司 | 雌激素受體α降解劑及其使用方法 |
| CA3265344A1 (en) * | 2022-08-19 | 2024-02-22 | University Of Louisiana Monroe | METHOD FOR THE DIAGNOSTIC AND TREATMENT OF PROSTATE CANCER USING ZINC FINGER-PATTERNED PROTEIN TYPE 1 ANTIBODIES |
| US20260109715A1 (en) | 2022-10-03 | 2026-04-23 | Public University Corporation Yokohama City University | Imidazopyridine derivatives with bicyclic structure |
| CN115639306B (zh) * | 2022-12-26 | 2023-03-28 | 四川大学华西医院 | 一种快速检测临床样本中抗癫痫药物浓度的方法 |
| WO2024157953A1 (ja) | 2023-01-24 | 2024-08-02 | 第一三共株式会社 | 置換ベンゼン化合物 |
| CN121419983A (zh) | 2023-01-26 | 2026-01-27 | 阿尔维纳斯运营股份有限公司 | 基于小脑蛋白的kras降解protac及其相关用途 |
| WO2024173718A2 (en) * | 2023-02-16 | 2024-08-22 | St. Jude Children's Research Hospital | Heterobifunctional binders of klhdc2 |
| CN116813608B (zh) * | 2023-06-08 | 2024-03-22 | 英矽智能科技(上海)有限公司 | 噻唑类化合物及其应用 |
| WO2025006753A2 (en) | 2023-06-30 | 2025-01-02 | Merck Patent Gmbh | Heterobifunctional compounds for the degradation of kras protein |
| WO2025006783A2 (en) | 2023-06-30 | 2025-01-02 | Merck Patent Gmbh | Heterobifunctional compounds for the degradation of kras |
| CN117205322A (zh) * | 2023-09-08 | 2023-12-12 | 河南大学 | Fer1l6基因在糖尿病防治中的应用 |
| WO2025063888A1 (en) | 2023-09-19 | 2025-03-27 | Kancure Pte. Ltd. | Survivin-targeted compounds |
| AU2024352092A1 (en) | 2023-09-28 | 2026-04-09 | Arvinas Operations, Inc. | Benzimidazole and benzimidazolone based protac compounds for the targeted degradation of leucine rich repeat kinase 2 (lrrk2) |
| CN121925410A (zh) | 2023-09-29 | 2026-04-24 | 第一三共株式会社 | 3-苯基丙胺衍生物 |
| US12599672B2 (en) * | 2023-10-03 | 2026-04-14 | PAQ Therapeutics Inc. | KRAS proteolysis targeting chimeras |
| WO2025096984A1 (en) * | 2023-11-02 | 2025-05-08 | The Regents Of The University Of California | Gtpase inhibitors and uses thereof |
| CN117756818B (zh) * | 2023-12-12 | 2025-04-29 | 北京医院 | 一种戊二酰亚胺类化合物及其制备方法和应用 |
| WO2025194014A1 (en) | 2024-03-15 | 2025-09-18 | Dem Biopharma, Inc. | Hetero aryl modulators of apmap and uses thereof |
| US12565492B2 (en) | 2024-08-09 | 2026-03-03 | Triana Biomedicines, Inc. | Anaplastic Lymphoma Kinase (ALK) degraders and uses thereof |
| CN118702679B (zh) * | 2024-08-26 | 2024-10-29 | 四川大学华西医院 | 一种具有ezh2/brd4双靶点活性的化合物、药物组合物及其制备方法和用途 |
| CN120330336A (zh) * | 2025-03-19 | 2025-07-18 | 中南大学湘雅医院 | 一种用于宫颈癌和/或宫颈癌前病变检测的甲基化标志物组合及其应用、产品、检测装置、计算机可读存储介质、电子终端和计算机程序 |
| CN120794955A (zh) * | 2025-07-07 | 2025-10-17 | 四川伊诺唯新生物医药有限公司 | 一种irak4靶向蛋白降解剂关键中间体的制备方法 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016197032A1 (en) * | 2015-06-04 | 2016-12-08 | Arvinas, Inc. | Imide-based modulators of proteolysis and associated methods of use |
Family Cites Families (194)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5650270A (en) | 1982-02-01 | 1997-07-22 | Northeastern University | Molecular analytical release tags and their use in chemical analysis |
| US5516931A (en) | 1982-02-01 | 1996-05-14 | Northeastern University | Release tag compounds producing ketone signal groups |
| US4650750A (en) | 1982-02-01 | 1987-03-17 | Giese Roger W | Method of chemical analysis employing molecular release tag compounds |
| US4709016A (en) | 1982-02-01 | 1987-11-24 | Northeastern University | Molecular analytical release tags and their use in chemical analysis |
| US5360811A (en) | 1990-03-13 | 1994-11-01 | Hoechst-Roussel Pharmaceuticals Incorporated | 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols and related compounds as anti-inflammatory agents |
| JP3545461B2 (ja) | 1993-09-10 | 2004-07-21 | エーザイ株式会社 | 二環式ヘテロ環含有スルホンアミド誘導体 |
| US6281230B1 (en) | 1996-07-24 | 2001-08-28 | Celgene Corporation | Isoindolines, method of use, and pharmaceutical compositions |
