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

Info

Publication number
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
Authority
JP
Japan
Prior art keywords
mmol
ezh2
cancer
compound
cells
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.)
Pending
Application number
JP2019522841A
Other languages
English (en)
Japanese (ja)
Other versions
JP2019537585A5 (https=
Inventor
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
Original Assignee
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
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 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 filed Critical 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
Publication of JP2019537585A publication Critical patent/JP2019537585A/ja
Publication of JP2019537585A5 publication Critical patent/JP2019537585A5/ja
Pending legal-status Critical Current

Links

Classifications

    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (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

Publications (2)

Publication Number Publication Date
JP2019537585A true JP2019537585A (ja) 2019-12-26
JP2019537585A5 JP2019537585A5 (https=) 2021-09-16

Family

ID=62024052

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2019522841A Pending JP2019537585A (ja) 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

Country Status (12)

Country Link
US (3) US20190255041A1 (https=)
EP (1) EP3532464A4 (https=)
JP (1) JP2019537585A (https=)
KR (1) KR20190084063A (https=)
CN (1) CN110167924A (https=)
AU (2) AU2017348322B8 (https=)
CA (1) CA3041840A1 (https=)
EA (1) EA201991071A1 (https=)
IL (1) IL266053A (https=)
MX (1) MX2019004950A (https=)
SG (2) SG10202104386UA (https=)
WO (1) WO2018081530A1 (https=)

