CN113423427B - Irak降解剂和其用途 - Google Patents

Irak降解剂和其用途

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Publication number
CN113423427B
CN113423427B CN201980089596.8A CN201980089596A CN113423427B CN 113423427 B CN113423427 B CN 113423427B CN 201980089596 A CN201980089596 A CN 201980089596A CN 113423427 B CN113423427 B CN 113423427B
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ring
nitrogen
sulfur
oxygen
independently selected
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CN113423427A (zh
Inventor
N·马伊诺尔菲
纪楠
A·F·克卢格
M·M·魏斯
张毅
X·郑
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Kemela Medical Co
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Kemela Medical Co
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Peptides Or Proteins (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Saccharide Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201980089596.8A 2018-11-30 2019-12-02 Irak降解剂和其用途 Active CN113423427B (zh)

Applications Claiming Priority (19)

Application Number Priority Date Filing Date Title
US201862774051P 2018-11-30 2018-11-30
US62/774,051 2018-11-30
US201962788460P 2019-01-04 2019-01-04
US62/788,460 2019-01-04
US201962793992P 2019-01-18 2019-01-18
US62/793,992 2019-01-18
US201962826743P 2019-03-29 2019-03-29
US62/826,743 2019-03-29
US201962831007P 2019-04-08 2019-04-08
US62/831,007 2019-04-08
US201962851427P 2019-05-22 2019-05-22
US62/851,427 2019-05-22
US201962868574P 2019-06-28 2019-06-28
US62/868,574 2019-06-28
US201962875347P 2019-07-17 2019-07-17
US62/875,347 2019-07-17
US201962879117P 2019-07-26 2019-07-26
US62/879,117 2019-07-26
PCT/US2019/064070 WO2020113233A1 (en) 2018-11-30 2019-12-02 Irak degraders and uses thereof

Publications (2)

Publication Number Publication Date
CN113423427A CN113423427A (zh) 2021-09-21
CN113423427B true CN113423427B (zh) 2026-03-13

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CN201980089596.8A Active CN113423427B (zh) 2018-11-30 2019-12-02 Irak降解剂和其用途

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US (5) US11352350B2 (https=)
EP (1) EP3886904B1 (https=)
JP (2) JP7623943B2 (https=)
KR (2) KR20250167680A (https=)
CN (1) CN113423427B (https=)
AU (1) AU2019389174A1 (https=)
BR (1) BR112021010484A2 (https=)
CA (1) CA3119773A1 (https=)
CO (1) CO2021007068A2 (https=)
IL (1) IL283471A (https=)
MX (1) MX2021006154A (https=)
PH (1) PH12021500026A1 (https=)
SG (1) SG11202105424PA (https=)
WO (1) WO2020113233A1 (https=)

Families Citing this family (90)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
WO2020010227A1 (en) 2018-07-06 2020-01-09 Kymera Therapeutics, Inc. Protein degraders and uses thereof
TWI721623B (zh) 2018-10-31 2021-03-11 美商基利科學股份有限公司 經取代之6-氮雜苯并咪唑化合物
TW202136261A (zh) 2018-10-31 2021-10-01 美商基利科學股份有限公司 經取代之6-氮雜苯并咪唑化合物
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
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
US11453681B2 (en) 2019-05-23 2022-09-27 Gilead Sciences, Inc. Substituted eneoxindoles and uses thereof
BR112021026517A2 (pt) * 2019-06-28 2022-05-10 Kymera Therapeutics Inc Degradadores de irak e usos dos mesmos
WO2021011868A1 (en) 2019-07-17 2021-01-21 Kymera Therapeutics, Inc. Irak degraders and uses thereof
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
WO2021127190A1 (en) 2019-12-17 2021-06-24 Kymera Therapeutics, Inc. Irak degraders and uses thereof
US20230122219A1 (en) * 2020-02-03 2023-04-20 Kymera Therapeutics, Inc. Irak degraders and uses thereof
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
WO2021247897A1 (en) * 2020-06-03 2021-12-09 Kymera Therapeutics, Inc. Deuterated irak degraders and uses thereof
MX2022016061A (es) * 2020-06-17 2023-02-02 Kymera Therapeutics Inc Degradadores de cinasa asociada al receptor interleucina-1 (irak) y usos de los mismos.