| US6306663B1 (en) | 1999-02-12 | 2001-10-23 | Proteinex, Inc. | Controlling protein levels in eucaryotic organisms |
| EP1382339B1 (en) | 1999-12-10 | 2007-12-05 | Pfizer Products Inc. | Compositions containing pyrrolo ¬2,3-d pyrimidine derivatives |
| DE10002509A1 (de) | 2000-01-21 | 2001-07-26 | Gruenenthal Gmbh | Substituierte Glutarimide |
| ES2243461T3 (es) | 2000-02-28 | 2005-12-01 | Sugen, Inc. | Compuestos de 3-(pirolillactona) -2-indolinona como inhibidores quinasa. |
| PE20020354A1 (es) | 2000-09-01 | 2002-06-12 | Novartis Ag | Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda) |
| US7208157B2 (en) | 2000-09-08 | 2007-04-24 | California Institute Of Technology | Proteolysis targeting chimeric pharmaceutical |
| US7041298B2 (en) | 2000-09-08 | 2006-05-09 | California Institute Of Technology | Proteolysis targeting chimeric pharmaceutical |
| EP1389617B1 (en) | 2001-04-27 | 2007-01-03 | Zenyaku Kogyo Kabushiki Kaisha | Heterocyclic compound and antitumor agent containing the same as active ingredient |
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| WO2004019973A1 (en) | 2002-08-14 | 2004-03-11 | Atugen Ag | Use of protein kinase n beta |
| KR20070087266A (ko) | 2003-04-03 | 2007-08-28 | 세마포르 파머슈티컬즈, 아이엔씨. | 피아이-3 키나아제 억제제 프로드러그 |
| CN1832939B (zh) | 2003-05-30 | 2010-04-28 | 杰明X医药品加拿大公司 | 用于治疗癌症或病毒病的三杂环化合物、组合物和方法 |
| US7173015B2 (en) | 2003-07-03 | 2007-02-06 | The Trustees Of The University Of Pennsylvania | Inhibition of Syk kinase expression |
| JP4398263B2 (ja) | 2004-01-13 | 2010-01-13 | 富士通株式会社 | 経路設計方法 |
| SI2612862T1 (sl) | 2004-05-13 | 2017-04-26 | Icos Corporation | Kinazolini kot inhibitorji humane fosfatidilinozitol 3-kinaze delta |
| TWI309240B (en) | 2004-09-17 | 2009-05-01 | Hoffmann La Roche | Anti-ox40l antibodies |
| DE602006010979D1 (de) | 2005-01-19 | 2010-01-21 | Rigel Pharmaceuticals Inc | Prodrugs aus 2,4-pyrimidindiamin-verbindungen und ihre verwendungen |
| AU2006230099B2 (en) | 2005-03-25 | 2012-04-19 | Gitr, Inc. | GITR binding molecules and uses therefor |
| EP1888550B1 (en) | 2005-05-12 | 2014-06-25 | AbbVie Bahamas Ltd. | Apoptosis promoters |
| GB0510390D0 (en) | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
| CN104356236B (zh) | 2005-07-01 | 2020-07-03 | E.R.施贵宝&圣斯有限责任公司 | 抗程序性死亡配体1(pd-l1)的人单克隆抗体 |
| US7402325B2 (en) | 2005-07-28 | 2008-07-22 | Phoenix Biotechnology, Inc. | Supercritical carbon dioxide extract of pharmacologically active components from Nerium oleander |
| BRPI0617162B8 (pt) | 2005-10-07 | 2021-05-25 | Exelixis Inc | compostos inibidores de fosfatidilinositol 3-quinase composições farmacêuticas que os contem e métodos de uso dos mesmos |
| CN103626742B (zh) | 2005-11-01 | 2017-04-26 | 塔格根公司 | 激酶的联-芳基间-嘧啶抑制剂 |
| EP2455382B1 (en) | 2005-12-13 | 2016-10-26 | Incyte Holdings Corporation | Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors |
| UA96283C2 (uk) | 2005-12-23 | 2011-10-25 | Зіланд Фарма А/С | Модифіковані міметики лізину |
| JO2660B1 (en) | 2006-01-20 | 2012-06-17 | نوفارتيس ايه جي | Pi-3 inhibitors and methods of use |
| MX2008013578A (es) | 2006-04-26 | 2009-03-23 | Hoffmann La Roche | Derivados de tieno [3,2-d]pirimidina utiles como inhibidores de fosfatidilinositol 3-cinasa(p13k). |
| BRPI0622054B8 (pt) | 2006-09-22 | 2021-05-25 | Oxford Amherst Llc | composto e composição farmacêutica |
| US20100279316A1 (en) | 2007-01-19 | 2010-11-04 | Leonid Gorelik | Antibodies to Phosphorylated IRAK4 |
| HRP20151386T1 (hr) | 2007-03-12 | 2016-02-26 | Ym Biosciences Australia Pty Ltd | Fenil aminopirimidinski spojevi i njihova primjena |
| WO2008118802A1 (en) | 2007-03-23 | 2008-10-02 | Regents Of The University Of Minnesota | Therapeutic compounds |
