IL251302B - History of boronic acid, their preparation and medicines containing them - Google Patents

History of boronic acid, their preparation and medicines containing them

Info

Publication number
IL251302B
IL251302B IL251302A IL25130217A IL251302B IL 251302 B IL251302 B IL 251302B IL 251302 A IL251302 A IL 251302A IL 25130217 A IL25130217 A IL 25130217A IL 251302 B IL251302 B IL 251302B
Authority
IL
Israel
Prior art keywords
preparation
acid derivatives
boronic acid
medicaments containing
medicaments
Prior art date
Application number
IL251302A
Other languages
English (en)
Hebrew (he)
Other versions
IL251302A0 (en
Inventor
Markus Klein
Oliver Schadt
Philipp Haselmayer
Mirelle Krier
Original Assignee
Merck Patent Gmbh
Markus Klein
Oliver Schadt
Philipp Haselmayer
Mirelle Krier
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, Markus Klein, Oliver Schadt, Philipp Haselmayer, Mirelle Krier filed Critical Merck Patent Gmbh
Publication of IL251302A0 publication Critical patent/IL251302A0/en
Publication of IL251302B publication Critical patent/IL251302B/en

Links

Classifications

    • 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
    • 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
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
IL251302A 2014-10-01 2017-03-21 History of boronic acid, their preparation and medicines containing them IL251302B (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP14003389 2014-10-01
PCT/EP2015/001973 WO2016050358A1 (en) 2014-10-01 2015-10-01 Boronic acid derivatives

Publications (2)

Publication Number Publication Date
IL251302A0 IL251302A0 (en) 2017-05-29
IL251302B true IL251302B (en) 2020-03-31

Family

ID=51751859

Family Applications (1)

Application Number Title Priority Date Filing Date
IL251302A IL251302B (en) 2014-10-01 2017-03-21 History of boronic acid, their preparation and medicines containing them

Country Status (21)

Country Link
US (1) US10669289B2 (enExample)
EP (1) EP3201206B1 (enExample)
JP (1) JP6662865B2 (enExample)
KR (1) KR102457840B1 (enExample)
CN (1) CN107001391B (enExample)
AU (1) AU2015327345B9 (enExample)
BR (1) BR112017006622A2 (enExample)
CA (1) CA2963203A1 (enExample)
CL (1) CL2017000792A1 (enExample)
DK (1) DK3201206T3 (enExample)
ES (1) ES2761774T3 (enExample)
IL (1) IL251302B (enExample)
MX (1) MX372823B (enExample)
MY (1) MY186911A (enExample)
NZ (1) NZ730981A (enExample)
PH (1) PH12017500293A1 (enExample)
RU (1) RU2717558C2 (enExample)
SG (1) SG11201702628XA (enExample)
UA (1) UA122672C2 (enExample)
WO (1) WO2016050358A1 (enExample)
ZA (1) ZA201703007B (enExample)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9453018B2 (en) 2014-10-01 2016-09-27 Bristol-Myers Squibb Company Pyrimidinones as factor XIa inhibitors
EP3201208B1 (en) 2014-10-01 2021-03-24 Merck Patent GmbH Boronic acid derivatives
US10294246B2 (en) 2014-10-01 2019-05-21 Merck Patent Gmbh Substituted boronic acids and boronate esters as immunoproteasome inhibitors
EP3201205B1 (en) 2014-10-01 2020-05-13 Merck Patent GmbH Boronic acid derivatives
PT3571208T (pt) 2017-01-18 2021-04-13 Principia Biopharma Inc Inibidores do imunoproteassoma
US11274109B2 (en) 2017-08-24 2022-03-15 Merck Patent Gmbh Boronic acid derivatives
WO2019042301A1 (zh) * 2017-08-29 2019-03-07 浙江海正药业股份有限公司 (E)-α,β-不饱和酰胺化合物及其制备方法和用途
EP3694528A4 (en) * 2017-10-13 2021-07-28 The Regents of the University of California MTORC1 MODULATORS
EP3710458B1 (en) * 2017-11-16 2026-03-25 Principia Biopharma Inc. Immunoproteasome inhibitors
ES2928787T3 (es) * 2017-11-16 2022-11-22 Principia Biopharma Inc Inhibidores del inmunoproteasoma
IL280376B2 (en) 2018-07-26 2024-08-01 Merck Patent Gmbh Boronic acid derivatives, their preparation and pharmaceutical compositions containing them
CN113135944A (zh) * 2020-01-19 2021-07-20 首药控股(北京)有限公司 硼酸衍生物
CN113135943A (zh) * 2020-01-19 2021-07-20 首药控股(北京)有限公司 硼酸衍生物
EP4377324A1 (en) 2021-07-29 2024-06-05 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
US20240425529A1 (en) * 2021-10-14 2024-12-26 Shouyao Holdings (beijing) Co., Ltd. Boric acid derivative
WO2023232830A1 (en) 2022-06-02 2023-12-07 Merck Patent Gmbh Boronic acid adducts

