CN115974840A - 人小脑蛋白配体和包含其的双官能化合物 - Google Patents

人小脑蛋白配体和包含其的双官能化合物 Download PDF

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CN115974840A
CN115974840A CN202310022082.9A CN202310022082A CN115974840A CN 115974840 A CN115974840 A CN 115974840A CN 202310022082 A CN202310022082 A CN 202310022082A CN 115974840 A CN115974840 A CN 115974840A
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syndrome
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disease
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安德鲁·P·克鲁斯
迈克尔·贝尔林
H·董
基特·R·霍恩伯格
Y·钱
劳伦斯·B·斯奈德
J·王
库尔特·齐默尔曼
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Arvinas Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—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 two hetero rings
    • C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • 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
    • C07D471/10—Spiro-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
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    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

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  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
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  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pyridine Compounds (AREA)
CN202310022082.9A 2017-01-31 2018-01-31 人小脑蛋白配体和包含其的双官能化合物 Pending CN115974840A (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201762452972P 2017-01-31 2017-01-31
US62/452,972 2017-01-31
PCT/US2018/016315 WO2018144649A1 (en) 2017-01-31 2018-01-31 Cereblon ligands and bifunctional compounds comprising the same
CN201880022865.4A CN110612294B (zh) 2017-01-31 2018-01-31 人小脑蛋白配体和包含其的双官能化合物

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US (3) US20180215731A1 (https=)
EP (1) EP3577109A4 (https=)
JP (2) JP2020506922A (https=)
KR (1) KR102747905B1 (https=)
CN (2) CN115974840A (https=)
AU (3) AU2018215212B2 (https=)
BR (1) BR112019015484A2 (https=)
CA (1) CA3050309A1 (https=)
CO (1) CO2019009424A2 (https=)
IL (3) IL312367A (https=)
MX (2) MX2019009046A (https=)
WO (1) WO2018144649A1 (https=)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2025011623A1 (zh) * 2023-07-12 2025-01-16 上海壹迪生物技术有限公司 氰基喹啉类靶向蛋白降解分子、其制备方法和应用
WO2025036489A1 (zh) 2023-08-17 2025-02-20 海思科医药集团股份有限公司 一种氰基芳香环衍生物及其在医药上的应用

Families Citing this family (276)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
US12312316B2 (en) 2015-01-20 2025-05-27 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
WO2016197114A1 (en) 2015-06-05 2016-12-08 Arvinas, Inc. Tank-binding kinase-1 protacs and associated methods of use
WO2017011371A1 (en) 2015-07-10 2017-01-19 Arvinas, Inc Mdm2-based modulators of proteolysis and associated methods of use
EP3337476A4 (en) 2015-08-19 2019-09-04 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
US20170281784A1 (en) 2016-04-05 2017-10-05 Arvinas, Inc. Protein-protein interaction inducing technology
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
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
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
WO2018053354A1 (en) 2016-09-15 2018-03-22 Arvinas, Inc. Indole derivatives as estrogen receptor degraders
EP3532464A4 (en) 2016-10-28 2020-07-08 Icahn School of Medicine at Mount Sinai COMPOSITIONS AND METHODS FOR THE TREATMENT OF EZH2 MEDIATION CANCER
IL290809B2 (en) * 2016-11-01 2024-01-01 Arvinas Operations Inc Tau-protein targeting protacs and associated methods of use
KR102674902B1 (ko) 2016-12-01 2024-06-14 아비나스 오퍼레이션스, 인코포레이티드 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 및 테트라히드로이소퀴놀린 유도체
MX2019007646A (es) 2016-12-23 2019-09-06 Arvinas Operations Inc Moleculas quimericas dirigidas a la proteolisis del egfr y metodos asociados de uso.
CN117510491A (zh) 2016-12-23 2024-02-06 阿尔维纳斯运营股份有限公司 用于迅速加速性纤维肉瘤多肽的靶向降解的化合物和方法
US10806737B2 (en) 2016-12-23 2020-10-20 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of fetal liver kinase polypeptides
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
US11191741B2 (en) 2016-12-24 2021-12-07 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide
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
KR102014478B1 (ko) * 2017-05-12 2019-08-26 한국화학연구원 신규한 피페리딘-2,6-디온 유도체 및 이의 용도
EP4717317A2 (en) 2017-06-20 2026-04-01 C4 Therapeutics, Inc. N/o-linked degrons and degronimers for protein degradation
TWI791552B (zh) 2017-07-10 2023-02-11 美商西建公司 抗增生化合物及其使用方法
CN118108706A (zh) 2017-09-04 2024-05-31 C4医药公司 戊二酰亚胺
CN111278816B (zh) 2017-09-04 2024-03-15 C4医药公司 二氢喹啉酮
CN118206529A (zh) 2017-09-04 2024-06-18 C4医药公司 二氢苯并咪唑酮
MX2020003190A (es) 2017-09-22 2020-11-11 Kymera Therapeutics Inc Degradadores de proteinas y usos de los mismos.
WO2019060693A1 (en) 2017-09-22 2019-03-28 Kymera Therapeutics, Inc. CRBN LIGANDS AND USES THEREOF
EP3710002A4 (en) 2017-11-16 2021-07-07 C4 Therapeutics, Inc. DEGRADER AND DEGRONE FOR TARGETED PROTEIN DEGRADATION
US11065231B2 (en) 2017-11-17 2021-07-20 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of interleukin-1 receptor- associated kinase 4 polypeptides
IL315310A (en) 2017-12-26 2024-10-01 Kymera Therapeutics Inc Irak degraders and uses thereof
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
US11220515B2 (en) 2018-01-26 2022-01-11 Yale University Imide-based modulators of proteolysis and associated methods of use
US11028088B2 (en) 2018-03-10 2021-06-08 Yale University Modulators of BTK proteolysis and methods of use
EP3774804A1 (en) 2018-03-26 2021-02-17 Novartis AG N-(3-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl)benzamide derivatives
JP2021519337A (ja) 2018-03-26 2021-08-10 シー４ セラピューティクス， インコーポレイテッド Ｉｋａｒｏｓの分解のためのセレブロン結合剤
US12539292B2 (en) 2018-04-01 2026-02-03 Arvinas Operations, Inc. BRM targeting compounds and associated methods of use
US20190300521A1 (en) 2018-04-01 2019-10-03 Arvinas Operations, Inc. Brm targeting compounds and associated methods of use
KR20210006356A (ko) 2018-04-04 2021-01-18 아비나스 오퍼레이션스, 인코포레이티드 단백질분해 조절제 및 연관된 사용 방법
CA3095912A1 (en) * 2018-04-13 2019-10-17 Arvinas Operations, Inc. Cereblon ligands and bifunctional compounds comprising the same
CN119751456A (zh) 2018-04-16 2025-04-04 C4医药公司 螺环化合物
CN118344338A (zh) 2018-04-23 2024-07-16 细胞基因公司 取代的4-氨基异吲哚啉-1,3-二酮化合物以及它们用于治疗淋巴瘤的用途
WO2019222272A1 (en) 2018-05-14 2019-11-21 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds
EP3578561A1 (en) 2018-06-04 2019-12-11 F. Hoffmann-La Roche AG Spiro compounds
US12060366B2 (en) 2018-06-29 2024-08-13 Dana-Farber Cancer Institute, Inc. Bispecific degraders
CA3102212A1 (en) 2018-06-29 2020-01-02 Dana-Farber Cancer Institute, Inc. Immunomodulatory compounds
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
AR116109A1 (es) 2018-07-10 2021-03-31 Novartis Ag Derivados de 3-(5-amino-1-oxoisoindolin-2-il)piperidina-2,6-diona y usos de los mismos
DK3820573T3 (da) 2018-07-10 2023-10-23 Novartis Ag 3-(5-hydroxy-1-oxoisoindolin-2-yl)piperidin-2,6-dion-derivativer og anvendelse deraf ved behandling af ikaros family zinc finger 2 (ikzf2)-afhængige sygdomme
US20200038513A1 (en) 2018-07-26 2020-02-06 Arvinas Operations, Inc. Modulators of fak proteolysis and associated methods of use
WO2020027225A1 (ja) 2018-07-31 2020-02-06 ファイメクス株式会社 複素環化合物
CN108774215A (zh) * 2018-08-15 2018-11-09 翟学旭 含氮杂环类衍生物及其在视网膜新生血管疾病中的应用
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
US11969472B2 (en) 2018-08-22 2024-04-30 Cullgen (Shanghai), Inc. Tropomyosin receptor kinase (TRK) degradation compounds and methods of use
MX2021001957A (es) 2018-08-22 2021-07-15 Cullgen Shanghai Inc Compuestos de degradacion y metodos de uso del receptor de tropomiosina quinasa (trk).
