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
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- agent
- nitrogen
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- sulfur
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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
-
- 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)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Dispersion Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Physiology (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nutrition Science (AREA)
- Dermatology (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) | EP3684365A4 (https=) |
| JP (3) | JP7366031B2 (https=) |
| AU (2) | AU2018338314B2 (https=) |
| CA (2) | CA3076613A1 (https=) |
| IL (4) | IL295603B2 (https=) |
| MX (3) | MX2020003190A (https=) |
| WO (1) | WO2019060742A1 (https=) |
Families Citing this family (106)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112019011200B1 (pt) | 2016-12-01 | 2021-12-28 | Arvinas Operations, Inc | Derivados de tetrahidronaftaleno e tetrahidroisoquinolina como degradadores do receptor de estrogênio |
| BR112019015312A2 (pt) | 2017-01-26 | 2020-03-10 | Arvinas Operations, Inc. | Moduladores da proteólise pelo receptor de estrogênio e métodos de uso associados |
| 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 |
| US11358948B2 (en) | 2017-09-22 | 2022-06-14 | Kymera Therapeutics, Inc. | CRBN ligands and uses thereof |
| CN111372585A (zh) | 2017-11-16 | 2020-07-03 | C4医药公司 | 用于靶蛋白降解的降解剂和降解决定子 |
| PT3728207T (pt) | 2017-12-21 | 2023-03-14 | Ribon Therapeutics Inc | Quinazolinonas como inibidores de parp14 |
| 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 |
| EP3773576A4 (en) | 2018-03-26 | 2021-12-29 | C4 Therapeutics, Inc. | Cereblon binders for the degradation of ikaros |
| US12539292B2 (en) | 2018-04-01 | 2026-02-03 | 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 |
| EP3781156A4 (en) | 2018-04-16 | 2022-05-18 | C4 Therapeutics, Inc. | SPIROCYCLIC COMPOUNDS |
| WO2020010227A1 (en) | 2018-07-06 | 2020-01-09 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| WO2020010177A1 (en) | 2018-07-06 | 2020-01-09 | Kymera Therapeutics, Inc. | Tricyclic crbn ligands 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 |
| MX2021003904A (es) | 2018-10-05 | 2021-10-26 | Annapurna Bio Inc | Compuestos y composiciones para el tratamiento de afecciones asociadas con la actividad del receptor apj. |
| CA3119773A1 (en) | 2018-11-30 | 2020-06-04 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| CN120698983A (zh) | 2018-12-20 | 2025-09-26 | C4医药公司 | 靶向蛋白降解 |
| CN120574283A (zh) * | 2019-04-05 | 2025-09-02 | 凯麦拉医疗公司 | Stat降解剂和其用途 |
| WO2020210630A1 (en) | 2019-04-12 | 2020-10-15 | C4 Therapeutics, Inc. | Tricyclic degraders of ikaros and aiolos |
| 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 |
| CA3135592A1 (en) | 2019-05-20 | 2020-11-26 | Xiaochao Ma | Therapeutic agents 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 |
| WO2020257278A2 (en) * | 2019-06-18 | 2020-12-24 | Dana-Farber Cancer Institute, Inc. | Small molecule target bromo/acetyl proteins and uses thereof |
| PH12022500002A1 (en) | 2019-06-28 | 2023-04-03 | Kymera Therapeutics Inc | Irak degraders and uses thereof |
| WO2021011868A1 (en) | 2019-07-17 | 2021-01-21 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| EP3999182A1 (en) | 2019-07-17 | 2022-05-25 | Arvinas Operations, Inc. | Tau-protein targeting compounds and associated methods of use |
| KR20220054347A (ko) | 2019-08-26 | 2022-05-02 | 아비나스 오퍼레이션스, 인코포레이티드 | 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 유도체로 유방암을 치료하는 방법 |