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5658885A (en) * 1993-04-27 1997-08-19 The Dupont Merck Pharmaceutical Company Amidino and guanidino substituted boronic acid inhibitors of trypsin-like enzymes
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
US5462964A (en) * 1993-10-20 1995-10-31 The Du Pont Merck Pharmaceutical Company Dipeptide boronic acid inhibitors of trypsin-like enzymes
AU5920400A (en) * 1999-07-07 2001-01-22 Du Pont Pharmaceuticals Company Cell-based assay systems for examining hcv ns3 protease activity
BR0314450A (pt) * 2002-09-09 2005-07-26 Trigen Ltd Sais de ácido borÈnico com adição de uma base farmaceuticamente aceitável, formulação farmacêutica, e uso dos referidos sais para preparar uma formulação farmacêutica
UA88771C2 (ru) * 2003-08-14 2009-11-25 Сефалон, Инк. Ингибиторы протеасомы и способ их применения (варианты)
US7576206B2 (en) * 2003-08-14 2009-08-18 Cephalon, Inc. Proteasome inhibitors and methods of using the same
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.
SG10201503168VA (en) 2010-04-22 2015-06-29 Mars Inc Inhibitors of arginase and their therapeutic applications
SG11201403254QA (en) 2011-12-22 2014-07-30 Ares Trading Sa Alpha-amino boronic acid derivatives, selective immunoproteasome inhibitors
SG10201908467RA (en) 2014-01-31 2019-10-30 Bristol Myers Squibb Co Macrocycles with hetrocyclic p2' groups as factor xia inhibitors
MX2017004298A (es) 2014-10-01 2017-07-19 Janssen Pharmaceuticals Inc Indoles mono o disustituidos como inhibidores de la replicacion del virus del denge.
US10294246B2 (en) 2014-10-01 2019-05-21 Merck Patent Gmbh Substituted boronic acids and boronate esters as immunoproteasome inhibitors
EP3201208B1 (en) 2014-10-01 2021-03-24 Merck Patent GmbH Boronic acid derivatives
ME03360B (me) 2014-10-01 2019-10-20 Janssen Pharmaceuticals Inc Mono- ili di-supsтituisani derivaтi indola као inhibiтori replikacije virusa denge
EP3201205B1 (en) 2014-10-01 2020-05-13 Merck Patent GmbH Boronic acid derivatives
NO2721243T3 (enExample) 2014-10-01 2018-10-20

Also Published As

Publication number Publication date
IL251302A0 (en) 2017-05-29
BR112017006622A2 (pt) 2018-07-03
DK3201206T3 (da) 2019-12-16
MY186911A (en) 2021-08-26
JP2017531646A (ja) 2017-10-26
AU2015327345B9 (en) 2020-06-18
KR20170067802A (ko) 2017-06-16
NZ730981A (en) 2024-01-26
AU2015327345B2 (en) 2019-12-05
ES2761774T3 (es) 2020-05-21
KR102457840B1 (ko) 2022-10-21
RU2017115192A3 (enExample) 2019-03-26
AU2015327345A1 (en) 2017-05-18
WO2016050358A1 (en) 2016-04-07
EP3201206A1 (en) 2017-08-09
JP6662865B2 (ja) 2020-03-11
RU2017115192A (ru) 2018-11-06
CA2963203A1 (en) 2016-04-07
US20180179232A1 (en) 2018-06-28
ZA201703007B (en) 2022-05-25
US10669289B2 (en) 2020-06-02
RU2717558C2 (ru) 2020-03-24
MX2017003999A (es) 2018-02-09
UA122672C2 (uk) 2020-12-28
CN107001391A (zh) 2017-08-01
MX372823B (es) 2020-07-03
PH12017500293A1 (en) 2017-06-28
SG11201702628XA (en) 2017-04-27
CN107001391B (zh) 2020-11-27
EP3201206B1 (en) 2019-09-18
CL2017000792A1 (es) 2017-11-10

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