CN109415386B - 硼酸衍生物及其治疗用途 - Google Patents

硼酸衍生物及其治疗用途 Download PDF

Info

Publication number
CN109415386B
CN109415386B CN201780041247.XA CN201780041247A CN109415386B CN 109415386 B CN109415386 B CN 109415386B CN 201780041247 A CN201780041247 A CN 201780041247A CN 109415386 B CN109415386 B CN 109415386B
Authority
CN
China
Prior art keywords
compound
optionally substituted
alkyl
equiv
pharmaceutically acceptable
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.)
Active
Application number
CN201780041247.XA
Other languages
English (en)
Chinese (zh)
Other versions
CN109415386A (zh
Inventor
斯科特·海克尔
拉贾·K·雷迪
托马兹·格林卡
奥尔加·罗德尼
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.)
Qpex Biopharma Inc
Original Assignee
Qpex Biopharma Inc
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 Qpex Biopharma Inc filed Critical Qpex Biopharma Inc
Publication of CN109415386A publication Critical patent/CN109415386A/zh
Application granted granted Critical
Publication of CN109415386B publication Critical patent/CN109415386B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • C07F5/05—Cyclic compounds having at least one ring containing boron but no carbon in the ring
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4196—1,2,4-Triazoles
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201780041247.XA 2016-06-30 2017-06-28 硼酸衍生物及其治疗用途 Active CN109415386B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662357165P 2016-06-30 2016-06-30
US62/357,165 2016-06-30
PCT/US2017/039787 WO2018005662A1 (en) 2016-06-30 2017-06-28 Boronic acid derivatives and therapeutic uses thereof

Publications (2)

Publication Number Publication Date
CN109415386A CN109415386A (zh) 2019-03-01
CN109415386B true CN109415386B (zh) 2022-04-19

Family

ID=60785544

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201780041247.XA Active CN109415386B (zh) 2016-06-30 2017-06-28 硼酸衍生物及其治疗用途

Country Status (23)