| 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 |
| CA3154386A1 (en) | 2019-10-17 | 2021-04-22 | Michael Berlin | Bifunctional molecules containing an e3 ubiquitine ligase binding moiety linked to a bcl6 targeting moiety |
| 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 |
| WO2021119159A1 (en) | 2019-12-10 | 2021-06-17 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| KR20220145325A (ko) | 2019-12-17 | 2022-10-28 | 카이메라 쎄라퓨틱스 인코포레이티드 | Irak 분해제 및 이의 용도 |
| 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 |
| EP4076524A4 (en) | 2019-12-17 | 2023-11-29 | Kymera Therapeutics, Inc. | IRAQ DEGRADERS AND USES THEREOF |
| EP4077319A1 (en) * | 2019-12-20 | 2022-10-26 | Calico Life Sciences LLC | Protein tyrosine phosphatase degraders and methods of use thereof |
| KR20220119415A (ko) | 2019-12-20 | 2022-08-29 | 씨4 테라퓨틱스, 인코포레이티드 | Egfr 분해를 위한 이소인돌리논 및 인다졸 화합물 |
| EP4081308A4 (en) | 2019-12-23 | 2024-01-24 | Kymera Therapeutics, Inc. | Smarca degraders and uses thereof |
| 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 |
| 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 |
| 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 |
| EP4122925A4 (en) * | 2020-03-17 | 2024-04-17 | Medshine Discovery Inc. | Proteolysis regulator and method for using same |
| CA3170503A1 (en) * | 2020-03-17 | 2021-09-23 | Nan JI | Stat degraders and uses thereof |
| KR20230005160A (ko) | 2020-03-19 | 2023-01-09 | 카이메라 쎄라퓨틱스 인코포레이티드 | Mdm2 분해제 및 이의 용도 |
| JP7644139B2 (ja) | 2020-03-21 | 2025-03-11 | アルヴィナス・オペレーションズ・インコーポレイテッド | インダゾール系化合物及び関連使用方法 |
| CA3172589A1 (en) * | 2020-05-21 | 2021-11-25 | 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 |
| JP2023530030A (ja) | 2020-06-19 | 2023-07-12 | シーフォー セラピューティクス, インコーポレイテッド | Braf分解剤 |
| KR102654220B1 (ko) * | 2020-07-07 | 2024-04-04 | 한국식품연구원 | Cmip 억제제를 포함하는 지방간 질환의 예방 또는 치료용 약학적 조성물 |
| US20230248834A1 (en) * | 2020-07-16 | 2023-08-10 | 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 |
| IL301830A (en) * | 2020-10-07 | 2023-06-01 | Kymera Therapeutics Inc | Stat degraders and uses thereof |
| JP7723743B2 (ja) * | 2020-11-20 | 2025-08-14 | フォグホーン セラピューティクス インコーポレイテッド | 化合物及びその使用 |
| EP4259144A4 (en) | 2020-12-09 | 2025-08-20 | Kymera Therapeutics Inc | SMARCA DEGRADING AGENTS AND THEIR USES |
| CN116867758A (zh) | 2020-12-30 | 2023-10-10 | 凯麦拉医疗公司 | Irak降解剂和其用途 |
| 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 |
| CN116867494A (zh) | 2021-02-15 | 2023-10-10 | 凯麦拉医疗公司 | Irak4降解剂和其用途 |
| US12171768B2 (en) | 2021-02-15 | 2024-12-24 | Kymera Therapeutics, Inc. | IRAK4 degraders and uses thereof |
| JP2024512501A (ja) | 2021-03-19 | 2024-03-19 | アルヴィナス・オペレーションズ・インコーポレイテッド | インダゾール系化合物及び関連使用方法 |
| 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 |
| KR20230171979A (ko) | 2021-04-16 | 2023-12-21 | 아비나스 오퍼레이션스, 인코포레이티드 | Bcl6 단백질 분해의 조절제 및 관련 사용 방법 |
| KR20240020735A (ko) | 2021-05-07 | 2024-02-15 | 카이메라 쎄라퓨틱스 인코포레이티드 | Cdk2 분해제 및 그 용도 |
| 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 |
| MX2023014059A (es) | 2021-06-08 | 2024-03-12 | C4 Therapeutics Inc | Terapeuticos para la degradacion de una proteina quiinasa de serina/ treonina mutante. |
| WO2022266248A1 (en) * | 2021-06-16 | 2022-12-22 | Biotheryx, Inc. | Sos1 protein degraders, pharmaceutical compositions thereof, and their therapeutic applications |
| EP4359409A1 (en) * | 2021-06-21 | 2024-05-01 | Calico Life Sciences LLC | Degrader compounds and uses thereof |
| WO2023283130A1 (en) | 2021-07-04 | 2023-01-12 | 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 |
