JP2019537585A - Ｅｚｈ２媒介性がんを治療するための組成物および方法 - Google Patents

Ｅｚｈ２媒介性がんを治療するための組成物および方法 Download PDF

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JP2019537585A
JP2019537585A JP2019522841A JP2019522841A JP2019537585A JP 2019537585 A JP2019537585 A JP 2019537585A JP 2019522841 A JP2019522841 A JP 2019522841A JP 2019522841 A JP2019522841 A JP 2019522841A JP 2019537585 A JP2019537585 A JP 2019537585A
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mmol
ezh2
cancer
compound
cells
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JP2019537585A5 (enExample
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ジン，ジアン
パーソンズ，ラモン
ストラティコプロス，イリアス
ヤン，シャオバオ
マ，アンチー
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アイカーン スクール オブ メディスン アット マウント シナイ
アイカーン スクール オブ メディスン アット マウント シナイ
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    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • 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
    • 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
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K47/545—Heterocyclic compounds
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Saccharide Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
JP2019522841A 2016-10-28 2017-10-27 Ｅｚｈ２媒介性がんを治療するための組成物および方法 Pending JP2019537585A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662414195P 2016-10-28 2016-10-28
US62/414,195 2016-10-28
PCT/US2017/058718 WO2018081530A1 (en) 2016-10-28 2017-10-27 Compositions and methods for treating ezh2-mediated cancer

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JP2019537585A true JP2019537585A (ja) 2019-12-26
JP2019537585A5 JP2019537585A5 (enExample) 2021-09-16

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US (3) US20190255041A1 (enExample)
EP (1) EP3532464A4 (enExample)
JP (1) JP2019537585A (enExample)
KR (1) KR20190084063A (enExample)
CN (1) CN110167924A (enExample)
AU (2) AU2017348322B8 (enExample)
CA (1) CA3041840A1 (enExample)
EA (1) EA201991071A1 (enExample)
IL (1) IL266053A (enExample)
MX (1) MX2019004950A (enExample)
SG (2) SG11201903483VA (enExample)
WO (1) WO2018081530A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2023517272A (ja) * 2020-08-13 2023-04-25 ハンミ ファーマシューティカル カンパニー リミテッド 新規なジオキソロイソキノリノン誘導体化合物及びその用途｛ｎｏｖｅｌ ｄｉｏｘｏｌｏｉｓｏｑｕｉｎｏｌｉｎｏｎｅ ｄｅｒｉｖａｔｉｖｅｓ ａｎｄ ｕｓｅ ｔｈｅｒｅｏｆ｝

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102667413B1 (ko) * 2016-10-27 2024-05-21 삼성전자주식회사 음성 명령에 기초하여 애플리케이션을 실행하는 방법 및 장치
KR20190084063A (ko) 2016-10-28 2019-07-15 이칸 스쿨 오브 메디슨 엣 마운트 시나이 Ｅｚｈ２-매개성 암 치료용 조성물 및 방법
WO2018106870A1 (en) 2016-12-08 2018-06-14 Icahn School Of Medicine At Mount Sinai Compositions and methods for treating cdk4/6-mediated cancer
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
JP2021515013A (ja) 2018-03-06 2021-06-17 アイカーン スクール オブ メディスン アット マウント シナイ セリンスレオニンキナーゼ（ａｋｔ）分解／破壊化合物および使用方法
FI3784663T3 (fi) 2018-04-23 2023-10-06 Celgene Corp Substituoituja 4-aminoisoindoliini-1,3-dioniyhdisteitä ja niiden käyttö lymfooman hoitamiseksi
EP3810145A4 (en) 2018-06-21 2022-06-01 Icahn School of Medicine at Mount Sinai Wd40 repeat domain protein 5 (wdr5) degradation / disruption compounds and methods of use
CN112969696B (zh) * 2018-11-02 2024-06-11 达纳-法伯癌症研究公司 乙酰化书写器抑制剂的开发及其用途
JP7503851B2 (ja) 2019-05-06 2024-06-21 アイカーン スクール オブ メディスン アット マウント シナイ Ｈｐｋ１の分解剤としてのヘテロ二官能性化合物
CN112457365B (zh) 2019-09-09 2023-06-09 中国医学科学院药物研究所 一类靶向蛋白质水解通路的功能分子及其制备和应用
JP7763753B2 (ja) 2019-09-26 2025-11-04 ノバルティス アーゲー アザキノリン化合物およびその使用
CN110862434B (zh) * 2019-10-28 2021-07-06 中山大学 一种可促进TGF-β1蛋白靶向降解的化合物及其制备方法与应用
EP4053122B1 (en) 2019-10-31 2024-10-09 Daegu-Gyeongbuk Medical Innovation Foundation Compound comprising ezh2 inhibitor and e3 ligase binder and pharmaceutical composition for preventing or treating ezh2-associated disease comprising same as active ingredient
WO2023205701A1 (en) 2022-04-20 2023-10-26 Kumquat Biosciences Inc. Macrocyclic heterocycles and uses thereof
CN111303133A (zh) * 2020-03-25 2020-06-19 清华大学 降解ezh2蛋白的小分子化合物
CN112920176B (zh) * 2020-05-25 2022-11-04 四川大学华西医院 可诱导prc2蛋白复合物核心亚基降解的双功能化合物和药物组合物及应用
US12103924B2 (en) 2020-06-01 2024-10-01 Icahn School Of Medicine At Mount Sinai Mitogen-activated protein kinase kinase (MEK) degradation compounds and methods of use
CN113214203A (zh) * 2020-12-16 2021-08-06 中山大学肿瘤防治中心（中山大学附属肿瘤医院、中山大学肿瘤研究所） 基于ezh2蛋白降解的小分子化合物及其应用
WO2022159650A1 (en) * 2021-01-22 2022-07-28 Icahn School Of Medicine At Mount Sinai HETEROBIFUNCTIONAL COMPOUNDS AS DEGRADERS OF eEF1A2
US12042543B2 (en) * 2021-04-30 2024-07-23 Northwestern University Substituted 3-amino-5-phenylbenzamide compounds as covalent inhibitors of enhancer zeste homolog 2 (EZH2) and proteolysis-targeting chimeric derivatives thereof (PROTACs) that induce degradation of EZH2
PE20252789A1 (es) 2023-05-24 2025-12-22 Kumquat Biosciences Inc Compuestos heterociclicos y usos de estos
CN121263417A (zh) 2023-06-30 2026-01-02 金橘生物科技公司 取代的稠合三环胺化合物及其作为ras抑制剂的用途
AU2024374420A1 (en) 2023-11-02 2026-04-16 Kumquat Biosciences Inc. Degraders and uses thereof
WO2025121807A1 (ko) * 2023-12-08 2025-06-12 인제대학교 산학협력단 Ezh2 저해제 및 mettl3 억제제를 포함하는 암의 예방 또는 치료용 약제학적 조성물
KR20250088371A (ko) * 2023-12-08 2025-06-17 인제대학교 산학협력단 Ezh2 저해제 및 jak3 억제제를 포함하는 암의 예방 또는 치료용 약학적 조성물
CN118420604A (zh) * 2024-03-29 2024-08-02 中国药科大学 一种以降冰片烯为疏水基团修饰的ezh2蛋白降解剂及其制备方法和应用

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015104677A1 (en) * 2014-01-10 2015-07-16 Piramal Enterprises Limited Heterocyclic compounds as ezh2 inhibitors
US20150291562A1 (en) * 2014-04-14 2015-10-15 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
WO2016073956A1 (en) * 2014-11-06 2016-05-12 Dana-Farber Cancer Institute, Inc. Ezh2 inhibitors and uses thereof
WO2016106518A1 (zh) * 2014-12-29 2016-07-07 深圳市日上光电股份有限公司 导线集成式照明灯箱
WO2016149668A1 (en) * 2015-03-18 2016-09-22 Arvinas, Inc. Compounds and methods for the enhanced degradation of targeted proteins
WO2017011590A1 (en) * 2015-07-13 2017-01-19 Arvinas, Inc. Alanine-based modulators of proteolysis and associated methods of use
JP2018526430A (ja) * 2015-07-10 2018-09-13 アルヴィナス・インコーポレイテッド タンパク質分解のｍｄｍ２系修飾因子および関連の使用方法
JP2019514883A (ja) * 2016-04-22 2019-06-06 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド サイクリン依存性キナーゼ４／６（ｃｄｋ４／６）阻害剤のｅ３リガーゼリガンドとのコンジュゲーションによるｃｄｋ４／６の分解および使用法

Family Cites Families (70)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5691147A (en) 1994-06-02 1997-11-25 Mitotix, Inc. CDK4 binding assay
US6486214B1 (en) 1997-09-10 2002-11-26 Rutgers, The State University Of New Jersey Polyanhydride linkers for production of drug polymers and drug polymer compositions produced thereby
JP3663382B2 (ja) 2000-02-15 2005-06-22 スージェン・インコーポレーテッド ピロール置換２−インドリノン蛋白質キナーゼ阻害剤
NZ590160A (en) 2003-11-21 2012-07-27 Array Biopharma Inc AKT protein kinase inhibitors
JP5274842B2 (ja) 2004-12-28 2013-08-28 エグゼリクシス， インコーポレイテッド 免疫疾患、炎症疾患および増殖疾患の処置のためのセリン−スレオニンキナーゼモジュレーター（ｐ７０Ｓ６Ｋ、Ａｋｔ−１およびＡｋｔ−２）としての［１Ｈ−ピペラゾ［３，４−ｄ］ピリミジン−４−イル］−ピペラジンまたは［１Ｈ−ピペラゾ［３，４−ｄ］ピリミジン−４−イル］−ピペラジン化合物
UA95641C2 (xx) 2006-07-06 2011-08-25 Эррей Биофарма Инк. Гідроксильовані піримідильні циклопентани як інгібітори акт протеїнкінази$гидроксилированные пиримидильные циклопентаны как ингибиторы акт протеинкиназы
ATE523499T1 (de) 2006-07-06 2011-09-15 Array Biopharma Inc Cyclopenta [d]-pyrimidine als akt-proteinkinasehemmer
CL2007002670A1 (es) 2006-09-15 2008-05-16 Celgene Corp Soc Organizada Ba Compuestos derivados de n-metilaminometil-isoindolina; composicion farmaceutica; forma de dosificacion, util para tratar o prevenir enfermedades tales como cancer, dolor, trastorno pulmonar, trastorno del snc y aterosclerosis.
WO2008109104A1 (en) 2007-03-07 2008-09-12 The Regents Of The University Of California Bivalent inhibitors of akt protein kinase
WO2009006567A2 (en) 2007-07-05 2009-01-08 Array Biopharma Inc. Pyrimidyl cyclopentanes as akt protein kinase inhibitors
CN101918373B (zh) 2007-07-05 2013-06-05 阵列生物制药公司 作为akt蛋白激酶抑制剂的嘧啶基环戊烷
WO2009134418A2 (en) 2008-04-30 2009-11-05 Fox Chase Cancer Center Assay for identifying agents that modulate epigenetic silencing, and agents identified thereby
CN102984941B (zh) 2009-09-04 2016-08-17 密执安大学评议会 用于治疗白血病的组合物和方法
PL3202460T3 (pl) 2010-02-11 2019-12-31 Celgene Corporation Pochodne arylometoksyizoindoliny i zawierające je kompozycje oraz sposoby ich zastosowania
WO2011159685A2 (en) 2010-06-16 2011-12-22 The Regents Of The University Of Michigan Inhibition of wdr5 interaction with its binding partners and therapeutic methods
WO2012078492A1 (en) 2010-12-06 2012-06-14 Celgene Corporation A combination therapy with lenalidomide and a cdk inhibitor for treating multiple myeloma
KR102668696B1 (ko) 2012-01-12 2024-05-29 예일 유니버시티 E3 유비퀴틴 리가아제에 의한 표적 단백질 및 다른 폴리펩티드의 증진된 분해를 위한 화합물 및 방법
WO2013170147A1 (en) 2012-05-11 2013-11-14 Yale University Compounds useful for promoting protein degradation and methods using same
USRE48175E1 (en) 2012-10-19 2020-08-25 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
DK2935222T3 (en) 2012-12-21 2019-01-07 Epizyme Inc PRMT5 INHIBITORS AND APPLICATIONS THEREOF
EP3083602A1 (en) 2013-12-20 2016-10-26 Pfizer Limited N-acylpiperidine ether tropomyosin-related kinase inhibitors
US9796701B2 (en) 2013-12-31 2017-10-24 Xuanzhu Pharma Co., Ltd. Kinase inhibitor and use thereof
CN106573073B (zh) 2014-06-13 2021-09-28 塔夫茨大学信托人 Fap激活的治疗剂以及其相关用途
WO2016022605A1 (en) 2014-08-04 2016-02-11 Epizyme, Inc. Prmt5 inhibitors and uses thereof
WO2016089883A1 (en) 2014-12-01 2016-06-09 Novartis Ag Compositions and methods for diagnosis and treatment of prostate cancer
WO2016105518A1 (en) * 2014-12-23 2016-06-30 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
AR103297A1 (es) 2014-12-30 2017-05-03 Forma Therapeutics Inc Pirrolo y pirazolopirimidinas como inhibidores de la proteasa 7 específica de ubiquitina
WO2016115480A1 (en) 2015-01-16 2016-07-21 Vedantra Pharmaceuticals, Inc. Multilamellar lipid vesicle compositions including a conjugated anaplastic lymphoma kinase (alk) variant and uses thereof
CN108137593B (zh) 2015-04-21 2021-01-05 上海交通大学医学院附属瑞金医院 蛋白激酶抑制剂的制备和用途
WO2016174130A1 (en) 2015-04-28 2016-11-03 Université De Strasbourg Clinical gene signature-based human cell culture model and uses thereof
CA2988414C (en) 2015-06-04 2023-09-26 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
MX2017016325A (es) 2015-06-22 2018-03-02 Ono Pharmaceutical Co Compuesto inhibidor de cinasa de tumor de mama (brk).
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
WO2017007612A1 (en) 2015-07-07 2017-01-12 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
CN105175284B (zh) 2015-07-21 2017-06-16 中国药科大学 酰胺类化合物、制备方法及其医药用途
WO2017024317A2 (en) 2015-08-06 2017-02-09 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
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
US9809603B1 (en) 2015-08-18 2017-11-07 Deuterx, Llc Deuterium-enriched isoindolinonyl-piperidinonyl conjugates and oxoquinazolin-3(4H)-yl-piperidinonyl conjugates and methods of treating medical disorders using same
US20170114098A1 (en) 2015-09-03 2017-04-27 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
BR112018008918A8 (pt) * 2015-11-02 2019-02-26 Univ Yale compostos de quimera proteólise dirigida e métodos para preparação e uso dos mesmos
JP2019507179A (ja) 2016-03-01 2019-03-14 プロペロン セラピューティックス インコーポレイテッド Ｗｄｒ５タンパク質−タンパク質結合の阻害剤
US11319299B2 (en) 2016-03-01 2022-05-03 Propellon Therapeutics Inc. Substituted carboxamides as inhibitors of WDR5 protein-protein binding
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
EP3454856B1 (en) 2016-05-10 2024-09-11 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
CN115819417A (zh) 2016-09-09 2023-03-21 因赛特公司 作为hpk1调节剂的吡唑并吡啶衍生物及其用于治疗癌症的用途
US20180072741A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyrimidine compounds and uses thereof
US10160763B2 (en) 2016-09-13 2018-12-25 Vanderbilt University WDR5 inhibitors and modulators
KR20190084063A (ko) 2016-10-28 2019-07-15 이칸 스쿨 오브 메디슨 엣 마운트 시나이 Ｅｚｈ２-매개성 암 치료용 조성물 및 방법
WO2018098280A1 (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
WO2018106870A1 (en) 2016-12-08 2018-06-14 Icahn School Of Medicine At Mount Sinai Compositions and methods for treating cdk4/6-mediated cancer
ES2909234T3 (es) 2016-12-21 2022-05-05 Ono Pharmaceutical Co Compuestos de 6-amino-7,9-dihidro-8H-purin-8-ona como inhibidores de Brk
JP2020505327A (ja) 2016-12-23 2020-02-20 アルビナス・オペレーションズ・インコーポレイテッドＡｒｖｉｎａｓ Ｏｐｅｒａｔｉｏｎｓ， Ｉｎｃ． Ｅｇｆｒタンパク質分解標的化キメラ分子およびその関連する使用方法
IL312367A (en) 2017-01-31 2024-06-01 Arvinas Operations Inc Cereblon ligands and bifunctional compounds comprising the same
WO2019084030A1 (en) 2017-10-24 2019-05-02 Genentech, Inc. (4-HYDROXYPYRROLIDIN-2-YL) -HYDROXAMATE COMPOUNDS AND METHODS OF USE
US20210283261A1 (en) 2017-12-05 2021-09-16 Icahn School Of Medicine At Mount Sinai Compositions and Methods for Treating ALK-Mediated Cancer
ES3041854T3 (en) 2018-01-22 2025-11-17 Bioventures Llc Bcl-2 proteins degraders for cancer treatment
CA3091041A1 (en) 2018-02-22 2019-08-29 Ichan School Of Medicine At Mount Sinai Protein arginine methyltransferase 5 (prmt5) degradation / disruption compounds and methods of use
JP2021515013A (ja) 2018-03-06 2021-06-17 アイカーン スクール オブ メディスン アット マウント シナイ セリンスレオニンキナーゼ（ａｋｔ）分解／破壊化合物および使用方法
EP3793523B8 (en) 2018-05-15 2026-01-21 The United States of America, as represented by the Secretary, Department of Health and Human Services Formulations and methods for the prevention and treatment of tumor metastasis and tumorigenesis
EP3810145A4 (en) 2018-06-21 2022-06-01 Icahn School of Medicine at Mount Sinai Wd40 repeat domain protein 5 (wdr5) degradation / disruption compounds and methods of use
CA3105121A1 (en) 2018-07-05 2020-01-09 Icahn School Of Medicine At Mount Sinai Protein tyrosine kinase 6 (ptk6) degradation / disruption compounds and methods of use
JP7503851B2 (ja) 2019-05-06 2024-06-21 アイカーン スクール オブ メディスン アット マウント シナイ Ｈｐｋ１の分解剤としてのヘテロ二官能性化合物
JP7706210B2 (ja) 2019-06-10 2025-07-11 ストロ バイオファーマ インコーポレーテッド ５Ｈ－ピロロ［３，２－ｄ］ピリミジン－２，４－ジアミノ化合物およびその抗体コンジュゲート
WO2021021904A1 (en) 2019-07-30 2021-02-04 The Scripps Research Institute Pharmacological inhibitors of the enl yeats domain
CN112552293A (zh) 2019-09-25 2021-03-26 珠海宇繁生物科技有限责任公司 一种protac小分子化合物及其应用
US11739101B2 (en) 2020-05-06 2023-08-29 Nurix Therapeutics, Inc. Bifunctional degraders of hematopoietic progenitor kinase and therapeutic uses thereof
US12103924B2 (en) 2020-06-01 2024-10-01 Icahn School Of Medicine At Mount Sinai Mitogen-activated protein kinase kinase (MEK) degradation compounds and methods of use
WO2022086937A1 (en) 2020-10-21 2022-04-28 Icahn School Of Medicine At Mount Sinai Heterobifunctional compounds as degraders of enl
CN112778303A (zh) 2020-12-31 2021-05-11 武汉九州钰民医药科技有限公司 Cdk4/6激酶抑制剂shr6390的制备方法
JP2024528722A (ja) 2021-07-30 2024-07-30 ベイジーン リミテッド ＨＰＫ１分解誘導薬としてのピロロ［２，３－ｂ］ピラジン系の二官能性化合物及びその使用

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015104677A1 (en) * 2014-01-10 2015-07-16 Piramal Enterprises Limited Heterocyclic compounds as ezh2 inhibitors
US20150291562A1 (en) * 2014-04-14 2015-10-15 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
WO2016073956A1 (en) * 2014-11-06 2016-05-12 Dana-Farber Cancer Institute, Inc. Ezh2 inhibitors and uses thereof
WO2016106518A1 (zh) * 2014-12-29 2016-07-07 深圳市日上光电股份有限公司 导线集成式照明灯箱
WO2016149668A1 (en) * 2015-03-18 2016-09-22 Arvinas, Inc. Compounds and methods for the enhanced degradation of targeted proteins
JP2018526430A (ja) * 2015-07-10 2018-09-13 アルヴィナス・インコーポレイテッド タンパク質分解のｍｄｍ２系修飾因子および関連の使用方法
WO2017011590A1 (en) * 2015-07-13 2017-01-19 Arvinas, Inc. Alanine-based modulators of proteolysis and associated methods of use
JP2019514883A (ja) * 2016-04-22 2019-06-06 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド サイクリン依存性キナーゼ４／６（ｃｄｋ４／６）阻害剤のｅ３リガーゼリガンドとのコンジュゲーションによるｃｄｋ４／６の分解および使用法

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
KYLE D. KONZE ET AL., ACS CHEMICAL BIOLOGY, vol. 8, no. 6, JPN6021037756, 2013, pages 1324 - 1334, ISSN: 0004608370 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2023517272A (ja) * 2020-08-13 2023-04-25 ハンミ ファーマシューティカル カンパニー リミテッド 新規なジオキソロイソキノリノン誘導体化合物及びその用途｛ｎｏｖｅｌ ｄｉｏｘｏｌｏｉｓｏｑｕｉｎｏｌｉｎｏｎｅ ｄｅｒｉｖａｔｉｖｅｓ ａｎｄ ｕｓｅ ｔｈｅｒｅｏｆ｝
JP7387907B2 (ja) 2020-08-13 2023-11-28 ハンミ ファーマシューティカル カンパニー リミテッド 新規なジオキソロイソキノリノン誘導体化合物及びその用途｛ｎｏｖｅｌ ｄｉｏｘｏｌｏｉｓｏｑｕｉｎｏｌｉｎｏｎｅ ｄｅｒｉｖａｔｉｖｅｓ ａｎｄ ｕｓｅ ｔｈｅｒｅｏｆ｝

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