Country Link
US (5) US10294249B2 (https=)
EP (1) EP3478693B1 (https=)
JP (1) JP7060245B2 (https=)
KR (1) KR102403296B1 (https=)
CN (1) CN109415386B (https=)
AU (1) AU2017290060B2 (https=)
BR (1) BR112018077015B1 (https=)
CA (1) CA3026582A1 (https=)
CL (1) CL2018003681A1 (https=)
CO (1) CO2018013978A2 (https=)
DK (1) DK3478693T3 (https=)
ES (1) ES2894251T3 (https=)
IL (1) IL263450B (https=)
MX (1) MX389349B (https=)
MY (1) MY196909A (https=)
PH (1) PH12018502747A1 (https=)
PL (1) PL3478693T3 (https=)
PT (1) PT3478693T (https=)
SA (1) SA518400742B1 (https=)
SG (1) SG11201811549UA (https=)
UA (1) UA124464C2 (https=)
WO (1) WO2018005662A1 (https=)
ZA (1) ZA201808327B (https=)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS60310B1 (sr) 2010-08-10 2020-07-31 Rempex Pharmaceuticals Inc Ciklični derivati estra boronske kiseline, postupak za pripremu injihove terapeutske upotrebe
EP2943204B1 (en) 2013-01-10 2019-03-13 Venatorx Pharmaceuticals Inc Beta-lactamase inhibitors
PT3154989T (pt) 2014-06-11 2021-05-18 Venatorx Pharmaceuticals Inc Inibidores de beta-lactamase
WO2016081297A1 (en) 2014-11-18 2016-05-26 Rempex Pharmaceuticals, Inc. Cyclic boronic acid ester derivatives and therapeutic uses thereof
US20180051041A1 (en) 2015-03-17 2018-02-22 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
CN108472284A (zh) 2015-09-11 2018-08-31 维纳拓尔斯制药公司 β-内酰胺酶抑制剂
ES2894251T3 (es) * 2016-06-30 2022-02-14 Qpex Biopharma Inc Derivados de ácido borónico y usos terapéuticos de los mismos
JOP20190188A1 (ar) 2017-02-01 2019-08-01 Rempex Pharmaceuticals Inc جهاز وعملية تدفق مستمرة لإنتاج مشتق حمض بورونيك
MA47743A (fr) 2017-03-06 2020-01-15 Venatorx Pharmaceuticals Inc Formes solides et compositions de combinaison comprenant un inhibiteur de bêta-lactamase et leurs utilisations
EP3630783A4 (en) 2017-05-26 2021-03-03 Venatorx Pharmaceuticals, Inc. PENICILLIN-BINDING PROTEIN INHIBITORS
US11332485B2 (en) 2017-05-26 2022-05-17 VenatoRx Pharmaceuticals, Inc. Penicillin-binding protein inhibitors
MX2020003495A (es) * 2017-10-11 2020-09-18 Qpex Biopharma Inc Derivados de acido boronico y sintesis de los mismos.
US12016868B2 (en) * 2018-04-20 2024-06-25 Qpex Biopharma, Inc. Boronic acid derivatives and therapeutic uses thereof
EP3802551A4 (en) 2018-05-25 2022-03-02 Venatorx Pharmaceuticals, Inc. Penicillin-binding protein inhibitors
CN113382713A (zh) * 2018-11-29 2021-09-10 维纳拓尔斯制药公司 包含β-内酰胺酶抑制剂的组合式组合物及其用途
PL3986419T3 (pl) 2019-06-19 2025-09-08 Qpex Biopharma, Inc. Pochodne kwasu boronowego i ich zastosowania terapeutyczne
TW202123945A (zh) * 2019-09-13 2021-07-01 日商鹽野義製藥股份有限公司 具有抗菌作用的醫藥組成物
EP4049680A4 (en) * 2019-10-25 2024-01-10 Sumitomo Pharma Co., Ltd. NEW SUBSTITUTED CONDENSED RING CONNECTION
WO2021188700A1 (en) * 2020-03-18 2021-09-23 Qpex Biopharma, Inc. Boronic acid derivatives and therapeutic uses thereof
BR112022022367A2 (pt) 2020-05-05 2023-01-10 Qpex Biopharma Inc Derivados e síntese de ácido borônico, formas polimórficas e usos terapêuticos dos mesmos
JP2023538645A (ja) * 2020-08-20 2023-09-08 フェーノ・セラピューティクス・カンパニー・リミテッド ボロン酸化合物
EP4319760A4 (en) * 2021-04-05 2025-01-08 Qpex Biopharma, Inc. CEFTIBUTENE DOSAGE REGIMEN
JP2024514055A (ja) 2021-04-13 2024-03-28 上海拓界生物医薬科技有限公司 β－ラクタマーゼ阻害剤としてのホウ酸誘導体
CN113150022B (zh) * 2021-04-23 2022-12-06 四川大学 3-取代五元环状硼酸酯衍生物及其药物组合物和制药用途
WO2023066292A1 (zh) * 2021-10-19 2023-04-27 上海济煜医药科技有限公司 三环类硼酸衍生物及其制备方法和应用
WO2023155869A1 (zh) * 2022-02-18 2023-08-24 辉诺生物医药科技（杭州）有限公司 新的硼酸类化合物的晶型及其制备方法
CN114716465B (zh) * 2022-05-06 2024-05-24 上海中医药大学 一种双环硼酸酯类化合物的制备方法及其应用
GB202306835D0 (en) 2023-05-09 2023-06-21 Adjutec Pharma As Therapy
WO2025111328A1 (en) 2023-11-21 2025-05-30 VenatoRx Pharmaceuticals, Inc. Citrate coordination complex of an orally-delivered beta-lactamase inhibitor and uses thereof
WO2025119216A1 (zh) * 2023-12-04 2025-06-12 珠海联邦制药股份有限公司 硼酸类β-内酰胺酶抑制剂及其制备方法和应用
WO2026067428A1 (zh) * 2024-09-30 2026-04-02 科睿迪(南京)医药科技有限公司 硼酸衍生物及其制备方法和应用