WO2020051235A1 (en) 2018-09-04 2020-03-12 C4 Therapeutics, Inc. Compounds for the degradation of brd9 or mth1
EP3848371A4 (en) * 2018-09-07 2022-06-08 Medshine Discovery Inc. TRICYCLIC FURAN-SUBSTITUTED PIPERIDONEE COMPOUND
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
US12227488B2 (en) * 2018-12-03 2025-02-18 Dana-Farber Cancer Institute, Inc. Small molecule degraders of Helios and methods of use
US11325889B2 (en) * 2018-12-19 2022-05-10 Celgene Corporation Substituted 3-((3-aminophenyl)amino)piperidine-2,6-dione compounds, compositions thereof, and methods of treatment therewith
PL3897636T3 (pl) 2018-12-19 2025-04-28 Celgene Corporation Podstawione związki 3-((3-aminofenylo)amino)piperydyno-2,6-dionu, ich kompozycje i sposoby leczenia nimi
CN120698983A (zh) * 2018-12-20 2025-09-26 C4医药公司 靶向蛋白降解
JP7555938B2 (ja) * 2019-01-30 2024-09-25 モンテリノ・セラピューティクス・インコーポレイテッド アンドロゲン受容体を標的とするユビキチン化のための二官能性化合物および方法
WO2020162725A1 (ko) * 2019-02-07 2020-08-13 한국화학연구원 표적 단백질 ｅｅｄ 분해 유도 데그라듀서, 이의 제조방법 및 이를 유효성분으로 함유하는 ｅｅｄ, ｅｚｈ2, 또는 ｐｒｃ2 관련 질환의 예방 또는 치료용 약학적 조성물
EP3924055B1 (en) 2019-02-15 2024-04-03 Novartis AG Substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
US20220143183A1 (en) * 2019-02-23 2022-05-12 New York University Photoswitchable protacs and synthesis and uses thereof
WO2020181232A1 (en) 2019-03-06 2020-09-10 C4 Therapeutics, Inc. Heterocyclic compounds for medical treatment
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
WO2020206608A1 (en) 2019-04-09 2020-10-15 Ranok Therapeutics (Hangzhou) Co., Ltd. Methods and compositions for targeted protein degradation
US12414995B2 (en) 2019-04-16 2025-09-16 Northwestern University Bifunctional compounds comprising Apcin-A and their use in the treatment of cancer
KR20220004100A (ko) * 2019-04-18 2022-01-11 하이노바 파마슈티컬스 인코포레이티드 안드로겐 수용체를 표적 분해하는 이중 기능성의 키메라 헤테로 고리 화합물 및 이의 용도
CN118908962A (zh) 2019-05-06 2024-11-08 西奈山伊坎医学院 作为hpk1的降解剂的异双功能化合物
CN113811333B (zh) 2019-05-14 2024-03-12 诺维逊生物股份有限公司 靶向抗癌核激素受体的化合物
WO2020251969A1 (en) * 2019-06-10 2020-12-17 Kymera Therapeutics, Inc. Smarca degraders and uses thereof
WO2020251972A1 (en) 2019-06-10 2020-12-17 Kymera Therapeutics, Inc. Smarca degraders and uses thereof
WO2020252397A1 (en) * 2019-06-12 2020-12-17 Baylor College Of Medicine Small molecule proteolysis-targeting chimeras and methods of use thereof
CR20210687A (es) 2019-06-25 2022-03-03 Gilead Sciences Inc PROTEÍNAS DE FUSIÓN FLT3L-Fc Y MÉTODOS DE USO
BR112021026517A2 (pt) 2019-06-28 2022-05-10 Kymera Therapeutics Inc Degradadores de irak e usos dos mesmos
CN119954801A (zh) 2019-07-17 2025-05-09 阿尔维纳斯运营股份有限公司 Tau蛋白靶向化合物及相关使用方法
WO2021011868A1 (en) 2019-07-17 2021-01-21 Kymera Therapeutics, Inc. Irak degraders and uses thereof
IL320609A (en) 2019-08-26 2025-07-01 Arvinas Operations Inc Methods for treating breast cancer with a history of tetrahydronaphthalene as estrogen receptor-disrupting agents
CA3151824A1 (en) * 2019-08-27 2021-03-04 The Regents Of The University Of Michigan Cereblon e3 ligase inhibitors
EP4043455A4 (en) * 2019-09-12 2023-09-20 Medshine Discovery Inc. BICYCLIC COMPOUND AS A CRBN PROTEIN REGULATOR
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
CR20220105A (es) * 2019-09-16 2022-06-13 Novartis Ag Degradadores bifuncionales de brd9 y sus métodos de uso
EP4038066A1 (en) 2019-10-01 2022-08-10 Arvinas Operations, Inc. Brm targeting compounds and associated methods of use
CN115397821B (zh) 2019-10-17 2024-09-03 阿尔维纳斯运营股份有限公司 含有与bcl6靶向部分连接的e3泛素连接酶结合部分的双官能分子
WO2021097046A1 (en) 2019-11-13 2021-05-20 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds
CN110885332B (zh) * 2019-12-06 2022-03-18 中国人民解放军第二军医大学 一种PDEδ蛋白降解靶向嵌合体及其制备方法和应用
US12551564B2 (en) 2019-12-10 2026-02-17 Kymera Therapeutics, Inc. IRAK degraders and uses thereof
GB201918414D0 (en) 2019-12-13 2020-01-29 Z Factor Ltd Compounds and their use for the treatment of Alpha1-Antitrypsin deficiency
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
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
CA3165168A1 (en) * 2019-12-19 2021-06-24 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
BR112022011827A2 (pt) 2019-12-20 2022-08-30 C4 Therapeutics Inc Composto, composição farmacêutica, uso de um composto, métodos para tratamento ou profilaxia de câncer e para tratar um paciente com um distúrbio mediado por receptor do fator de crescimento epidérmico, e, invenção
BR112022012410A2 (pt) 2019-12-23 2022-08-30 Kymera Therapeutics Inc Degradadores smarca e usos dos mesmos
WO2021133917A1 (en) 2019-12-23 2021-07-01 Kymera Therapeutics, Inc. Smarca inhibitors and uses thereof
CA3162523A1 (en) 2019-12-23 2021-07-01 Hongfu LU Protein degradation agent compound preparation method and application
JP2023511280A (ja) * 2020-01-14 2023-03-17 ザ・トラスティーズ・オブ・コロンビア・ユニバーシティ・イン・ザ・シティ・オブ・ニューヨーク 内因性の脱ユビキチン化酵素をリダイレクトすることによる標的化されたタンパク質の安定化のための組成物及び方法
TW202140475A (zh) * 2020-01-16 2021-11-01 大陸商江蘇恆瑞醫藥股份有限公司 稠合醯亞胺類衍生物、其製備方法及其在醫藥上的應用
WO2021143822A1 (zh) * 2020-01-16 2021-07-22 江苏恒瑞医药股份有限公司 并环酰亚胺类衍生物、其制备方法及其在医药上的应用
US11618751B1 (en) 2022-03-25 2023-04-04 Ventus Therapeutics U.S., Inc. Pyrido-[3,4-d]pyridazine amine derivatives useful as NLRP3 derivatives