| CA3236265A1 (en) | 2021-10-29 | 2023-05-04 | William Leong | Irak4 degraders and synthesis thereof |
| CA3239730A1 (en) * | 2021-12-11 | 2023-06-15 | Christopher De Savi | Stat3 degraders and uses thereof |
| JP2025503429A (ja) * | 2021-12-14 | 2025-02-04 | プレーザー セラピューティクス インコーポレイティド | ポリユビキチン化による標的タンパク質またはポリペプチドの分解用の新規化合物 |
| CA3243560A1 (en) | 2022-01-31 | 2023-08-03 | 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 |
| AU2023278399A1 (en) | 2022-06-02 | 2024-12-19 | Xizang Haisco Pharmaceutical Co., Ltd. | Compound for inhibiting or degrading bcl6 and use thereof in pharmaceutics |
| CA3249074A1 (en) | 2022-06-06 | 2023-12-14 | C4 Therapeutics, Inc. | BICYCLIC SUBSTITUTION GLUTARIMIDE CEREBLON BINDERS |
| WO2023250058A1 (en) * | 2022-06-22 | 2023-12-28 | Kymera Therapeutics, Inc. | Stat degraders and uses thereof |
| JP2025521686A (ja) | 2022-06-27 | 2025-07-10 | リレー セラピューティクス, インコーポレイテッド | エストロゲン受容体アルファ分解剤及びその使用 |
| WO2024006776A1 (en) | 2022-06-27 | 2024-01-04 | Relay Therapeutics, Inc. | Estrogen receptor alpha degraders and medical use thereof |
| JP2025527601A (ja) * | 2022-08-19 | 2025-08-22 | ユニバーシティ オブ ルイジアナ モンロー | ジンクフィンガータンパク質様1抗体を使用して前立腺がんを診断および処置する方法 |
| CN119998290A (zh) | 2022-10-03 | 2025-05-13 | 公立大学法人横滨市立大学 | 具有二环性结构的咪唑并吡啶衍生物 |
| 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 |
| CN120569372A (zh) | 2023-01-24 | 2025-08-29 | 第一三共株式会社 | 经取代的苯化合物 |
| US12448399B2 (en) | 2023-01-26 | 2025-10-21 | Arvinas Operations, Inc. | Cereblon-based KRAS degrading PROTACs and uses related thereto |
| 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 |
| 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 |
| 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 |
| TW202515874A (zh) | 2023-09-28 | 2025-04-16 | 美商亞文納營運公司 | 用於靶向降解富含白胺酸之重複激酶2(lrrk2)的基於苯并咪唑及苯并咪唑酮之protac化合物 |
| TW202530189A (zh) | 2023-09-29 | 2025-08-01 | 日商第一三共股份有限公司 | 3-苯基丙基胺衍生物 |
| CN121941690A (zh) * | 2023-10-03 | 2026-04-28 | Paq医疗公司 | Kras蛋白水解靶向嵌合体 |
| 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 |
| CN119842908B (zh) * | 2025-03-19 | 2025-06-24 | 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 |
| US4650750A (en) | 1982-02-01 | 1987-03-17 | Giese Roger W | Method of chemical analysis employing molecular release tag compounds |
| US5516931A (en) | 1982-02-01 | 1996-05-14 | Northeastern University | Release tag compounds producing ketone signal groups |
| 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 |
| DE60037345T2 (de) | 1999-12-10 | 2008-11-13 | Pfizer Products Inc., Groton | Pyrrolo(2,3-d)pyrimidin-Verbindungen |
| DE10002509A1 (de) | 2000-01-21 | 2001-07-26 | Gruenenthal Gmbh | Substituierte Glutarimide |
| EP1259514B9 (en) | 2000-02-28 | 2005-11-09 | Sugen, Inc. | 3-(pyrolyllactone)-2-indolinone compounds as kinase inhibitors |
| PE20020354A1 (es) | 2000-09-01 | 2002-06-12 | Novartis Ag | Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda) |
| WO2002020740A2 (en) | 2000-09-08 | 2002-03-14 | California Institute Of Technology | Proteolysis targeting chimeric pharmaceutical |
| US7208157B2 (en) | 2000-09-08 | 2007-04-24 | California Institute Of Technology | Proteolysis targeting chimeric pharmaceutical |
| DE60217322T2 (de) | 2001-04-27 | 2007-10-04 | Zenyaku Kogyo K.K. | Heterocyclische verbindung und antitumormittel, das diese als wirkstoff enthält |
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| PT1536827E (pt) | 2002-08-14 | 2009-03-20 | Silence Therapeutics Ag | Utilização de proteína cinase n beta |
| AU2004228668B2 (en) | 2003-04-03 | 2011-10-27 | Park Funding, Llc | PI-3 kinase inhibitor prodrugs |