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3686398A (en) * 1970-07-20 1972-08-22 Chevron Res 10,9-boroxarophenanthrene as fungicides
US4353807A (en) * 1981-03-24 1982-10-12 Mobil Oil Corporation Lubricants and fuels containing boroxarophenanthrene compounds
CN101754959A (zh) * 2007-07-23 2010-06-23 伊利诺斯大学理事会 控制硼酸反应性的体系
WO2010130708A1 (en) * 2009-05-12 2010-11-18 Novartis International Pharmaceutical Ltd. Beta-lactamase inhibitors
CN101939053A (zh) * 2007-09-06 2011-01-05 默沙东公司 可溶性的鸟苷酸环化酶活化剂
CN103180328A (zh) * 2010-08-10 2013-06-26 莱姆派克斯制药公司 环硼酸酯衍生物及其治疗用途
EP2406233B1 (en) * 2009-03-09 2013-11-13 Bristol-Myers Squibb Company Aza pyridone analogs useful as melanin concentrating hormone receptor-1 antagonists
WO2014089365A1 (en) * 2012-12-07 2014-06-12 Venatorx Pharmaceuticals, Inc Beta-lactamase inhibitors

Family Cites Families (118)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4194047A (en) 1975-11-21 1980-03-18 Merck & Co., Inc. Substituted N-methylene derivatives of thienamycin
US4260543A (en) 1978-07-03 1981-04-07 Merck & Co., Inc. Crystalline N-formimidoyl thienamycin
US4409214A (en) 1979-11-19 1983-10-11 Fujisawa Pharmaceutical, Co., Ltd. 7-Acylamino-3-vinylcephalosporanic acid derivatives and processes for the preparation thereof
FR2573070B1 (fr) 1984-11-13 1987-01-30 Rhone Poulenc Sante Procede de preparation de composes carbonyles
US4783443A (en) 1986-03-03 1988-11-08 The University Of Chicago Amino acyl cephalosporin derivatives
CA1283404C (en) 1986-07-01 1991-04-23 Shigeru Sanai Cephalosporin compounds, processes for their preparation and antibacterial agents
NZ220764A (en) 1986-07-02 1989-09-27 Shionogi & Co Crystalline form of 7beta((z)-2-(2-aminothiazol-4-yl)-4- carboxybut-2-enoylamino)-3-cephem-4-carboxylic acid and pharmaceutical compositions
ZA893284B (en) 1988-05-04 1990-03-28 Igen Inc Peptide analogs and their use as haptens to elicit catalytic antibodies
US5442100A (en) 1992-08-14 1995-08-15 The Procter & Gamble Company β-aminoalkyl and β-N-peptidylaminoalkyl boronic acids
US5888998A (en) 1997-04-24 1999-03-30 Synphar Laboratories, Inc. 2-oxo-1-azetidine sulfonic acid derivatives as potent β-lactamase inhibitors
AU8140898A (en) 1997-06-13 1998-12-30 Northwestern University Inhibitors of beta-lactamases and uses therefor
US6184363B1 (en) 1997-06-13 2001-02-06 Northwestern University Inhibitors of β-lactamases and uses therefor
WO2000035904A1 (en) 1998-12-16 2000-06-22 Northwestern University INHIBITORS OF β-LACTAMASES AND USES THEREFOR
AU2190400A (en) 1998-12-16 2000-07-03 Northwestern University Inhibitors of beta-lactamases and uses therefor
TR200200795T2 (tr) 1999-09-25 2002-07-22 Smithkline Beecham P. L. C. 5-HT1B antagonistleri olarak piperazin türevleri
JP2003513890A (ja) 1999-10-28 2003-04-15 メルク エンド カムパニー インコーポレーテッド 新規なコハク酸系メタロ−β−ラクタマーゼ阻害薬およびそれの細菌感染治療での使用
WO2002022137A1 (en) 2000-09-12 2002-03-21 Shoichet Brian K β-LACTAM ANALOGS AND USES THEREFOR
ATE298750T1 (de) 2000-09-14 2005-07-15 Pantherix Ltd 3-(heteroarylacetamido)-2-oxo-azetidin-1- sulfonsäure derivate als antibakterielle mittel
AU2002243508A1 (en) 2001-01-10 2002-07-24 Bristol-Myers Squibb Company Patent Department Alpha-aminoboronic acids prepared by novel synthetic methods
DE10118698A1 (de) 2001-04-17 2002-11-07 Jerini Ag Verfahren zur Immobilisierung und damit hergestellte Anordnungen von Verbindungen auf einer planaren Oberfläche
AU2002360732A1 (en) * 2001-12-26 2003-07-24 Guilford Pharmaceuticals Change inhibitors of dipeptidyl peptidase iv
