CN111094317A - 一种具有cd73抑制活性的膦酸衍生物、其制备方法和应用 - Google Patents

一种具有cd73抑制活性的膦酸衍生物、其制备方法和应用 Download PDF

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CN111094317A
CN111094317A CN201880057756.6A CN201880057756A CN111094317A CN 111094317 A CN111094317 A CN 111094317A CN 201880057756 A CN201880057756 A CN 201880057756A CN 111094317 A CN111094317 A CN 111094317A
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deuterium
cancer
radical
substituted
cycloalkyl
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CN111094317B (zh
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邓海兵
赵保卫
应海燕
喻红平
陈椎
徐耀昌
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Abbisko Therapeutics Co Ltd
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Abbisko Therapeutics Co Ltd
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    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7076—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16—Purine radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16—Purine radicals
    • C07H19/20—Purine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16—Purine radicals
    • C07H19/20—Purine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • C07H19/207—Purine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids the phosphoric or polyphosphoric acids being esterified by a further hydroxylic compound, e.g. flavine adenine dinucleotide or nicotinamide-adenine dinucleotide
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Abstract

本发明涉及一种式(Ⅰ)结构具有CD73抑制活性的膦酸衍生物、其制备方法和应用。本发明系列化合物可广泛应用于制备治疗至少部分由CD73介导的癌症或肿瘤、自身免疫性疾病及紊乱、代谢性疾病的药物，特别是治疗黑色素瘤、结肠癌、胰腺癌、乳腺癌、***癌、肺癌、白血病、脑瘤、淋巴瘤、卵巢癌和卡波西氏肉瘤的药物，有望开发成新一代CD73抑制剂药物。

Description

PCT国内申请，说明书已公开。

Claims (22)

  1. PCT国内申请，权利要求书已公开。
CN201880057756.6A 2017-12-29 2018-12-26 一种具有cd73抑制活性的膦酸衍生物、其制备方法和应用 Active CN111094317B (zh)

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CN2017114695777 2017-12-29
CN201711469577 2017-12-29
PCT/CN2018/123908 WO2019129059A1 (zh) 2017-12-29 2018-12-26 一种具有cd73抑制活性的膦酸衍生物、其制备方法和应用

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114286824A (zh) * 2019-04-16 2022-04-05 博奥阿迪斯生物科技公司 Cd73抑制剂
CN115960106A (zh) * 2022-11-03 2023-04-14 中国药科大学 线粒体rna聚合酶抑制剂及其衍生物、药物组合物和医药用途

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CA3008171A1 (en) 2015-12-22 2017-06-29 SHY Therapeutics LLC Compounds for the treatment of cancer and inflammatory disease
IL310023A (en) 2017-06-21 2024-03-01 SHY Therapeutics LLC Compounds interacting with the RAS superfamily for the treatment of cancer, inflammation, RAS pathology and fibrotic diseases
TWI821559B (zh) * 2019-04-28 2023-11-11 大陸商上海和譽生物醫藥科技有限公司 一種cd73抑制劑，其製備方法和應用
WO2021040356A1 (en) * 2019-08-23 2021-03-04 Kainos Medicine, Inc. C-nucleosides, c-nucleotides and their analogs, equivalents and prodrugs thereof for ectonucleotidase inhibition
TWI794742B (zh) 2020-02-18 2023-03-01 美商基利科學股份有限公司 抗病毒化合物
WO2021254417A1 (zh) * 2020-06-17 2021-12-23 贝达药业股份有限公司 双环类化合物及其应用
WO2022221514A1 (en) 2021-04-16 2022-10-20 Gilead Sciences, Inc. Methods of preparing carbanucleosides using amides
WO2023102472A1 (en) * 2021-12-01 2023-06-08 The Scripps Research Institute Antiviral prodrugs and formulations thereof
WO2023201267A1 (en) 2022-04-13 2023-10-19 Gilead Sciences, Inc. Combination therapy for treating trop-2 expressing cancers

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US9029346B1 (en) * 2013-12-13 2015-05-12 The Johns Hopkins University Irreversible inhibitors of DNA polymerase beta
WO2017120508A1 (en) * 2016-01-08 2017-07-13 Arcus Biosciences, Inc. Modulators of 5'-nucleotidase, ecto and the use thereof

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US11058704B2 (en) * 2016-10-03 2021-07-13 Arcus Biosciences, Inc. Inhibitors of adenosine 5′-nucleotidase
WO2018208980A1 (en) * 2017-05-10 2018-11-15 Oric Pharmaceuticals, Inc. Cd73 inhibitors

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9029346B1 (en) * 2013-12-13 2015-05-12 The Johns Hopkins University Irreversible inhibitors of DNA polymerase beta
WO2017120508A1 (en) * 2016-01-08 2017-07-13 Arcus Biosciences, Inc. Modulators of 5'-nucleotidase, ecto and the use thereof

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114286824A (zh) * 2019-04-16 2022-04-05 博奥阿迪斯生物科技公司 Cd73抑制剂
CN115960106A (zh) * 2022-11-03 2023-04-14 中国药科大学 线粒体rna聚合酶抑制剂及其衍生物、药物组合物和医药用途
CN115960106B (zh) * 2022-11-03 2024-03-26 中国药科大学 线粒体rna聚合酶抑制剂及其衍生物、药物组合物和医药用途

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