CN107001391B - 硼酸衍生物 - Google Patents

硼酸衍生物 Download PDF

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Publication number
CN107001391B
CN107001391B CN201580053501.9A CN201580053501A CN107001391B CN 107001391 B CN107001391 B CN 107001391B CN 201580053501 A CN201580053501 A CN 201580053501A CN 107001391 B CN107001391 B CN 107001391B
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CN
China
Prior art keywords
amino
ethyl
boronic acid
acetyl
prop
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CN201580053501.9A
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Chinese (zh)
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CN107001391A (zh
Inventor
M.克莱因
O.沙特
P.哈泽尔迈尔
M.克里尔
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Merck Patent GmbH
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Merck Patent GmbH
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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
    • 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

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)
CN201580053501.9A 2014-10-01 2015-10-01 硼酸衍生物 Active CN107001391B (zh)

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 (2)

Publication Number Publication Date
CN107001391A CN107001391A (zh) 2017-08-01
CN107001391B true CN107001391B (zh) 2020-11-27

Family

ID=51751859

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201580053501.9A Active CN107001391B (zh) 2014-10-01 2015-10-01 硼酸衍生物

Country Status (21)

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

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

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5462964A (en) * 1993-10-20 1995-10-31 The Du Pont Merck Pharmaceutical Company Dipeptide boronic acid inhibitors of trypsin-like enzymes
WO1996012499A1 (en) * 1994-10-25 1996-05-02 The Du Pont Merck Pharmaceutical Company Amidino and guanidino substituted inhibitors of trypsin-like enzymes
WO2001002424A2 (en) * 1999-07-07 2001-01-11 Du Pont Pharmaceuticals Company Peptide boronic acid inhibitors of hepatitis c virus protease
CN1867572A (zh) * 2003-08-14 2006-11-22 赛福伦公司 蛋白酶体抑制剂及其使用方法
WO2013092979A1 (en) * 2011-12-22 2013-06-27 Ares Trading S.A. Alpha-amino boronic acid derivatives, selective immunoproteasome inhibitors

Family Cites Families (12)

* 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
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
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
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 (https=) 2014-10-01 2018-10-20

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5462964A (en) * 1993-10-20 1995-10-31 The Du Pont Merck Pharmaceutical Company Dipeptide boronic acid inhibitors of trypsin-like enzymes
WO1996012499A1 (en) * 1994-10-25 1996-05-02 The Du Pont Merck Pharmaceutical Company Amidino and guanidino substituted inhibitors of trypsin-like enzymes
WO2001002424A2 (en) * 1999-07-07 2001-01-11 Du Pont Pharmaceuticals Company Peptide boronic acid inhibitors of hepatitis c virus protease
CN1867572A (zh) * 2003-08-14 2006-11-22 赛福伦公司 蛋白酶体抑制剂及其使用方法
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
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 (https=) 2019-03-26
AU2015327345A1 (en) 2017-05-18
WO2016050358A1 (en) 2016-04-07
EP3201206A1 (en) 2017-08-09
JP6662865B2 (ja) 2020-03-11
IL251302B (en) 2020-03-31
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
EP3201206B1 (en) 2019-09-18
CL2017000792A1 (es) 2017-11-10

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