| EP1987839A1 (en) | 2007-04-30 | 2008-11-05 | I.N.S.E.R.M. Institut National de la Sante et de la Recherche Medicale | Cytotoxic anti-LAG-3 monoclonal antibody and its use in the treatment or prevention of organ transplant rejection and autoimmune disease |
| PE20090717A1 (es) | 2007-05-18 | 2009-07-18 | Smithkline Beecham Corp | Derivados de quinolina como inhibidores de la pi3 quinasa |
| ES2776406T3 (es) | 2007-07-12 | 2020-07-30 | Gitr Inc | Terapias de combinación que emplean moléculas de enlazamiento a GITR |
| EP2044949A1 (en) | 2007-10-05 | 2009-04-08 | Immutep | Use of recombinant lag-3 or the derivatives thereof for eliciting monocyte immune response |
| EP2217716A4 (en) | 2007-11-09 | 2011-02-09 | Salk Inst For Biological Studi | USE OF TAM RECEPTOR INHIBITORS AS ANTIMICROBIAL AGENTS |
| 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 |
| US8158616B2 (en) | 2008-03-11 | 2012-04-17 | Incyte Corporation | Azetidine and cyclobutane derivatives as JAK inhibitors |
| JP2011518841A (ja) | 2008-04-24 | 2011-06-30 | ニューリンク ジェネティクス， インコーポレイテッド | Ｉｄｏ阻害剤 |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| AR072999A1 (es) | 2008-08-11 | 2010-10-06 | Medarex Inc | Anticuerpos humanos que se unen al gen 3 de activacion linfocitaria (lag-3) y los usos de estos |
| AU2009333580B2 (en) | 2008-12-09 | 2016-07-07 | Genentech, Inc. | Anti-PD-L1 antibodies and their use to enhance T-cell function |
| US8921037B2 (en) | 2008-12-16 | 2014-12-30 | Bo Han | PF4-depleted platelet rich plasma preparations and methods for hard and soft tissue repair |
| EP2473531A4 (en) | 2009-09-03 | 2013-05-01 | Merck Sharp & Dohme | Anti-gitr antibodies |
| JP2012254939A (ja) | 2009-10-07 | 2012-12-27 | Astellas Pharma Inc | オキサゾール化合物 |
| US8722720B2 (en) | 2009-10-28 | 2014-05-13 | Newlink Genetics Corporation | Imidazole derivatives as IDO inhibitors |
| PH12012500881A1 (en) | 2009-12-10 | 2017-07-26 | Hoffmann La Roche | Antibodies binding preferentially human csf1r extracellular domain 4 and their use |
| JP5998060B2 (ja) | 2010-03-04 | 2016-09-28 | マクロジェニクス，インコーポレーテッド | Ｂ７−ｈ３と反応性のある抗体、その免疫学的に活性なフラグメントおよびその使用 |
| CN102918061B (zh) | 2010-03-05 | 2016-06-08 | 霍夫曼-拉罗奇有限公司 | 针对人csf-1r的抗体及其用途 |
| CA2789076C (en) | 2010-03-05 | 2017-11-21 | F. Hoffmann-La Roche Ag | Antibodies against human colony stimulating factor-1 receptor and uses thereof |
| US8114621B2 (en) | 2010-03-12 | 2012-02-14 | Saladax Biomedical Inc. | Lenalidomide and thalidomide immunoassays |
| MX378336B (es) | 2010-05-04 | 2025-03-10 | Five Prime Therapeutics Inc | Anticuerpos que se unen a factor estimulante de colonias 1 (csf1r). |
| SG186389A1 (en) | 2010-06-30 | 2013-01-30 | Univ Brandeis | Small-molecule-targeted protein degradation |
| JP5985473B2 (ja) | 2010-07-13 | 2016-09-06 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | ＩＲＡＫ４モジュレーターとしてのピラゾロ［１，５ａ］ピリミジン及びチエノ［３，２ｂ］ピリミジン誘導体 |
| PT2614082T (pt) | 2010-09-09 | 2018-12-03 | Pfizer | Moléculas de ligação a 4-1bb |
| KR20180099933A (ko) | 2010-11-19 | 2018-09-05 | 리간드 파마슈티칼스 인코포레이티드 | 복소환 아민 및 이의 용도 |
| AU2011338615B2 (en) | 2010-12-07 | 2017-07-27 | Yale University | Small-molecule hydrophobic tagging of fusion proteins and induced degradation of same |
| PH12013501201A1 (en) | 2010-12-09 | 2013-07-29 | Univ Pennsylvania | Use of chimeric antigen receptor-modified t cells to treat cancer |
| BR112013015460B1 (pt) | 2010-12-20 | 2022-01-25 | Merck Serono S.A. | Derivados de indazolil triazol, kit, e composição farmacêutica |
| US8703941B2 (en) | 2011-01-10 | 2014-04-22 | Nimbus Iris, Inc. | IRAK inhibitors and uses thereof |
| WO2012129258A1 (en) | 2011-03-22 | 2012-09-27 | Merck Sharp & Dohme Corp. | Amidopyrazole inhibitors of interleukin receptor-associated kinases |
