TWI819225B - 作為eed抑制劑之咪唑并嘧啶及其用途 - Google Patents

作為eed抑制劑之咪唑并嘧啶及其用途 Download PDF

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Publication number
TWI819225B
TWI819225B TW109124012A TW109124012A TWI819225B TW I819225 B TWI819225 B TW I819225B TW 109124012 A TW109124012 A TW 109124012A TW 109124012 A TW109124012 A TW 109124012A TW I819225 B TWI819225 B TW I819225B
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Taiwan
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group
alkyl
compound
methyl
optionally substituted
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TW109124012A
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TW202116772A (zh
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少萌 王
蘿涵 雷傑
王章偉
王覓
盧建鋒
朝業 楊
薩拉斯 伊斯特 費南德茲
珍妮 史塔基
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美國密西根州立大學
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/22Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains four or more hetero rings
    • 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
    • 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
    • C07D471/22Heterocyclic 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 systems contains four or more hetero 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
    • A61K31/495Heterocyclic 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
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • C07D487/12Heterocyclic 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 three hetero rings
    • C07D487/14Ortho-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
    • C07D487/12Heterocyclic 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 three hetero rings
    • C07D487/16Peri-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
    • C07D487/22Heterocyclic 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 four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/16Peri-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/16Peri-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/22Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/22Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
TW109124012A 2019-07-16 2020-07-16 作為eed抑制劑之咪唑并嘧啶及其用途 TWI819225B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201962874606P 2019-07-16 2019-07-16
US62/874,606 2019-07-16
US201962944608P 2019-12-06 2019-12-06
US62/944,608 2019-12-06

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TW202116772A TW202116772A (zh) 2021-05-01
TWI819225B true TWI819225B (zh) 2023-10-21

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US (2) US12145944B2 (https=)
EP (1) EP3999510A1 (https=)
JP (1) JP7738909B2 (https=)
KR (1) KR102911673B1 (https=)
CN (2) CN114127073B (https=)
AU (1) AU2020315401B2 (https=)
BR (1) BR112022000713A2 (https=)
CA (1) CA3138560A1 (https=)
CL (1) CL2022000093A1 (https=)
IL (1) IL288872B1 (https=)
MX (1) MX2022000550A (https=)
PE (1) PE20220750A1 (https=)
PH (1) PH12021553233A1 (https=)
TW (1) TWI819225B (https=)
UA (1) UA130084C2 (https=)
WO (1) WO2021011713A1 (https=)
ZA (1) ZA202109518B (https=)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113636993B (zh) * 2020-05-11 2022-08-19 苏州亚盛药业有限公司 (5-氟-2,3-二氢苯并呋喃-4-基)甲胺或其盐的制备方法及其中间体
CA3203975A1 (en) 2020-12-03 2022-06-09 Battelle Memorial Institute Polymer nanoparticle and dna nanostructure compositions and methods for non-viral delivery
CN115028631A (zh) * 2021-03-05 2022-09-09 中国科学院上海药物研究所 三氮唑并嘧啶衍生物、其药物组合物及用途
CN115212311B (zh) * 2021-04-19 2024-08-09 苏州亚盛药业有限公司 一种药物组合及其用途
TW202312995A (zh) * 2021-08-11 2023-04-01 大陸商上海青煜醫藥科技有限公司 氮雜芳基化合物、其製備方法及應用
JP2024529118A (ja) * 2021-08-13 2024-08-01 アセンテージ ファーマ(スーチョウ)カンパニー,リミティド 疾患又は障害の治療方法
CN116514814A (zh) * 2022-01-30 2023-08-01 苏州亚盛药业有限公司 一种大环类化合物或其盐、溶剂合物的结晶形式或无定形形式
CA3258934A1 (en) * 2022-06-09 2023-12-14 Battelle Memorial Institute NON-VIRAL ADMINISTRATION OF SMALL MOLECULE THERAPEUTIC AGENTS
WO2024251197A1 (zh) 2023-06-06 2024-12-12 苏州亚盛药业有限公司 Eed抑制剂固体分散体、包含其的口服制剂及其制备方法
AU2024353375A1 (en) 2023-09-29 2026-04-09 Battelle Memorial Institute Polymer nanoparticle compositions for in vivo expression of polypeptides
WO2025113665A1 (zh) * 2023-11-30 2025-06-05 上海海雁医药科技有限公司 稠四杂环衍生物及其药物组合物和用途
WO2025122954A1 (en) 2023-12-08 2025-06-12 Battelle Memorial Institute Use of dna origami nanostructures for molecular information based data storage systems

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017221100A1 (en) * 2016-06-20 2017-12-28 Novartis Ag Imidazopyrimidine compounds useful for the treatment of cancer

