CN112313220A - Pd-l1拮抗剂化合物 - Google Patents

Pd-l1拮抗剂化合物 Download PDF

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Publication number
CN112313220A
CN112313220A CN202080003296.6A CN202080003296A CN112313220A CN 112313220 A CN112313220 A CN 112313220A CN 202080003296 A CN202080003296 A CN 202080003296A CN 112313220 A CN112313220 A CN 112313220A
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Prior art keywords
alkylene
compound
alkyl
added
cycloalkyl
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CN202080003296.6A
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CN112313220B (zh
Inventor
李磐
徐贝帝
温俏冬
冯恩光
王骥
路杨
周瑜
俞智勇
黄芝英
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Xiamen Baotai Biotechnology Co ltd
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Hangzhou Arnold Biomedical Technology Co ltd
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Priority to CN202110060670.2A priority Critical patent/CN112876458B/zh
Priority to CN202110060576.7A priority patent/CN112876411A/zh
Priority to CN202110060679.3A priority patent/CN112876463B/zh
Publication of CN112313220A publication Critical patent/CN112313220A/zh
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    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/145Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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 linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • 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
    • 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
    • C07D471/10Spiro-condensed systems

Abstract

本发明提供了一种式(I)化合物及其药物组合物,以及使用式(I)化合物预防和/或治疗免疫相关病症的方法。

Description

PCT国内申请,说明书已公开。

Claims (24)

  1. PCT国内申请,权利要求书已公开。
CN202080003296.6A 2019-02-21 2020-02-20 Pd-l1拮抗剂化合物 Active CN112313220B (zh)

Priority Applications (3)

Application Number Priority Date Filing Date Title
CN202110060670.2A CN112876458B (zh) 2019-02-21 2020-02-20 细胞程序性死亡-配体-1拮抗剂化合物
CN202110060576.7A CN112876411A (zh) 2019-02-21 2020-02-20 化合物及其在合成pdl1拮抗剂类药物分子中的应用
CN202110060679.3A CN112876463B (zh) 2019-02-21 2020-02-20 一种制备pd-l1拮抗剂的中间体及其制备方法

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN2019101303131 2019-02-21
CN201910130313 2019-02-21
CN201910695768 2019-07-30
CN2019106957688 2019-07-30
PCT/CN2020/075938 WO2020169058A1 (zh) 2019-02-21 2020-02-20 Pd-l1拮抗剂化合物

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CN202110060576.7A Division CN112876411A (zh) 2019-02-21 2020-02-20 化合物及其在合成pdl1拮抗剂类药物分子中的应用
CN202110060679.3A Division CN112876463B (zh) 2019-02-21 2020-02-20 一种制备pd-l1拮抗剂的中间体及其制备方法
CN202110060670.2A Division CN112876458B (zh) 2019-02-21 2020-02-20 细胞程序性死亡-配体-1拮抗剂化合物

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CN112313220B CN112313220B (zh) 2023-11-03

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CN202110060576.7A Pending CN112876411A (zh) 2019-02-21 2020-02-20 化合物及其在合成pdl1拮抗剂类药物分子中的应用
CN202110060670.2A Active CN112876458B (zh) 2019-02-21 2020-02-20 细胞程序性死亡-配体-1拮抗剂化合物
CN202080003296.6A Active CN112313220B (zh) 2019-02-21 2020-02-20 Pd-l1拮抗剂化合物
CN202110060679.3A Active CN112876463B (zh) 2019-02-21 2020-02-20 一种制备pd-l1拮抗剂的中间体及其制备方法

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CN202110060576.7A Pending CN112876411A (zh) 2019-02-21 2020-02-20 化合物及其在合成pdl1拮抗剂类药物分子中的应用
CN202110060670.2A Active CN112876458B (zh) 2019-02-21 2020-02-20 细胞程序性死亡-配体-1拮抗剂化合物

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US (1) US20220227733A1 (zh)
EP (1) EP3929188A4 (zh)
JP (1) JP7281834B2 (zh)
CN (4) CN112876411A (zh)
TW (1) TW202045487A (zh)
WO (1) WO2020169058A1 (zh)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115066423A (zh) * 2019-12-26 2022-09-16 杭州阿诺生物医药科技有限公司 Pd-l1拮抗剂化合物

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023104744A1 (en) 2021-12-06 2023-06-15 Helmholtz-Zentrum Dresden-Rossendorf E.V. 3-((3-([1,1'-biphenyl]-3-ylmethoxy)phenoxy)methyl)benzonitrile derivatives and the use thereof

Citations (3)

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WO2018009505A1 (en) * 2016-07-08 2018-01-11 Bristol-Myers Squibb Company 1,3-dihydroxy-phenyl derivatives useful as immunomodulators
WO2018195321A1 (en) * 2017-04-20 2018-10-25 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
CN109665968A (zh) * 2017-10-16 2019-04-23 四川科伦博泰生物医药股份有限公司 并环化合物及其制备方法和用途

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WO2009015037A2 (en) * 2007-07-21 2009-01-29 Albany Molecular Research, Inc. 5-pyridinone substituted indazoles
MX2016002544A (es) * 2013-09-04 2016-06-17 Squibb Bristol Myers Co Compuestos utiles como inmunomoduladores.
US9850225B2 (en) * 2014-04-14 2017-12-26 Bristol-Myers Squibb Company Compounds useful as immunomodulators
EP3459925B1 (en) * 2016-05-23 2021-08-11 Tianjin Chase Sun Pharmaceutical Co., Ltd. Method for preparing 2-hydroxyl-4-(2, 3-disubstituted benzyloxy)-5-substituted benzaldehyde derivative
WO2018119263A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Heterocyclic compounds derivatives as pd-l1 internalization inducers

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018009505A1 (en) * 2016-07-08 2018-01-11 Bristol-Myers Squibb Company 1,3-dihydroxy-phenyl derivatives useful as immunomodulators
WO2018195321A1 (en) * 2017-04-20 2018-10-25 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
CN109665968A (zh) * 2017-10-16 2019-04-23 四川科伦博泰生物医药股份有限公司 并环化合物及其制备方法和用途

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115066423A (zh) * 2019-12-26 2022-09-16 杭州阿诺生物医药科技有限公司 Pd-l1拮抗剂化合物
CN115066423B (zh) * 2019-12-26 2024-02-02 厦门宝太生物科技股份有限公司 Pd-l1拮抗剂化合物

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CN112876411A (zh) 2021-06-01
WO2020169058A1 (zh) 2020-08-27
TW202045487A (zh) 2020-12-16
CN112876463B (zh) 2022-11-11
CN112313220B (zh) 2023-11-03
JP2022501397A (ja) 2022-01-06
CN112876463A (zh) 2021-06-01
EP3929188A4 (en) 2022-10-12
CN112876458B (zh) 2022-10-04
EP3929188A1 (en) 2021-12-29
JP7281834B2 (ja) 2023-05-26
CN112876458A (zh) 2021-06-01
US20220227733A1 (en) 2022-07-21

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Address after: 361000 floor 3-5, No. 188, Pingcheng South Road, Haicang street, Haicang District, Xiamen City, Fujian Province

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