| NO2694640T3 (https=) | 2011-04-15 | 2018-03-17 | ||
| KR101970025B1 (ko) | 2011-04-20 | 2019-04-17 | 메디뮨 엘엘씨 | Ｂ7-ｈ1 및 ｐｄ-1과 결합하는 항체 및 다른 분자들 |
| WO2013042137A1 (en) | 2011-09-19 | 2013-03-28 | Aurigene Discovery Technologies Limited | Bicyclic heterocycles as irak4 inhibitors |
| WO2013066729A1 (en) | 2011-10-31 | 2013-05-10 | Merck Sharp & Dohme Corp. | Aminopyrimidinones as interleukin receptor-associated kinase inhibitors |
| HRP20201595T1 (hr) | 2011-11-28 | 2020-12-11 | Merck Patent Gmbh | Anti-pd-l1 protutijela i njihova uporaba |
| BR112014012624A2 (pt) | 2011-12-15 | 2018-10-09 | F Hoffmann-La Roche Ag | anticorpos, composição farmacêutica, ácido nucleico, vetores de expressão, célula hospedeira, método para a produção de um anticorpo recombinante e uso do anticorpo |
| CN104582705A (zh) | 2012-01-10 | 2015-04-29 | 林伯士艾瑞斯公司 | 白介素-1受体相关激酶(irak)抑制剂和其用途 |
| WO2013106646A2 (en) | 2012-01-12 | 2013-07-18 | Yale University | Compounds and methods for the inhibition of vcb e3 ubiquitin ligase |
| CA2861066C (en) | 2012-01-12 | 2024-01-02 | Yale University | Compounds and methods for the enhanced degradation of targeted proteins and other polypeptides by an e3 ubiquitin ligase |
| CN104254533B (zh) | 2012-01-13 | 2017-09-08 | 百时美施贵宝公司 | 用作激酶抑制剂的噻唑或噻二唑取代的吡啶基化合物 |
| WO2013106614A1 (en) | 2012-01-13 | 2013-07-18 | Bristol-Myers Squibb Company | Triazolyl-substituted pyridyl compounds useful as kinase inhibitors |
| EP2802576B1 (en) | 2012-01-13 | 2018-06-27 | Bristol-Myers Squibb Company | Heterocyclic-substituted pyridyl compounds useful as kinase inhibitors |
| RU2014136332A (ru) | 2012-02-06 | 2016-03-27 | Дженентек, Инк. | Композиции и способы применения ингибиторов csf1r |
| AR090263A1 (es) | 2012-03-08 | 2014-10-29 | Hoffmann La Roche | Terapia combinada de anticuerpos contra el csf-1r humano y las utilizaciones de la misma |
| EP2847220A1 (en) | 2012-05-11 | 2015-03-18 | Five Prime Therapeutics, Inc. | Methods of treating conditions with antibodies that bind colony stimulating factor 1 receptor (csf1r) |
| AR091649A1 (es) | 2012-07-02 | 2015-02-18 | Bristol Myers Squibb Co | Optimizacion de anticuerpos que se fijan al gen de activacion de linfocitos 3 (lag-3) y sus usos |
| SG11201500005SA (en) | 2012-07-10 | 2015-01-29 | Ares Trading Sa | Pyrimidine pyrazolyl derivatives |
| US20140018361A1 (en) | 2012-07-11 | 2014-01-16 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| WO2014011906A2 (en) | 2012-07-11 | 2014-01-16 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| HK1210696A1 (en) | 2012-07-11 | 2016-05-06 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| CN107759690A (zh) | 2012-08-31 | 2018-03-06 | 戊瑞治疗有限公司 | 用结合群落刺激因子1受体(csf1r)的抗体治疗病状的方法 |
| US9422331B2 (en) | 2012-09-19 | 2016-08-23 | Hoffmann-La Roche Inc. | 2-oxo-2,3,4,5-tetrahydro-1 H-benzo[B]diazepines and their use in the treatment of cancer |
| WO2014058691A1 (en) | 2012-10-08 | 2014-04-17 | Merck Sharp & Dohme Corp. | Inhibitors of irak4 activity |
| WO2014058685A1 (en) | 2012-10-08 | 2014-04-17 | Merck Sharp & Dohme Corp. | Inhibitors of irak4 activity |
| US9758522B2 (en) | 2012-10-19 | 2017-09-12 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged small molecules as inducers of protein degradation |
| KR20150079963A (ko) | 2012-11-08 | 2015-07-08 | 브리스톨-마이어스 스큅 컴퍼니 | 키나제 조절제로서 유용한 헤테로아릴 치환된 피리딜 화합물 |
| GB201311910D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel Compounds |
| EP2953944B1 (en) | 2013-02-07 | 2017-04-26 | Merck Patent GmbH | Pyridazinone-amides derivatives |
| LT2953952T (lt) | 2013-02-07 | 2017-08-25 | Merck Patent Gmbh | Makrocikliniai piridazinono dariniai |
