AU2017370694A1 - Compositions and methods for treating CDK4/6-mediated cancer - Google Patents

Compositions and methods for treating CDK4/6-mediated cancer Download PDF

Info

Publication number
AU2017370694A1
AU2017370694A1 AU2017370694A AU2017370694A AU2017370694A1 AU 2017370694 A1 AU2017370694 A1 AU 2017370694A1 AU 2017370694 A AU2017370694 A AU 2017370694A AU 2017370694 A AU2017370694 A AU 2017370694A AU 2017370694 A1 AU2017370694 A1 AU 2017370694A1
Authority
AU
Australia
Prior art keywords
cdk4
cancer
alkyl
amino
compound
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Abandoned
Application number
AU2017370694A
Other languages
English (en)
Inventor
Tamer AHMED
Jian Jin
Zoi KAROULIA
Jing Liu
Poulikos Poulikakos
Xuewei Wu
Yan Xiong
Xiaobao Yang
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Icahn School of Medicine at Mount Sinai
Original Assignee
Icahn School of Medicine at Mount Sinai
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Icahn School of Medicine at Mount Sinai filed Critical Icahn School of Medicine at Mount Sinai
Publication of AU2017370694A1 publication Critical patent/AU2017370694A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • 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
    • 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)

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Engineering & Computer Science (AREA)
  • Zoology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Genetics & Genomics (AREA)
  • Wood Science & Technology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2017370694A 2016-12-08 2017-12-07 Compositions and methods for treating CDK4/6-mediated cancer Abandoned AU2017370694A1 (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
AU2017370694A1 true AU2017370694A1 (en) 2019-07-25

Family

ID=62491322

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2017370694A Abandoned AU2017370694A1 (en) 2016-12-08 2017-12-07 Compositions and methods for treating CDK4/6-mediated cancer

Country Status (7)