FR2835186B1 (fr) 2002-01-28 2006-10-20 Aventis Pharma Sa Nouveaux composes heterocycliques, actifs comme inhibiteurs de beta-lactamases
JP2003229277A (ja) 2002-02-04 2003-08-15 Matsushita Electric Ind Co Ltd 発光素子材料およびそれを用いた発光素子並びに装置
AUPS065102A0 (en) 2002-02-20 2002-03-14 Unisearch Limited Fluorous acetalation
AU2003261974A1 (en) 2002-09-11 2004-04-30 Kureha Chemical Industry Company, Limited Amine compounds and use thereof
AU2003268752A1 (en) 2002-10-30 2004-05-25 Sumitomo Chemical Company, Limited High-molecular compounds and polymerer light emitting devices made by using the same
US7439253B2 (en) 2002-12-06 2008-10-21 Novexel Heterocyclic compounds, their preparation and their use as medicaments, in particular as antibacterials and beta-lactamase inhibitors
US7271186B1 (en) 2002-12-09 2007-09-18 Northwestern University Nanomolar β-lactamase inhibitors
MXPA05006798A (es) 2002-12-20 2006-03-09 Migenix Corp Ligandos de adenina nucleotido translocasa (ant) y composiciones y metodos relacionados a estos.
TW200418791A (en) 2003-01-23 2004-10-01 Bristol Myers Squibb Co Pharmaceutical compositions for inhibiting proteasome
JP4233365B2 (ja) 2003-03-25 2009-03-04 三井化学株式会社 アザジオール錯体化合物、及び該化合物を用いる光記録媒体
US7842941B2 (en) 2003-10-06 2010-11-30 Sumitomo Chemical Company, Limited Aromatic compound
BRPI0415185A (pt) 2003-10-10 2006-11-28 Pfizer Prod Inc 2h-[1,2,4]triazol[4,3-a]pirazinas substituìdas como inibidores da gsk-3
SG134333A1 (en) * 2003-11-12 2007-08-29 Phenomix Corp Heterocyclic boronic acid compounds
TW200600494A (en) 2004-03-08 2006-01-01 Chugai Pharmaceutical Co Ltd Bisphenyl compounds useful as vitamin d3 receptor agonists
US20060019116A1 (en) 2004-07-22 2006-01-26 Eastman Kodak Company White electroluminescent device with anthracene derivative host
TW200618820A (en) 2004-11-05 2006-06-16 Alza Corp Liposome formulations of boronic acid compounds
US20060178357A1 (en) 2005-02-10 2006-08-10 Buynak John D Chphalosporin-derived mercaptans as inhibitors of serine and metallo-beta-lactamases
EP2343304B1 (en) 2005-02-16 2015-06-10 Anacor Pharmaceuticals, Inc. Biocidal boronophthalide compounds
US7612203B2 (en) 2005-02-22 2009-11-03 Teva Pharmaceutical Industries Ltd. Rosuvastatin and salts thereof free of rosuvastatin alkylether and a process for the preparation thereof
WO2006101779A2 (en) 2005-03-15 2006-09-28 The University Of Chicago Non-aqueous electrolytes for lithium ion batteries
US7825139B2 (en) * 2005-05-25 2010-11-02 Forest Laboratories Holdings Limited (BM) Compounds and methods for selective inhibition of dipeptidyl peptidase-IV
TW200734311A (en) 2005-11-21 2007-09-16 Astrazeneca Ab New compounds
CA2783572C (en) 2005-12-07 2016-08-09 Basilea Pharmaceutica Ag Useful combinations of monobactam antibiotics with beta-lactamase inhibitors
PT1988779E (pt) 2006-02-16 2015-09-04 Anacor Pharmaceuticals Inc Moléculas pequenas contendo boro como agentes antiinflamatórios
AU2007300531A1 (en) 2006-09-27 2008-04-03 Merck Sharp & Dohme Corp. Novel inhibitors of beta-lactamase
RU2488394C2 (ru) 2007-03-23 2013-07-27 Базилеа Фармацойтика Аг Комбинированные лекарственные средства для лечения бактериальных инфекций
GB0719366D0 (en) 2007-10-03 2007-11-14 Smithkline Beecham Corp Compounds
JP2011504468A (ja) 2007-11-13 2011-02-10 プロテズ・ファーマシューティカルズ・インコーポレイテッド β−ラクタマーゼ阻害剤
US20100120715A1 (en) 2007-11-13 2010-05-13 Burns Christopher J Beta-lactamase inhibitors
ES2533826T3 (es) 2008-01-18 2015-04-15 Merck Sharp & Dohme Corp. Inhibidores de beta-lactamasa
US8129398B2 (en) 2008-03-19 2012-03-06 Bristol-Myers Squibb Company HIV integrase inhibitors
