CN112513052A - 氮杂环丁烷衍生物的硼酸酯 - Google Patents

氮杂环丁烷衍生物的硼酸酯 Download PDF

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CN112513052A
CN112513052A CN201980047480.8A CN201980047480A CN112513052A CN 112513052 A CN112513052 A CN 112513052A CN 201980047480 A CN201980047480 A CN 201980047480A CN 112513052 A CN112513052 A CN 112513052A
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compound
formula
ring
pharmaceutically acceptable
acceptable salt
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CN112513052B (zh
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熊剑
谢程
徐雄彬
陈新海
黎健
陈曙辉
张爱明
张喜全
田心
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Chia Tai Tianqing Pharmaceutical Group Co Ltd
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Chia Tai Tianqing Pharmaceutical Group Co Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/04—Esters of boric acids
    • 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
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • 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
    • A61K31/69—Boron compounds
    • 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
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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

Abstract

一种氮杂环丁烷衍生物的硼酸酯化合物，具体地涉及式(I)所示的化合物或其药学上可接受的盐、其互变异构体、其立体异构体或其几何异构体，以及其在制备用于治疗或预防多发性骨髓瘤的药物中的用途。
Figure DDA0002899929660000011

Description

PCT国内申请，说明书已公开。

Claims (21)

  1. PCT国内申请，权利要求书已公开。
CN201980047480.8A 2018-08-02 2019-08-02 氮杂环丁烷衍生物的硼酸酯 Active CN112513052B (zh)

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CN202211634916.3A CN115772188A (zh) 2018-08-02 2019-08-02 氮杂环丁烷衍生物的硼酸酯

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CN201810872672 2018-08-02
CN201810872672X 2018-08-02
CN2018109891283 2018-08-28
CN201810989128 2018-08-28
PCT/CN2019/098990 WO2020025037A1 (zh) 2018-08-02 2019-08-02 氮杂环丁烷衍生物的硼酸酯

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US (1) US11466036B2 (zh)
EP (1) EP3831834A4 (zh)
JP (1) JP7434273B2 (zh)
KR (1) KR20210040109A (zh)
CN (2) CN112513052B (zh)
AU (1) AU2019315561B2 (zh)
BR (1) BR112021001963B1 (zh)
CA (1) CA3107925A1 (zh)
IL (1) IL280489B2 (zh)
MX (1) MX2021001089A (zh)
PH (1) PH12021550248A1 (zh)
SG (1) SG11202100907TA (zh)
TW (1) TWI810344B (zh)
WO (1) WO2020025037A1 (zh)
ZA (1) ZA202100661B (zh)

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WO2023198060A1 (zh) * 2022-04-12 2023-10-19 正大天晴药业集团股份有限公司 蛋白酶体抑制剂与抗pd-1抗体的药物组合

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006086600A1 (en) * 2005-02-11 2006-08-17 Cephalon, Inc. Proteasome inhibitors and methods of using the same
CN101638414A (zh) * 2008-07-30 2010-02-03 江苏先声药物研究有限公司 肽硼酸及其酯类化合物、制备方法及其用途
WO2012177835A1 (en) * 2011-06-22 2012-12-27 Cephalon, Inc. Proteasome inhibitors and processes for their preparation, purification and use
CN105732683A (zh) * 2016-03-25 2016-07-06 南京林业大学 一类羧酸与α氨基酸组成的二肽硼酸及其酯类化合物、制备方法及其用途
WO2018157820A1 (zh) * 2017-02-28 2018-09-07 正大天晴药业集团股份有限公司 氮杂环丁烷衍生物

Family Cites Families (3)

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Publication number Priority date Publication date Assignee Title
KR101690571B1 (ko) 2008-06-17 2016-12-28 밀레니엄 파머슈티컬스 인코퍼레이티드 보로네이트 에스테르 화합물 및 이의 제약학적 조성물
HUE060305T2 (hu) 2011-08-30 2023-02-28 Tufts College FAP-aktivált proteaszóma inhibitorok a szolid tumorok kezelésére
CN108440583B (zh) 2017-01-23 2020-12-04 成都奥璟生物科技有限公司 一种新的硼酸衍生物及其药物组合物

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006086600A1 (en) * 2005-02-11 2006-08-17 Cephalon, Inc. Proteasome inhibitors and methods of using the same
CN101638414A (zh) * 2008-07-30 2010-02-03 江苏先声药物研究有限公司 肽硼酸及其酯类化合物、制备方法及其用途
WO2012177835A1 (en) * 2011-06-22 2012-12-27 Cephalon, Inc. Proteasome inhibitors and processes for their preparation, purification and use
CN105732683A (zh) * 2016-03-25 2016-07-06 南京林业大学 一类羧酸与α氨基酸组成的二肽硼酸及其酯类化合物、制备方法及其用途
WO2018157820A1 (zh) * 2017-02-28 2018-09-07 正大天晴药业集团股份有限公司 氮杂环丁烷衍生物

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
MENG LEI等: "Design,synthesis,in vitro and in vivo evaluation,and structure-activity relationship (SAR) discussion of novel dipeptidyl boronic acid proteasome inhibitors as orally available anti-cancer agents for the treatment of multiple myeloma and mechanism studies", 《BIOORGANIC & MEDICINAL CHEMISTRY》 *
YONGQIANG ZHU等: "Design, synthesis, biological evaluation, and structure-activity relationship (SAR) discussion of dipeptidyl boronate proteasome inhibitors, Part I: comprehensive understanding of the SAR of α-amino acid boronates", 《J. MED. CHEM.》 *

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US20210163507A1 (en) 2021-06-03
IL280489A (en) 2021-03-25
BR112021001963A2 (pt) 2021-04-27
SG11202100907TA (en) 2021-03-30
JP7434273B2 (ja) 2024-02-20
EP3831834A4 (en) 2021-10-27
PH12021550248A1 (en) 2021-11-03
MX2021001089A (es) 2021-05-12
CA3107925A1 (en) 2020-02-06
CN112513052B (zh) 2022-12-16
BR112021001963B1 (pt) 2024-02-15
WO2020025037A1 (zh) 2020-02-06
JP2021531302A (ja) 2021-11-18
IL280489B1 (en) 2024-02-01
ZA202100661B (en) 2023-08-30
TWI810344B (zh) 2023-08-01
EP3831834A1 (en) 2021-06-09
IL280489B2 (en) 2024-06-01
US11466036B2 (en) 2022-10-11
CN115772188A (zh) 2023-03-10
AU2019315561A1 (en) 2021-02-25
TW202007690A (zh) 2020-02-16
KR20210040109A (ko) 2021-04-12
AU2019315561B2 (en) 2024-01-25

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