US20230265116A1 (en) * 2020-07-16 2023-08-24 Beigene, Ltd. Degradation of (egfr) by conjugation of egfr inhibitors with e3 ligase ligand and methods of use
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
US11857535B2 (en) 2020-07-30 2024-01-02 Kymera Therapeutics, Inc. Methods of treating mutant lymphomas
CN113512025B (zh) * 2020-07-31 2023-01-06 四川大学 一种吲唑酯类化合物及其制药用途
TWI833104B (zh) 2020-08-05 2024-02-21 大陸商上海領泰生物醫藥科技有限公司 靶向蛋白降解化合物及其製備方法和應用
EP4238968A4 (en) * 2020-10-26 2024-10-23 Leadingtac Pharmaceutical (Shaoxing) Co., Ltd INDAZOLE DERIVATIVE, ITS PREPARATION PROCESS AND ITS USE
EP4240422A4 (en) * 2020-11-05 2025-05-07 Kronos Bio, Inc. Compounds and methods for modulating CDK9 activity
CA3200608A1 (en) * 2020-12-09 2022-06-16 Xiaozhang Zheng Irak degraders and uses thereof
CN114621231B (zh) * 2020-12-14 2025-09-12 杭州中美华东制药有限公司 一种靶向降解/抑制活性的嵌合化合物及其制备方法和用途
PH12023500015A1 (en) 2020-12-30 2024-03-11 Kymera Therapeutics Inc Irak degraders and uses thereof
WO2022161414A1 (zh) * 2021-01-26 2022-08-04 成都茵创园医药科技有限公司 芳香化合物、含其的药物组合物及其应用
US20240165243A1 (en) 2021-02-10 2024-05-23 Beigene Switzerland Gmbh Egfr degraders and methods of use
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
KR20240004476A (ko) 2021-04-08 2024-01-11 쿠리스 인코퍼레이션 암 치료를 위한 병용 요법
AU2022271290A1 (en) 2021-05-07 2023-11-23 Kymera Therapeutics, Inc. Cdk2 degraders and uses thereof
WO2022251224A1 (en) * 2021-05-28 2022-12-01 Recurium Ip Holdings, Llc Wee1 inhibitors and methods for treating cancer
CN115504963A (zh) * 2021-06-22 2022-12-23 苏州开拓药业股份有限公司 一种c-Myc蛋白降解剂
US20250171417A1 (en) 2021-08-11 2025-05-29 Xizang Haisco Pharmaceutical Co., Ltd. Heterocyclic derivative, and composition and pharmaceutical use thereof
CA3229646A1 (en) 2021-08-23 2023-03-02 Zhengqing YE Irak4 degradation agent, and preparation method therefor and use thereof
TWI899502B (zh) * 2021-09-08 2025-10-01 大陸商南京明德新藥研發有限公司 戊二醯亞胺類化合物與其應用
EP4406953A4 (en) * 2021-09-26 2025-07-16 Medshine Discovery Inc 2,6-PIPERIDINEDIONE COMPOUND AND ITS APPLICATION
US12187744B2 (en) 2021-10-29 2025-01-07 Kymera Therapeutics, Inc. IRAK4 degraders and synthesis thereof
EP4444716A1 (en) * 2021-12-06 2024-10-16 Kainos Medicine, Inc. Compositions and methods for treating cancer
AU2022405474A1 (en) * 2021-12-08 2024-07-18 Gluetacs Therapeutics (Shanghai) Co., Ltd. E3 ubiquitin ligase ligand compound, protein degrader developed based thereon and their applications
KR20230091052A (ko) * 2021-12-14 2023-06-22 (주)프레이저테라퓨틱스 폴리유비퀴틴화에 의한 표적 단백질 또는 폴리펩티드의 분해용 신규 화합물
TW202333670A (zh) 2022-01-04 2023-09-01 大陸商海思科醫藥集團股份有限公司 抑制並降解irak4的化合物及其藥物组合物和藥學上的應用
EP4472967A4 (en) * 2022-01-31 2026-04-15 Kymera Therapeutics Inc Iraqi Degradation Agents and Their Uses
JP7805983B2 (ja) 2022-03-22 2026-01-26 アッヴィ・インコーポレイテッド ブルトン型チロシンキナーゼを分解するためのピリミジン
EP4499068A4 (en) * 2022-03-31 2026-03-25 Kymera Therapeutics Inc Iraqi Degradation Agents and Their Uses
WO2023201274A1 (en) 2022-04-12 2023-10-19 Genzyme Corporation Use of an irak4 modulator for gene therapy
CN119630802A (zh) 2022-04-12 2025-03-14 建新公司 Irak4调节剂用于基因疗法的用途
CN119585287A (zh) 2022-05-06 2025-03-07 Paq医疗公司 Kras g12d蛋白水解靶向嵌合体
KR20250020448A (ko) 2022-06-02 2025-02-11 시젱 하이스코 파마수티칼 씨오., 엘티디. Bcl6을 억제하거나 분해하는 화합물 및 의약학에서의 응용