EP2285384A4 (en) 2008-05-12 2012-04-25 Anacor Pharmaceuticals Inc BORN SMALL MOLECULES
CN102098918A (zh) 2008-05-13 2011-06-15 帕纳德制药公司 用于治疗癌症和神经退行性疾病的生物活性化合物
US20120046242A1 (en) 2008-12-24 2012-02-23 Massachusetts Institute Of Technology Molecular activators of the wnt/beta-catenin pathway
WO2010097675A1 (en) 2009-02-27 2010-09-02 Dhanuka Laboratories Ltd. An improved preparation process for cefpodoxime proxetil
WO2010144338A1 (en) 2009-06-08 2010-12-16 Abraxis Bioscience, Llc Triazine derivatives and their therapeutical applications
MX2012001156A (es) 2009-07-28 2012-05-08 Anacor Pharmaceuticals Inc Moleculas que contienen boro trisustituidas.
EP2539348A4 (en) 2010-02-26 2013-07-24 Gary Igor Dmitrienko CEPHALOSPORIN DERIVATIVES AS BETA LACTAMASE HEMMER AND COMPOSITIONS THEREFOR AND METHOD FOR THEIR USE
MX2012011298A (es) 2010-03-31 2012-11-06 Millennium Pharm Inc Derivados del acido 1-amino-2-ciclopropiletilboronico.
US20110288063A1 (en) 2010-05-19 2011-11-24 Naeja Pharmaceutical Inc. Novel fused bridged bicyclic heteroaryl substituted 6-alkylidene penems as potent beta-lactamase inhibitors
US8822516B2 (en) 2010-06-10 2014-09-02 Technion Research & Development Foundation Limited Process for the preparation of iodides
HRP20160305T1 (hr) 2010-10-26 2016-07-01 Mars, Incorporated Borati kao inhibitori arginaze
WO2012067664A1 (en) 2010-11-18 2012-05-24 Glaxo Group Limited Compounds
EP2487159A1 (en) 2011-02-11 2012-08-15 MSD Oss B.V. RorgammaT inhibitors
EP2508506A1 (en) 2011-04-08 2012-10-10 LEK Pharmaceuticals d.d. Preparation of sitagliptin intermediates
CN102320960A (zh) 2011-08-02 2012-01-18 安徽东健化工科技有限公司 一种6-氟水杨酸的制备方法
US9012491B2 (en) 2011-08-31 2015-04-21 Rempex Pharmaceuticals, Inc. Heterocyclic boronic acid ester derivatives and therapeutic uses thereof
WO2013053372A1 (en) 2011-10-13 2013-04-18 Therabor Pharmaceuticals Boronic acid inhibitors of beta-lactamases
WO2013056163A1 (en) 2011-10-14 2013-04-18 The Regents Of The University Of California Beta-lactamase inhibitors
SG11201403254QA (en) 2011-12-22 2014-07-30 Ares Trading Sa Alpha-amino boronic acid derivatives, selective immunoproteasome inhibitors
EP2802593A1 (en) 2012-01-09 2014-11-19 The University of Tromsoe Therapeutic boron-containing compounds
EP2615080A1 (en) 2012-01-12 2013-07-17 LEK Pharmaceuticals d.d. Preparation of Optically Pure ß-Amino Acid Type Active Pharmaceutical Ingredients and Intermediates thereof
EP2814483A2 (en) 2012-02-15 2014-12-24 Rempex Pharmaceuticals, Inc. Methods of treating bacterial infections
US9156858B2 (en) 2012-05-23 2015-10-13 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
US10561675B2 (en) 2012-06-06 2020-02-18 Rempex Pharmaceuticals, Inc. Cyclic boronic acid ester derivatives and therapeutic uses thereof
KR20150103269A (ko) 2013-01-04 2015-09-09 렘펙스 파머수티클스 인코퍼레이티드 보론산 유도체 및 그의 치료적 용도
US9101638B2 (en) 2013-01-04 2015-08-11 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
KR20150103270A (ko) 2013-01-04 2015-09-09 렘펙스 파머수티클스 인코퍼레이티드 보론산 유도체 및 그의 치료적 용도
US9241947B2 (en) 2013-01-04 2016-01-26 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
EP2943204B1 (en) 2013-01-10 2019-03-13 Venatorx Pharmaceuticals Inc Beta-lactamase inhibitors
WO2014151958A1 (en) 2013-03-14 2014-09-25 VenatoRx Pharmaceuticals, Inc. Beta-lactamase inhibitors
US9127024B2 (en) 2013-03-15 2015-09-08 Intrexon Corporation Boron-containing diacylhydrazines
SI3140310T1 (sl) 2014-05-05 2020-01-31 Rempex Pharmaceuticals, Inc. Sinteza boronatnih soli in njihova uporaba
