CN111868056A - 1,2,4-噁二唑类化合物及其制备方法和医药用途 - Google Patents

1,2,4-噁二唑类化合物及其制备方法和医药用途 Download PDF

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CN111868056A
CN111868056A CN201980018242.4A CN201980018242A CN111868056A CN 111868056 A CN111868056 A CN 111868056A CN 201980018242 A CN201980018242 A CN 201980018242A CN 111868056 A CN111868056 A CN 111868056A
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compound
alkyl
halogen
cycloalkyl
cyclopropyl
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CN111868056B (zh
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殷惠军
闫旭
宗利斌
刘春艳
史建新
王斌
米桢
司春枫
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National Institutes of Pharmaceutical R&D 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
    • A61K31/33—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
    • 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
    • A61K31/41—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
    • A61K31/4245—Oxadiazoles
    • 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
    • A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

涉及1,2,4‑噁二唑类化合物及其制备方法和医药用途，特别涉及通式(I)所示的化合物、其制备方法及含有该化合物的药物组合物，及其作为法尼醇衍生物X受体(Farnesoid X receptor，FXR)激动剂的用途，该化合物及含有该化合物的药物组合物可以用于治疗和/或预防与FXR活性相关的疾病，例如胆汁郁积病症、糖尿病及其并发症、如非酒精性脂肪肝(NAFLD)、非酒精性脂肪肝炎(NASH)、肥胖或代谢综合征(血脂障碍、糖尿病和体重指数异常高的合并病症)、心血管疾病等。其中通式(I)中的各取代基的定义与说明书中的定义相同。

Description

PCT国内申请，说明书已公开。

Claims (14)

  1. PCT国内申请，权利要求书已公开。
CN201980018242.4A 2018-07-11 2019-07-09 1,2,4-噁二唑类化合物及其制备方法和医药用途 Active CN111868056B (zh)

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CN2018107560036 2018-07-11
CN201810756003 2018-07-11
PCT/CN2019/095201 WO2020011146A1 (zh) 2018-07-11 2019-07-09 1,2,4-噁二唑类化合物及其制备方法和医药用途

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114315844A (zh) * 2022-01-18 2022-04-12 中国科学院上海药物研究所 一类fxr调节剂及其制备方法和用途

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3919489A4 (en) * 2019-01-31 2022-10-12 The National Institutes of Pharmaceutical R&D Co., Ltd AROMATIC RING OR HETEROAROMATIC RING COMPOUNDS, PROCESS FOR THEIR PRODUCTION AND MEDICAL USE
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
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
CN114315830A (zh) * 2020-09-30 2022-04-12 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
CN117202905A (zh) 2021-01-14 2023-12-08 埃尼奥制药公司 Fxr激动剂和ifn用于治疗hbv感染的协同效果
CN117320722A (zh) 2021-04-28 2023-12-29 埃尼奥制药公司 使用fxr激动剂作为联合治疗强烈增强tlr3激动剂的作用

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2016100161A1 (en) * 2014-12-19 2016-06-23 Merck Sharp & Dohme Corp. Ethyldiamine orexin receptor antagonists
WO2018067704A1 (en) * 2016-10-04 2018-04-12 Enanta Pharmaceuticals, Inc. Isoxazole analogs as fxr agonists and methods of use thereof

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CU24152B1 (es) * 2010-12-20 2016-02-29 Irm Llc 1,2 oxazol-8-azabiciclo[3,2,1]octano 8 il como moduladores de fxr

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2016100161A1 (en) * 2014-12-19 2016-06-23 Merck Sharp & Dohme Corp. Ethyldiamine orexin receptor antagonists
WO2018067704A1 (en) * 2016-10-04 2018-04-12 Enanta Pharmaceuticals, Inc. Isoxazole analogs as fxr agonists and methods of use thereof

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114315844A (zh) * 2022-01-18 2022-04-12 中国科学院上海药物研究所 一类fxr调节剂及其制备方法和用途

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WO2020011146A1 (zh) 2020-01-16

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