CA3045037A1 - Compositions and methods for treating cdk4/6-mediated cancer - Google Patents

Compositions and methods for treating cdk4/6-mediated cancer Download PDF

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Publication number
CA3045037A1
CA3045037A1 CA3045037A CA3045037A CA3045037A1 CA 3045037 A1 CA3045037 A1 CA 3045037A1 CA 3045037 A CA3045037 A CA 3045037A CA 3045037 A CA3045037 A CA 3045037A CA 3045037 A1 CA3045037 A1 CA 3045037A1
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Prior art keywords
cancer
cdk4
alkyl
amino
compound
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Abandoned
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CA3045037A
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English (en)
French (fr)
Inventor
Jian Jin
Xiaobao Yang
Jing Liu
Yan Xiong
Poulikos Poulikakos
Zoi KAROULIA
Xuewei Wu
Tamer AHMED
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Icahn School of Medicine at Mount Sinai
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Icahn School of Medicine at Mount Sinai
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Publication of CA3045037A1 publication Critical patent/CA3045037A1/en
Abandoned legal-status Critical Current

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/43Enzymes; Proenzymes; Derivatives thereof
    • A61K38/45Transferases (2)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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
    • A61K47/55Medicinal 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, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12YENZYMES
    • C12Y203/00Acyltransferases (2.3)
    • C12Y203/02Aminoacyltransferases (2.3.2)

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Gastroenterology & Hepatology (AREA)
  • General Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
CA3045037A 2016-12-08 2017-12-07 Compositions and methods for treating cdk4/6-mediated cancer Abandoned CA3045037A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662431806P 2016-12-08 2016-12-08
US62/431,806 2016-12-08
PCT/US2017/065027 WO2018106870A1 (en) 2016-12-08 2017-12-07 Compositions and methods for treating cdk4/6-mediated cancer

Publications (1)

Publication Number Publication Date
CA3045037A1 true CA3045037A1 (en) 2018-06-14

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CA3045037A Abandoned CA3045037A1 (en) 2016-12-08 2017-12-07 Compositions and methods for treating cdk4/6-mediated cancer

Country Status (7)

Country Link
US (2) US11541051B2 (enExample)
EP (1) EP3551185A4 (enExample)
JP (1) JP2020514252A (enExample)
CN (1) CN110267659A (enExample)
AU (1) AU2017370694A1 (enExample)
CA (1) CA3045037A1 (enExample)
WO (1) WO2018106870A1 (enExample)