EP3139930B1 (en) 2014-05-05 2024-08-14 Melinta Therapeutics, Inc. Salts and polymorphs of cyclic boronic acid ester derivatives and therapeutic uses thereof
WO2015179308A1 (en) 2014-05-19 2015-11-26 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
PT3154989T (pt) 2014-06-11 2021-05-18 Venatorx Pharmaceuticals Inc Inibidores de beta-lactamase
US9511142B2 (en) 2014-06-11 2016-12-06 VenatoRx Pharmaceuticals, Inc. Beta-lactamase inhibitors
EA201692301A1 (ru) 2014-07-01 2017-06-30 Ремпекс Фармасьютикалз, Инк. Производные бороновой кислоты и их терапевтическое применение
WO2016065282A1 (en) 2014-10-24 2016-04-28 The Regents Of The University Of Michigan Nasal formulation, nasal kit, and method for enhancing nasal nitric oxide (no) levels
WO2016081297A1 (en) 2014-11-18 2016-05-26 Rempex Pharmaceuticals, Inc. Cyclic boronic acid ester derivatives and therapeutic uses thereof
WO2016116892A1 (en) 2015-01-24 2016-07-28 Wockhardt Limited Antibacterial compositions
US20180051041A1 (en) 2015-03-17 2018-02-22 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
ES2942329T3 (es) 2015-04-24 2023-05-31 Melinta Therapeutics Inc Régimen de dosificación de vaborbactam y meropenem para el tratamiento de infecciones bacterianas en sujetos con función renal reducida
WO2017100537A1 (en) 2015-12-10 2017-06-15 VenatoRx Pharmaceuticals, Inc. Beta-lactamase inhibitors
ES2894251T3 (es) 2016-06-30 2022-02-14 Qpex Biopharma Inc Derivados de ácido borónico y usos terapéuticos de los mismos
AU2017295866A1 (en) 2016-07-14 2019-01-17 Achaogen, Inc. Combination of ceftibuten and clavulanic acid for use in the treatment of bacterial infections
CN106397455B (zh) 2016-08-30 2018-08-31 山东罗欣药业集团恒欣药业有限公司 一种抗感染药物头孢布烯晶体化合物及其组合物
CN106397454B (zh) 2016-08-30 2018-08-24 山东罗欣药业集团股份有限公司 一种抗感染药物头孢布烯晶型化合物及其组合物
CN114591223B (zh) 2016-09-16 2025-01-24 恩塔西斯治疗有限公司 β-内酰胺酶抑制剂化合物
CN106432271A (zh) 2016-09-21 2017-02-22 临沂草之美医药科技有限公司 一种治疗外科手术感染的药物头孢布烯晶体化合物
CN106420617A (zh) 2016-09-21 2017-02-22 临沂草之美医药科技有限公司 一种治疗外科手术感染的药物头孢布烯粉针剂
CN106432272A (zh) 2016-09-21 2017-02-22 临沂草之美医药科技有限公司 一种制备治疗外科手术感染的药物头孢布烯晶体化合物的方法
CN106397457A (zh) 2016-09-21 2017-02-15 临沂草之美医药科技有限公司 一种治疗外科手术感染的药物头孢布烯晶体化合物
CN106432270A (zh) 2016-09-21 2017-02-22 临沂草之美医药科技有限公司 一种制备治疗外科手术感染的药物头孢布烯晶体化合物的方法
CN106420760A (zh) 2016-09-21 2017-02-22 临沂草之美医药科技有限公司 一种治疗外科手术感染的药物头孢布烯组合物
US10085999B1 (en) 2017-05-10 2018-10-02 Arixa Pharmaceuticals, Inc. Beta-lactamase inhibitors and uses thereof
MX2020003495A (es) 2017-10-11 2020-09-18 Qpex Biopharma Inc Derivados de acido boronico y sintesis de los mismos.
WO2019093450A1 (ja) 2017-11-10 2019-05-16 塩野義製薬株式会社 ジアザビシクロオクタン誘導体
US12016868B2 (en) 2018-04-20 2024-06-25 Qpex Biopharma, Inc. Boronic acid derivatives and therapeutic uses thereof
CN109293678A (zh) 2018-11-20 2019-02-01 湖北凌晟药业有限公司 一种头孢布烯的制备方法
CN113382713A (zh) 2018-11-29 2021-09-10 维纳拓尔斯制药公司 包含β-内酰胺酶抑制剂的组合式组合物及其用途
PL3986419T3 (pl) 2019-06-19 2025-09-08 Qpex Biopharma, Inc. Pochodne kwasu boronowego i ich zastosowania terapeutyczne
MX2022002537A (es) 2019-08-29 2022-03-22 Arixa Pharmaceuticals Inc Combinaciones administradas via oral de antibioticos beta-lactama y derivados de avibactam para tratar infecciones bacterianas.
WO2021188700A1 (en) 2020-03-18 2021-09-23 Qpex Biopharma, Inc. Boronic acid derivatives and therapeutic uses thereof
BR112022022367A2 (pt) 2020-05-05 2023-01-10 Qpex Biopharma Inc Derivados e síntese de ácido borônico, formas polimórficas e usos terapêuticos dos mesmos
EP4319760A4 (en) 2021-04-05 2025-01-08 Qpex Biopharma, Inc. CEFTIBUTENE DOSAGE REGIMEN
EP4362950A4 (en) 2021-07-01 2025-08-13 Qpex Biopharma Inc CRYSTALLINE FORMS OF CEFTIBUTEN