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

Families Citing this family (71)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ME03557B (me) 2013-03-15 2020-07-20 G1 Therapeutics Inc Privremena zaštiтa normalnih ćelija током hemoterapije
WO2018005863A1 (en) * 2016-07-01 2018-01-04 G1 Therapeutics, Inc. Pyrimidine-based compounds for the treatment of cancer
RU2019102647A (ru) 2016-07-01 2020-08-03 Г1 Терапьютикс, Инк. Антипролиферационные средства на основе пиримидина
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
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
EP4467143B1 (en) 2017-07-10 2026-03-11 Celgene Corporation Method for preparing 4-(4-(4-(((2-(2,6-dioxopiperidin-3-yl)-l-oxoisoindolin-4-yl)oxy)methyl)benzyl)piperazin-l-yl)-3-fluorobenzonitrile
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
WO2019126731A1 (en) 2017-12-22 2019-06-27 Petra Pharma Corporation Aminopyridine derivatives as phosphatidylinositol phosphate kinase inhibitors
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
US12539292B2 (en) 2018-04-01 2026-02-03 Arvinas Operations, Inc. BRM targeting compounds and associated methods of use
FI3784663T3 (fi) 2018-04-23 2023-10-06 Celgene Corp Substituoituja 4-aminoisoindoliini-1,3-dioniyhdisteitä ja niiden käyttö lymfooman hoitamiseksi
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
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
US11091522B2 (en) 2018-07-23 2021-08-17 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
JP7297053B2 (ja) 2018-08-20 2023-06-23 アルビナス・オペレーションズ・インコーポレイテッド 神経変性疾患を治療するためのe3ユビキチンリガーゼ結合活性を有するキメラ(protac)化合物を標的とし、アルファ-シヌクレインタンパク質を標的とするタンパク質分解
CN112912143A (zh) * 2018-10-08 2021-06-04 美国密歇根州立大学试剂中心 小分子mdm2蛋白降解剂
MX2021004191A (es) 2018-10-15 2021-05-27 Nurix Therapeutics Inc Compuestos bifuncionales para degradar la tirosina cinasa de bruton (btk) mediante la trayectoria de ubiquitina proteosoma.
US20220002291A1 (en) * 2018-11-02 2022-01-06 The Wistar Institute Of Anatomy And Biology Proteolysis-targeting chimeras
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
US12582722B2 (en) 2019-02-13 2026-03-24 Nurix Therapeutics, Inc. Bifunctional compounds for degrading BTK via ubiquitin proteosome pathway
WO2020173440A1 (en) * 2019-02-27 2020-09-03 Cullgen (Shanghai), Inc. Cyclic-amp response element binding protein (cbp) and/or adenoviral e1a binding protein of 300 kda (p300) degradation compounds and methods of use
EP3941607A1 (en) 2019-03-21 2022-01-26 Codiak BioSciences, Inc. Process for preparing extracellular vesicles
US20240108747A1 (en) 2019-03-21 2024-04-04 Lonza Sales Ag Extracellular vesicle conjugates and uses thereof
CN114269331A (zh) * 2019-03-28 2022-04-01 埃萨制药股份有限公司 雄激素受体调节剂和用作蛋白水解靶向嵌合体配体的方法
US11485735B2 (en) * 2019-04-25 2022-11-01 Wuxi Shuangliang Biotechnology Co., Ltd. Selective CDK4/6 inhibitor and preparation thereof
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
CA3142713A1 (en) * 2019-06-03 2020-12-10 Regents Of The University Of Minnesota Compounds that degrade kinases and uses thereof
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
EP3999182A1 (en) 2019-07-17 2022-05-25 Arvinas Operations, Inc. Tau-protein targeting compounds and associated methods of use
ES3031581T3 (en) * 2019-08-05 2025-07-09 Dana Farber Cancer Inst 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
CA3154386A1 (en) 2019-10-17 2021-04-22 Michael Berlin Bifunctional molecules containing an e3 ubiquitine ligase binding moiety linked to a bcl6 targeting moiety
WO2021113557A1 (en) 2019-12-04 2021-06-10 Nurix Therapeutics, Inc. Bifunctional compounds for degrading btk via ubiquitin proteosome pathway
AU2020405427B2 (en) 2019-12-16 2025-01-09 Lunella Biotech, Inc. Selective CDK4/6 inhibitor cancer therapeutics
CN118652252A (zh) 2019-12-16 2024-09-17 卢内拉生物技术有限公司 选择性cdk4/6抑制剂型癌症治疗药物
US20230099031A1 (en) * 2019-12-17 2023-03-30 Orionis Biosciences, Inc. Bifunctional agents for protein recruitment and/or degradation
WO2021126973A1 (en) * 2019-12-17 2021-06-24 Orionis Biosciences, Inc. Compounds modulating protein recruitment and/or degradation
US12441722B2 (en) 2020-01-15 2025-10-14 University Of Florida Research Foundation, Incorporated Therapeutic agents and methods of treatment
WO2021150945A1 (en) * 2020-01-23 2021-07-29 Icahn School Of Medicine At Mount Sinai Methods of diagnosing and treating cancer
KR20230012547A (ko) 2020-05-19 2023-01-26 쥐원 쎄라퓨틱스, 인크. 의학적 장애의 치료를 위한 시클린-의존성 키나제 억제 화합물
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
EP4165046B1 (en) * 2020-06-11 2025-09-17 Lunella Biotech, Inc. Selective cdk4/6 inhibitor cancer therapeutics
AU2021311245A1 (en) * 2020-07-21 2023-03-09 Ubix Therapeutics, Inc. Compound for androgen receptor degradation, and pharmaceutical use thereof
US20240041876A1 (en) * 2020-08-18 2024-02-08 Daegu Gyeongbuk Institute Of Science And Technology Pharmaceutical composition for prevention or treatment of degenerative brain diseases comprising abemaciclib as active ingredient
KR102601028B1 (ko) * 2020-08-18 2023-11-10 재단법인대구경북과학기술원 아베마시클립을 유효성분으로 포함하는 퇴행성 뇌질환의 예방 또는 치료용 약학적 조성물
WO2022047145A1 (en) 2020-08-28 2022-03-03 Arvinas Operations, Inc. Rapidly accelerating fibrosarcoma protein degrading compounds and associated methods of use
WO2022066928A2 (en) 2020-09-23 2022-03-31 Codiak Biosciences, Inc. 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
WO2022113003A1 (en) 2020-11-27 2022-06-02 Rhizen Pharmaceuticals Ag Cdk inhibitors
WO2022149057A1 (en) 2021-01-05 2022-07-14 Rhizen Pharmaceuticals Ag Cdk inhibitors
AU2022207648A1 (en) 2021-01-13 2023-07-27 Monte Rosa Therapeutics Ag Isoindolinone compounds
KR20230171979A (ko) 2021-04-16 2023-12-21 아비나스 오퍼레이션스, 인코포레이티드 Bcl6 단백질 분해의 조절제 및 관련 사용 방법
CA3236073A1 (en) 2021-10-26 2023-05-04 Robert J. Brown Piperidinylpyrazine-carboxamide compounds for treating and preventing cancer and for degrading btk
EP4446324A4 (en) * 2021-12-08 2026-05-06 Gluetacs Therapeutics Shanghai Co Ltd Ligand compounds for e3 ubiquitin ligase, protein degraders developed on basis of ligand compounds, and uses thereof
US20230295118A1 (en) * 2022-03-18 2023-09-21 EnhancedBio Inc. Compounds and methods for the targeted degradation of cyclin dependent kinases
JP2025516555A (ja) * 2022-05-10 2025-05-30 バイオセリックス, インコーポレイテッド Cdkタンパク質分解因子、医薬組成物、及び治療応用
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
WO2024054591A1 (en) 2022-09-07 2024-03-14 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use
WO2024056077A1 (en) * 2022-09-15 2024-03-21 Cullgen (Shanghai) , Inc. Modified proteins and protein binders and degraders
WO2024086361A1 (en) * 2022-10-21 2024-04-25 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
EP4705307A1 (en) * 2023-05-03 2026-03-11 St. Jude Children's Research Hospital, Inc. A sequence selective dna binding molecule (syngrader)
PE20252789A1 (es) 2023-05-24 2025-12-22 Kumquat Biosciences Inc Compuestos heterociclicos y usos de estos
WO2024256569A1 (en) * 2023-06-13 2024-12-19 Rijksuniversiteit Groningen Novel cdk degraders
WO2026067249A1 (en) * 2024-09-29 2026-04-02 K2 Medicines (Nanjing) Co., Ltd. Cdk4 or cdk4/6 dual degrader and use thereof

