JP6672176B2 - ボロン酸誘導体およびその治療的使用 - Google Patents

ボロン酸誘導体およびその治療的使用 Download PDF

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JP6672176B2
JP6672176B2 JP2016568679A JP2016568679A JP6672176B2 JP 6672176 B2 JP6672176 B2 JP 6672176B2 JP 2016568679 A JP2016568679 A JP 2016568679A JP 2016568679 A JP2016568679 A JP 2016568679A JP 6672176 B2 JP6672176 B2 JP 6672176B2
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alkyl
amino
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hydroxy
halogen
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JP2017517508A5 (enExample
JP2017517508A (ja
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レディ、ラジャ
グリンカ、トマシュ
ヘッカー、スコット
トトロフ、マキシム
ロドニー、オルガ
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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
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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
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic 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
    • A61K31/407Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/41961,2,4-Triazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/429Thiazoles condensed with heterocyclic ring systems
    • A61K31/43Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/545Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/545Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine
    • A61K31/546Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine containing further heterocyclic rings, e.g. cephalothin
    • 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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • 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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2016568679A 2014-05-19 2015-05-18 ボロン酸誘導体およびその治療的使用 Active JP6672176B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462000400P 2014-05-19 2014-05-19
US62/000,400 2014-05-19
PCT/US2015/031400 WO2015179308A1 (en) 2014-05-19 2015-05-18 Boronic acid derivatives and therapeutic uses thereof

Publications (3)

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JP2017517508A JP2017517508A (ja) 2017-06-29
JP2017517508A5 JP2017517508A5 (enExample) 2018-07-05
JP6672176B2 true JP6672176B2 (ja) 2020-03-25

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US (1) US9963467B2 (enExample)
EP (1) EP3145936B1 (enExample)
JP (1) JP6672176B2 (enExample)
KR (1) KR20170007448A (enExample)
CN (1) CN106459096B (enExample)
AU (1) AU2015264418A1 (enExample)
BR (1) BR112016026291A2 (enExample)
CA (1) CA2947041A1 (enExample)
EA (1) EA201691988A1 (enExample)
MX (1) MX2016015093A (enExample)
WO (1) WO2015179308A1 (enExample)

Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL3412676T3 (pl) 2010-08-10 2021-04-06 Melinta Therapeutics, Inc. Cykliczne pochodne estrowe kwasu boronowego, sposób otrzymywania oraz ich zastosowania terapeutyczne
PL2928898T3 (pl) 2012-12-07 2021-10-25 VenatoRx Pharmaceuticals, Inc. Inhibitory beta-laktamaz
EP2941246A4 (en) 2013-01-04 2016-12-21 Rempex Pharmaceuticals Inc BORONIC ACID DERIVATIVES AND THEIR THERAPEUTIC USES
ES2730013T3 (es) * 2013-01-10 2019-11-07 Venatorx Pharmaceuticals Inc Inhibidores de betalactamasa
US9944658B2 (en) 2013-03-14 2018-04-17 VenatoRx Pharmaceuticals, Inc. Beta-lactamase inhibitors
US9687497B1 (en) 2014-05-05 2017-06-27 Rempex Pharmaceuticals, Inc. Salts and polymorphs of cyclic boronic acid ester derivatives and therapeutic uses thereof
EP3140310B1 (en) 2014-05-05 2019-08-07 Rempex Pharmaceuticals, Inc. Synthesis of boronate salts and uses thereof
US9511142B2 (en) 2014-06-11 2016-12-06 VenatoRx Pharmaceuticals, Inc. Beta-lactamase inhibitors
US20150361108A1 (en) * 2014-06-11 2015-12-17 VenatoRx Pharmaceuticals, Inc. Orally bioavailable beta-lactamase inhibitors
ES2874579T3 (es) 2014-06-11 2021-11-05 Venatorx Pharmaceuticals Inc Inhibidores de betalactamasa
US10206937B2 (en) 2014-07-01 2019-02-19 Qpex Biopharma, Inc. Boronic acid derivatives and therapeutic uses thereof
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
JP2018525350A (ja) 2015-07-02 2018-09-06 ホライズン オルファン エルエルシー Ado耐性システアミン類似体およびその使用
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
WO2017100537A1 (en) * 2015-12-10 2017-06-15 VenatoRx Pharmaceuticals, Inc. Beta-lactamase inhibitors
MY196909A (en) 2016-06-30 2023-05-09 Qpex Biopharma Inc Boronic acid derivatives and therapeutic uses thereof
US10889600B2 (en) 2016-08-04 2021-01-12 VenatoRx Pharmaceuticals, Inc. Boron-containing compounds
JOP20190188A1 (ar) 2017-02-01 2019-08-01 Rempex Pharmaceuticals Inc جهاز وعملية تدفق مستمرة لإنتاج مشتق حمض بورونيك
WO2018199291A1 (ja) * 2017-04-28 2018-11-01 大日本住友製薬株式会社 ヘテロ環誘導体
US11267826B2 (en) 2017-05-26 2022-03-08 VenatoRx Pharmaceuticals, Inc. Penicillin-binding protein inhibitors
EP3630782A4 (en) 2017-05-26 2021-03-03 Venatorx Pharmaceuticals, Inc. Penicillin-binding protein inhibitors
TW201906616A (zh) * 2017-07-06 2019-02-16 日商大日本住友製藥股份有限公司 醯胺衍生物
WO2019009369A1 (ja) * 2017-07-06 2019-01-10 大日本住友製薬株式会社 イミン誘導体
EP3694864B1 (en) 2017-10-11 2025-03-05 Qpex Biopharma, Inc. Boronic acid derivatives and synthesis thereof
AU2019256351B2 (en) 2018-04-20 2024-02-29 Qpex Biopharma, Inc. Boronic acid derivatives and therapeutic uses thereof
CN118638140A (zh) 2018-04-27 2024-09-13 住友制药株式会社 氧代取代化合物
EP3802551A4 (en) 2018-05-25 2022-03-02 Venatorx Pharmaceuticals, Inc. Penicillin-binding protein inhibitors
EP3886798B1 (en) 2018-11-29 2026-01-28 Venatorx Pharmaceuticals, Inc. Combination compositions comprising a beta-lactamase inhibitor and uses thereof
WO2020138499A1 (ja) * 2018-12-28 2020-07-02 大日本住友製薬株式会社 アルキル置換化合物
ES3036963T3 (en) 2019-06-19 2025-09-25 Qpex Biopharma Inc Boronic acid derivatives and therapeutic uses thereof
JP7550421B2 (ja) * 2019-10-25 2024-09-13 住友ファーマ株式会社 オキソ置換化合物からなる医薬
WO2021079984A1 (ja) * 2019-10-25 2021-04-29 大日本住友製薬株式会社 新規置換縮環型化合物
MX2022011565A (es) * 2020-03-18 2023-02-27 Qpex Biopharma Inc Derivados de acido boronico y usos terapeuticos de los mismos.
US12552815B2 (en) 2020-05-05 2026-02-17 Qpex Biopharma, Inc. Boronic acid derivatives and synthesis, polymorphic forms, and therapeutic uses thereof
CN115490713A (zh) * 2021-06-17 2022-12-20 上海济煜医药科技有限公司 硼酸衍生物及其制备方法和应用