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3686398A (en) * 1970-07-20 1972-08-22 Chevron Res 10,9-boroxarophenanthrene as fungicides
US4353807A (en) * 1981-03-24 1982-10-12 Mobil Oil Corporation Lubricants and fuels containing boroxarophenanthrene compounds
CN101754959A (zh) * 2007-07-23 2010-06-23 伊利诺斯大学理事会 控制硼酸反应性的体系
CN101939053A (zh) * 2007-09-06 2011-01-05 默沙东公司 可溶性的鸟苷酸环化酶活化剂
EP2406233B1 (en) * 2009-03-09 2013-11-13 Bristol-Myers Squibb Company Aza pyridone analogs useful as melanin concentrating hormone receptor-1 antagonists
WO2010130708A1 (en) * 2009-05-12 2010-11-18 Novartis International Pharmaceutical Ltd. Beta-lactamase inhibitors
CN103180328A (zh) * 2010-08-10 2013-06-26 莱姆派克斯制药公司 环硼酸酯衍生物及其治疗用途
WO2014089365A1 (en) * 2012-12-07 2014-06-12 Venatorx Pharmaceuticals, Inc Beta-lactamase inhibitors
CN105026407A (zh) * 2012-12-07 2015-11-04 维纳拓尔斯制药公司 β-内酰胺酶抑制剂