| EP2970334B1 (en) | 2013-03-15 | 2018-05-23 | Biogen MA Inc. | Macrocyclic compounds as irak4 inhibitors for the treatment of inflammatory diseases |
| BR112016006319A2 (pt) | 2013-09-27 | 2017-08-01 | Nimbus Iris Inc | inibidores de irak e usos dos mesmos |
| CN105899505B (zh) | 2013-11-08 | 2018-08-28 | 武田药品工业株式会社 | 用于治疗自身免疫病症的吡唑 |
| JP6680683B2 (ja) | 2013-11-18 | 2020-04-15 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | テトラヒドロ−ベンゾジアゼピノン類 |
| JP6496731B2 (ja) | 2013-11-27 | 2019-04-03 | シグナルケム・ライフサイエンシーズ・コーポレイションＳｉｇｎａｌｃｈｅｍ Ｌｉｆｅｓｃｉｅｎｃｅｓ Ｃｏｒｐｏｒａｔｉｏｎ | Ｔａｍファミリーキナーゼ阻害剤としてのアミノピリジン誘導体 |
| TWI667233B (zh) | 2013-12-19 | 2019-08-01 | 德商拜耳製藥公司 | 新穎吲唑羧醯胺，其製備方法、含彼等之醫藥製劑及其製造醫藥之用途 |
| TW201609693A (zh) | 2014-01-03 | 2016-03-16 | 必治妥美雅史谷比公司 | 雜芳基取代之菸鹼醯胺化合物 |
| SG11201605408RA (en) | 2014-01-10 | 2016-07-28 | Aurigene Discovery Tech Ltd | Indazole compounds as irak4 inhibitors |
| FI3805233T3 (fi) | 2014-01-13 | 2024-04-17 | Aurigene Oncology Ltd | N-(5-(3-hydroksipyrrolidin-1-yyli)-2-morfolinooksatsolo[4,5-b]pyridin-6-yyli)-2-(2-metylipyridin-4-yyli)okatsoli-karboksamidin (r)- (s)-enantiomeerit irak4-estäjänä syövän hoitoon |
| RU2016137674A (ru) | 2014-03-17 | 2018-04-18 | Ф. Хоффманн-Ля Рош Аг | Производные пиперидиндиона |
| MA39838B1 (fr) | 2014-04-04 | 2019-05-31 | Pfizer | Composés bicycliques hétéroaryle ou aryle fusionnés et leur utilisation en tant qu'inhibiteurs irak4 |
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| AU2015247817C1 (en) | 2014-04-14 | 2022-02-10 | Arvinas Operations, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| US20160058872A1 (en) * | 2014-04-14 | 2016-03-03 | Arvinas, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| JP2017513954A (ja) | 2014-04-22 | 2017-06-01 | ニンバス アイリス， インコーポレイテッド | Ｉｒａｋ阻害剤およびその使用 |
| JP2017518348A (ja) | 2014-06-20 | 2017-07-06 | オーリジーン ディスカバリー テクノロジーズ リミテッドＡｕｒｉｇｅｎｅ Ｄｉｓｃｏｖｅｒｙ Ｔｅｃｈｎｏｌｏｇｉｅｓ Ｌｉｍｉｔｅｄ | Ｉｒａｋ４阻害剤としての置換インダゾール化合物 |
| WO2015200795A1 (en) | 2014-06-27 | 2015-12-30 | Celgene Corporation | Compositions and methods for inducing conformational changes in cereblon other e3 ubiquitin ligases |
| US10246456B2 (en) | 2014-07-18 | 2019-04-02 | Biogen Ma Inc. | IRAK4 inhibiting agents |
| US20160022642A1 (en) | 2014-07-25 | 2016-01-28 | Yale University | Compounds Useful for Promoting Protein Degradation and Methods Using Same |
| US10071164B2 (en) | 2014-08-11 | 2018-09-11 | Yale University | Estrogen-related receptor alpha based protac compounds and associated methods of use |
| EP3200790B1 (en) | 2014-09-30 | 2020-08-26 | Merck Sharp & Dohme Corp. | Inhibitors of irak4 activity |
| US9969749B2 (en) | 2014-09-30 | 2018-05-15 | Merck Sharp & Dohme Corp. | Inhibitors of IRAK4 activity |
| US9926330B2 (en) | 2014-09-30 | 2018-03-27 | Merck Sharp & Dohme Corp. | Inhibitors of IRAK4 activity |
| US9932350B2 (en) | 2014-09-30 | 2018-04-03 | Merck Sharp & Dohme Corp. | Inhibitors of IRAK4 activity |
| CA2964982C (en) | 2014-11-20 | 2022-07-05 | Merck Patent Gmbh | Heteroaryl compounds as irak inhibitors and uses thereof |
| US9694084B2 (en) | 2014-12-23 | 2017-07-04 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| JP6815318B2 (ja) * | 2014-12-23 | 2021-01-20 | ダナ−ファーバー キャンサー インスティテュート，インコーポレイテッド | 二官能性分子によって標的化タンパク質分解を誘導する方法 |
| US12312316B2 (en) | 2015-01-20 | 2025-05-27 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| 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 |
| WO2016144848A1 (en) | 2015-03-12 | 2016-09-15 | Merck Sharp & Dohme Corp. | Pyrrolotriazine inhibitors of irak4 activity |
| EP3268003B1 (en) | 2015-03-12 | 2020-07-29 | Merck Sharp & Dohme Corp. | Thienopyrazine inhibitors of irak4 activity |
| US10040798B2 (en) | 2015-03-12 | 2018-08-07 | Merck Sharp & Dohme Corp. | Pyrrolopyridazine inhibitors of IRAK4 activity |