CA3258387A1 (en) * 2022-06-09 2023-12-14 Beone Medicines I Gmbh Degradation of irak4 by conjugation of irak4 inhibitors with e3 ligase ligand and methods of use
TWI896986B (zh) * 2022-06-15 2025-09-11 大陸商杭州多域生物技術有限公司 一種五元并六元化合物、製備方法、藥物組合物和應用
CN116925085B (zh) * 2022-07-23 2026-03-31 成都茵创园医药科技有限公司 Irak降解剂及其用途
EP4570792A1 (en) * 2022-08-10 2025-06-18 Gluetacs Therapeutics (Shanghai) Co., Ltd. Compound based on isoindoline-substituted glutarimide backbone and use thereof
CN116253661A (zh) * 2022-08-25 2023-06-13 科睿驰（深圳）医疗科技发展有限公司 一种含有碘代芳基或碘代杂芳基的酰胺化合物及其制备方法和应用
WO2024073507A1 (en) 2022-09-28 2024-04-04 Theseus Pharmaceuticals, Inc. Macrocyclic compounds and uses thereof
JP2025534698A (ja) * 2022-10-13 2025-10-17 カイメラ セラピューティクス， インコーポレイテッド Ｉｒａｋ４デグレーダーの塩の形態
CN115557916B (zh) * 2022-10-20 2023-11-14 恒光新材料(江苏)股份有限公司 吗啉基乙基二甲氨基丙基醚的制备方法
AU2023373192A1 (en) * 2022-11-04 2025-04-17 St. Jude Children's Research Hospital, Inc. Nlrp12 and nlrc5 modulators and methods for using the same to modulate diseases
CN119894895A (zh) 2022-11-04 2025-04-25 领泰生物医药(绍兴)有限公司 Irak4降解剂及其用途
WO2024148060A1 (en) * 2023-01-04 2024-07-11 Kymera Therapeutics, Inc. Mk2 degraders and uses thereof
WO2024194756A1 (en) 2023-03-17 2024-09-26 Pfizer Inc. Modulating the innate immunity of rna
CN121358727A (zh) * 2023-03-24 2026-01-16 漳州片仔癀药业股份有限公司 2,6-哌啶二酮类化合物盐型和晶型的制备方法及其应用
EP4692082A1 (en) * 2023-03-24 2026-02-11 Zhangzhou Pien Tze Huang Pharmaceutical Co., Ltd. Crystal form of 2,6-piperidinedione compound, and preparation method therefor and use thereof
US20240374588A1 (en) 2023-04-07 2024-11-14 Astrazeneca Ab Irak4 protacs
PE20260451A1 (es) 2023-05-08 2026-02-25 Bristol Myers Squibb Co Compuestos de feniloxazolona sustituida
KR20260010407A (ko) * 2023-05-11 2026-01-20 셀진 코포레이션 Irak4의 리간드 지정 분해제로서의 헤테로아릴 화합물
CN121219294A (zh) * 2023-05-11 2025-12-26 细胞基因公司 作为irk4的配体定向降解剂的杂芳基化合物
TW202517298A (zh) 2023-07-04 2025-05-01 大陸商西藏海思科製藥有限公司 抑制並降解irak4的化合物的藥物组合物及其在藥學上的應用
WO2025011655A1 (zh) 2023-07-13 2025-01-16 成都茵创园医药科技有限公司 芳香化合物、含其的药物组合物及其应用
EP4495105A1 (en) 2023-07-17 2025-01-22 Basf Se 3-(4-hydroxybut-2-ynoxy)propanoic acid ester, amide and nitrile derivatives as corrosion protection agents
EP4495108A1 (en) 2023-07-17 2025-01-22 Basf Se 3-[2-(2-oxo-1,3-dioxolan-4-ylidene)ethoxy]propanoic acid derivatives as precursors of monomers in polymerisations
CN121816348A (zh) 2023-08-11 2026-04-07 深圳众格生物科技有限公司 一种降解irak4的蛋白降解靶向嵌合体化合物及其应用
WO2025036451A1 (zh) * 2023-08-15 2025-02-20 潘普洛纳生物科技（深圳）有限公司 靶向irak蛋白抑制或降解的化合物及其应用
AU2024334386A1 (en) * 2023-08-30 2026-02-19 Kymera Therapeutics, Inc. Stat6 degraders and uses thereof
US12599672B2 (en) 2023-10-03 2026-04-14 PAQ Therapeutics Inc. KRAS proteolysis targeting chimeras
WO2025126115A1 (en) 2023-12-13 2025-06-19 Beigene Switzerland Gmbh Degradation of irak4 by conjugation of irak4 inhibitors with e3 ligase ligands and methods of use
TW202535949A (zh) 2023-12-20 2025-09-16 美商必治妥美雅史谷比公司 靶向IL-18受體β(IL-18RB)之抗體及相關方法
WO2025152147A1 (zh) * 2024-01-19 2025-07-24 浙江普洛家园药业有限公司 一种e3泛素连接酶配体的关键中间体的制备方法
WO2025168131A1 (zh) * 2024-02-08 2025-08-14 清华大学 一种多靶降解剂及其用途
WO2025221780A1 (en) 2024-04-16 2025-10-23 Genzyme Corporation Salts of irak4 degrader