Families Citing this family (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9464092B2 (en) 2013-03-15 2016-10-11 G1 Therapeutics, Inc. Transient protection of normal cells during chemotherapy
WO2018005863A1 (en) * 2016-07-01 2018-01-04 G1 Therapeutics, Inc. Pyrimidine-based compounds for the treatment of cancer
WO2018005860A1 (en) 2016-07-01 2018-01-04 G1 Therapeutics, Inc. Pyrimidine-based antiproliferative agents
MX2019004950A (es) 2016-10-28 2019-09-26 Icahn School Med Mount Sinai Composiciones y metodos para tratar el cancer mediado por el potenciador del homologo zeste 2.
CA3045037A1 (en) 2016-12-08 2018-06-14 Icahn School Of Medicine At Mount Sinai Compositions and methods for treating cdk4/6-mediated cancer
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
HRP20241553T1 (hr) 2017-07-10 2025-01-17 Celgene Corporation 4-(4-(4-(((2-(2,6-dioksopiperidin-3-il)-l-oksoizoindolin-4-il)oksi)metil)benzil)piperazin-l-il)-3-fluorobenzonitril kao antiproliferativni spoj
CN109516989B (zh) * 2017-09-17 2021-12-31 上海美志医药科技有限公司 一类抑制并降解cdk的化合物
JP7569688B2 (ja) 2017-12-22 2024-10-18 ハイバーセル,インコーポレイテッド ホスファチジルイノシトールリン酸キナーゼ阻害剤としてのアミノピリジン誘導体
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
CA3096404A1 (en) 2018-04-23 2019-10-31 Celgene Corporation Substituted 4-aminoisoindoline-1,3-dione compounds and their use for treating lymphoma
CN110615779B (zh) * 2018-06-20 2023-03-24 上海科技大学 制备来那度胺衍生物的方法
WO2019246570A1 (en) 2018-06-21 2019-12-26 Icahn School Of Medicine At Mount Sinai Wd40 repeat domain protein 5 (wdr5) degradation / disruption compounds and methods of use
JP2021529807A (ja) * 2018-07-05 2021-11-04 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 タンパク質チロシンキナーゼ6(ptk6)分解/破壊化合物および使用方法
WO2020023502A1 (en) * 2018-07-23 2020-01-30 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
CN108948136A (zh) * 2018-08-06 2018-12-07 浙江华海药业股份有限公司 一种赖诺普利杂质及其制备方法
CN110835345A (zh) * 2018-08-17 2020-02-25 中国科学院上海药物研究所 一类细胞周期依赖性激酶的降解剂、其制备方法、药物组合物及其用途
US11707452B2 (en) 2018-08-20 2023-07-25 Arvinas Operations, Inc. Modulators of alpha-synuclein proteolysis and associated methods of use
US11046703B2 (en) * 2018-10-08 2021-06-29 The Regents Of The University Of Michigan Small molecule MDM2 protein degraders
AU2019360928B2 (en) * 2018-10-15 2023-11-09 Nurix Therapeutics, Inc. Bifunctional compounds for degrading BTK via ubiquitin proteosome pathway
CN113825752A (zh) * 2018-11-02 2021-12-21 威斯特解剖及生物研究所 蛋白水解靶向嵌合体
US20220016102A1 (en) * 2018-11-21 2022-01-20 Shanghaitech University Er protein regulators and use thereof
CN113660937A (zh) * 2019-02-08 2021-11-16 佛罗里达大学研究基金公司 治疗剂和治疗方法
CN113646002A (zh) * 2019-02-27 2021-11-12 上海睿跃生物科技有限公司 环amp反应元件结合蛋白(cbp)和/或300kda腺病毒e1a结合蛋白(p300)降解化合物和使用方法
CN113747925B (zh) 2019-03-21 2024-10-15 隆萨销售股份公司 胞外囊泡缀合物及其用途
US12233356B2 (en) 2019-03-21 2025-02-25 Lonza Sales Ag Process for preparing extracellular vesicles
JP2022521825A (ja) * 2019-03-28 2022-04-12 エッサ ファーマ,インコーポレイテッド アンドロゲン受容体モジュレーター及びタンパク質分解誘導キメラリガンドとして使用するための方法
US11485735B2 (en) * 2019-04-25 2022-11-01 Wuxi Shuangliang Biotechnology Co., Ltd. Selective CDK4/6 inhibitor and preparation thereof
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
EP3976621A4 (en) * 2019-06-03 2023-11-15 Regents of the University of Minnesota KINASE DEGRADING COMPOUNDS AND THEIR USE
TW202112767A (zh) 2019-06-17 2021-04-01 美商佩特拉製藥公司 作為磷脂酸肌醇磷酸激酶抑制劑之胺基吡啶衍生物
CN114867727B (zh) 2019-07-17 2025-02-21 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
EP4010336B1 (en) * 2019-08-05 2025-04-02 Dana-Farber Cancer Institute, Inc. Degraders of cyclin-dependent kinase 7 (cdk7) and uses thereof