| EP3267996B1 (en) | 2015-03-12 | 2020-11-11 | Merck Sharp & Dohme Corp. | Pyrazolopyrimidine inhibitors of irak4 activity |
| US10155765B2 (en) | 2015-03-12 | 2018-12-18 | Merck Sharp & Dohme Corp. | Carboxamide inhibitors of IRAK4 activity |
| US10730870B2 (en) | 2015-03-18 | 2020-08-04 | Arvinas Operations, Inc. | Compounds and methods for the enhanced degradation of targeted proteins |
| EA039043B1 (ru) | 2015-04-22 | 2021-11-25 | Райджел Фармасьютикалз, Инк. | Пиразольные соединения и способ получения и применения данных соединений |
| GB201506871D0 (en) | 2015-04-22 | 2015-06-03 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| UY36660A (es) | 2015-04-30 | 2016-11-30 | Bayer Pharma AG | Combinaciones de inhibidores de irak4 |
| WO2016197114A1 (en) | 2015-06-05 | 2016-12-08 | Arvinas, Inc. | Tank-binding kinase-1 protacs and associated methods of use |
| TW201718571A (zh) | 2015-06-24 | 2017-06-01 | 必治妥美雅史谷比公司 | 經雜芳基取代之胺基吡啶化合物 |
| CN105085620B (zh) | 2015-06-25 | 2018-05-08 | 中山大学附属第一医院 | 一种靶向泛素化降解Smad3的化合物 |
| WO2017004134A1 (en) | 2015-06-29 | 2017-01-05 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| WO2017004133A1 (en) | 2015-06-29 | 2017-01-05 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| WO2017007612A1 (en) | 2015-07-07 | 2017-01-12 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| WO2017011371A1 (en) | 2015-07-10 | 2017-01-19 | Arvinas, Inc | Mdm2-based modulators of proteolysis and associated methods of use |
| CA2988436A1 (en) | 2015-07-13 | 2017-01-19 | Arvinas, Inc. | Alanine-based modulators of proteolysis and associated methods of use |
| BR112018000624A2 (pt) | 2015-07-15 | 2018-09-18 | Aurigene Discovery Technologies Limited | compostos de indazol e azaindazol como inibidores de irak-4 |
| JP2018524365A (ja) | 2015-07-15 | 2018-08-30 | アウリジーン ディスカバリー テクノロジーズ リミテッド | Ｉｒａｋ−４阻害剤としての置換アザ化合物 |
| EP3337476A4 (en) | 2015-08-19 | 2019-09-04 | Arvinas, Inc. | Compounds and methods for the targeted degradation of bromodomain-containing proteins |
| ES2865199T3 (es) | 2015-08-27 | 2021-10-15 | Pfizer | Compuestos de heteroarilo o arilo condensados bicíclicos como moduladores de IRAK4 |
| KR102650026B1 (ko) | 2015-09-18 | 2024-03-22 | 메르크 파텐트 게엠베하 | Irak 억제제로서의 헤테로아릴 화합물 및 이의 용도 |
| CN108290879B (zh) | 2015-09-18 | 2022-01-11 | 默克专利有限公司 | 用作irak抑制剂的杂芳基化合物及其用途 |
| WO2017059280A1 (en) | 2015-10-02 | 2017-04-06 | The University Of North Carolina At Chapel Hill | Novel pan-tam inhibitors and mer/axl dual inhibitors |
| AU2016349781A1 (en) | 2015-11-02 | 2018-05-10 | Yale University | Proteolysis targeting chimera compounds and methods of preparing and using same |
| EP3394066A2 (en) | 2015-12-22 | 2018-10-31 | H. Hoffnabb-La Roche Ag | PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS |
| US20200216454A1 (en) | 2015-12-30 | 2020-07-09 | Dana-Farber Cancer Institute, Inc. | Bifunctional molecules for her3 degradation and methods of use |
| US20190016703A1 (en) | 2015-12-30 | 2019-01-17 | Dana-Farber Cancer Institute, Inc. | Bifunctional compounds for her3 degradation and methods of use |
| WO2017127430A1 (en) | 2016-01-20 | 2017-07-27 | Biogen Ma Inc. | Irak4 inhibiting agents |
| US11395820B2 (en) | 2016-03-16 | 2022-07-26 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Small molecules against cereblon to enhance effector t cell function |
| US20170281784A1 (en) | 2016-04-05 | 2017-10-05 | Arvinas, Inc. | Protein-protein interaction inducing technology |
| AU2017246452C1 (en) | 2016-04-06 | 2021-06-03 | The Regents Of The University Of Michigan | MDM2 protein degraders |
| WO2017176958A1 (en) | 2016-04-06 | 2017-10-12 | The Regents Of The University Of Michigan | Monofunctional intermediates for ligand-dependent target protein degradation |