| ES2382377T3 (es) | 2003-05-30 | 2012-06-07 | Gemin X Pharmaceuticals Canada Inc. | Compuestos triheterocíclicos, composiciones, y métodos para tratar cáncer |
| EP1692153A4 (en) | 2003-07-03 | 2007-03-21 | Univ Pennsylvania | INHIBITION OF EXPRESSION OF SYK-KINASE |
| JP4398263B2 (ja) | 2004-01-13 | 2010-01-13 | 富士通株式会社 | 経路設計方法 |
| WO2005113556A1 (en) | 2004-05-13 | 2005-12-01 | Icos Corporation | Quinazolinones as inhibitors of human phosphatidylinositol 3-kinase delta |
| TWI380996B (zh) | 2004-09-17 | 2013-01-01 | Hoffmann La Roche | 抗ox40l抗體 |
| AU2006206458B2 (en) | 2005-01-19 | 2012-10-25 | Rigel Pharmaceuticals, Inc. | Prodrugs of 2,4-pyrimidinediamine compounds and their uses |
| PT2343320T (pt) | 2005-03-25 | 2018-01-23 | Gitr Inc | Anticorpos anti-gitr e as suas utilizações |
| PL1888550T3 (pl) | 2005-05-12 | 2014-12-31 | Abbvie Bahamas Ltd | Promotory apoptozy |
| GB0510390D0 (en) | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
| PT1907424E (pt) | 2005-07-01 | 2015-10-09 | Squibb & Sons Llc | Anticorpos monoclonais humanos para o ligando 1 de morte programada (pd-l1) |
| US7402325B2 (en) | 2005-07-28 | 2008-07-22 | Phoenix Biotechnology, Inc. | Supercritical carbon dioxide extract of pharmacologically active components from Nerium oleander |
| US7989622B2 (en) | 2005-10-07 | 2011-08-02 | Exelixis, Inc. | Phosphatidylinositol 3-kinase inhibitors and methods of their use |
| JP5191391B2 (ja) | 2005-11-01 | 2013-05-08 | ターゲジェン インコーポレーティッド | キナーゼのビ−アリールメタ−ピリミジン阻害剤 |
| SG10202003901UA (en) | 2005-12-13 | 2020-05-28 | Incyte Holdings Corp | 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 |
| WO2007129161A2 (en) | 2006-04-26 | 2007-11-15 | F. Hoffmann-La Roche Ag | Thieno [3, 2-d] pyrimidine derivative useful as pi3k inhibitor |
| DK2526933T3 (en) | 2006-09-22 | 2015-05-18 | Pharmacyclics Inc | Inhibitors of Bruton's tyrosine kinase |
| US20100279316A1 (en) | 2007-01-19 | 2010-11-04 | Leonid Gorelik | Antibodies to Phosphorylated IRAK4 |
| KR101566840B1 (ko) | 2007-03-12 | 2015-11-06 | 와이엠 바이오사이언시즈 오스트레일리아 피티와이 엘티디 | 페닐 아미노 피리미딘 화합물 및 이의 용도 |
| 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 |
| US8591886B2 (en) | 2007-07-12 | 2013-11-26 | Gitr, Inc. | Combination therapies employing GITR binding molecules |
| EP2044949A1 (en) | 2007-10-05 | 2009-04-08 | Immutep | Use of recombinant lag-3 or the derivatives thereof for eliciting monocyte immune response |
| EP2219671A4 (en) | 2007-11-09 | 2011-02-09 | Salk Inst For Biological Studi | USE OF TAM RECEPTOR INHIBITORS AS IMMU ENHANCERS AND TAM ACTIVATORS AS IMMUNOSUPPRESSORS |
| US10047066B2 (en) | 2007-11-30 | 2018-08-14 | Newlink Genetics Corporation | IDO inhibitors |
| HUE029767T2 (en) | 2008-03-11 | 2017-04-28 | Incyte Holdings Corp | JAK inhibitor azetidine and cyclobutane derivatives |
| CA2722159C (en) | 2008-04-24 | 2016-04-05 | Newlink Genetics Corporation | Substituted phenylimidazole compounds and their use as ido inhibitors |
| 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 |
| EP3255060A1 (en) | 2008-12-09 | 2017-12-13 | F. Hoffmann-La Roche AG | 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 |
| KR101790802B1 (ko) | 2009-09-03 | 2017-10-27 | 머크 샤프 앤드 돔 코포레이션 | 항-gitr 항체 |
| JP2012254939A (ja) | 2009-10-07 | 2012-12-27 | Astellas Pharma Inc | オキサゾール化合物 |
| EP2493862B1 (en) | 2009-10-28 | 2016-10-05 | Newlink Genetics Corporation | Imidazole derivatives as ido inhibitors |
| ES2722300T3 (es) | 2009-12-10 | 2019-08-09 | Hoffmann La Roche | Anticuerpos que se unen preferentemente al dominio extracelular 4 de CSF1R y su uso |
| EP2542256B1 (en) | 2010-03-04 | 2019-05-22 | MacroGenics, Inc. | Antibodies reactive with b7-h3, immunologically active fragments thereof and uses thereof |