WO2025221962A1 (en) * 2024-04-17 2025-10-23 Kymera Therapeutics, Inc. Irak4 degrader formulations and uses thereof
CN118542932B (zh) * 2024-04-22 2026-01-06 浙江大学 环指蛋白114在制备治疗白内障药物中的应用
WO2026007998A1 (zh) * 2024-07-03 2026-01-08 正大天晴药业集团股份有限公司 稠合杂环化合物及其用途
US12565492B2 (en) 2024-08-09 2026-03-03 Triana Biomedicines, Inc. Anaplastic Lymphoma Kinase (ALK) degraders and uses thereof
WO2026046113A1 (zh) * 2024-08-26 2026-03-05 上海齐鲁制药研究中心有限公司 一种irak-4降解剂的多晶型
WO2026060321A1 (en) 2024-09-13 2026-03-19 Olema Pharmaceuticals, Inc. Kat6 degrader compounds and method thereof
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 (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016144844A1 (en) * 2015-03-12 2016-09-15 Merck Sharp & Dohme Corp. Carboxamide inhibitors of irak4 activity
WO2016169989A1 (en) * 2015-04-22 2016-10-27 Glaxosmithkline Intellectual Property Development Limited Iap e3 ligase directed proteolysis targeting chimeric molecules

Family Cites Families (282)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4045485A (en) 1968-07-02 1977-08-30 Syntex Corporation Naphthyl acetaldehyde derivatives; methods of use thereof; and processes for the preparation thereof
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
US5650270A (en) 1982-02-01 1997-07-22 Northeastern University Molecular analytical release tags and their use in chemical analysis
US4709016A (en) 1982-02-01 1987-11-24 Northeastern University Molecular analytical release tags and their use in chemical analysis
US5217866A (en) 1985-03-15 1993-06-08 Anti-Gene Development Group Polynucleotide assay reagent and method
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
WO1996007655A1 (en) 1994-09-06 1996-03-14 Banyu Pharmaceutical Co., Ltd. Novel carbapenem derivative
US6281230B1 (en) 1996-07-24 2001-08-28 Celgene Corporation Isoindolines, method of use, and pharmaceutical compositions
CA2269561C (en) 1998-04-22 2007-06-05 Dainippon Ink And Chemicals, Inc. Naphthalene derivative and liquid crystal composition comprising the same
US6306663B1 (en) 1999-02-12 2001-10-23 Proteinex, Inc. Controlling protein levels in eucaryotic organisms
IL131264A0 (en) 1999-08-05 2001-01-28 Yeda Res & Dev Photochromic naphthopyran compounds
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
US20030045552A1 (en) 2000-12-27 2003-03-06 Robarge Michael J. Isoindole-imide compounds, compositions, and uses thereof
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
GB0706793D0 (en) 2007-04-05 2007-05-16 Evotec Ag 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
US8370032B2 (en) 2007-07-12 2013-02-05 Toyota Motor Engineering & Manufacturing North America, Inc. Systems and methods for shift control for vehicular transmission
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
EP2536706B1 (en) 2010-02-11 2017-06-14 Celgene Corporation Arylmethoxy isoindoline derivatives and compositions comprising and methods of using the same
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
CA2789076C (en) 2010-03-05 2017-11-21 F. Hoffmann-La Roche Ag Antibodies against human colony stimulating factor-1 receptor and uses thereof
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
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).