Family Cites Families (89)

* 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
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
US6075014A (en) 1997-06-13 2000-06-13 Northwestern University Inhibitors of β-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
WO2000035905A1 (en) 1998-12-16 2000-06-22 Northwestern University INHIBITORS OF β-LACTAMASES AND USES THEREFOR
HUP0202787A3 (en) 1999-09-25 2003-12-29 Smithkline Beecham Plc Piperazine derivatives as 5-ht1b antagonists, process for their preparation and pharmaceutical compositions containing them
AU762935B2 (en) 1999-10-28 2003-07-10 Merck & Co., Inc. Novel succinic acid metallo-beta-lactamase inhibitors and their use in treating bacterial infections
AU2001292732A1 (en) 2000-09-12 2002-03-26 Larry C. Blasczcak Beta-lactam analogs and uses therefor
WO2002022613A1 (en) 2000-09-14 2002-03-21 Pantherix Limited 3-(heteroaryl acetamido)-2-oxo-azetidine-1-sulfonic acids derivatives as antibacterial agents
WO2002054931A2 (en) 2001-01-10 2002-07-18 Bristol Myers Squibb Company P 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
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
JP2006511587A (ja) 2002-12-20 2006-04-06 ミジェニックス コーポレイション アデニンヌクレオチドトランスロカーゼ(ant)リガンドならびにそれに関連する組成物および方法
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
WO2005033090A1 (ja) 2003-10-06 2005-04-14 Sumitomo Chemical Company, Limited 芳香族化合物
EP1678180B1 (en) 2003-10-10 2007-08-08 Pfizer Products Incorporated Substituted 2h-[1,2,4]triazolo 4,3-a pyrazines as gsk-3 inhibitors
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
JP5038912B2 (ja) 2005-02-16 2012-10-03 アナコール ファーマシューティカルズ,インコーポレイテッド ホウ素含有小分子
CA2683975A1 (en) 2005-02-22 2006-08-31 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
TW200734311A (en) 2005-11-21 2007-09-16 Astrazeneca Ab New compounds
ATE529111T1 (de) 2005-12-07 2011-11-15 Basilea Pharmaceutica Ag Nützliche monobactam-antibiotika
NZ570257A (en) 2006-02-16 2011-11-25 Anacor Pharmaceuticals Inc Boron-containing small molecules as anti-inflammatory agents
WO2008039420A2 (en) 2006-09-27 2008-04-03 Merck & Co., Inc. Novel inhibitors of beta-lactamase
KR101320718B1 (ko) 2007-03-23 2013-10-21 바실리어 파마슈티카 아게 세균 감염 치료용 조합 약제
GB0719366D0 (en) 2007-10-03 2007-11-14 Smithkline Beecham Corp Compounds
CN101983203A (zh) 2007-11-13 2011-03-02 诺瓦提斯国际药物有限公司 β-内酰胺酶抑制剂
US20100120715A1 (en) 2007-11-13 2010-05-13 Burns Christopher J Beta-lactamase inhibitors
MY162532A (en) 2008-01-18 2017-06-15 Merck Sharp & Dohme Beta-lactamase inhibitors
US8129398B2 (en) 2008-03-19 2012-03-06 Bristol-Myers Squibb Company HIV integrase inhibitors
US20100256092A1 (en) 2008-05-12 2010-10-07 Anacor Pharmaceuticals, Inc. Boron-containing small molecules
US20110124634A1 (en) 2008-05-13 2011-05-26 Poniard Pharmaceuticals, Inc. Bioactive compounds for treatment of cancer and neurodegenerative diseases
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
US20100292185A1 (en) 2009-05-12 2010-11-18 Burns Christopher J Beta-lactamase inhibitors
US20120238576A1 (en) 2009-06-08 2012-09-20 California Capital Equity, Llc Triazine Derivatives and their Therapeutical Applications
