CN107074885B - 硼酸衍生物 - Google Patents

硼酸衍生物 Download PDF

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Publication number
CN107074885B
CN107074885B CN201580053454.8A CN201580053454A CN107074885B CN 107074885 B CN107074885 B CN 107074885B CN 201580053454 A CN201580053454 A CN 201580053454A CN 107074885 B CN107074885 B CN 107074885B
Authority
CN
China
Prior art keywords
ethyl
amino
boronic acid
phenyl
alkyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
CN201580053454.8A
Other languages
English (en)
Chinese (zh)
Other versions
CN107074885A (zh
Inventor
M.克莱因
O.沙特
P.哈泽尔迈尔
M.布施
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Patent GmbH
Original Assignee
Merck Patent GmbH
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck Patent GmbH filed Critical Merck Patent GmbH
Publication of CN107074885A publication Critical patent/CN107074885A/zh
Application granted granted Critical
Publication of CN107074885B publication Critical patent/CN107074885B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • 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
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
CN201580053454.8A 2014-10-01 2015-10-01 硼酸衍生物 Expired - Fee Related CN107074885B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14003391.1 2014-10-01
EP14003391 2014-10-01
PCT/EP2015/001931 WO2016050356A1 (en) 2014-10-01 2015-10-01 Boronic acid derivatives

Publications (2)

Publication Number Publication Date
CN107074885A CN107074885A (zh) 2017-08-18
CN107074885B true CN107074885B (zh) 2020-11-27

Family

ID=51690788

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201580053454.8A Expired - Fee Related CN107074885B (zh) 2014-10-01 2015-10-01 硼酸衍生物

Country Status (14)

Country Link
US (1) US10253049B2 (cg-RX-API-DMAC10.html)
EP (1) EP3201208B1 (cg-RX-API-DMAC10.html)
JP (1) JP6896618B2 (cg-RX-API-DMAC10.html)
KR (1) KR20170062518A (cg-RX-API-DMAC10.html)
CN (1) CN107074885B (cg-RX-API-DMAC10.html)
AU (1) AU2015327412B2 (cg-RX-API-DMAC10.html)
BR (1) BR112017006349A2 (cg-RX-API-DMAC10.html)
CA (1) CA2963198A1 (cg-RX-API-DMAC10.html)
ES (1) ES2876287T3 (cg-RX-API-DMAC10.html)
IL (1) IL251299A0 (cg-RX-API-DMAC10.html)
MX (1) MX2017004043A (cg-RX-API-DMAC10.html)
RU (1) RU2017115191A (cg-RX-API-DMAC10.html)
SG (1) SG11201702620SA (cg-RX-API-DMAC10.html)
WO (1) WO2016050356A1 (cg-RX-API-DMAC10.html)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2015327345B9 (en) 2014-10-01 2020-06-18 Merck Patent Gmbh Boronic acid derivatives
EP3201207B1 (en) 2014-10-01 2021-02-24 Merck Patent GmbH Boronic acid derivatives
US10640520B2 (en) 2014-10-01 2020-05-05 Merck Patent Gmbh Boronic acid derivatives
HUE054460T2 (hu) * 2017-01-18 2021-09-28 Principia Biopharma Inc Immunproteaszóma-gátlók
IL272806B2 (en) * 2017-08-24 2023-09-01 Merck Patent Gmbh The history of boronic acid, its preparation and pharmaceutical preparations containing it
WO2019060651A1 (en) 2017-09-21 2019-03-28 Kezar Life Sciences POLY THERAPY FOR IMMUNOLOGICAL DISEASES
MX2021000214A (es) * 2018-07-26 2021-03-31 Merck Patent Gmbh Derivados de acido boronico.
CN113135943A (zh) * 2020-01-19 2021-07-20 首药控股(北京)有限公司 硼酸衍生物
CN113135944A (zh) * 2020-01-19 2021-07-20 首药控股(北京)有限公司 硼酸衍生物
US20240287102A1 (en) 2021-07-29 2024-08-29 Merck Patent Gmbh Novel crystalline forms of [(1r)-2-(1-benzofuran-3-yl)-1-{[(1s,2r,4r)-7-oxabicyclo[2.2.1]heptan-2-yl]formamido}ethyl]boronic acid, adducts thereof, and processes to obtain
JP7734276B2 (ja) * 2021-10-14 2025-09-04 ショウヤオ ホールディングス(ベイジン) カンパニー, リミテッド ボロン酸誘導体
CN117003776A (zh) * 2022-04-29 2023-11-07 科辉智药生物科技(深圳)有限公司 一种硼酸类蛋白酶体抑制剂及其用途
WO2023232830A1 (en) 2022-06-02 2023-12-07 Merck Patent Gmbh Boronic acid adducts

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001002424A2 (en) * 1999-07-07 2001-01-11 Du Pont Pharmaceuticals Company Peptide boronic acid inhibitors of hepatitis c virus protease
CN101983203A (zh) * 2007-11-13 2011-03-02 诺瓦提斯国际药物有限公司 β-内酰胺酶抑制剂
WO2013092979A1 (en) * 2011-12-22 2013-06-27 Ares Trading S.A. Alpha-amino boronic acid derivatives, selective immunoproteasome inhibitors

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL111175A0 (en) * 1993-10-07 1994-12-29 Du Pont Merck Pharma Electrophilic peptide analogs as inhibitors of trypsin-like serine proteases and pharmaceutical compositions containing them
US6083903A (en) * 1994-10-28 2000-07-04 Leukosite, Inc. Boronic ester and acid compounds, synthesis and uses
US7589066B2 (en) * 2005-03-11 2009-09-15 The University Of North Carolina At Chapel Hill Potent and specific immunoproteasome inhibitors
AR075090A1 (es) * 2008-09-29 2011-03-09 Millennium Pharm Inc Derivados de acido 1-amino-2-ciclobutiletilboronico inhibidores de proteosoma,utiles como agentes anticancerigenos, y composiciones farmaceuticas que los comprenden.
AU2011223795B2 (en) * 2010-03-01 2015-11-05 Onyx Therapeutics, Inc. Compounds for immunoproteasome inhibition
MX2015006715A (es) * 2012-12-03 2015-08-14 Hoffmann La Roche Compuestos de acido triazolboronico sustituido.
EP3201207B1 (en) 2014-10-01 2021-02-24 Merck Patent GmbH Boronic acid derivatives
US10640520B2 (en) 2014-10-01 2020-05-05 Merck Patent Gmbh Boronic acid derivatives
AU2015327345B9 (en) 2014-10-01 2020-06-18 Merck Patent Gmbh Boronic acid derivatives

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001002424A2 (en) * 1999-07-07 2001-01-11 Du Pont Pharmaceuticals Company Peptide boronic acid inhibitors of hepatitis c virus protease
CN101983203A (zh) * 2007-11-13 2011-03-02 诺瓦提斯国际药物有限公司 β-内酰胺酶抑制剂
WO2013092979A1 (en) * 2011-12-22 2013-06-27 Ares Trading S.A. Alpha-amino boronic acid derivatives, selective immunoproteasome inhibitors

Also Published As

Publication number Publication date
CN107074885A (zh) 2017-08-18
EP3201208B1 (en) 2021-03-24
MX2017004043A (es) 2017-07-04
US10253049B2 (en) 2019-04-09
JP2018502048A (ja) 2018-01-25
WO2016050356A1 (en) 2016-04-07
ES2876287T3 (es) 2021-11-12
IL251299A0 (en) 2017-05-29
BR112017006349A2 (pt) 2017-12-12
RU2017115191A3 (cg-RX-API-DMAC10.html) 2019-02-12
KR20170062518A (ko) 2017-06-07
US20180105538A1 (en) 2018-04-19
EP3201208A1 (en) 2017-08-09
JP6896618B2 (ja) 2021-06-30
AU2015327412B2 (en) 2020-01-16
CA2963198A1 (en) 2016-04-07
RU2017115191A (ru) 2018-11-06
AU2015327412A1 (en) 2017-05-18
SG11201702620SA (en) 2017-04-27

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Granted publication date: 20201127