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
EP4045496A1 (en) 2019-10-17 2022-08-24 Arvinas Operations, Inc. Bifunctional molecules containing an e3 ubiquitine ligase binding moiety linked to a bcl6 targeting moiety
KR20220113986A (ko) 2019-12-16 2022-08-17 루넬라 바이오테크 인코포레이티드 선택적 cdk 4/6 억제제 암 치료제
JP7681599B2 (ja) 2019-12-16 2025-05-22 ルネラ・バイオテック・インコーポレーテッド 選択的cdk4/6阻害剤のがん治療薬
EP4076530A4 (en) * 2019-12-17 2024-04-10 Orionis Biosciences, Inc. BIFUNCTIONAL AGENTS FOR RECRUITMENT AND/OR DEGRADATION OF PROTEINS
AU2020404956A1 (en) * 2019-12-17 2022-07-07 Orionis Biosciences, Inc. Compounds modulating protein recruitment and/or degradation
CN115038697A (zh) 2020-01-15 2022-09-09 佛罗里达大学研究基金公司 治疗剂和治疗方法
WO2021150945A1 (en) * 2020-01-23 2021-07-29 Icahn School Of Medicine At Mount Sinai Methods of diagnosing and treating cancer
EP4652997A2 (en) 2020-05-19 2025-11-26 Pharmacosmos Holding A/s Cyclin-dependent kinase inhibiting compounds for the treatment of medical disorders
WO2021237100A1 (en) 2020-05-21 2021-11-25 Codiak Biosciences, Inc. Methods of targeting extracellular vesicles to lung
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
AU2021287380A1 (en) * 2020-06-11 2023-01-05 Lunella Biotech, Inc. Selective CDK4/6 inhibitor cancer therapeutics
KR102646850B1 (ko) * 2020-07-21 2024-03-13 주식회사 유빅스테라퓨틱스 안드로겐 수용체 분해용 화합물 및 이들의 의약 용도
KR102601028B1 (ko) * 2020-08-18 2023-11-10 재단법인대구경북과학기술원 아베마시클립을 유효성분으로 포함하는 퇴행성 뇌질환의 예방 또는 치료용 약학적 조성물
WO2022039421A1 (ko) * 2020-08-18 2022-02-24 재단법인대구경북과학기술원 아베마시클립을 유효성분으로 포함하는 퇴행성 뇌질환의 예방 또는 치료용 약학적 조성물
US12180193B2 (en) 2020-08-28 2024-12-31 Arvinas Operations, Inc. Accelerating fibrosarcoma protein degrading compounds and associated methods of use
US20240241020A1 (en) 2020-09-23 2024-07-18 Lonza Sales Ag Process for preparing extracellular vesicles
CN114349738B (zh) * 2020-10-14 2023-05-05 清华大学 一类靶向降解cdk2的小分子缀合物及其应用
AR124154A1 (es) 2020-11-27 2023-02-22 Rhizen Pharmaceuticals Ag Inhibidores de cdk
WO2022149057A1 (en) 2021-01-05 2022-07-14 Rhizen Pharmaceuticals Ag Cdk inhibitors
EP4277901A1 (en) 2021-01-13 2023-11-22 Monte Rosa Therapeutics, Inc. Isoindolinone compounds
AU2022259683A1 (en) 2021-04-16 2023-10-19 Arvinas Operations, Inc. Modulators of bcl6 proteolysis and associated methods of use
JP2024542984A (ja) 2021-10-26 2024-11-19 ニューリックス セラピューティクス,インコーポレイテッド がんを治療および予防するためのピペリジニルピラジン-カルボキサミド化合物、およびbtkを分解するためのピペリジニルピラジン-カルボキサミド化合物
CN116239566A (zh) * 2021-12-08 2023-06-09 标新生物医药科技(上海)有限公司 E3泛素连接酶配体化合物、基于该配体化合物开发的蛋白降解剂及它们的应用
US20230295118A1 (en) * 2022-03-18 2023-09-21 EnhancedBio Inc. Compounds and methods for the targeted degradation of cyclin dependent kinases
AU2023268542A1 (en) * 2022-05-10 2024-11-14 Biotheryx, Inc. Cdk protein degraders, pharmaceutical compositions, and therapeutic applications
CN114957249B (zh) * 2022-05-20 2023-04-21 东南大学 一种不可逆共价结合cdk抑制剂及其制备方法和应用
US11957759B1 (en) 2022-09-07 2024-04-16 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (RAF) degrading compounds and associated methods of use
JP2025530372A (ja) * 2022-09-15 2025-09-11 クルゲン(シャンハイ),インク. 修飾タンパク質ならびにタンパク質結合剤および分解剤
EP4605088A1 (en) * 2022-10-21 2025-08-27 Novartis AG Molecular glue degrader compounds and uses thereof
CN115650968B (zh) * 2022-12-27 2023-03-21 英矽智能科技(上海)有限公司 作为cdk选择性抑制剂的新型哒嗪酮化合物
WO2024229287A1 (en) * 2023-05-03 2024-11-07 St. Jude Children's Research Hospital, Inc. A sequence selective dna binding molecule (syngrader)
AU2024276994A1 (en) 2023-05-24 2025-10-23 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
WO2024256569A1 (en) * 2023-06-13 2024-12-19 Rijksuniversiteit Groningen Novel cdk degraders