KR20130031233A (ko) 2009-07-28 2013-03-28 아나코르 파마슈티칼스 인코포레이티드 삼치환된 붕소 함유 분자
CA2828114A1 (en) 2010-02-26 2011-09-01 Gary Igor DMITRIENKO Cephalosporin derivatives useful as .beta.-lactamase inhibitors and compositions and methods of use thereof
JP5933523B2 (ja) 2010-03-31 2016-06-08 ミレニアム ファーマシューティカルズ, インコーポレイテッドMillennium Pharmaceuticals, Inc. 1−アミノ−2−シクロプロピルエチルボロン酸の誘導体
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
PL3412676T3 (pl) 2010-08-10 2021-04-06 Melinta Therapeutics, Inc. Cykliczne pochodne estrowe kwasu boronowego, sposób otrzymywania oraz ich zastosowania terapeutyczne
RS54750B1 (sr) 2010-10-26 2016-10-31 Mars Inc 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
WO2013033461A1 (en) 2011-08-31 2013-03-07 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
US9688702B2 (en) 2011-12-22 2017-06-27 Ares Trading Alpha-amino boronic acid derivatives, selective immunoproteasome inhibitors
US20150018311A1 (en) 2012-01-09 2015-01-15 University of Tromsø 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
PL2928898T3 (pl) 2012-12-07 2021-10-25 VenatoRx Pharmaceuticals, Inc. Inhibitory beta-laktamaz
KR20150103270A (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
US9241947B2 (en) * 2013-01-04 2016-01-26 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
EP2941246A4 (en) * 2013-01-04 2016-12-21 Rempex Pharmaceuticals Inc BORONIC ACID DERIVATIVES AND THEIR THERAPEUTIC USES
US8999885B2 (en) 2013-01-09 2015-04-07 General Electric Company Methods of activating charcoal resulting from biomass gasification
ES2730013T3 (es) 2013-01-10 2019-11-07 Venatorx Pharmaceuticals Inc Inhibidores de betalactamasa
US9944658B2 (en) 2013-03-14 2018-04-17 VenatoRx Pharmaceuticals, Inc. Beta-lactamase inhibitors
CN105283439B (zh) 2013-03-15 2018-02-02 英特瑞克斯顿股份有限公司 含硼的二酰基肼类化合物
EP3140310B1 (en) 2014-05-05 2019-08-07 Rempex Pharmaceuticals, Inc. Synthesis of boronate salts and uses thereof
US9687497B1 (en) 2014-05-05 2017-06-27 Rempex Pharmaceuticals, Inc. Salts and polymorphs of cyclic boronic acid ester derivatives and therapeutic uses thereof
US9511142B2 (en) 2014-06-11 2016-12-06 VenatoRx Pharmaceuticals, Inc. Beta-lactamase inhibitors
ES2874579T3 (es) 2014-06-11 2021-11-05 Venatorx Pharmaceuticals Inc Inhibidores de betalactamasa
US10206937B2 (en) 2014-07-01 2019-02-19 Qpex Biopharma, Inc. Boronic acid derivatives and therapeutic uses thereof
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
AU2016252555A1 (en) 2015-04-24 2017-11-09 Melinta Therapeutics, Inc. Methods of treating bacterial infections

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EP3145936B1 (en) 2020-09-30
CN106459096A (zh) 2017-02-22
WO2015179308A1 (en) 2015-11-26
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AU2015264418A1 (en) 2016-11-10
EP3145936A1 (en) 2017-03-29
EP3145936A4 (en) 2018-01-17
JP2017517508A (ja) 2017-06-29
US9963467B2 (en) 2018-05-08
BR112016026291A2 (pt) 2017-08-15
US20170088561A1 (en) 2017-03-30
KR20170007448A (ko) 2017-01-18

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