| US9169323B2 (en) | 2010-03-05 | 2015-10-27 | Hoffmann-La Roche Inc. | Antibodies against human CSF-1R |
| JP5989547B2 (ja) | 2010-03-05 | 2016-09-07 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | ヒトcsf−1rに対する抗体及びその使用 |
| US8114621B2 (en) | 2010-03-12 | 2012-02-14 | Saladax Biomedical Inc. | Lenalidomide and thalidomide immunoassays |
| HRP20190047T1 (hr) | 2010-05-04 | 2019-02-22 | Five Prime Therapeutics, Inc. | Protutijela koja se vežu na csf1r |
| CN103153335A (zh) | 2010-06-30 | 2013-06-12 | 布兰代斯大学 | 小分子靶定的蛋白质降解 |
| CN110003219A (zh) | 2010-07-13 | 2019-07-12 | 弗·哈夫曼-拉罗切有限公司 | 作为irak4调节剂的吡唑并[1,5a]嘧啶和噻吩并[3,2b]嘧啶衍生物 |
| MX337040B (es) | 2010-09-09 | 2016-02-09 | Pfizer | Moleculas de union a 4-1bb. |
| RU2632900C2 (ru) | 2010-11-19 | 2017-10-11 | Лиганд Фармасьютикалс Инкорпорейтед | Гетероциклические амины и их применение |
| CA2823837A1 (en) | 2010-12-07 | 2012-06-14 | 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 |
| WO2012097013A1 (en) | 2011-01-10 | 2012-07-19 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| US9169260B2 (en) | 2011-03-22 | 2015-10-27 | Merck Sharp & Dohme Corp. | Amidopyrazole inhibitors of interleukin receptor-associated kinases |
| NO2694640T3 (https=) | 2011-04-15 | 2018-03-17 | ||
| JP6072771B2 (ja) | 2011-04-20 | 2017-02-01 | メディミューン,エルエルシー | B7−h1およびpd−1に結合する抗体およびその他の分子 |
| WO2013042137A1 (en) | 2011-09-19 | 2013-03-28 | Aurigene Discovery Technologies Limited | Bicyclic heterocycles as irak4 inhibitors |
| US9221809B2 (en) | 2011-10-31 | 2015-12-29 | Merck Sharp & Dohme Corp. | Aminopyrimidinones as interleukin receptor-associated kinase inhibitors |
| KR101764096B1 (ko) | 2011-11-28 | 2017-08-02 | 메르크 파텐트 게엠베하 | 항-pd-l1 항체 및 그의 용도 |
| RU2658603C2 (ru) | 2011-12-15 | 2018-06-21 | Ф.Хоффманн-Ля Рош Аг | Антитела против человеческого csf-1r и их применения |
| JP6126131B2 (ja) | 2012-01-10 | 2017-05-10 | 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 |
| WO2013106646A2 (en) | 2012-01-12 | 2013-07-18 | Yale University | Compounds and methods for the inhibition of vcb e3 ubiquitin ligase |
| KR102668696B1 (ko) | 2012-01-12 | 2024-05-29 | 예일 유니버시티 | E3 유비퀴틴 리가아제에 의한 표적 단백질 및 다른 폴리펩티드의 증진된 분해를 위한 화합물 및 방법 |
| CN104169275B (zh) | 2012-01-13 | 2017-06-09 | 百时美施贵宝公司 | 用作激酶抑制剂的三唑取代的吡啶化合物 |
| EP2802576B1 (en) | 2012-01-13 | 2018-06-27 | Bristol-Myers Squibb Company | Heterocyclic-substituted pyridyl compounds useful as kinase inhibitors |
| ES2575604T3 (es) | 2012-01-13 | 2016-06-29 | Bristol-Myers Squibb Company | Compuestos de piridilo sustituidos con tiazolilo o tiadiazolilo útiles como inhibidores cinasa |
| KR20140127855A (ko) | 2012-02-06 | 2014-11-04 | 제넨테크, 인크. | Csf1r 억제제를 사용하는 조성물 및 방법 |
| 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 |
| RU2670743C9 (ru) | 2012-05-11 | 2018-12-19 | Файв Прайм Терапьютикс, Инк. | Способы лечения состояний антителами, которые связывают рецептор колониестимулирующего фактора 1 (csf1r) |
| UY34887A (es) | 2012-07-02 | 2013-12-31 | Bristol Myers Squibb Company Una Corporacion Del Estado De Delaware | Optimización de anticuerpos que se fijan al gen de activación de linfocitos 3 (lag-3) y sus usos |
| JP6189434B2 (ja) | 2012-07-10 | 2017-08-30 | アレス トレーディング ソシエテ アノニム | ピリミジンピラゾリル誘導体 |
| WO2014011906A2 (en) | 2012-07-11 | 2014-01-16 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| WO2014011902A1 (en) | 2012-07-11 | 2014-01-16 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| WO2014011911A2 (en) | 2012-07-11 | 2014-01-16 | 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 |