HRP20181598T1 (hr) 2010-06-03 2018-11-30 Abbvie Biotechnology Ltd Uporaba i pripravci za liječenje hidradenitis suppurativa (hs)
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
RU2606120C2 (ru) 2011-08-31 2017-01-10 Хантсман Эдванст Матириалз (Свитзеленд) Гмбх Способ пропитки реакторов с воздушным сердечником, подвергнутый пропитке реактор с воздушным сердечником и применение системы пропитки
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
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
WO2013106646A2 (en) 2012-01-12 2013-07-18 Yale University Compounds and methods for the inhibition of vcb e3 ubiquitin ligase
WO2013106614A1 (en) 2012-01-13 2013-07-18 Bristol-Myers Squibb Company Triazolyl-substituted pyridyl compounds useful as kinase inhibitors
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
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
HK1210696A1 (en) 2012-07-11 2016-05-06 Nimbus Iris, Inc. Irak inhibitors and uses thereof
WO2014011906A2 (en) 2012-07-11 2014-01-16 Nimbus Iris, Inc. Irak inhibitors and uses thereof
BR112015002285B1 (pt) 2012-08-09 2022-05-10 Celgene Corporation Uso do composto 3-(4-((4-(morfolinometil)benzil)oxi)-1-oxoisoindolin-2-il)piperidina-2,6-diona para tratar ou gerenciar câncer
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
WO2014058685A1 (en) 2012-10-08 2014-04-17 Merck Sharp & Dohme Corp. Inhibitors of irak4 activity
WO2014058691A1 (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
US9315494B2 (en) 2012-11-08 2016-04-19 Bristol-Myers Squibb Company Alkyl-amide-substituted pyridyl compounds useful as modulators of IL-12, IL-23 and/or IFNα responses
JP2016505012A (ja) * 2013-01-10 2016-02-18 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
GB201311910D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel Compounds
LT2953952T (lt) 2013-02-07 2017-08-25 Merck Patent Gmbh Makrocikliniai piridazinono dariniai
EP2953944B1 (en) 2013-02-07 2017-04-26 Merck Patent GmbH Pyridazinone-amides derivatives
EP2970334B1 (en) 2013-03-15 2018-05-23 Biogen MA Inc. Macrocyclic compounds as irak4 inhibitors for the treatment of inflammatory diseases
WO2014142237A1 (ja) 2013-03-15 2014-09-18 日本ゼオン株式会社 中空重合体粒子の水性分散液およびその製造方法
BR112016006319A2 (pt) 2013-09-27 2017-08-01 Nimbus Iris Inc inibidores de irak e usos dos mesmos
MX2021012208A (es) 2013-10-04 2023-01-19 Infinity Pharmaceuticals Inc Compuestos heterocíclicos y usos de los mismos.
