CA2963203A1 - Boronic acid derivatives - Google Patents

Boronic acid derivatives Download PDF

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Publication number
CA2963203A1
CA2963203A1 CA2963203A CA2963203A CA2963203A1 CA 2963203 A1 CA2963203 A1 CA 2963203A1 CA 2963203 A CA2963203 A CA 2963203A CA 2963203 A CA2963203 A CA 2963203A CA 2963203 A1 CA2963203 A1 CA 2963203A1
Authority
CA
Canada
Prior art keywords
amino
ethyl
boronic acid
prop
acetyl
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.)
Pending
Application number
CA2963203A
Other languages
English (en)
French (fr)
Inventor
Markus Klein
Oliver Schadt
Philipp HASELMAYER
Mireille Krier
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 CA2963203A1 publication Critical patent/CA2963203A1/en
Pending legal-status Critical Current

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Classifications

    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Vascular Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CA2963203A 2014-10-01 2015-10-01 Boronic acid derivatives Pending CA2963203A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14003389.5 2014-10-01
EP14003389 2014-10-01
PCT/EP2015/001973 WO2016050358A1 (en) 2014-10-01 2015-10-01 Boronic acid derivatives

Publications (1)

Publication Number Publication Date
CA2963203A1 true CA2963203A1 (en) 2016-04-07

Family

ID=51751859

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2963203A Pending CA2963203A1 (en) 2014-10-01 2015-10-01 Boronic acid derivatives

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
US10640520B2 (en) 2014-10-01 2020-05-05 Merck Patent Gmbh Boronic acid derivatives
EP3201207B1 (en) 2014-10-01 2021-02-24 Merck Patent GmbH Boronic acid derivatives
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
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
CN111065619B (zh) * 2017-08-29 2022-08-12 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
US10807951B2 (en) * 2017-10-13 2020-10-20 The Regents Of The University Of California mTORC1 modulators
WO2019099582A1 (en) * 2017-11-16 2019-05-23 Principia Biopharma Inc. Immunoproteasome inhibitors
PL3710457T3 (pl) 2017-11-16 2023-02-20 Principia Biopharma Inc. Inhibitory immunoproteasomu
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
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
US5462964A (en) * 1993-10-20 1995-10-31 The Du Pont Merck Pharmaceutical Company Dipeptide 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
WO2001002424A2 (en) * 1999-07-07 2001-01-11 Du Pont Pharmaceuticals Company Peptide boronic acid inhibitors of hepatitis c virus protease
DE60305113T2 (de) * 2002-09-09 2006-12-07 Trigen Ltd. Borsäuresalze und deren Verwendung in der Bereitstellung von Medikamente für die Thrombosebehandlung
US7576206B2 (en) * 2003-08-14 2009-08-18 Cephalon, Inc. Proteasome inhibitors and methods of using the same
TWI345465B (en) * 2003-08-14 2011-07-21 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.
EP2560978B1 (en) * 2010-04-22 2019-01-30 Mars, Incorporated Inhibitors of arginase and their therapeutic applications
SG10201605152SA (en) * 2011-12-22 2016-08-30 Ares Trading Sa Alpha-amino boronic acid derivatives, selective immunoproteasome inhibitors
JP6505727B2 (ja) 2014-01-31 2019-04-24 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company ヘテロ環式p2’基を有する第xia因子阻害剤としてのマクロ環
EP3201208B1 (en) 2014-10-01 2021-03-24 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
NO2721243T3 (enExample) 2014-10-01 2018-10-20
BR112017006708A2 (pt) 2014-10-01 2017-12-26 Janssen Pharmaceuticals Inc indóis mono- ou dissubstituídos como inibidores da replicação viral de dengue
US9944598B2 (en) 2014-10-01 2018-04-17 Janssen Pharmaceuticals, Inc. Mono- or di-substituted indole derivatives as dengue viral replication inhibitors

Also Published As

Publication number Publication date
JP6662865B2 (ja) 2020-03-11
KR20170067802A (ko) 2017-06-16
SG11201702628XA (en) 2017-04-27
AU2015327345A1 (en) 2017-05-18
AU2015327345B9 (en) 2020-06-18
JP2017531646A (ja) 2017-10-26
KR102457840B1 (ko) 2022-10-21
EP3201206B1 (en) 2019-09-18
DK3201206T3 (da) 2019-12-16
ZA201703007B (en) 2022-05-25
BR112017006622A2 (pt) 2018-07-03
CL2017000792A1 (es) 2017-11-10
RU2017115192A3 (enExample) 2019-03-26
MX2017003999A (es) 2018-02-09
PH12017500293A1 (en) 2017-06-28
US20180179232A1 (en) 2018-06-28
UA122672C2 (uk) 2020-12-28
IL251302B (en) 2020-03-31
CN107001391B (zh) 2020-11-27
NZ730981A (en) 2024-01-26
RU2717558C2 (ru) 2020-03-24
US10669289B2 (en) 2020-06-02
IL251302A0 (en) 2017-05-29
CN107001391A (zh) 2017-08-01
WO2016050358A1 (en) 2016-04-07
RU2017115192A (ru) 2018-11-06
ES2761774T3 (es) 2020-05-21
EP3201206A1 (en) 2017-08-09
AU2015327345B2 (en) 2019-12-05
MX372823B (es) 2020-07-03
MY186911A (en) 2021-08-26

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