| JP2019515932A (ja) * | 2016-04-29 | 2019-06-13 | アスター バイオテック リミテッド ライアビリティ カンパニー | チロシンキナーゼｂｃｒ−ａｂｌ阻害剤としての新規複素環化合物 |
| 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 |
| EP3454862B1 (en) | 2016-05-10 | 2024-09-11 | C4 Therapeutics, Inc. | Spirocyclic degronimers for target protein degradation |
| WO2017197056A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Bromodomain targeting degronimers for target protein degradation |
| 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 |
| WO2017201069A1 (en) | 2016-05-18 | 2017-11-23 | Biotheryx, Inc. | Oxoindoline derivatives as protein function modulators |
| EP3458101B1 (en) | 2016-05-20 | 2020-12-30 | H. Hoffnabb-La Roche Ag | Protac antibody conjugates and methods of use |
| WO2017205762A1 (en) | 2016-05-27 | 2017-11-30 | Pharmacyclics Llc | Inhibitors of interleukin-1 receptor-associated kinase |
| WO2017205766A1 (en) | 2016-05-27 | 2017-11-30 | Pharmacyclics Llc | Inhibitors of interleukin-1 receptor-associated kinase |
| WO2017207385A1 (de) | 2016-05-31 | 2017-12-07 | Bayer Pharma Aktiengesellschaft | Substituierte 3-methylindazole, verfahren zu ihrer herstellung, pharmazeutische präparate, die diese enthalten, sowie deren verwendung zur herstellung von arzneimitteln |
| GB201610147D0 (en) | 2016-06-10 | 2016-07-27 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| JP7065840B2 (ja) | 2016-06-27 | 2022-05-12 | ライジェル ファーマシューティカルズ， インコーポレイテッド | ２，４－ジアミノ－ピリミジン化合物ならびに該化合物の作製法および使用法 |
| US10646488B2 (en) | 2016-07-13 | 2020-05-12 | Araxes Pharma Llc | Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof |
| JP2019196309A (ja) | 2016-09-15 | 2019-11-14 | 武田薬品工業株式会社 | 複素環化合物 |
| US10925868B2 (en) | 2016-11-10 | 2021-02-23 | Dana-Farber Cancer Institute, Inc. | Degradation of protein kinases by conjugation of protein kinase inhibitors with E3 ligase ligand and methods of use |
| CA3042731A1 (en) | 2016-11-22 | 2018-05-31 | Dana-Farber Cancer Institute, Inc. | Inhibitors of interleukin-1 receptor-associated kinases and uses thereof |
| BR112019015484A2 (pt) | 2017-01-31 | 2020-04-28 | Arvinas Operations Inc | ligantes de cereblon e compostos bifuncionais compreendendo os mesmos |
| TW202340194A (zh) | 2017-02-16 | 2023-10-16 | 美商基利科學股份有限公司 | 吡咯并[1,2-b]嗒𠯤衍生物 |
| PE20191817A1 (es) | 2017-05-11 | 2019-12-27 | Bristol Myers Squibb Co | Tienopiridinas y benzotiofenos utiles como inhibidores de cinasa 4 asociada al receptor de interleucina 1 (irak4) |
| EP4717317A2 (en) | 2017-06-20 | 2026-04-01 | C4 Therapeutics, Inc. | N/o-linked degrons and degronimers for protein degradation |
| CN118108706A (zh) | 2017-09-04 | 2024-05-31 | C4医药公司 | 戊二酰亚胺 |
| WO2019060693A1 (en) | 2017-09-22 | 2019-03-28 | Kymera Therapeutics, Inc. | CRBN LIGANDS AND USES THEREOF |
| WO2019084030A1 (en) | 2017-10-24 | 2019-05-02 | Genentech, Inc. | (4-HYDROXYPYRROLIDIN-2-YL) -HYDROXAMATE COMPOUNDS AND METHODS OF USE |
| EP3700901A1 (en) | 2017-10-24 | 2020-09-02 | Genentech, Inc. | (4-hydroxypyrrolidin-2-yl)-heterocyclic compounds and methods of use thereof |
| EP3710002A4 (en) | 2017-11-16 | 2021-07-07 | C4 Therapeutics, Inc. | DEGRADER AND DEGRONE FOR TARGETED PROTEIN DEGRADATION |
| US11065231B2 (en) | 2017-11-17 | 2021-07-20 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of interleukin-1 receptor- associated kinase 4 polypeptides |
| IL315310A (en) * | 2017-12-26 | 2024-10-01 | Kymera Therapeutics Inc | Irak degraders and uses thereof |
| WO2019140380A1 (en) | 2018-01-12 | 2019-07-18 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| WO2019140387A1 (en) | 2018-01-12 | 2019-07-18 | Kymera Therapeutics, Inc. | Crbn ligands and uses thereof |