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
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
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
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
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
US9796701B2 (en) 2013-12-31 2017-10-24 Xuanzhu Pharma Co., Ltd. Kinase inhibitor and use thereof
WO2015104677A1 (en) 2014-01-10 2015-07-16 Piramal Enterprises Limited Heterocyclic compounds as ezh2 inhibitors
RU2738833C9 (ru) 2014-04-14 2022-02-28 Арвинас, Оперэйшнз, Инк. Имидные модуляторы протеолиза и способы их применения
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
WO2016073956A1 (en) 2014-11-06 2016-05-12 Dana-Farber Cancer Institute, Inc. Ezh2 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
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
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
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
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
EP3319944A4 (en) 2015-07-10 2019-04-24 Arvinas, Inc. MDM2-BASED MODULATORS OF PROTEOLYSIS AND RELATED USE METHODS
BR112017028269A2 (pt) 2015-07-13 2018-09-04 Arvinas Inc composto, composição farmacêutica, uso de uma quantidade efetiva de um composto, estado ou condição de doença, e, método para identificar um composto.
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
US11319299B2 (en) 2016-03-01 2022-05-03 Propellon Therapeutics Inc. Substituted carboxamides as inhibitors of WDR5 protein-protein binding
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
EP3445765A4 (en) * 2016-04-22 2019-09-18 Dana Farber Cancer Institute, Inc. DECREASE OF CYCLINE-DEPENDENT KINASE 4/6 (CDK4 / 6) BY CONJUGATION OF CDK4 / 6 INHIBITORS WITH E3-LIGASE LIGANDS AND METHODS OF USE
EP3454856B1 (en) 2016-05-10 2024-09-11 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
CN109790143A (zh) * 2016-05-10 2019-05-21 C4医药公司 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体
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
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
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
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
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
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

Also Published As

Publication number Publication date
US20190336503A1 (en) 2019-11-07
WO2018106870A1 (en) 2018-06-14
CA3045037A1 (en) 2018-06-14
US20220054488A1 (en) 2022-02-24
EP3551185A4 (en) 2021-07-14
EP3551185A1 (en) 2019-10-16
CN110267659A (zh) 2019-09-20
US11541051B2 (en) 2023-01-03
JP2020514252A (ja) 2020-05-21

Similar Documents

Publication Publication Date Title
AU2017370694A1 (en) Compositions and methods for treating CDK4/6-mediated cancer
JP7792942B2 (ja) テトラヒドロ-ピリド[3,4-b]インドールエストロゲン受容体モジュレーター及びその使用
KR20250021402A (ko) 헤테로환 화합물 및 이의 용도
WO2019113071A1 (en) Compositions and methods for treating alk-mediated cancer
US10316049B2 (en) Tank-binding kinase inhibitor compounds
US12110295B2 (en) WD40 repeat domain protein 5 (WDR5) degradation/disruption compounds and methods of use
CA3091041A1 (en) Protein arginine methyltransferase 5 (prmt5) degradation / disruption compounds and methods of use
EP3724178B1 (en) 1-(piperidinocarbonylmethyl)-2-oxopiperazine derivatives for treating cancer
BR102019002873A2 (pt) inibidores de pd-1/pd-l1
JP2022531446A (ja) Hpk1の分解剤としてのヘテロ二官能性化合物
JP2022516685A (ja) ホスファターゼ結合化合物およびそれらを使用する方法
CA3096424A1 (en) Pladienolide derivatives as spliceosome targeting agents for treating cancer
CA3105121A1 (en) Protein tyrosine kinase 6 (ptk6) degradation / disruption compounds and methods of use
CN118201896A (zh) PI3K-α抑制剂和其使用方法
EP3830082B1 (en) Cdk inhibitors and uses thereof
EP4709730A1 (en) Heteroaryl compounds as ligand directed degraders of irak4
JPWO2018186366A1 (ja) 新規サイクリン依存性キナーゼ8及び/又は19阻害剤
HK40054608B (en) Cdk inhibitors and uses thereof
HK40054608A (en) Cdk inhibitors and uses thereof

Legal Events

Date Code Title Description
MK4 Application lapsed section 142(2)(d) - no continuation fee paid for the application