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
CN104650092B (zh) * 2013-11-16 2017-11-10 广东东阳光药业有限公司 取代的杂芳基化合物及其组合物和用途
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
CN106255689B (zh) 2014-03-19 2019-09-17 勃林格殷格翰国际有限公司 杂芳基syk抑制剂
MA39838B1 (fr) 2014-04-04 2019-05-31 Pfizer Composés bicycliques hétéroaryle ou aryle fusionnés et leur utilisation en tant qu'inhibiteurs irak4
US20160058872A1 (en) 2014-04-14 2016-03-03 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
AU2015247817C1 (en) 2014-04-14 2022-02-10 Arvinas Operations, Inc. Imide-based modulators of proteolysis and associated methods of use
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
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
US9141124B1 (en) 2014-06-25 2015-09-22 Elite Semiconductor Memory Technology Inc. Bandgap reference circuit
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
CN105461694B (zh) * 2014-09-27 2019-05-24 广东东阳光药业有限公司 取代的杂芳基化合物及其组合物和用途
US9926330B2 (en) 2014-09-30 2018-03-27 Merck Sharp & Dohme Corp. Inhibitors of IRAK4 activity
EP3200790B1 (en) 2014-09-30 2020-08-26 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
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
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
US12312316B2 (en) 2015-01-20 2025-05-27 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
EP3267996B1 (en) 2015-03-12 2020-11-11 Merck Sharp & Dohme Corp. Pyrazolopyrimidine inhibitors of irak4 activity
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
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
UY36660A (es) 2015-04-30 2016-11-30 Bayer Pharma AG Combinaciones de inhibidores de irak4
HUE054149T2 (hu) 2015-06-04 2021-08-30 Arvinas Operations Inc Proteolízis imid-alapú modulátorai és ezekkel kapcsolatos felhasználási eljárások
WO2016197114A1 (en) 2015-06-05 2016-12-08 Arvinas, Inc. Tank-binding kinase-1 protacs and associated methods of use
US10702527B2 (en) 2015-06-12 2020-07-07 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
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
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
US9848583B2 (en) 2015-07-02 2017-12-26 Ellis Junior Smith Retractable leash
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
US10669234B2 (en) 2015-07-14 2020-06-02 Mission Therapeutics Limited Cyanopyrrolidines as dub inhibitors for the treatment of cancer
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
GB201516243D0 (en) * 2015-09-14 2015-10-28 Glaxosmithkline Ip Dev Ltd Novel compounds
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
KR102650026B1 (ko) 2015-09-18 2024-03-22 메르크 파텐트 게엠베하 Irak 억제제로서의 헤테로아릴 화합물 및 이의 용도
BR112018006689A2 (pt) 2015-10-02 2018-10-09 Dana Farber Cancer Inst Inc terapia de combinação de inibidores de bromodomínio e bloqueio de ponto de controle
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
EP3383363B1 (en) 2015-11-30 2021-01-06 Anacor Pharmaceuticals, Inc. Topical pharmaceutical formulations for treating inflammatory-related conditions
WO2017108744A1 (de) 2015-12-22 2017-06-29 Bayer Pharma Aktiengesellschaft Neue substituierte indazole, verfahren zu ihrer herstellung, pharmazeutische präparate die diese enthalten, sowie deren verwendung zur herstellung von arzneimitteln
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
EP3423446B1 (de) 2016-03-03 2020-09-16 Bayer Pharma Aktiengesellschaft Neue 2-substituierte indazole, verfahren zu ihrer herstellung, pharmazeutische präparate die diese enthalten, sowie deren verwendung zur herstellung von arzneimitteln
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
WO2017197056A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Bromodomain targeting 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
EP3454862B1 (en) 2016-05-10 2024-09-11 C4 Therapeutics, Inc. Spirocyclic 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
WO2017223243A1 (en) * 2016-06-21 2017-12-28 X4 Pharmaceuticals, Inc. Cxcr4 inhibitors and uses thereof
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
US11542261B2 (en) 2016-08-17 2023-01-03 Children's Hospital Medical Center Substituted Imidazo[1,2-a]-pyridines as IRAK 1/4 and FLT3 inhibitors
JP2019196309A (ja) 2016-09-15 2019-11-14 武田薬品工業株式会社 複素環化合物
WO2018064589A1 (en) 2016-09-29 2018-04-05 Dana-Farber Cancer Institute, Inc. Targeted protein degradation using a mutant e3 ubiquitin ligase
WO2018071606A1 (en) 2016-10-11 2018-04-19 Arvinas, Inc. Compounds and methods for the targeted degradation of androgen receptor
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
MX2019007646A (es) * 2016-12-23 2019-09-06 Arvinas Operations Inc Moleculas quimericas dirigidas a la proteolisis del egfr y metodos asociados de uso.