KR20260017503A (ko) 2020-02-14 2026-02-05 길리애드 사이언시즈, 인코포레이티드 Ccr8에 결합하는 항체 및 융합 단백질, 및 이의 용도
EP4107158A1 (en) 2020-02-19 2022-12-28 Nurix Therapeutics, Inc. Bifunctional degraders of interleukin-1 receptor-associated kinases and therapeutic use thereof
WO2023205701A1 (en) 2022-04-20 2023-10-26 Kumquat Biosciences Inc. Macrocyclic heterocycles and uses thereof
CA3173262A1 (en) 2020-02-26 2021-09-02 Cullgen (Shanghai), Inc. Tropomyosin receptor kinase (trk) degradation compounds and methods of use
EP3875456A1 (en) * 2020-03-02 2021-09-08 Technische Universität Darmstadt Hetero-bifunctional proteolysis-targeting chimeras (protacs) for the selective degradation of fk506-binding proteins (fkbps)
CN111249276B (zh) * 2020-03-05 2021-07-13 南京巴傲得生物科技有限公司 吲哚布洛芬制备cbp溴区抑制试剂的用途
AU2021231898A1 (en) 2020-03-05 2022-10-27 C4 Therapeutics, Inc. Compounds for targeted degradation of BRD9
US20230123104A1 (en) * 2020-03-06 2023-04-20 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Crystal of tricyclic compound acting on crbn protein and preparation method therefor
CN113387931A (zh) * 2020-03-13 2021-09-14 四川海思科制药有限公司 一种具有抑制或降解蛋白激酶的化合物及其制备方法和药学上的应用
WO2021185291A1 (zh) * 2020-03-17 2021-09-23 南京明德新药研发有限公司 蛋白降解调节剂与其使用方法
JP2023518202A (ja) * 2020-03-18 2023-04-28 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 Ｐｅｔトレーサーｐｂｂ３に基づく異常タウの標的化ディグレーダー
US12528785B2 (en) 2020-03-19 2026-01-20 Kymera Therapeutics, Inc. MDM2 degraders and uses thereof
US20230158158A1 (en) * 2020-03-27 2023-05-25 Uppthera Pyrazolo quinazoline derivative compounds inducing selective degradation of plk1
WO2021210878A1 (ko) * 2020-04-17 2021-10-21 광주과학기술원 Crbn 결합 펩티드 및 이를 이용한 알츠하이머 병 예방 또는 치료용 조성물
CN113563414B (zh) * 2020-04-29 2022-08-12 泰比棣医药科技(石家庄)有限公司 一种组织靶向的蛋白靶向降解化合物及其用途
CN113582974B (zh) * 2020-04-30 2022-05-17 江西济民可信集团有限公司 一类作为蛋白降解剂的化合物及其制备方法和医药用途
US20230357249A1 (en) * 2020-05-14 2023-11-09 The Regents Of The University Of Michigan Androgen receptor protein degraders with a tricyclic cereblon ligand
AU2021275146A1 (en) * 2020-05-21 2022-09-29 Dana-Farber Cancer Institute, Inc. Piperidine-2,6-diones as small molecule degraders of Helios and methods of use
TW202210483A (zh) 2020-06-03 2022-03-16 美商凱麥拉醫療公司 Irak降解劑之結晶型
CN113801098B (zh) * 2020-06-12 2023-05-30 上海济煜医药科技有限公司 酞嗪酮类化合物及其制备方法和医药用途
WO2021255212A1 (en) 2020-06-19 2021-12-23 F. Hoffmann-La Roche Ag Braf degraders
CA3178172A1 (en) * 2020-06-22 2021-12-30 Eric Fischer Protein tag to induce ligand dependent degradation of protein/protein-fusions
KR102559329B1 (ko) * 2020-07-02 2023-07-25 포항공과대학교 산학협력단 신규한 프로탁 키메라 화합물, 이를 포함하는 표적 단백질 분해를 통한 질환의 예방, 개선 또는 치료용 약학적 조성물
WO2022007903A1 (zh) * 2020-07-09 2022-01-13 四川海思科制药有限公司 一种能够抑制并降解雄激素受体的化合物及其药物组合物和药学上的应用
WO2022019597A1 (ko) * 2020-07-21 2022-01-27 주식회사 유빅스테라퓨틱스 안드로겐 수용체 분해용 화합물 및 이들의 의약 용도
KR20220014952A (ko) * 2020-07-29 2022-02-08 한국화학연구원 안드로겐 수용체의 저해 또는 분해용 화합물 및 이들의 의약 용도
KR20230048373A (ko) * 2020-08-03 2023-04-11 캡터 테라퓨틱스 에스.에이. 저분자량 단백질 분해제 및 이의 응용
EP4192458A4 (en) 2020-08-05 2024-09-04 C4 Therapeutics, Inc. COMPOUNDS FOR TARGETED DEGRADATION OF RET
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
JP7834721B2 (ja) 2020-08-28 2026-03-24 アルビナス・オペレーションズ・インコーポレイテッド 急速進行性線維肉腫タンパク質分解化合物及び関連する使用方法
WO2022048605A1 (zh) * 2020-09-04 2022-03-10 南昌奥瑞药业有限公司 一种杂环化合物、其制备方法、中间体、组合物以及应用
CN114163444B (zh) * 2020-09-11 2023-07-14 江苏恒瑞医药股份有限公司 一种用于雄激素受体蛋白靶向降解的嵌合体化合物、其制备方法及其在医药上的应用
AR123492A1 (es) 2020-09-14 2022-12-07 Arvinas Operations Inc Formas cristalinas y amorfas de un compuesto para la degradación dirigida del receptor de estrógeno
CN114181277A (zh) * 2020-09-15 2022-03-15 江苏恒瑞医药股份有限公司 一种用于雄激素受体蛋白靶向降解的嵌合体化合物、其制备方法及其在医药上的应用
WO2022066835A1 (en) 2020-09-23 2022-03-31 St. Jude Children's Research Hospital, Inc. Substituted n-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)arylsulfonamide analogs as modulators of cereblon protein
EP4221756A1 (en) * 2020-09-30 2023-08-09 Astrazeneca AB Compounds and their use in treating cancer
CN116457339A (zh) * 2020-10-14 2023-07-18 C4医药公司 用于医学治疗的降解新底物的三环化合物
AU2021365850A1 (en) 2020-10-21 2023-06-08 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor protein
EP4259144A4 (en) 2020-12-09 2025-08-20 Kymera Therapeutics Inc SMARCA DEGRADING AGENTS AND THEIR USES
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
JP2024504932A (ja) 2021-01-13 2024-02-02 モンテ ローザ セラピューティクス， インコーポレイテッド イソインドリノン化合物
EP4289841A4 (en) * 2021-02-04 2025-02-19 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Benzo seven-membered ring bifunctional compound and application 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
US20240383868A1 (en) * 2021-02-19 2024-11-21 Kymera Therapeutics, Inc. Smarca degraders and uses thereof
CN116940571A (zh) * 2021-03-15 2023-10-24 诺华股份有限公司 苯并异噁唑衍生物及其用途
EP4308559A1 (en) * 2021-03-15 2024-01-24 Novartis AG Benzisoxazole derivatives and uses thereof
KR20230160299A (ko) 2021-03-23 2023-11-23 누베이션 바이오 인크. 항암 핵 호르몬 수용체 표적화 화합물
MX2023011166A (es) * 2021-03-29 2023-09-29 Jiangsu Hengrui Pharmaceuticals Co Ltd Compuesto de tetrahidronaftaleno, metodo de preparacion y uso del mismo en medicina.