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Synthesis and biological evaluation of enantiomerically pure cyclopropyl analogues of combretastatin A4;Nancy Ty et al.;《Bioorganic & Medicinal Chemistry》;20121221;第21卷;第1357-1366页 *

Also Published As

Publication number Publication date
MY196909A (en) 2023-05-09
CL2018003681A1 (es) 2019-04-26
CO2018013978A2 (es) 2019-02-08
IL263450B (en) 2022-01-01
US10294249B2 (en) 2019-05-21
CA3026582A1 (en) 2018-01-04
US10570159B2 (en) 2020-02-25
MX389349B (es) 2025-03-20
WO2018005662A1 (en) 2018-01-04
PH12018502747A1 (en) 2019-12-11
US20180002351A1 (en) 2018-01-04
PL3478693T3 (pl) 2021-12-13
RU2018143900A3 (https=) 2020-09-29
SA518400742B1 (ar) 2023-02-28
JP7060245B2 (ja) 2022-04-26
UA124464C2 (uk) 2021-09-22
US20200181177A1 (en) 2020-06-11
KR20190025953A (ko) 2019-03-12
RU2018143900A (ru) 2020-07-30
AU2017290060A1 (en) 2018-12-20
SG11201811549UA (en) 2019-01-30
EP3478693A1 (en) 2019-05-08
US12509475B2 (en) 2025-12-30
DK3478693T3 (da) 2021-09-20
NZ749864A (en) 2025-06-27
JP2019527196A (ja) 2019-09-26
EP3478693A4 (en) 2020-02-19
ZA201808327B (en) 2022-04-28
ES2894251T3 (es) 2022-02-14
KR102403296B1 (ko) 2022-05-27
US20190233443A1 (en) 2019-08-01
PT3478693T (pt) 2021-10-25
EP3478693B1 (en) 2021-07-21
AU2017290060B2 (en) 2021-07-22
CN109415386A (zh) 2019-03-01
US20250034175A1 (en) 2025-01-30
BR112018077015B1 (pt) 2022-05-03
MX2018015892A (es) 2019-06-20
US11999759B2 (en) 2024-06-04
BR112018077015A2 (pt) 2019-04-02
IL263450A (en) 2019-01-31
US11180512B2 (en) 2021-11-23
US20220056055A1 (en) 2022-02-24

Similar Documents

Publication Publication Date Title
CN109415386B (zh) 硼酸衍生物及其治疗用途
JP6700203B2 (ja) ボロン酸誘導体およびその治療的使用
JP6672176B2 (ja) ボロン酸誘導体およびその治療的使用
JP6324409B2 (ja) ボロン酸誘導体及びその治療的使用
JP2016509594A (ja) ボロン酸誘導体及びその治療的使用
US12016868B2 (en) Boronic acid derivatives and therapeutic uses thereof
CN112469725A (zh) 青霉素结合蛋白抑制剂
RU2773346C2 (ru) Производные бороновой кислоты и их терапевтические применения
HK40000809B (en) Boronic acid derivatives and therapeutic uses thereof
HK40047984A (en) Penicillin-binding protein inhibitors
BR112020021356B1 (pt) Derivados de ácido borônico e usos terapêuticos dos mesmos

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant