AU2012356890B2 - Alpha-amino boronic acid derivatives, selective immunoproteasome inhibitors - Google Patents

Alpha-amino boronic acid derivatives, selective immunoproteasome inhibitors Download PDF

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Publication number
AU2012356890B2
AU2012356890B2 AU2012356890A AU2012356890A AU2012356890B2 AU 2012356890 B2 AU2012356890 B2 AU 2012356890B2 AU 2012356890 A AU2012356890 A AU 2012356890A AU 2012356890 A AU2012356890 A AU 2012356890A AU 2012356890 B2 AU2012356890 B2 AU 2012356890B2
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ethyl
boronic acid
hplc
formula
compound
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AU2012356890A1 (en
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Stefano Crosignani
Federica MORANDI
Jeyaprakashnarayanan SEENISAMY
Dominique Swinnen
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Ares Trading SA
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Ares Trading SA
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • C07F5/025Boronic and borinic acid compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/69Boron compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
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    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
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    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
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    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Neurology (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
AU2012356890A 2011-12-22 2012-12-21 Alpha-amino boronic acid derivatives, selective immunoproteasome inhibitors Ceased AU2012356890B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201161579076P 2011-12-22 2011-12-22
US61/579,076 2011-12-22
EP11195107 2011-12-22
EP11195107.5 2011-12-22
PCT/EP2012/076595 WO2013092979A1 (en) 2011-12-22 2012-12-21 Alpha-amino boronic acid derivatives, selective immunoproteasome inhibitors

Publications (2)

Publication Number Publication Date
AU2012356890A1 AU2012356890A1 (en) 2014-08-07
AU2012356890B2 true AU2012356890B2 (en) 2017-06-08

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AU2012356890A Ceased AU2012356890B2 (en) 2011-12-22 2012-12-21 Alpha-amino boronic acid derivatives, selective immunoproteasome inhibitors

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US (1) US9688702B2 (enExample)
EP (1) EP2793900B1 (enExample)
JP (1) JP6129203B2 (enExample)
KR (1) KR20140114391A (enExample)
CN (1) CN104321060B (enExample)
AU (1) AU2012356890B2 (enExample)
BR (1) BR112014015363A2 (enExample)
CA (1) CA2860142C (enExample)
EA (1) EA201400735A1 (enExample)
ES (1) ES2699267T3 (enExample)
HK (1) HK1206261A1 (enExample)
IL (1) IL233200A (enExample)
MX (1) MX352652B (enExample)
SG (2) SG11201403254QA (enExample)
WO (1) WO2013092979A1 (enExample)

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US10561675B2 (en) 2012-06-06 2020-02-18 Rempex Pharmaceuticals, Inc. Cyclic boronic acid ester derivatives and therapeutic uses thereof
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AU2014204045B2 (en) * 2013-01-04 2018-10-18 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
US9101638B2 (en) 2013-01-04 2015-08-11 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
US9241947B2 (en) 2013-01-04 2016-01-26 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
JP6346904B2 (ja) 2013-01-10 2018-06-20 ベナトルクス ファーマシューティカルズ,インク. ベータ−ラクタマーゼ阻害剤
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JP6672176B2 (ja) 2014-05-19 2020-03-25 レンペックス・ファーマシューティカルズ・インコーポレイテッド ボロン酸誘導体およびその治療的使用
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KR102764027B1 (ko) 2015-10-15 2025-02-07 코넬 유니버시티 프로테아좀 억제제 및 이의 용도
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JP7060245B2 (ja) 2016-06-30 2022-04-26 キューペックス バイオファーマ, インコーポレイテッド ボロン酸誘導体およびその治療的使用
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HK1206261A1 (en) 2016-01-08
WO2013092979A1 (en) 2013-06-27
BR112014015363A8 (pt) 2017-06-13
CN104321060A (zh) 2015-01-28
IL233200A0 (en) 2014-07-31
CN104321060B (zh) 2018-08-07
MX352652B (es) 2017-12-04
US20140364396A1 (en) 2014-12-11
MX2014007362A (es) 2014-08-01
US9688702B2 (en) 2017-06-27
CA2860142A1 (en) 2013-06-27
JP2015502387A (ja) 2015-01-22
IL233200A (en) 2017-08-31
SG10201605152SA (en) 2016-08-30
ES2699267T3 (es) 2019-02-08
EA201400735A1 (ru) 2015-04-30
AU2012356890A1 (en) 2014-08-07
EP2793900A1 (en) 2014-10-29
EP2793900B1 (en) 2018-08-22
CA2860142C (en) 2020-10-27
SG11201403254QA (en) 2014-07-30
JP6129203B2 (ja) 2017-05-17
BR112014015363A2 (pt) 2017-06-13
KR20140114391A (ko) 2014-09-26

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