CN115141179B (zh) * 2021-03-31 2024-09-13 江苏恒瑞医药股份有限公司 一种新型苯并杂环基类衍生物、其制备方法及其在医药上的应用
US20240217968A1 (en) * 2021-03-31 2024-07-04 Duke Street Bio Limited Pharmaceutical compound
US11319319B1 (en) 2021-04-07 2022-05-03 Ventus Therapeutics U.S., Inc. Compounds for inhibiting NLRP3 and uses thereof
CN117279910A (zh) 2021-04-16 2023-12-22 阿尔维纳斯运营股份有限公司 Bcl6蛋白水解的调节剂和其相关使用方法
CN113603676B (zh) * 2021-04-28 2022-05-24 浙江工业大学 基于厄洛替尼靶向降解egfr蛋白小分子化合物及其制备方法和应用
US12006314B2 (en) * 2021-05-03 2024-06-11 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds
KR20240017814A (ko) 2021-05-05 2024-02-08 바이오젠 엠에이 인코포레이티드 브루톤 티로신 키나제의 분해를 표적으로 하는 화합물
AU2022271290A1 (en) 2021-05-07 2023-11-23 Kymera Therapeutics, Inc. Cdk2 degraders and uses thereof
TW202313094A (zh) 2021-05-18 2023-04-01 美商基利科學股份有限公司 使用ＦＬＴ３Ｌ—Ｆｃ融合蛋白之方法
WO2022250350A1 (ko) * 2021-05-26 2022-12-01 주식회사 이노큐어테라퓨틱스 피페리딘디온 유도체
KR102474999B1 (ko) * 2021-05-26 2022-12-07 주식회사 이노큐어테라퓨틱스 피페리딘디온 유도체
JP2024519628A (ja) * 2021-05-26 2024-05-21 イノキュア セラピューティクス インコーポレイテッド ピペリジンジオン誘導体
KR102489160B1 (ko) * 2021-05-26 2023-01-18 주식회사 이노큐어테라퓨틱스 피페리딘디온 유도체
WO2022255889A1 (en) * 2021-06-01 2022-12-08 Captor Therapeutics S.A. Compounds which bind to cereblon, and use thereof
WO2022255888A1 (en) * 2021-06-01 2022-12-08 Captor Therapeutics S.A. Targeted protein degradation using bifunctional compounds that bind ubiquitin ligase and target mcl-1 protein
WO2022255890A1 (en) * 2021-06-01 2022-12-08 Captor Therapeutics S.A. Compounds which bind to cereblon, and use thereof
WO2022261250A1 (en) 2021-06-08 2022-12-15 C4 Therapeutics, Inc. Therapeutics for the degradation of mutant braf
EP4359404A4 (en) * 2021-06-25 2025-06-04 Celgene Corporation Cereblon-binding compounds, compositions thereof and methods of treatment therewith
EP4359407A4 (en) * 2021-06-25 2025-04-30 Celgene Corporation CEREBLON-BINDING COMPOUNDS, COMPOSITIONS THEREOF AND METHODS OF TREATMENT USING THEM
JP2024526192A (ja) * 2021-06-25 2024-07-17 セルジーン コーポレーション セレブロン結合化合物、その組成物及びそれによる治療方法
US20250129047A1 (en) 2021-07-04 2025-04-24 Newave Pharmaceutical Inc. Isoquinoline derivatives as mutant egfr modulators and uses thereof
KR20240035526A (ko) 2021-07-07 2024-03-15 바이오젠 엠에이 인코포레이티드 Irak4 단백질의 분해를 표적하는 화합물
WO2023283372A1 (en) 2021-07-07 2023-01-12 Biogen Ma Inc. Compounds for targeting degradation of irak4 proteins
KR20240035820A (ko) 2021-07-09 2024-03-18 플렉시움 인코포레이티드 Ikzf2를 조절하는 아릴 화합물 및 약학 조성물
EP4157849A4 (en) * 2021-08-10 2024-12-11 Uppthera, Inc. NOVEL PLK1 DEGRADATION-INDUCING COMPOUND
US20250171417A1 (en) * 2021-08-11 2025-05-29 Xizang Haisco Pharmaceutical Co., Ltd. Heterocyclic derivative, and composition and pharmaceutical use thereof
FI4367118T3 (fi) 2021-08-18 2025-04-09 Nurix Therapeutics Inc Interleukiini-1-reseptoriin liittyvien kinaasien bifunktionaalisia hajotusaineita ja niiden terapeuttinen käyttö
CA3229646A1 (en) * 2021-08-23 2023-03-02 Zhengqing YE Irak4 degradation agent, and preparation method therefor and use thereof
WO2023034411A1 (en) 2021-09-01 2023-03-09 Oerth Bio Llc Compositions and methods for targeted degradation of proteins in a plant cell
CN115746058A (zh) * 2021-09-03 2023-03-07 南京知和医药科技有限公司 一种多环化合物在制备抗肿瘤药物方面的用途
WO2023056443A1 (en) * 2021-10-01 2023-04-06 Dana-Farber Cancer Institute, Inc. Binders of cereblon and methods of use thereof
WO2023059792A1 (en) * 2021-10-06 2023-04-13 C4 Thrapeutics, Inc. Coronavirus non-structural protein 3 degrading compounds
AU2022370021B2 (en) * 2021-10-22 2026-04-16 Gluetacs Therapeutics (Shanghai) Co., Ltd. Crbn e3 ligase ligand compound, protein degrading agent developed on the basis of ligand compound, and their applications
US20230183216A1 (en) 2021-10-28 2023-06-15 Gilead Sciences, Inc. Pyridizin-3(2h)-one derivatives
EP4422756A1 (en) 2021-10-29 2024-09-04 Gilead Sciences, Inc. Cd73 compounds
US12187744B2 (en) 2021-10-29 2025-01-07 Kymera Therapeutics, Inc. IRAK4 degraders and synthesis thereof
WO2023081224A1 (en) * 2021-11-03 2023-05-11 St. Jude Children's Research Hospital, Inc. Substituted n-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4- yl)methyl)benzamide analogs as modulators of cereblon protein
WO2023081452A1 (en) * 2021-11-05 2023-05-11 University Of South Carolina Small-molecule degraders of cdk8 and cdk19
CA3238118A1 (en) * 2021-11-18 2023-05-25 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Fused imide derivative
WO2023096987A1 (en) 2021-11-24 2023-06-01 Arvinas Operations, Inc. Brm targeting compounds and associated methods of use
JP2024541480A (ja) 2021-11-24 2024-11-08 アルビナス・オペレーションズ・インコーポレイテッド Ｂｒｍ標的化化合物及び関連使用方法
JP2024543129A (ja) 2021-11-25 2024-11-19 江蘇恒瑞医薬股▲ふん▼有限公司 アンドロゲン受容体タンパク質の標的分解のためのキメラ化合物、その調製方法及びその医薬的使用
CN118488946A (zh) 2021-12-22 2024-08-13 吉利德科学公司 Ikaros锌指家族降解剂及其用途
EP4452415B1 (en) 2021-12-22 2026-02-25 Gilead Sciences, Inc. Ikaros zinc finger family degraders and uses thereof
CN114085213B (zh) * 2022-01-20 2022-03-25 苏州国匡医药科技有限公司 一种arv-471的制备方法
TW202340168A (zh) 2022-01-28 2023-10-16 美商基利科學股份有限公司 Ｐａｒｐ７抑制劑
EP4472967A4 (en) 2022-01-31 2026-04-15 Kymera Therapeutics Inc Iraqi Degradation Agents and Their Uses
CA3253296A1 (en) 2022-03-17 2023-09-21 Gilead Sciences, Inc. Zinc Finger Degradation Agents of the Ikaros Family and Their Uses
CN119301111A (zh) * 2022-03-24 2025-01-10 葛兰素史密斯克莱知识产权发展有限公司 作为protac中的降解决定子的2,4-二氧代四氢嘧啶基衍生物
WO2023205719A1 (en) 2022-04-21 2023-10-26 Gilead Sciences, Inc. Kras g12d modulating compounds
WO2023212599A2 (en) * 2022-04-26 2023-11-02 Endotarget Inc. Compounds and methods for targeted degradation of estrogen receptors
JP2025523393A (ja) 2022-06-06 2025-07-23 シーフォー セラピューティクス， インコーポレイテッド 二環式置換グルタルイミドセレブロンバインダー
AU2023300784A1 (en) * 2022-06-30 2025-01-02 Anhorn Medicines Co., Ltd. Bifunctional compound and pharmaceutical composition comprising the bifunctional compound, and method for treating androgen receptor related diseases by using the same
US20240116928A1 (en) 2022-07-01 2024-04-11 Gilead Sciences, Inc. Cd73 compounds
KR20250047743A (ko) * 2022-07-12 2025-04-04 리젠츠 오브 더 유니버시티 오브 미시간 에스트로겐 수용체 분해제로서의 테트라하이드로나프탈렌 유도체
CN116496253B (zh) * 2022-08-19 2024-10-11 中国人民解放军军事科学院军事医学研究院 c-MET蛋白靶向降解剂及其医药应用
CN115089588A (zh) * 2022-08-22 2022-09-23 云南大学 达沙布韦作为e3连接酶新型配体构建protac的应用
WO2024050016A1 (en) 2022-08-31 2024-03-07 Oerth Bio Llc Compositions and methods for targeted inhibition and degradation of proteins in an insect cell
EP4584258A1 (en) 2022-09-07 2025-07-16 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use
WO2024054954A1 (en) * 2022-09-08 2024-03-14 Halda Therapeutics Opco, Inc. Heterobifunctional compounds and methods of treating disease
WO2024054953A1 (en) * 2022-09-08 2024-03-14 Halda Therapeutics Opco, Inc. Heterobifunctional compounds and methods of treating disease
WO2024054955A1 (en) * 2022-09-08 2024-03-14 Halda Therapeutics Opco, Inc. Heterobifunctional compounds and methods of treating disease
CN118019736A (zh) * 2022-09-08 2024-05-10 标新生物医药科技(上海)有限公司 基于cereblon蛋白设计的分子胶化合物及其应用
CN120303264A (zh) 2022-09-09 2025-07-11 医诺康治疗公司 CK1α和双重CK1α/GSPT1降解化合物
CN119855812A (zh) * 2022-09-14 2025-04-18 海南先声再明医药股份有限公司 多并环类化合物及其用途
WO2024064316A1 (en) 2022-09-23 2024-03-28 Regents Of The University Of Michigan Compounds and compositions as smarca2/4 inhibitors and uses thereof
WO2024073475A1 (en) * 2022-09-27 2024-04-04 Oncopia Therapeutics, Inc. D/B/A Proteovant Therapeutics, Inc. Cereblon ligands and uses thereof
US20260098027A1 (en) * 2022-09-29 2026-04-09 Jiangsu Hengrui Pharmaceuticals Co., Ltd. Pharmaceutically acceptable salt and crystal form of tetrahydronaphthalene derivative, and preparation method
WO2024067793A1 (zh) * 2022-09-29 2024-04-04 海南先声再明医药股份有限公司 一类稠环化合物及其用途
CN117801051A (zh) * 2022-09-30 2024-04-02 苏州德亘生物医药有限公司 一类eRF3a靶向蛋白降解机制治疗人类肿瘤的药物
JP2026500894A (ja) 2022-10-24 2026-01-09 アルヴィナス・オペレーションズ・インコーポレイテッド アンドロゲン受容体の標的分解のための化合物及び方法
US12331048B2 (en) 2022-10-31 2025-06-17 Ventus Therapeutics U.S., Inc. Pyrido-[3,4-d]pyridazine amine derivatives useful as NLRP3 inhibitors
KR20240076745A (ko) * 2022-11-22 2024-05-30 주식회사 이노큐어테라퓨틱스 신규한 c-MET 단백질 리간드를 포함하는 디그레이더 및 이를 포함하는 약학 조성물
WO2024112122A1 (ko) * 2022-11-22 2024-05-30 주식회사 이노큐어테라퓨틱스 Brd 단백질을 분해하는 디그레이더 및 이를 포함하는 약학 조성물
JP2025538556A (ja) * 2022-11-22 2025-11-28 イノキュア セラピューティクス，インコーポレイテッド Ｃｍｅｔタンパク質を分解するための分解剤、およびそれを含む薬学的組成物
WO2024123195A1 (en) * 2022-12-06 2024-06-13 Captor Therapeutics S.A. Targeted protein degradation using prodrugs of bifunctional compounds that bind ubiquitin ligase and target mcl-1 protein
JP2025540970A (ja) * 2022-12-06 2025-12-17 キャプター セラピューティクス エス．エー． ユビキチンリガーゼ及びターゲットｍｃｌ－１タンパク質に結合する二機能性化合物を使用するターゲティングされたタンパク質分解
EP4638436A1 (en) 2022-12-22 2025-10-29 Gilead Sciences, Inc. Prmt5 inhibitors and uses thereof
WO2024153025A1 (zh) * 2023-01-16 2024-07-25 南京明德新药研发有限公司 取代的苯并七元环化合物及其应用
CN121419983A (zh) 2023-01-26 2026-01-27 阿尔维纳斯运营股份有限公司 基于小脑蛋白的kras降解protac及其相关用途
KR20250145679A (ko) * 2023-02-16 2025-10-13 브리스톨-마이어스 스큅 컴퍼니 Ret 키나제의 분해제로서의 이소인돌리논 글루타르이미드 및 페닐 글루타르이미드 유사체
CN116253719B (zh) * 2023-03-06 2025-04-01 苏州国匡医药科技有限公司 一种雌激素和雄激素受体双重降解剂及其应用
US20240374588A1 (en) 2023-04-07 2024-11-14 Astrazeneca Ab Irak4 protacs
CN120882725A (zh) 2023-04-11 2025-10-31 吉利德科学公司 Kras调节化合物
AU2024256729A1 (en) * 2023-04-20 2025-09-25 Auron Therapeutics, Inc. Technologies targeting cell states
WO2024220917A1 (en) 2023-04-21 2024-10-24 Gilead Sciences, Inc. Prmt5 inhibitors and uses thereof
CN120981456A (zh) 2023-05-24 2025-11-18 金橘生物科技公司 杂环化合物及其用途
CN119451952A (zh) * 2023-06-01 2025-02-14 标新生物医药科技(上海)有限公司 氧代异吲哚啉基取代的四氢嘧啶二酮衍生物及其应用
EP4722206A1 (en) * 2023-06-01 2026-04-08 Haihe Biopharma Co., Ltd. Benzo(hetero)cycloalkyl compounds for androgen receptor-dependent diseases
CN120202200A (zh) * 2023-06-01 2025-06-24 标新生物医药科技(上海)有限公司 基于氧代异吲哚啉基取代的四氢嘧啶二酮的化合物及其应用
TW202515566A (zh) 2023-06-14 2025-04-16 瑞典商阿斯特捷利康公司 Ｓｍａｒｃａ２降解劑及其用途
MX2025015084A (es) 2023-06-14 2026-02-03 Astrazeneca Ab Degradadores de smarca2 y usos de estos
AU2024312123A1 (en) * 2023-06-23 2026-01-08 Fox Chase Chemical Diversity Center, Inc. Targeted degraders of hiv-1 nef for the treatment of hiv disease
AU2024307234A1 (en) 2023-06-30 2026-01-29 Kumquat Biosciences Inc. Substituted condensed tricyclic amine compounds and uses thereof as ras inhibitors
WO2025006783A2 (en) 2023-06-30 2025-01-02 Merck Patent Gmbh Heterobifunctional compounds for the degradation of kras
US20250042922A1 (en) 2023-06-30 2025-02-06 Gilead Sciences, Inc. Kras modulating compounds
WO2025006753A2 (en) 2023-06-30 2025-01-02 Merck Patent Gmbh Heterobifunctional compounds for the degradation of kras protein
US20250066328A1 (en) 2023-07-26 2025-02-27 Gilead Sciences, Inc. Parp7 inhibitors
AU2024297978A1 (en) 2023-07-26 2026-02-05 Gilead Sciences, Inc. Parp7 inhibitors
WO2025049555A1 (en) 2023-08-31 2025-03-06 Oerth Bio Llc Compositions and methods for targeted inhibition and degradation of proteins in an insect cell
WO2025054347A1 (en) 2023-09-08 2025-03-13 Gilead Sciences, Inc. Kras g12d modulating compounds
AU2024337913A1 (en) 2023-09-08 2026-03-26 Gilead Sciences, Inc. Pyrimidine-containing polycyclic derivatives as kras g12d modulating compounds
CN119613374A (zh) * 2023-09-14 2025-03-14 中国科学院上海药物研究所 吲唑酮类化合物、其制备方法、药物组合物及其应用
WO2025063888A1 (en) 2023-09-19 2025-03-27 Kancure Pte. Ltd. Survivin-targeted compounds
IL326555A (en) 2023-09-22 2026-04-01 Glaxosmithkline Ip Dev Ltd Androgen receptor protax
CN121925410A (zh) 2023-09-29 2026-04-24 第一三共株式会社 3-苯基丙胺衍生物
WO2025075693A1 (en) * 2023-10-02 2025-04-10 Purdue Research Foundation Shp2 degraders for cancer therapy
WO2025096855A1 (en) 2023-11-02 2025-05-08 Kumquat Biosciences Inc. Degraders and uses thereof
US20250154172A1 (en) 2023-11-03 2025-05-15 Gilead Sciences, Inc. Prmt5 inhibitors and uses thereof
US20250177539A1 (en) * 2023-12-01 2025-06-05 Astrazeneca Ab Er degraders and uses thereof
WO2025137640A1 (en) 2023-12-22 2025-06-26 Gilead Sciences, Inc. Azaspiro wrn inhibitors
WO2025136129A1 (en) * 2023-12-22 2025-06-26 Captor Therapeutics S.A. Targeted protein degradation using bifunctional compounds that bind ubiquitin ligase and target protein kinase c
WO2025179161A1 (en) 2024-02-21 2025-08-28 Innovo Therapeutics, Inc. Protein degrading compounds
WO2025188857A1 (en) * 2024-03-05 2025-09-12 University Of Florida Research Foundation, Incorporated Hdac8 degraders and uses thereof
TW202543650A (zh) 2024-03-08 2025-11-16 美商海爾達醫療運營公司 異雙官能化合物及其在治療疾病中之用途
WO2025212557A1 (en) * 2024-04-01 2025-10-09 The Johns Hopkins University Delivery of aurora kinase inhibitors using nano-scale drug delivery platforms by covalent conjugation
US20250376484A1 (en) 2024-05-21 2025-12-11 Gilead Sciences, Inc. Prmt5 inhibitors and uses thereof
KR20260001534A (ko) * 2024-06-27 2026-01-05 한미약품 주식회사 신규한 이종이작용기 단백질 분해제 및 이의 용도
WO2026039365A1 (en) 2024-08-12 2026-02-19 Gilead Sciences, Inc. Kras modulating compounds
CN119241498B (zh) * 2024-09-26 2026-04-07 天津科技大学 一种具有抗mash活性的acly靶向protac嵌合体、方法和应用

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015160845A2 (en) * 2014-04-14 2015-10-22 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
US20160243247A1 (en) * 2014-12-23 2016-08-25 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
WO2016197032A1 (en) * 2015-06-04 2016-12-08 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
WO2017007612A1 (en) * 2015-07-07 2017-01-12 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
WO2017011371A1 (en) * 2015-07-10 2017-01-19 Arvinas, Inc Mdm2-based modulators of proteolysis and associated methods of use

Family Cites Families (137)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2460304C2 (de) 1974-12-20 1983-08-04 Grünenthal GmbH, 5190 Stolberg 1-n-Propyl-4-phthalimido-piperidin-2,6-dion, Verfahren zu seiner Herstellung und dieses enthaltende Arzneimittel
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
US5510357A (en) 1995-02-28 1996-04-23 Eli Lilly And Company Benzothiophene compounds as anti-estrogenic agents
NZ333903A (en) 1996-07-24 2000-02-28 Celgene Corp Substituted 2(2,6-dioxopiperidin-3-yl)phthalimides and -1oxoisoindolines and method of reducing TNF-alpha levels in a mammal
CA2287387C (en) 1997-05-14 2010-02-16 Sloan-Kettering Institute For Cancer Research Methods and compositions for destruction of selected proteins
JP2001517664A (ja) 1997-09-23 2001-10-09 イーライ・リリー・アンド・カンパニー ベンゾチオフェン類
ES2241192T3 (es) 1997-12-17 2005-10-16 MERCK & CO., INC. (A NEW JERSEY CORP.) Antagonistas del receptor de integrina.
JP2002523455A (ja) 1998-08-31 2002-07-30 スージェン・インコーポレーテッド 蛋白質キナーゼ活性の調節剤としての幾何学的に制限された２−インドリノン誘導体
US6306663B1 (en) 1999-02-12 2001-10-23 Proteinex, Inc. Controlling protein levels in eucaryotic organisms
US6333344B1 (en) 1999-05-05 2001-12-25 Merck & Co. Prolines as antimicrobial agents
BR0111298A (pt) 2000-06-28 2005-05-10 Bristol Myers Squibb Co Moduladores seletivos dos receptores de andrógenos e métodos para identificação, projeto e uso dos mesmos
PE20020354A1 (es) 2000-09-01 2002-06-12 Novartis Ag Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda)
US7041298B2 (en) 2000-09-08 2006-05-09 California Institute Of Technology Proteolysis targeting chimeric pharmaceutical
US7208157B2 (en) 2000-09-08 2007-04-24 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
CA2432932A1 (en) 2001-02-16 2002-08-29 Mark A. Scialdone Angiogenesis-inhibitory tripeptides, compositions and their methods of use
GB0106953D0 (en) 2001-03-20 2001-05-09 Univ Aberdeen Neufofibrillary labels
HN2002000136A (es) 2001-06-11 2003-07-31 Basf Ag Inhibidores de la proteasa del virus hiv, compuestos que contienen a los mismos, sus usos farmaceuticos y los materiales para su sintesis
US7030141B2 (en) 2001-11-29 2006-04-18 Christopher Franklin Bigge Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
CN102342938B (zh) 2002-05-17 2014-08-20 细胞基因公司 用于治疗和控制实体瘤的方法及组合物
WO2004020434A1 (ja) 2002-08-30 2004-03-11 Eisai Co., Ltd. 含窒素芳香環誘導体
DE602004025708D1 (de) * 2003-07-11 2010-04-08 Proteologics Inc Ubiquitin-ligase-hemmer und verwandte verfahren
EP1781598A1 (en) 2004-07-08 2007-05-09 Warner-Lambert Company LLC Androgen modulators
CN100383139C (zh) 2005-04-07 2008-04-23 天津和美生物技术有限公司 可抑制细胞释放肿瘤坏死因子的哌啶-2，6-二酮衍生物
WO2006113942A2 (en) 2005-04-20 2006-10-26 Schering Corporation Method of inhibiting cathepsin activity
CN102206216B (zh) 2005-06-22 2014-11-12 普莱希科公司 作为蛋白质激酶抑制剂的吡咯并[2,3-b]吡啶衍生物
KR20080042158A (ko) 2005-08-31 2008-05-14 셀진 코포레이션 이소인돌-이미드 화합물과 이를 포함하는 조성물 및 이를이용한 방법
BRPI0708524A2 (pt) 2006-03-03 2011-05-31 Novartis Ag compostos de n-formil hidroxilamina
KR101456722B1 (ko) 2006-03-29 2014-10-31 더 리전트 오브 더 유니버시티 오브 캘리포니아 디아릴티오히단토인 화합물
JP2009544620A (ja) 2006-07-20 2009-12-17 リガンド・ファーマシューティカルズ・インコーポレイテッド 自己免疫疾患及び炎症のためのプロリン尿素ｃｃｒ１アンタゴニスト
RU2448101C2 (ru) 2006-08-30 2012-04-20 Селджин Корпорейшн 5-замещенные изоиндолиновые соединения
MX2009001989A (es) 2006-08-30 2009-03-09 Celgene Corp Compuestos de isoindolina 5-substituidos.
US8877780B2 (en) 2006-08-30 2014-11-04 Celgene Corporation 5-substituted isoindoline compounds
CA2668286C (en) 2006-11-03 2014-09-16 Pharmacyclics, Inc. Bruton's tyrosine kinase activity probe and method of using
WO2008087643A2 (en) * 2007-01-16 2008-07-24 Proteologics Ltd Methods for enhancing the therapeutic efficacy of topoisomerase inhibitors
KR20100038108A (ko) 2007-07-25 2010-04-12 브리스톨-마이어스 스큅 컴퍼니 트리아진 키나제 억제제
CN101820765A (zh) 2007-07-31 2010-09-01 安德鲁科技有限公司 包含雄激素受体降解(ard)增强剂的组合物和预防性或治疗性治疗皮肤病与脱发的方法
WO2009084693A1 (ja) 2007-12-28 2009-07-09 Mitsubishi Tanabe Pharma Corporation 抗癌剤
PE20110547A1 (es) 2008-10-29 2011-08-04 Celgene Corp Compuestos de isoindolina con actividad anticancerigena
US8691187B2 (en) 2009-03-23 2014-04-08 Eli Lilly And Company Imaging agents for detecting neurological disorders
WO2010141805A1 (en) 2009-06-05 2010-12-09 Janssen Pharmaceutica Nv Heterocyclic amides as modulators of trpa1
JP2012532929A (ja) * 2009-07-13 2012-12-20 プレジデント アンド フェロウズ オブ ハーバード カレッジ 二機能性のステープリングされたポリペプチドおよびそれらの使用
EP2536706B1 (en) 2010-02-11 2017-06-14 Celgene Corporation Arylmethoxy isoindoline derivatives and compositions comprising and methods of using the same
US8198300B2 (en) 2010-04-29 2012-06-12 Universidad De Chile Method for preventing tau protein aggregation and treating Alzheimer's disease with a quinoline derivative compound
MX354217B (es) 2010-05-14 2018-02-19 Dana Farber Cancer Inst Inc Composiciones y metodos para el tratamiento de leucemia.
PL2902030T3 (pl) 2010-05-14 2017-07-31 Dana-Farber Cancer Institute, Inc. Związki tienotriazolodiazepinowe do leczenia nowotworu
SG186389A1 (en) 2010-06-30 2013-01-30 Univ Brandeis Small-molecule-targeted protein degradation
WO2012040389A2 (en) 2010-09-22 2012-03-29 Presidio Pharmaceuticals, Inc. Substituted bicyclic hcv inhibitors
EP2619184B1 (en) 2010-09-24 2018-05-23 The Regents of the University of Michigan Deubiquitinase inhibitors and methods for use of the same
CN102477033A (zh) 2010-11-23 2012-05-30 苏州波锐生物医药科技有限公司 苯并噻酚类化合物及其在制备预防和/或治疗乳腺癌骨质疏松症药物中的用途
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
AU2011338615B2 (en) 2010-12-07 2017-07-27 Yale University Small-molecule hydrophobic tagging of fusion proteins and induced degradation of same
US20140243282A1 (en) 2010-12-31 2014-08-28 Satish Reddy Kallam Methods and compositions for designing novel conjugate therapeutics
CA2834535A1 (en) 2011-04-29 2012-11-01 Celgene Corporation Methods for the treatment of cancer and inflammatory diseases using cereblon as a predictor
US9273046B2 (en) 2011-12-31 2016-03-01 Beigene, Ltd. Fused tricyclic compounds as Raf kinase inhibitors
WO2013106646A2 (en) 2012-01-12 2013-07-18 Yale University Compounds and methods for the inhibition of vcb e3 ubiquitin ligase
CA2861066C (en) * 2012-01-12 2024-01-02 Yale University Compounds and methods for the enhanced degradation of targeted proteins and other polypeptides by an e3 ubiquitin ligase
US20150141470A1 (en) 2012-05-08 2015-05-21 The Broad Institute, Inc. Diagnostic and treatment methods in patients having or at risk of developing resistance to cancer therapy
US20150119435A1 (en) 2012-05-11 2015-04-30 Yale University Compounds useful for promoting protein degradation and methods using same
MX2014015986A (es) 2012-06-25 2016-02-11 Oncoethix Gmbh Metodo para tratar linfoma utilizando compuestos de tienotriazolodiazepina.
CA2879454A1 (en) 2012-07-19 2014-01-23 Drexel University Novel sigma receptor ligands and methods of modulating cellular protein homeostasis using same
JP6407504B2 (ja) 2012-09-21 2018-10-17 アログ・ファーマシューティカルズ・インコーポレイテッドＡｒｏｇ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． 恒常的に活性であるリン酸化型ｆｌｔ３キナーゼの阻害方法
GB201311910D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel Compounds
NL2011274C2 (en) 2013-08-06 2015-02-09 Illumicare Ip B V 51 Groundbreaking platform technology for specific binding to necrotic cells.
EP2958923A1 (de) 2013-02-22 2015-12-30 Bayer Pharma Aktiengesellschaft 4-substituierte pyrrolo- und pyrazolo-diazepine
US9492460B2 (en) 2013-02-27 2016-11-15 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
WO2015011084A1 (de) 2013-07-23 2015-01-29 Bayer Pharma Aktiengesellschaft Substituierte dihydropyrido[3,4-b]pyrazinone als duale inhibitoren von bet-proteinen und polo-like kinasen
JP6542212B2 (ja) 2013-07-31 2019-07-10 ゼニス・エピジェネティクス・リミテッドＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｌｔｄ． ブロモドメイン阻害剤としての新規キナゾリノン
US20150051208A1 (en) 2013-08-14 2015-02-19 Boehringer Ingelheim International Gmbh Pyridinones
US9428513B2 (en) 2013-11-07 2016-08-30 Boehringer Ingelheim International Gmbh Triazolopyrazine
JP6553632B2 (ja) 2013-11-18 2019-07-31 フォーマ セラピューティクス，インコーポレイテッド Ｂｅｔブロモドメイン阻害剤としてのテトラヒドロキノリン組成物
US9399640B2 (en) 2013-11-26 2016-07-26 Incyte Corporation Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors
US9458156B2 (en) 2014-12-23 2016-10-04 Bristol-Myers Squibb Company Tricyclic compounds as anticancer agents
US20150259288A1 (en) 2014-03-14 2015-09-17 City Of Hope 5-bromo-indirubins
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
US20160058872A1 (en) 2014-04-14 2016-03-03 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
TW201613916A (en) 2014-06-03 2016-04-16 Gilead Sciences Inc TANK-binding kinase inhibitor compounds
CA2953237C (en) 2014-06-06 2024-06-11 The Scripps Research Institute Sulfur(vi) fluoride compounds and methods for the preparation thereof
WO2015195863A1 (en) 2014-06-20 2015-12-23 Constellation Pharmaceuticals, Inc. Hydrated 2-((4s)-6-(4-chlorophenyl)-1 -methyl-4h-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide
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
AU2015326910B2 (en) 2014-10-02 2018-03-01 Glaxosmithkline Intellectual Property (No.2) Limited Compound
BR112017008714A2 (pt) 2014-10-27 2017-12-19 Tensha Therapeutics Inc inibidores de bromodomínio
CN107406424B (zh) * 2014-12-18 2020-08-25 豪夫迈·罗氏有限公司 雌激素受体调节剂及其用途
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
GB201504314D0 (en) 2015-03-13 2015-04-29 Univ Dundee Small molecules
US10730870B2 (en) 2015-03-18 2020-08-04 Arvinas Operations, Inc. Compounds and methods for the enhanced degradation of targeted proteins
GB201506871D0 (en) * 2015-04-22 2015-06-03 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201506872D0 (en) 2015-04-22 2015-06-03 Ge Oil & Gas Uk Ltd Novel compounds
WO2016197114A1 (en) 2015-06-05 2016-12-08 Arvinas, Inc. Tank-binding kinase-1 protacs 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
WO2017024318A1 (en) 2015-08-06 2017-02-09 Dana-Farber Cancer Institute, Inc. Targeted protein degradation to attenuate adoptive t-cell therapy associated adverse inflammatory responses
EP3337476A4 (en) 2015-08-19 2019-09-04 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
GB201516243D0 (en) 2015-09-14 2015-10-28 Glaxosmithkline Ip Dev Ltd Novel compounds
AU2016349781A1 (en) * 2015-11-02 2018-05-10 Yale University Proteolysis targeting chimera compounds and methods of preparing and using same
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
EP3445357B1 (en) 2016-04-22 2021-05-26 Dana-Farber Cancer Institute, Inc. Bifunctional molecules for degradation of egfr and methods of use
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
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
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
WO2018053354A1 (en) 2016-09-15 2018-03-22 Arvinas, Inc. Indole derivatives as estrogen receptor degraders
WO2018071606A1 (en) 2016-10-11 2018-04-19 Arvinas, Inc. Compounds and methods for the targeted degradation of androgen receptor
IL290809B2 (en) 2016-11-01 2024-01-01 Arvinas Operations Inc Tau-protein targeting protacs and associated methods of use
CA3042301A1 (en) 2016-11-22 2018-05-31 Dana-Farber Cancer Institute, Inc. Degradation of protein kinases by conjugation of protein kinase inhibitors with e3 ligase ligand and methods of use
KR102674902B1 (ko) 2016-12-01 2024-06-14 아비나스 오퍼레이션스, 인코포레이티드 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 및 테트라히드로이소퀴놀린 유도체
US10806737B2 (en) 2016-12-23 2020-10-20 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of fetal liver kinase polypeptides
CN117510491A (zh) 2016-12-23 2024-02-06 阿尔维纳斯运营股份有限公司 用于迅速加速性纤维肉瘤多肽的靶向降解的化合物和方法
MX2019007646A (es) 2016-12-23 2019-09-06 Arvinas Operations Inc Moleculas quimericas dirigidas a la proteolisis del egfr y metodos asociados de uso.
US11191741B2 (en) 2016-12-24 2021-12-07 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide
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
US10787443B2 (en) 2017-04-28 2020-09-29 Zamboni Chem Solutions Inc. RAF-degrading conjugate compounds
AU2018261331C1 (en) 2017-05-01 2022-08-04 Spg Therapeutics, Inc. Tripartite androgen receptor eliminators, methods and uses thereof
WO2019079701A1 (en) 2017-10-20 2019-04-25 Dana-Farber Cancer Institute, Inc. HETEROBIFUNCTIONAL COMPOUNDS HAVING IMPROVED SPECIFICITY FOR BRD4 BROMODOMAINE
US11220515B2 (en) 2018-01-26 2022-01-11 Yale University Imide-based modulators of proteolysis and associated methods of use
DK3904350T3 (da) 2018-04-12 2023-11-13 Bayer Ag N-(cyclopropylmethyl)-5-(methylsulfonyl)-n-{1-[1-(pyrimidin-2-yl)-1h-1,2,4-triazol-5-yl]ethyl}benzamidderivater og de tilsvarende pyridincarboxamidderivater som pesticider
CA3165238A1 (en) 2019-12-19 2021-06-24 Jacobio Pharmaceuticals Co., Ltd. Kras mutant protein inhibitors
CR20220291A (es) 2019-12-19 2022-08-10 Bayer Ag Derivados de furoindazol
CN114867715A (zh) 2019-12-19 2022-08-05 斯奇诺西维 粘附性光保护化合物及其用途
EP4077324A1 (en) 2019-12-19 2022-10-26 Debiopharm International SA Novel compounds and their use
CA3165168A1 (en) 2019-12-19 2021-06-24 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
JP7554829B2 (ja) 2019-12-19 2024-09-20 ヤンセン ファーマシューティカ エヌ．ベー． 置換直鎖スピロ誘導体
CA3162523A1 (en) 2019-12-23 2021-07-01 Hongfu LU Protein degradation agent compound preparation method and application
KR20220132543A (ko) 2019-12-27 2022-09-30 루핀 리미티드 치환된 삼환 화합물
KR20230028268A (ko) 2020-05-29 2023-02-28 뵈링거 잉겔하임 애니멀 헬스 유에스에이 인코포레이티드 구충성 헤테로시클릭 화합물
JP2023501757A (ja) 2020-05-29 2023-01-18 ブループリント メディシンズ コーポレイション プラルセチニブ薬学的組成物
KR20230118147A (ko) 2020-12-11 2023-08-10 아비나스 오퍼레이션스, 인코포레이티드 전립선암 치료 방법
CN117120034A (zh) 2021-02-15 2023-11-24 普洛佩拉治疗公司 阿比特龙前药
JP2026500894A (ja) 2022-10-24 2026-01-09 アルヴィナス・オペレーションズ・インコーポレイテッド アンドロゲン受容体の標的分解のための化合物及び方法
KR20250163975A (ko) 2023-03-30 2025-11-21 아비나스 오퍼레이션스, 인코포레이티드 안드로겐 수용체의 표적 분해를 위한 화합물의 결정질 형태
CN121487737A (zh) 2023-06-30 2026-02-06 阿维纳斯企业公司 用于雄激素受体的靶向降解的化合物和方法

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015160845A2 (en) * 2014-04-14 2015-10-22 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
US20160243247A1 (en) * 2014-12-23 2016-08-25 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
WO2016197032A1 (en) * 2015-06-04 2016-12-08 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
WO2017007612A1 (en) * 2015-07-07 2017-01-12 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
WO2017011371A1 (en) * 2015-07-10 2017-01-19 Arvinas, Inc Mdm2-based modulators of proteolysis and associated methods of use

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2025011623A1 (zh) * 2023-07-12 2025-01-16 上海壹迪生物技术有限公司 氰基喹啉类靶向蛋白降解分子、其制备方法和应用
WO2025036489A1 (zh) 2023-08-17 2025-02-20 海思科医药集团股份有限公司 一种氰基芳香环衍生物及其在医药上的应用

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