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
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
JP2020514252A (ja) 2016-12-08 2020-05-21 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 Ｃｄｋ４／６媒介性がんを治療するための組成物および方法
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
CA3092677A1 (en) 2018-03-06 2019-09-12 Icahn School Of Medicine At Mount Sinai Serine threonine kinase (akt) degradation / disruption compounds and methods of use
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
CA3104298A1 (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
JP7712867B2 (ja) * 2018-11-02 2025-07-24 ダナ－ファーバー キャンサー インスティテュート，インコーポレイテッド アセチル化ライター阻害剤の開発およびその使用
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
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
DK4034535T3 (da) 2019-09-26 2026-04-07 Novartis Ag Aza-quinolinforbindelser og anvendelser deraf
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
KR102505664B1 (ko) * 2019-10-31 2023-03-03 재단법인 대구경북첨단의료산업진흥재단 Ezh2 저해제　및　e3 리가제 바인더를 포함하는 화합물 및 이를 유효성분으로 함유하는 ezh2 관련 질환의 예방 또는 치료용 약학적 조성물
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
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
AU2024307234A1 (en) 2023-06-30 2026-01-29 Kumquat Biosciences Inc. Substituted condensed tricyclic amine compounds and uses thereof as ras inhibitors
WO2025096855A1 (en) 2023-11-02 2025-05-08 Kumquat Biosciences Inc. Degraders and uses thereof
KR20250088371A (ko) * 2023-12-08 2025-06-17 인제대학교 산학협력단 Ezh2 저해제 및 jak3 억제제를 포함하는 암의 예방 또는 치료용 약학적 조성물
KR20250088374A (ko) * 2023-12-08 2025-06-17 인제대학교 산학협력단 Ezh2 저해제 및 mettl3 억제제를 포함하는 암의 예방 또는 치료용 약제학적 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
SI1255752T1 (sl) 2000-02-15 2007-12-31 Pharmacia & Upjohn Co Llc S pirolom substituirani zaviralci 2-indolinon protein kinaza
CA2546754A1 (en) 2003-11-21 2005-06-09 Array Biopharma Inc. Akt protein kinase inhibitors
CA2590961C (en) 2004-12-28 2013-11-26 Exelixis, Inc. [1h-pyrazolo[3,4-d]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-threonine kinase modulators (p70s6k, atk1 and atk2) for the treatment of immunological, inflammatory and proliferative diseases
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
EP2049500B1 (en) 2006-07-06 2011-09-07 Array Biopharma, Inc. Cyclopenta [d] pyrimidines as akt protein kinase inhibitors
PL2076260T3 (pl) 2006-09-15 2011-08-31 Celgene Corp Związki N-metyloaminometylo-izoindolu, kompozycje zawierające te związki, oraz metody ich stosowania
WO2008109104A1 (en) 2007-03-07 2008-09-12 The Regents Of The University Of California Bivalent inhibitors of akt protein kinase
CN103396409B (zh) 2007-07-05 2015-03-11 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
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
EP2473054B1 (en) 2009-09-04 2017-06-14 The Regents of the University of Michigan Compositions and methods for treatment of leukemia
EP2536706B1 (en) 2010-02-11 2017-06-14 Celgene Corporation Arylmethoxy isoindoline derivatives and compositions comprising and methods of using the same
CN103189067A (zh) 2010-06-16 2013-07-03 密执安大学评议会 Wdr5与其结合配偶体的相互作用的抑制及治疗方法
WO2012078492A1 (en) 2010-12-06 2012-06-14 Celgene Corporation A combination therapy with lenalidomide and a cdk inhibitor for treating multiple myeloma
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
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
UA118548C2 (uk) 2012-12-21 2019-02-11 Епізайм, Інк. Тетрагідро- та дигідроізохіноліни як інгібітори prmt5 та їх застосування
US20170305857A1 (en) 2013-12-20 2017-10-26 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
JP6744826B2 (ja) 2014-06-13 2020-08-19 バック バイオサイエンシーズ, エルエルシーBach BioSciences, LLC Ｆａｐ活性化治療剤及びそれに関連する使用
EP3177288A4 (en) 2014-08-04 2018-04-04 Epizyme, Inc. Prmt5 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
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
US10364247B2 (en) 2015-04-21 2019-07-30 Ruijin Hospital Affiliated To Shanghai Jiao Tong University School Of Medicine Preparation and use of novel protein kinase inhibitors
EP3289074B1 (en) 2015-04-28 2023-10-04 Université de Strasbourg Clinical gene signature-based human cell culture model and uses thereof
HUE054149T2 (hu) 2015-06-04 2021-08-30 Arvinas Operations Inc Proteolízis imid-alapú modulátorai és ezekkel kapcsolatos felhasználási eljárások
RU2719477C2 (ru) 2015-06-22 2020-04-17 Оно Фармасьютикал Ко., Лтд. Соединение, ингибирующее 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
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
WO2017024317A2 (en) 2015-08-06 2017-02-09 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
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
WO2017040990A1 (en) 2015-09-03 2017-03-09 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
AU2016349781A1 (en) 2015-11-02 2018-05-10 Yale University Proteolysis targeting chimera compounds and methods of preparing and using same
CA3015417A1 (en) 2016-03-01 2017-09-08 Propellon Therapeutics Inc. Inhibitors of wdr5 protein-protein binding
JP7624690B2 (ja) 2016-03-01 2025-01-31 プロペロン セラピューティクス 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
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
EP4491236A3 (en) 2016-05-10 2025-04-02 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
TW201811799A (zh) 2016-09-09 2018-04-01 美商英塞特公司 吡唑并嘧啶化合物及其用途
UA125650C2 (uk) 2016-09-09 2022-05-11 Інсайт Корпорейшн Регулятори нрk1 на основі похідних піразолопіридину та їх застосування для лікування раку
US10160763B2 (en) 2016-09-13 2018-12-25 Vanderbilt University WDR5 inhibitors and modulators
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
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
JP2020514252A (ja) 2016-12-08 2020-05-21 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 Ｃｄｋ４／６媒介性がんを治療するための組成物および方法
US11052091B2 (en) 2016-12-21 2021-07-06 Ono Pharmaceutical Co., Ltd. BRK inhibitory compound
MX2019007646A (es) 2016-12-23 2019-09-06 Arvinas Operations Inc Moleculas quimericas dirigidas a la proteolisis del egfr y metodos asociados de uso.
BR112019015484A2 (pt) 2017-01-31 2020-04-28 Arvinas Operations Inc ligantes de cereblon e compostos bifuncionais compreendendo os mesmos
WO2019084030A1 (en) 2017-10-24 2019-05-02 Genentech, Inc. (4-HYDROXYPYRROLIDIN-2-YL) -HYDROXAMATE COMPOUNDS AND METHODS OF USE
WO2019113071A1 (en) 2017-12-05 2019-06-13 Icahn School Of Medicine At Mount Sinai Compositions and methods for treating alk-mediated cancer
EP3743069B1 (en) 2018-01-22 2025-08-06 BioVentures, LLC Bcl-2 proteins degraders for cancer treatment
WO2019165189A1 (en) 2018-02-22 2019-08-29 Icahn School Of Medicine At Mount Sinai Protein arginine methyltransferase 5 (prmt5) degradation / disruption compounds and methods of use
CA3092677A1 (en) 2018-03-06 2019-09-12 Icahn School Of Medicine At Mount Sinai Serine threonine kinase (akt) degradation / disruption compounds and methods of use
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
CA3104298A1 (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
EP3817745A4 (en) 2018-07-05 2022-04-06 Icahn School of Medicine at Mount Sinai PROTEIN TYROSINE KINASE 6 (PTK6) DEGRADATION/DISPUTED COMPOUNDS AND METHODS OF USE
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
CN114269749B (zh) 2019-06-10 2024-10-01 苏特罗生物制药公司 5H-吡咯并[3,2-d]嘧啶-2,4-二氨基化合物及其抗体偶联物
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
WO2023006063A1 (en) 2021-07-30 2023-02-02 Beigene, Ltd. PYRROLO [2, 3-b] PYRAZINE-BASED BIFUNCTIONAL COMPOUNDS AS HPK1 DEGRADERS AND THE USE THEREOF