| US11802132B2 (en) | 2018-02-23 | 2023-10-31 | Dana-Farber Cancer Institute, Inc. | Small molecules for inducing selective protein degradation and uses thereof |
| US20220356185A1 (en) | 2018-07-06 | 2022-11-10 | Kymera Therapeutics, Inc. | Mertk degraders and uses thereof |
| WO2020010227A1 (en) | 2018-07-06 | 2020-01-09 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| US11292792B2 (en) | 2018-07-06 | 2022-04-05 | Kymera Therapeutics, Inc. | Tricyclic CRBN ligands and uses thereof |
-
2018
- 2018-09-21 MX MX2020003190A patent/MX2020003190A/es unknown
- 2018-09-21 US US16/649,732 patent/US11623932B2/en active Active
- 2018-09-21 EP EP25195747.8A patent/EP4624467A3/en active Pending
- 2018-09-21 IL IL273432A patent/IL273432B/en unknown
- 2018-09-21 WO PCT/US2018/052242 patent/WO2019060742A1/en not_active Ceased
- 2018-09-21 EP EP18857581.5A patent/EP3684365A4/en active Pending
- 2018-09-21 CA CA3283159A patent/CA3283159A1/en active Pending
- 2018-09-21 AU AU2018338314A patent/AU2018338314B2/en active Active
- 2018-09-21 CA CA3076613A patent/CA3076613A1/en active Pending
- 2018-09-21 JP JP2020538753A patent/JP7366031B2/ja active Active
- 2018-09-21 IL IL322809A patent/IL322809A/en unknown
- 2018-09-21 IL IL307995A patent/IL307995A/en unknown
- 2018-09-21 IL IL295603A patent/IL295603B2/en unknown
-
2020
- 2020-03-20 MX MX2023015185A patent/MX2023015185A/es unknown
- 2020-03-20 MX MX2022013526A patent/MX2022013526A/es unknown
-
2022
- 2022-06-10 US US17/837,449 patent/US20230115184A1/en active Pending
-
2023
- 2023-10-10 JP JP2023175302A patent/JP7818560B2/ja active Active
-
2025
- 2025-03-12 AU AU2025201796A patent/AU2025201796A1/en not_active Abandoned
- 2025-08-19 US US19/304,052 patent/US20260085075A1/en active Pending
- 2025-08-20 JP JP2025136973A patent/JP2025170324A/ja active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016197032A1 (en) * | 2015-06-04 | 2016-12-08 | Arvinas, Inc. | Imide-based modulators of proteolysis and associated methods of use |
Also Published As
| Publication number | Publication date |
|---|---|
| EP3684365A1 (en) | 2020-07-29 |
| IL295603B1 (en) | 2023-11-01 |
| US20210238193A1 (en) | 2021-08-05 |
| US11623932B2 (en) | 2023-04-11 |
| IL322809A (en) | 2025-10-01 |
| JP2023175972A (ja) | 2023-12-12 |
| WO2019060742A1 (en) | 2019-03-28 |
| US20230115184A1 (en) | 2023-04-13 |
| EP4624467A2 (en) | 2025-10-01 |
| JP7366031B2 (ja) | 2023-10-20 |
| IL273432B (en) | 2022-09-01 |
| EP3684365A4 (en) | 2021-09-08 |
| CA3283159A1 (en) | 2026-03-02 |
| JP2025170324A (ja) | 2025-11-18 |
| IL295603B2 (en) | 2024-03-01 |
| AU2018338314A1 (en) | 2020-04-09 |
| AU2025201796A9 (en) | 2025-04-17 |
| US20260085075A1 (en) | 2026-03-26 |
| IL307995A (en) | 2023-12-01 |
| MX2022013526A (es) | 2022-11-16 |
| MX2023015185A (es) | 2024-01-23 |
| IL295603A (en) | 2022-10-01 |
| IL273432A (en) | 2020-05-31 |
| MX2020003190A (es) | 2020-11-11 |
| JP7818560B2 (ja) | 2026-02-20 |
| EP4624467A3 (en) | 2026-03-11 |
| AU2025201796A1 (en) | 2025-04-03 |
| CA3076613A1 (en) | 2019-03-28 |
| JP2020534375A (ja) | 2020-11-26 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US12006329B2 (en) | Protein degraders and uses thereof | |
| AU2018338314B2 (en) | Protein degraders and uses thereof | |
| US12540127B2 (en) | CRBN ligands and uses thereof | |
| US11932635B2 (en) | CRBN ligands and uses thereof | |
| US11897882B2 (en) | Tricyclic crbn ligands and uses thereof | |
| US12454520B2 (en) | Protein degraders and uses thereof | |
| US20230093080A1 (en) | Protein degraders and uses thereof | |
| WO2021011631A1 (en) | Fused-glutarimide crbn ligands and uses thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FGA | Letters patent sealed or granted (standard patent) |