CN108322937B (zh) 2017-01-18 2020-08-11 上海诺基亚贝尔股份有限公司 无线接入网中用于网络切片的资源分配方法和编排器
AU2018211975B2 (en) * 2017-01-26 2022-05-26 Arvinas Operations, Inc. Modulators of estrogen receptor proteolysis and associated methods of use
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)
EP3630291B9 (en) 2017-05-26 2024-05-29 Cancer Research Technology Limited Benzimidazolone derived inhibitors of bcl6
WO2018226542A1 (en) 2017-06-09 2018-12-13 Arvinas, Inc. Modulators of proteolysis and associated methods of use
WO2018232288A1 (en) 2017-06-16 2018-12-20 Genentech, Inc. Diagnostic and therapeutic methods for irak4-mediated disorders and conditions
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
MX2020003190A (es) * 2017-09-22 2020-11-11 Kymera Therapeutics Inc Degradadores de proteinas y usos de los mismos.
JP7311162B2 (ja) 2017-10-10 2023-07-19 アルデイラ セラピューティクス， インコーポレイテッド 炎症性障害の処置
EP3700901A1 (en) 2017-10-24 2020-09-02 Genentech, Inc. (4-hydroxypyrrolidin-2-yl)-heterocyclic compounds and methods of use thereof
WO2019084030A1 (en) 2017-10-24 2019-05-02 Genentech, Inc. (4-HYDROXYPYRROLIDIN-2-YL) -HYDROXAMATE COMPOUNDS AND METHODS OF USE
WO2019094772A1 (en) 2017-11-10 2019-05-16 The Regents Of The University Of Michigan Ash1l degraders and methods of treatment therewith
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
WO2019111218A1 (en) 2017-12-08 2019-06-13 Cadila Healthcare Limited Novel heterocyclic compounds as irak4 inhibitors
CN109912655B (zh) 2017-12-13 2021-12-10 上海科技大学 Alk蛋白降解剂及其抗肿瘤应用
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
WO2019160915A1 (en) * 2018-02-14 2019-08-22 Dana-Farber Cancer Institute, Inc. Irak degraders 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
EP3578561A1 (en) 2018-06-04 2019-12-11 F. Hoffmann-La Roche AG Spiro compounds
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
CA3102996A1 (en) 2018-07-20 2020-01-23 Dana-Farber Cancer Institute, Inc. Degraders that target proteins via keap1
US12109193B2 (en) 2018-07-31 2024-10-08 Loxo Oncology Inc. Spray-dried dispersions, formulations, and polymorphs of (s)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropan-2-yl)-1H-pyrazole-4-carboxamide
EP3841100A1 (en) 2018-08-20 2021-06-30 Arvinas Operations, Inc. Proteolysis targeting chimeric (protac) compound with e3 ubiquitin ligase binding activity and targeting alpha-synuclein protein for treating neurodegenerative diseases
MX2021001957A (es) 2018-08-22 2021-07-15 Cullgen Shanghai Inc Compuestos de degradacion y metodos de uso del receptor de tropomiosina quinasa (trk).
CN110862375B (zh) 2018-08-27 2022-10-25 深圳铂立健医药有限公司 吡唑化合物及其药物组合物和应用
JP7712867B2 (ja) 2018-11-02 2025-07-24 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 アセチル化ライター阻害剤の開発およびその使用
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
WO2020150626A1 (en) 2019-01-18 2020-07-23 Biogen Ma Inc. Imidazo[1,2-a]pyridinyl derivatives as irak4 inhibitors
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
US20220324880A1 (en) 2019-06-10 2022-10-13 Kymara Therapeutics, Inc. Smarca inhibitors and uses thereof
US20230072658A1 (en) 2019-06-10 2023-03-09 Kymera Therapeutics, Inc. Smarca degraders and uses thereof
WO2020251972A1 (en) 2019-06-10 2020-12-17 Kymera Therapeutics, Inc. Smarca degraders and uses thereof
WO2020251969A1 (en) 2019-06-10 2020-12-17 Kymera Therapeutics, Inc. Smarca degraders and uses thereof
BR112021026517A2 (pt) 2019-06-28 2022-05-10 Kymera Therapeutics Inc Degradadores de irak e usos dos mesmos