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｝

Also Published As

Publication number Publication date
IL266053A (en) 2019-06-30
EA201991071A1 (ru) 2019-11-29
WO2018081530A1 (en) 2018-05-03
EP3532464A1 (en) 2019-09-04
AU2017348322B8 (en) 2021-12-23
AU2017348322A8 (en) 2021-12-23
SG11201903483VA (en) 2019-05-30
AU2022201488A1 (en) 2022-03-24
EP3532464A4 (en) 2020-07-08
US12274697B2 (en) 2025-04-15
SG10202104386UA (en) 2021-05-28
MX2019004950A (es) 2019-09-26
KR20190084063A (ko) 2019-07-15
US11510920B2 (en) 2022-11-29
CA3041840A1 (en) 2018-05-03
US20190255041A1 (en) 2019-08-22
AU2017348322A1 (en) 2019-06-13
US20230114294A1 (en) 2023-04-13
AU2017348322B2 (en) 2021-12-09
US20200338070A1 (en) 2020-10-29
CN110167924A (zh) 2019-08-23

Similar Documents

Publication Publication Date Title
JP2019537585A (ja) Ｅｚｈ２媒介性がんを治療するための組成物および方法
US20210163464A1 (en) Pyridine compound
US20210283261A1 (en) Compositions and Methods for Treating ALK-Mediated Cancer
EP3791897A1 (en) Hsp90 inhibitor drug conjugates
CA3045037A1 (en) Compositions and methods for treating cdk4/6-mediated cancer
Jiang et al. Design, synthesis, and biological evaluation of Bcr-Abl PROTACs to overcome T315I mutation
JP2021107456A (ja) インドリノン化合物の使用
JP2020531440A (ja) 活性酸素種スカベンジャー誘導体の調製および使用
EP3481822A1 (en) MULTIFUNCTIONAL INHIBITORS OF MEK/PI3K AND mTOR/MEK/PI3K BIOLOGICAL PATHWAYS AND THERAPEUTIC METHODS USING THE SAME
CN109922834B (zh) 用于治疗癌症的卟啉化合物和组合物
EP4605088A1 (en) Molecular glue degrader compounds and uses thereof
CA3224123A1 (en) Small molecule inhibition of deubiquitinating enzyme josephin domain containing 1 (josd1) as a targeted therapy for leukemias with mutant janus kinase 2 (jak2)
AU2015256266B2 (en) BH4 antagonists and methods related thereto
WO2025226951A1 (en) Molecular glue degrader compounds and uses thereof
WO2025056913A1 (en) Compound and method
WO2019171379A1 (en) Compounds for inhibiting protein degradation and methods of use thereof in the treatment of cancer
CN120435320A (zh) 用于放射成像和癌症治疗的化合物
HK40008068B (zh) 用於治疗癌症的卟啉化合物和组合物
HK40008068A (en) Porphyrin compounds and compositions useful for treating cancer
HK40005148B (en) Pyridine compound
HK40005148A (en) Pyridine compound
HK1120406A (en) Combination administration of an indolinone with a chemotherapeutic agent for cell proliferation disorders

Legal Events

Date Code Title Description
A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20201026

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20210802

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20210922

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20211005

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20211224

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20220405

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A821

Effective date: 20220405

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20220712