Family Cites Families (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5093330A (en) 1987-06-15 1992-03-03 Ciba-Geigy Corporation Staurosporine derivatives substituted at methylamino nitrogen
JP2001523958A (ja) 1997-03-21 2001-11-27 ブライハム アンド ウィミンズ ホスピタル,インコーポレイテッド 免疫療法のctla−4結合ペプチド
PL354286A1 (en) 1999-08-23 2003-12-29 Dana-Farber Cancer Institutedana-Farber Cancer Institute Pd-1, a receptor for b7-4, and uses therefor
EP1212422B1 (en) 1999-08-24 2007-02-21 Medarex, Inc. Human ctla-4 antibodies and their uses
AU2003281200A1 (en) 2002-07-03 2004-01-23 Tasuku Honjo Immunopotentiating compositions
DK2439273T3 (da) 2005-05-09 2019-06-03 Ono Pharmaceutical Co Humane monoklonale antistoffer til programmeret død-1(pd-1) og fremgangsmåder til behandling af cancer ved anvendelse af anti-pd-1- antistoffer alene eller i kombination med andre immunterapeutika
BR122017025062B8 (pt) 2007-06-18 2021-07-27 Merck Sharp & Dohme anticorpo monoclonal ou fragmento de anticorpo para o receptor de morte programada humano pd-1, polinucleotídeo e composição compreendendo o referido anticorpo ou fragmento
AR072999A1 (es) 2008-08-11 2010-10-06 Medarex Inc Anticuerpos humanos que se unen al gen 3 de activacion linfocitaria (lag-3) y los usos de estos
AU2009288730B2 (en) 2008-08-25 2013-06-20 Amplimmune, Inc. Compositions of PD-1 antagonists and methods of use
EP3255060A1 (en) 2008-12-09 2017-12-13 F. Hoffmann-La Roche AG Anti-pd-l1 antibodies and their use to enhance t-cell function
JP4965623B2 (ja) 2009-09-30 2012-07-04 インターナショナル・ビジネス・マシーンズ・コーポレーション 所定のソフトウェアの実行パラメータを入力フィールドへ入力することを支援するための方法、システム、およびプログラム
US8907053B2 (en) 2010-06-25 2014-12-09 Aurigene Discovery Technologies Limited Immunosuppression modulating compounds
WO2013006490A2 (en) 2011-07-01 2013-01-10 Cellerant Therapeutics, Inc. Antibodies that specifically bind to tim3
WO2013043569A1 (en) 2011-09-20 2013-03-28 Vical Incorporated Synergistic anti-tumor efficacy using alloantigen combination immunotherapy
KR101764096B1 (ko) 2011-11-28 2017-08-02 메르크 파텐트 게엠베하 항-pd-l1 항체 및 그의 용도
HK1203971A1 (en) 2012-05-15 2015-11-06 Bristol-Myers Squibb Company Cancer immunotherapy by disrupting pd-1/pd-l1 signaling
UY34887A (es) 2012-07-02 2013-12-31 Bristol Myers Squibb Company Una Corporacion Del Estado De Delaware Optimización de anticuerpos que se fijan al gen de activación de linfocitos 3 (lag-3) y sus usos
WO2014022332A1 (en) 2012-07-31 2014-02-06 The Brigham And Women's Hospital, Inc. Modulation of the immune response
US10344088B2 (en) 2013-03-15 2019-07-09 Glaxosmithkline Intellectual Property Development Limited Antigen binding proteins
WO2015036499A1 (en) 2013-09-11 2015-03-19 Medimmune Limited Anti-b7-h1 antibodies for treating tumors
AU2015225867B2 (en) 2014-03-07 2020-02-06 University Health Network Methods and compositions for modifying the immune response
KR102442436B1 (ko) 2014-03-14 2022-09-15 노파르티스 아게 Lag-3에 대한 항체 분자 및 그의 용도
UY36462A (es) 2014-12-23 2016-07-29 Novartis Ag Compuestos de triazolopirimidina y usos de los mismos
WO2017221092A1 (en) 2016-06-20 2017-12-28 Novartis Ag Triazolopyridine compounds and uses thereof
JP7631193B2 (ja) 2018-10-22 2025-02-18 アルミス インコーポレイテッド Tyk2阻害剤およびその使用
CA3142351A1 (en) 2019-05-31 2020-12-03 Ikena Oncology, Inc. Tead inhibitors and uses thereof
CA3141826A1 (en) 2019-05-31 2020-12-03 Ikena Oncology, Inc. Tead inhibitors and uses thereof
BR112022010924A2 (pt) 2019-12-06 2022-09-06 Vertex Pharma Tetra-hidrofuranos substituídos como moduladores de canais de sódio

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017221100A1 (en) * 2016-06-20 2017-12-28 Novartis Ag Imidazopyrimidine compounds useful for the treatment of cancer

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ZA202109518B (en) 2023-10-25
PE20220750A1 (es) 2022-05-10
CN118745185A (zh) 2024-10-08
TW202116772A (zh) 2021-05-01
CL2022000093A1 (es) 2022-10-28
IL288872B1 (en) 2026-04-01
EP3999510A1 (en) 2022-05-25
JP7738909B2 (ja) 2025-09-16
US20250034162A1 (en) 2025-01-30
BR112022000713A2 (pt) 2022-03-22
WO2021011713A8 (en) 2022-01-06
AU2020315401B2 (en) 2025-05-22
US12145944B2 (en) 2024-11-19
US20220227778A1 (en) 2022-07-21
CN114127073B (zh) 2024-05-31
IL288872A (en) 2022-02-01
MX2022000550A (es) 2022-02-10
KR20220035116A (ko) 2022-03-21
UA130084C2 (uk) 2025-11-05
JP2022541436A (ja) 2022-09-26
CN114127073A (zh) 2022-03-01
PH12021553233A1 (en) 2022-09-19
AU2020315401A1 (en) 2022-02-17
WO2021011713A1 (en) 2021-01-21
KR102911673B1 (ko) 2026-01-13
CA3138560A1 (en) 2021-01-21

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