| WO2014044622A1 (en) | 2012-09-19 | 2014-03-27 | F. Hoffmann-La Roche Ag | 2-oxo-2,3,4,5-tetrahydro-1 h-benzo[b]diazepines and their use in the treatment of cancer |
| EP2903613B1 (en) | 2012-10-08 | 2017-11-22 | Merck Sharp & Dohme Corp. | Pyrazole derivatives useful as inhibitors of irak4 activity |
| WO2014058685A1 (en) | 2012-10-08 | 2014-04-17 | Merck Sharp & Dohme Corp. | Inhibitors of irak4 activity |
| USRE48175E1 (en) | 2012-10-19 | 2020-08-25 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged small molecules as inducers of protein degradation |
| BR112015009850A2 (pt) | 2012-11-08 | 2017-07-11 | Bristol Myers Squibb Co | compostos de piridila substituídos por heteroarila úteis como moduladores de quinase |
| GB201311910D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel Compounds |
| HUE032863T2 (en) | 2013-02-07 | 2017-11-28 | Merck Patent Gmbh | Piridazinonamid derivatives |
| HRP20171302T1 (hr) | 2013-02-07 | 2017-10-20 | Merck Patent Gmbh | Makrociklički derivati piridazinona |
| US9617282B2 (en) | 2013-03-15 | 2017-04-11 | Biogen Ma Inc. | Macrocyclic compounds as IRAK4 inhibitors for the treatment of inflammatory diseases |
| CN106232122A (zh) | 2013-09-27 | 2016-12-14 | 林伯士艾瑞斯公司 | Irak抑制剂和其用途 |
| WO2015068856A1 (en) | 2013-11-08 | 2015-05-14 | Takeda Pharmaceutical Company Limited | Pyrazole for the treatment autoimmune disorders |
| MX2016006432A (es) | 2013-11-18 | 2016-07-19 | Hoffmann La Roche | Tetrahidro-benzodiazepinonas. |
| US10233176B2 (en) | 2013-11-27 | 2019-03-19 | Signalchem Lifesciences Corporation | Aminopyridine derivatives as TAM family kinase inhibitors |
| 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 |
| UY35935A (es) | 2014-01-03 | 2015-06-30 | Bristol Myers Squibb Company Una Corporación Del Estado De Delaware | Compuestos de nicotinamida sustituida con heteroarilo como inhibidores de quinasa y moduladores de irak-4 |
| EP3092226B1 (en) | 2014-01-10 | 2019-03-13 | Aurigene Discovery Technologies Limited | Indazole compounds as irak4 inhibitors |
| LT3466955T (lt) | 2014-01-13 | 2021-02-25 | Aurigene Discovery Technologies Limited | Oksazol[4,5-b]piridino ir tiazol[4,5-b]piridino darinių, kaip irak4 inhibitorių, skirtų vėžio gydymui, gamybos būdas |
| MA39749A (fr) | 2014-03-17 | 2017-01-25 | Hoffmann La Roche | Dérivés de pipéridine-dione |
| DK3126330T3 (en) | 2014-04-04 | 2019-04-23 | Pfizer | BICYCLE-FUSED HETEROARYL OR ARYL COMPOUNDS AND USE THEREOF AS IRAC4 INHIBITORS |
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| RU2738833C9 (ru) | 2014-04-14 | 2022-02-28 | Арвинас, Оперэйшнз, Инк. | Имидные модуляторы протеолиза и способы их применения |
| US20160058872A1 (en) * | 2014-04-14 | 2016-03-03 | Arvinas, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| KR20160145803A (ko) | 2014-04-22 | 2016-12-20 | 님버스 아이리스 인코포레이티드 | Irak 억제제 및 이의 용도 |
| AU2015275730A1 (en) | 2014-06-20 | 2016-12-15 | Aurigene Discovery Technologies Limited | Substituted indazole compounds as IRAK4 inhibitors |
| EP3827836A1 (en) | 2014-06-27 | 2021-06-02 | Celgene Corporation | Compositions and methods for inducing conformational changes in cereblon and 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 |
| EP3200788B1 (en) | 2014-09-30 | 2019-09-18 | Merck Sharp & Dohme Corp. | Inhibitors of irak4 activity |
| US9932350B2 (en) | 2014-09-30 | 2018-04-03 | Merck Sharp & Dohme Corp. | Inhibitors of IRAK4 activity |
| US9969749B2 (en) | 2014-09-30 | 2018-05-15 | Merck Sharp & Dohme Corp. | Inhibitors of IRAK4 activity |
| EP3200790B1 (en) | 2014-09-30 | 2020-08-26 | Merck Sharp & Dohme Corp. | Inhibitors of irak4 activity |