WO2020264490A1 (en) 2019-06-28 2020-12-30 Kymera Therapeutics, Inc. Irak degraders and uses thereof
US20230303526A1 (en) 2019-06-28 2023-09-28 Kymera Therapeutics, Inc. Irak degraders and uses thereof
WO2021011634A1 (en) 2019-07-15 2021-01-21 Kymera Therapeutics, Inc. Protein degraders and uses thereof
US20220281831A1 (en) 2019-07-15 2022-09-08 Kymera Therapeutics, Inc. Fused-glutarimide crbn ligands and uses thereof
WO2021011871A1 (en) 2019-07-17 2021-01-21 Kymera Therapeutics, Inc. Mertk degraders and uses thereof
WO2021011868A1 (en) 2019-07-17 2021-01-21 Kymera Therapeutics, Inc. Irak degraders and uses thereof
WO2021018118A1 (en) 2019-07-29 2021-02-04 Janssen Pharmaceutica Nv Compounds and methods for the targeted degradation of interleukin-1 receptor-associated kinase 1 proteins
JP2022548095A (ja) 2019-09-16 2022-11-16 ノバルティス アーゲー 接着分解剤及びその使用方法
US12551564B2 (en) 2019-12-10 2026-02-17 Kymera Therapeutics, Inc. IRAK degraders and uses thereof
US20230219945A1 (en) 2019-12-17 2023-07-13 Kymera Therapeutics, Inc. Irak degraders and uses thereof
WO2021127190A1 (en) 2019-12-17 2021-06-24 Kymera Therapeutics, Inc. Irak degraders and uses thereof
WO2021127283A2 (en) 2019-12-17 2021-06-24 Kymera Therapeutics, Inc. Irak degraders and uses thereof
US20230122219A1 (en) 2020-02-03 2023-04-20 Kymera Therapeutics, Inc. Irak degraders and uses thereof
WO2021222366A1 (en) 2020-04-28 2021-11-04 Kymera Therapeutics, Inc. Irak inhibitors and uses thereof
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
WO2021247897A1 (en) 2020-06-03 2021-12-09 Kymera Therapeutics, Inc. Deuterated irak degraders and uses thereof
MX2022016061A (es) 2020-06-17 2023-02-02 Kymera Therapeutics Inc Degradadores de cinasa asociada al receptor interleucina-1 (irak) y usos de los mismos.
US11857535B2 (en) 2020-07-30 2024-01-02 Kymera Therapeutics, Inc. Methods of treating mutant lymphomas
TWI833104B (zh) 2020-08-05 2024-02-21 大陸商上海領泰生物醫藥科技有限公司 靶向蛋白降解化合物及其製備方法和應用
EP4232059A4 (en) 2020-10-21 2024-09-11 Kymera Therapeutics, Inc. DOUBLE DEGRADERS AND USES THEREOF
CA3200608A1 (en) 2020-12-09 2022-06-16 Xiaozhang Zheng Irak degraders and uses thereof
PH12023500015A1 (en) 2020-12-30 2024-03-11 Kymera Therapeutics Inc Irak degraders and uses thereof
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
US20240383887A1 (en) 2021-05-07 2024-11-21 Kymera Therapeutics, Inc. Deuterated irak degraders and uses thereof
US12187744B2 (en) 2021-10-29 2025-01-07 Kymera Therapeutics, Inc. IRAK4 degraders and synthesis thereof
WO2023137439A1 (en) 2022-01-14 2023-07-20 Kymera Therapeutics, Inc. Irak4 degraders and uses thereof
EP4472967A4 (en) 2022-01-31 2026-04-15 Kymera Therapeutics Inc Iraqi Degradation Agents and Their Uses
EP4499068A4 (en) 2022-03-31 2026-03-25 Kymera Therapeutics Inc Iraqi Degradation Agents and Their Uses
JP2025534698A (ja) 2022-10-13 2025-10-17 カイメラ セラピューティクス， インコーポレイテッド Ｉｒａｋ４デグレーダーの塩の形態
IL321211A (en) 2022-12-13 2025-07-01 Kymera Therapeutics Inc IRAK4 joints and their uses

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016144844A1 (en) * 2015-03-12 2016-09-15 Merck Sharp & Dohme Corp. Carboxamide inhibitors of irak4 activity
WO2016169989A1 (en) * 2015-04-22 2016-10-27 Glaxosmithkline Intellectual Property Development Limited Iap e3 ligase directed proteolysis targeting chimeric molecules

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