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CN111263759A - 异噁唑衍生物及其制备方法和用途 - Google Patents

异噁唑衍生物及其制备方法和用途 Download PDF

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Publication number
CN111263759A
CN111263759A CN201880068730.1A CN201880068730A CN111263759A CN 111263759 A CN111263759 A CN 111263759A CN 201880068730 A CN201880068730 A CN 201880068730A CN 111263759 A CN111263759 A CN 111263759A
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CN111263759B (zh
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刘金明
蔡家强
吴勇勇
尹伟
王利春
王晶翼
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Sichuan Kelun Biotech Biopharmaceutical Co Ltd
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    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
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    • 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
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    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

本发明一般涉及异噁唑衍生物及其制备方法和用途。具体地，本发明提供类法尼醇X受体(FXR)激动剂化合物以及其立体异构体、互变异构体、多晶型物、溶剂合物(如水合物)、药学可接受的盐、酯、代谢物、N‑氧化物以及其化学保护的形式和前药。本发明还提供所述化合物的制备方法、中间体、包含所述化合物的药物组合物和药盒以及它们用于治疗由FXR介导的疾病或病症的用途。

Description

PCT国内申请，说明书已公开。

Claims (16)

  1. PCT国内申请，权利要求书已公开。
CN201880068730.1A 2017-12-22 2018-12-07 异噁唑衍生物及其制备方法和用途 Active CN111263759B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN201711402082 2017-12-22
CN2017114020822 2017-12-22
CN201810038649 2018-01-16
CN2018100386490 2018-01-16
PCT/CN2018/119715 WO2019120088A1 (zh) 2017-12-22 2018-12-07 异噁唑衍生物及其制备方法和用途

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CN111263759A true CN111263759A (zh) 2020-06-09
CN111263759B CN111263759B (zh) 2023-03-28

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US (1) US11667629B2 (zh)
EP (1) EP3730491B1 (zh)
JP (1) JP7243959B2 (zh)
KR (1) KR20200102415A (zh)
CN (1) CN111263759B (zh)
WO (1) WO2019120088A1 (zh)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112805279A (zh) * 2018-12-07 2021-05-14 四川科伦博泰生物医药股份有限公司 异噁唑衍生物及其制备方法和用途
CN113412261A (zh) * 2019-04-08 2021-09-17 四川科伦博泰生物医药股份有限公司 苯并咪唑化合物、其制备方法及其用途
CN114195777A (zh) * 2020-09-18 2022-03-18 凯思凯迪（上海）医药科技有限公司 新型fxr小分子激动剂制备及其用途

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110128432B (zh) 2018-02-02 2021-03-02 广东东阳光药业有限公司 含氮三环化合物及其在药物中的应用
CN112955448B (zh) * 2019-01-31 2023-02-03 中国医药研究开发中心有限公司 芳环或芳杂环类化合物及其制备方法和医药用途
BR112021020681A2 (pt) * 2019-04-19 2021-12-07 Shanghai Inst Materia Medica Cas Agonista de molécula pequena de fxr e método de preparação para o mesmo e uso do mesmo
CN112812114B (zh) * 2019-11-15 2024-05-28 四川科伦博泰生物医药股份有限公司 异噁唑衍生物、包含其的药物组合物及其制备方法和用途
CN114945361A (zh) 2020-01-15 2022-08-26 法国国家卫生及研究医学协会 Fxr激动剂在治疗丁型肝炎病毒感染中的用途
CN114195776B (zh) * 2020-09-18 2023-06-20 凯思凯迪（上海）医药科技有限公司 新型fxr小分子激动剂制备及其用途
CN114315830B (zh) * 2020-09-30 2025-08-12 中国科学院上海药物研究所 Fxr小分子激动剂及其制备方法和用途
AU2022209084A1 (en) 2021-01-14 2023-08-10 Centre Leon Bérard Synergistic effect of a fxr agonist and ifn for the treatment of hbv infection
WO2022229302A1 (en) 2021-04-28 2022-11-03 Enyo Pharma Strong potentiation of tlr3 agonists effects using fxr agonists as a combined treatment
CN113666883B (zh) * 2021-07-23 2023-06-16 华南理工大学 一种合成4-乙烯基异噁唑衍生物的方法
EP4245365B1 (en) * 2022-03-16 2025-05-07 Cascade Pharmaceuticals, Inc. A fxr small molecule agonist, the preparation and use thereof

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CN107108595A (zh) * 2014-12-17 2017-08-29 吉利德科学公司 新的fxr(nr1h4)调节化合物

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CN104045635A (zh) * 2014-06-23 2014-09-17 华东理工大学 3,4,5-三取代异恶唑类化合物及其用途
JP2017537960A (ja) 2014-12-18 2017-12-21 ノバルティス アーゲー 肝疾患および胃腸疾患の治療に使用するためのｆｘｒアゴニストとしてのアザビシクロオクタン誘導体
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WO2009149795A2 (en) * 2008-05-26 2009-12-17 Phenex Pharmaceuticals Ag Heterocyclic cyclopropyl-substituted fxr binding compounds
CN103391937A (zh) * 2010-12-20 2013-11-13 Irm责任有限公司 用于调控法尼醇x受体的组合物和方法
CN107108595A (zh) * 2014-12-17 2017-08-29 吉利德科学公司 新的fxr(nr1h4)调节化合物

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112805279A (zh) * 2018-12-07 2021-05-14 四川科伦博泰生物医药股份有限公司 异噁唑衍生物及其制备方法和用途
CN112805279B (zh) * 2018-12-07 2023-09-12 四川科伦博泰生物医药股份有限公司 异噁唑衍生物及其制备方法和用途
CN113412261A (zh) * 2019-04-08 2021-09-17 四川科伦博泰生物医药股份有限公司 苯并咪唑化合物、其制备方法及其用途
CN114195777A (zh) * 2020-09-18 2022-03-18 凯思凯迪（上海）医药科技有限公司 新型fxr小分子激动剂制备及其用途
CN114195777B (zh) * 2020-09-18 2023-06-20 凯思凯迪（上海）医药科技有限公司 新型fxr小分子激动剂制备及其用途

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EP3730491A4 (en) 2021-06-09
JP7243959B2 (ja) 2023-03-22
EP3730491B1 (en) 2022-07-20
KR20200102415A (ko) 2020-08-31
JP2021506745A (ja) 2021-02-22
WO2019120088A1 (zh) 2019-06-27
EP3730491A1 (en) 2020-10-28
US20200339558A1 (en) 2020-10-29
US11667629B2 (en) 2023-06-06
CN111263759B (zh) 2023-03-28

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