Family Cites Families (52)

* 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
PT1255752E (pt) 2000-02-15 2007-10-17 Pharmacia & Upjohn Co Llc Inibidores de proteína quinases: 2-indolinonas substituídas com pirrolo
TW200819435A (en) 2006-09-15 2008-05-01 Celgene Corp N-methylaminomethyl isoindole compounds and compositions comprising and methods of using the same
WO2008109104A1 (en) 2007-03-07 2008-09-12 The Regents Of The University Of California Bivalent inhibitors of akt protein kinase
SI2173723T1 (sl) 2007-07-05 2011-12-30 Array Biopharma Inc Pirimidil ciklopentani kot inhibitorji AKT-protein-kinaze
US20110172107A1 (en) 2008-04-30 2011-07-14 Fox Chase Cancer Center Assay for identifying agents that modulate epigenetic silencing, and agents identified thereby
WO2011029054A1 (en) 2009-09-04 2011-03-10 The Regents Of The University Of Michigan Compositions and methods for treatment of leukemia
SG10201501062SA (en) 2010-02-11 2015-04-29 Celgene Corp Arylmethoxy isoindoline derivatives and compositions comprising and methods of using the same
US20140031325A1 (en) 2010-12-06 2014-01-30 Celgene Corporation Combination therapy with lenalidomide and a cdk inhibitor for treating multiple myeloma
EP3608317A1 (en) * 2012-01-12 2020-02-12 Yale University Compounds & methods for the enhanced degradation of targeted proteins & other polypeptides by an e3 ubiquitin ligase
US20150119435A1 (en) 2012-05-11 2015-04-30 Yale University Compounds useful for promoting protein degradation and methods using same
US9758522B2 (en) * 2012-10-19 2017-09-12 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
WO2014100719A2 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Prmt5 inhibitors and uses thereof
WO2015101293A1 (zh) 2013-12-31 2015-07-09 山东轩竹医药科技有限公司 激酶抑制剂及其用途
WO2015104677A1 (en) 2014-01-10 2015-07-16 Piramal Enterprises Limited Heterocyclic compounds as ezh2 inhibitors
KR20250127179A (ko) 2014-04-14 2025-08-26 아비나스 오퍼레이션스, 인코포레이티드 단백질분해의 이미드-기초된 조절인자 및 연관된 이용 방법
CN113786495A (zh) 2014-06-13 2021-12-14 塔夫茨大学信托人 Fap激活的治疗剂以及其相关用途
US11236082B2 (en) 2014-11-06 2022-02-01 Dana-Farber Cancer Institute, Inc. EZH2 inhibitors and uses thereof
EP3227446A1 (en) 2014-12-01 2017-10-11 Novartis AG Compositions and methods for diagnosis and treatment of prostate cancer
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
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
TWI770525B (zh) 2014-12-30 2022-07-11 美商瓦洛健康公司 作為泛素特異性蛋白酶7抑制劑之吡咯并及吡唑并嘧啶
US20180000906A1 (en) 2015-01-16 2018-01-04 Vedantra Pharmaceuticals, Inc. Multilamellar lipid vesicle compositions including a conjugated anaplastic lymphoma kinase (alk) variant and uses thereof
EP3270917A4 (en) 2015-03-18 2018-08-08 Arvinas, Inc. Compounds and methods for the enhanced degradation of targeted proteins
WO2016174130A1 (en) 2015-04-28 2016-11-03 Université De Strasbourg Clinical gene signature-based human cell culture model and uses thereof
JP6819585B2 (ja) 2015-06-22 2021-01-27 小野薬品工業株式会社 Brk阻害化合物
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
WO2017007612A1 (en) 2015-07-07 2017-01-12 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
US20170008904A1 (en) 2015-07-10 2017-01-12 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
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
EP3423437A4 (en) 2016-03-01 2019-07-24 Propellon Therapeutics Inc. INHIBITORS OF WDR5 PROTEIN PROTEIN BINDING
AU2017226004B2 (en) 2016-03-01 2021-07-22 Propellon Therapeutics Inc. Inhibitors of WDR5 protein-protein binding
US10865204B2 (en) * 2016-04-22 2020-12-15 Dana-Farber Cancer Institute, Inc. Degradation of cyclin-dependent kinase 4/6 (CDK4/6) by conjugation of CDK4/6 inhibitors with E3 ligase ligand and methods of use
EP3454856B1 (en) 2016-05-10 2024-09-11 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
WO2017197051A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Amine-linked c3-glutarimide degronimers for target protein degradation
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
MX2019004950A (es) 2016-10-28 2019-09-26 Icahn School Med Mount Sinai Composiciones y metodos para tratar el cancer mediado por el potenciador del homologo zeste 2.
CA3045037A1 (en) 2016-12-08 2018-06-14 Icahn School Of Medicine At Mount Sinai Compositions and methods for treating cdk4/6-mediated cancer
JP7047772B2 (ja) 2016-12-21 2022-04-05 小野薬品工業株式会社 Brk阻害化合物
US20210283261A1 (en) 2017-12-05 2021-09-16 Icahn School Of Medicine At Mount Sinai Compositions and Methods for Treating ALK-Mediated Cancer
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
JP7421499B2 (ja) 2018-05-15 2024-01-24 アメリカ合衆国 腫瘍転移および腫瘍発生の予防および治療のための製剤および方法
WO2019246570A1 (en) 2018-06-21 2019-12-26 Icahn School Of Medicine At Mount Sinai Wd40 repeat domain protein 5 (wdr5) degradation / disruption compounds and methods of use
US20220242871A1 (en) 2019-06-10 2022-08-04 Sutro Biopharma, Inc. 5H-PYRROLO[3,2-d]PYRIMIDINE-2,4-DIAMINO COMPOUNDS AND ANTIBODY CONJUGATES THEREOF
US20220274980A1 (en) 2019-07-30 2022-09-01 The Scripps Research Institute Pharmacological inhibitors of the enl yeats domain
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
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

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