| JP6787892B2 (ja) | 2014-11-20 | 2020-11-18 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングMerck Patent Gesellschaft mit beschraenkter Haftung | Irakインヒビターとしてのヘテロアリール化合物及びその使用 |
| 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 |
| 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 |
| WO2016144847A1 (en) | 2015-03-12 | 2016-09-15 | Merck Sharp & Dohme Corp. | Pyrrolopyridazine inhibitors of irak4 activity |
| WO2016144848A1 (en) | 2015-03-12 | 2016-09-15 | Merck Sharp & Dohme Corp. | Pyrrolotriazine inhibitors of irak4 activity |
| US10329294B2 (en) | 2015-03-12 | 2019-06-25 | Merck Sharp & Dohme Corp. | Pyrazolopyrimidine inhibitors of IRAK4 activity |
| WO2016144849A1 (en) | 2015-03-12 | 2016-09-15 | Merck Sharp & Dohme Corp. | Thienopyrazine inhibitors of irak4 activity |
| US10155765B2 (en) | 2015-03-12 | 2018-12-18 | Merck Sharp & Dohme Corp. | Carboxamide inhibitors of IRAK4 activity |
| EP3270917A4 (en) | 2015-03-18 | 2018-08-08 | Arvinas, Inc. | Compounds and methods for the enhanced degradation of targeted proteins |
| LT3286181T (lt) | 2015-04-22 | 2021-04-26 | Rigel Pharmaceuticals, Inc. | Pirazolo junginiai ir junginių gamybos bei naudojimo būdas |
| GB201506871D0 (en) | 2015-04-22 | 2015-06-03 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| TW201701879A (zh) | 2015-04-30 | 2017-01-16 | 拜耳製藥公司 | Irak4抑制劑組合 |
| WO2016197114A1 (en) | 2015-06-05 | 2016-12-08 | Arvinas, Inc. | Tank-binding kinase-1 protacs and associated methods of use |
| EP3313840B1 (en) | 2015-06-24 | 2019-07-24 | Bristol-Myers Squibb Company | Heteroaryl substituted aminopyridine compounds |
| 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 |
| WO2017004133A1 (en) | 2015-06-29 | 2017-01-05 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| WO2017004134A1 (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 |
| 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. |
| CN108024971A (zh) | 2015-07-15 | 2018-05-11 | 奥列基因发现技术有限公司 | 作为irak-4抑制剂的取代的氮杂化合物 |
| JP2018524372A (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阻害剤としてのインダゾール及びアザインダゾール化合物 |
| US10772962B2 (en) | 2015-08-19 | 2020-09-15 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of bromodomain-containing proteins |
| HUE053705T2 (hu) | 2015-08-27 | 2021-07-28 | Pfizer | Biciklusos kondenzált heteroaril- vagy aril- vegyületek IRAK4 modulátorokként |
| CN108602776B (zh) | 2015-09-18 | 2021-12-03 | 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 |
| BR112018003812B1 (pt) | 2015-09-18 | 2024-04-30 | Merck Patent Gmbh | Compostos de heteroarila como inibidores de irak, seu uso, composição farmacêutica, e kit |
| 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 |
| BR112018008918A8 (pt) | 2015-11-02 | 2019-02-26 | Univ Yale | compostos de quimera proteólise dirigida e métodos para preparação e uso dos mesmos |
| CN108473498B (zh) | 2015-12-22 | 2021-11-02 | 豪夫迈·罗氏有限公司 | 作为IRAK4调节剂的吡唑并[1,5a]嘧啶衍生物 |
| WO2017117473A1 (en) | 2015-12-30 | 2017-07-06 | Dana-Farber Cancer Institute, Inc. | Bifunctional molescules for her3 degradation and methods of use |
| WO2017117474A1 (en) | 2015-12-30 | 2017-07-06 | Dana-Farber Cancer Institute, Inc. | Bifunctional compounds for her3 degradation and methods of use |
| US11427561B2 (en) | 2016-01-20 | 2022-08-30 | Biogen Ma Inc. | IRAK4 inhibiting agents |
| BR112018068906A2 (pt) | 2016-03-16 | 2019-01-22 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | composição, método, método de redução de risco, prevenção ou tratamento de um indivíduo que tem uma doença ou distúrbio autoimune, método de indução de degradação de uma proteína-alvo numa célula, método para reduzir o risco, prevenir ou tratar um estado da doença ou afecção num paciente em que a atividade proteica desregulada é responsável pelo referido estado da doença ou afecção, método para reduzir o risco, prevenir ou tratar câncer num indivíduo e método de tratamento de uma doença ou distúrbio genético num indivíduo |
| 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 |
| US10759808B2 (en) | 2016-04-06 | 2020-09-01 | The Regents Of The University Of Michigan | Monofunctional intermediates for ligand-dependent target protein degradation |
| CN109790144A (zh) * | 2016-04-29 | 2019-05-21 | 爱仕达生物技术有限责任公司 | 新型杂环化合物作为酪氨酸激酶bcr-abl抑制剂 |
| WO2017197056A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Bromodomain targeting 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 |
| ES2990061T3 (es) | 2016-05-10 | 2024-11-28 | C4 Therapeutics Inc | Degronímeros espirocíclicos para la degradación de proteínas diana |
| 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 |
| WO2017201069A1 (en) | 2016-05-18 | 2017-11-23 | Biotheryx, Inc. | Oxoindoline derivatives as protein function modulators |
| CN118436801A (zh) | 2016-05-20 | 2024-08-06 | 豪夫迈·罗氏有限公司 | Protac抗体缀合物及其使用方法 |
| WO2017205766A1 (en) | 2016-05-27 | 2017-11-30 | Pharmacyclics Llc | Inhibitors of interleukin-1 receptor-associated kinase |
| WO2017205762A1 (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 |
| EP3475263B1 (en) | 2016-06-27 | 2022-12-28 | Rigel Pharmaceuticals, Inc. | 2,4-diamino-pyrimidine compounds and their use as irak4 inhibitors |
| 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 |
| AU2017363313B2 (en) | 2016-11-22 | 2021-06-24 | Dana-Farber Cancer Institute, Inc. | Inhibitors of interleukin-1 receptor-associated kinases and uses thereof |
| IL312367A (en) | 2017-01-31 | 2024-06-01 | Arvinas Operations Inc | Cereblon ligands and bifunctional compounds comprising the same |
| 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 |
| PT3621960T (pt) | 2017-05-11 | 2021-09-16 | Bristol Myers Squibb Co | Tienopiridinas e benzotiofenos úteis como inibidores de irak4 |
| 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 |
| CN118108706A (zh) | 2017-09-04 | 2024-05-31 | C4医药公司 | 戊二酰亚胺 |
| US11358948B2 (en) * | 2017-09-22 | 2022-06-14 | 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 |
| WO2019084026A1 (en) | 2017-10-24 | 2019-05-02 | Genentech, Inc. | (4-HYDROXYPYRROLIDIN-2-YL) -HETEROCYCLIC COMPOUNDS AND METHODS OF USE |
| CN111372585A (zh) | 2017-11-16 | 2020-07-03 | C4医药公司 | 用于靶蛋白降解的降解剂和降解决定子 |
| 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 |
| IL315310A (en) | 2017-12-26 | 2024-10-01 | Kymera Therapeutics Inc | Irak degraders and uses thereof |
| WO2019140387A1 (en) | 2018-01-12 | 2019-07-18 | Kymera Therapeutics, Inc. | Crbn ligands and uses thereof |
| WO2019140380A1 (en) | 2018-01-12 | 2019-07-18 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| CA3090417A1 (en) | 2018-02-23 | 2019-08-29 | Dana-Farber Cancer Institute, Inc. | Small molecules for inducing selective protein degradation and uses thereof |
| WO2020010210A1 (en) | 2018-07-06 | 2020-01-09 | Kymera Therapeutics, Inc. | Mertk degraders and uses thereof |
| WO2020010227A1 (en) | 2018-07-06 | 2020-01-09 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| WO2020010177A1 (en) | 2018-07-06 | 2020-01-09 | Kymera Therapeutics, Inc. | Tricyclic crbn ligands and uses thereof |
-
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- 2018-09-21 WO PCT/US2018/052242 patent/WO2019060742A1/en not_active Ceased
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
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