CN102015700B - 抗菌稠合噻唑 - Google Patents

抗菌稠合噻唑 Download PDF

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Publication number
CN102015700B
CN102015700B CN200880126437.2A CN200880126437A CN102015700B CN 102015700 B CN102015700 B CN 102015700B CN 200880126437 A CN200880126437 A CN 200880126437A CN 102015700 B CN102015700 B CN 102015700B
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CN
China
Prior art keywords
ethyl
urea
thiazol
benzo
mmol
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.)
Expired - Fee Related
Application number
CN200880126437.2A
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English (en)
Chinese (zh)
Other versions
CN102015700A (zh
Inventor
D·J·海顿
L·G·洽普勒斯基
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Biota Europe Ltd
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Biota Europe Ltd
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Publication of CN102015700A publication Critical patent/CN102015700A/zh
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Publication of CN102015700B publication Critical patent/CN102015700B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/428Thiazoles condensed with carbocyclic rings
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62Benzothiazoles
    • C07D277/68Benzothiazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C07D277/82Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
CN200880126437.2A 2007-12-13 2008-12-12 抗菌稠合噻唑 Expired - Fee Related CN102015700B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB0724342.1 2007-12-13
GBGB0724342.1A GB0724342D0 (en) 2007-12-13 2007-12-13 Anitbacterial compositions
PCT/GB2008/004114 WO2009074812A1 (en) 2007-12-13 2008-12-12 Antibacterial condensed thiazoles

Publications (2)

Publication Number Publication Date
CN102015700A CN102015700A (zh) 2011-04-13
CN102015700B true CN102015700B (zh) 2014-12-03

Family

ID=39048076

Family Applications (1)

Application Number Title Priority Date Filing Date
CN200880126437.2A Expired - Fee Related CN102015700B (zh) 2007-12-13 2008-12-12 抗菌稠合噻唑

Country Status (14)

Country Link
US (1) US8299065B2 (https=)
EP (1) EP2231653B1 (https=)
JP (1) JP5539898B2 (https=)
KR (1) KR20100105847A (https=)
CN (1) CN102015700B (https=)
AU (1) AU2008334427B2 (https=)
BR (1) BRPI0820656A2 (https=)
CA (1) CA2709021A1 (https=)
EA (1) EA018104B1 (https=)
ES (1) ES2416059T3 (https=)
GB (1) GB0724342D0 (https=)
MX (1) MX2010006428A (https=)
NZ (1) NZ586508A (https=)
WO (1) WO2009074812A1 (https=)

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EA201270566A1 (ru) * 2009-10-16 2012-11-30 Риб-Экс Фармасьютикалз, Инк. Противомикробные соединения и способы их получения и применения
NZ599290A (en) 2009-10-16 2014-10-31 Melinta Therapeutics Inc Antimicrobial compounds and methods of making and using the same
BR112012024705A2 (pt) * 2010-03-31 2016-06-07 Actelion Pharmaceuticals Ltd derivados antibacterianos de isoquinolin-3-ilureia
US8648192B2 (en) 2010-05-26 2014-02-11 Boehringer Ingelheim International Gmbh 2-oxo-1,2-dihydropyridin-4-ylboronic acid derivatives
WO2012045124A1 (en) * 2010-10-08 2012-04-12 Biota Europe Ltd Bacteria topoisomerase ii inhibiting 2-ethylcarbamoylamino-1, 3-benzothiazol-5-yls
US8476281B2 (en) 2011-01-14 2013-07-02 Vertex Pharmaceuticals Incorporated Solid forms of gyrase inhibitor (R)-1-ethyl-3-[6-fluoro-5-[2-(1-hydroxy-1-methyl-ethyl)pyrimidin-5-yl]-7-(tetrahydrofuran-2-yl)-1H-benzimidazol-2-yl]urea
CN103384665B (zh) 2011-01-14 2018-01-09 斯派罗吹耐姆公司 制备促旋酶和拓扑异构酶抑制剂的方法
AU2012205415B2 (en) 2011-01-14 2017-02-02 Spero Therapeutics, Inc. Pyrimidine gyrase and topoisomerase IV inhibitors
WO2012097270A1 (en) 2011-01-14 2012-07-19 Vertex Pharmaceuticals Incorporated Solid forms of gyrase inhibitor (r)-1-ethyl-3-[5-[2-{1-hydroxy-1-methyl-ethyl}pyrimidin-5-yl]-7-(tetrahydrofuran-2-yl}-1h-benzimidazol-2-yl]urea
EP2691399B1 (en) * 2011-03-28 2016-07-13 F.Hoffmann-La Roche Ag Thiazolopyrimidine compounds
AR088729A1 (es) 2011-03-29 2014-07-02 Actelion Pharmaceuticals Ltd Derivados de 3-ureidoisoquinolin-8-ilo y una composicion farmaceutica
MY173518A (en) 2011-04-15 2020-01-30 Melinta Therapeutics Inc Antimicrobial compounds and methods of making and using the same
CN103702994B (zh) 2011-06-20 2016-03-23 沃泰克斯药物股份有限公司 旋转酶和拓扑异构酶抑制剂的磷酸酯
WO2013106756A2 (en) 2012-01-13 2013-07-18 Rutgers, The State University Of New Jersey Antimicrobial agents
EP2828245A1 (en) 2012-03-21 2015-01-28 Rutgers, The State University of New Jersey Antimicrobial agents
WO2013138860A1 (en) 2012-03-22 2013-09-26 Biota Europe Limited Antibacterial compounds
CA2878481A1 (en) * 2012-07-10 2014-01-16 Bayer Pharma Aktiengesellschaft Method for preparing substituted triazolopyridines
US9572809B2 (en) 2012-07-18 2017-02-21 Spero Trinem, Inc. Combination therapy to treat Mycobacterium diseases
WO2014015105A1 (en) 2012-07-18 2014-01-23 Vertex Pharmaceuticals Incorporated Solid forms of (r)-2-(5-(2-(3-ethylureido)-6-fluoro-7-(tetrahydrofuran-2-yl)-1h-benzo[d]imidazol-5-yl)pyrimidin-2-yl)propan-2-yl dihydrogen phosphate and salts thereof
US9434695B2 (en) 2012-07-18 2016-09-06 Sunshine Lake Pharma Co., Ltd Nitrogenous heterocyclic derivatives and their application in drugs
SG11201504873RA (en) 2012-12-21 2015-07-30 Janssen Sciences Ireland Uc Antibacterial compounds
EP3038623A4 (en) 2013-09-09 2017-04-19 Melinta Therapeutics, Inc. Antimicrobial compounds and methods of making and using the same
CA2923214A1 (en) 2013-09-09 2015-03-12 Melinta Therapeutics, Inc. Antimicrobial compounds and methods of making and using the same
US9458150B2 (en) 2013-11-08 2016-10-04 Rutgers, The State University Of New Jersey Antimicrobial agents
MX2016010057A (es) 2014-02-03 2017-04-27 Spero Gyrase Inc Compuestos antibacterianos.
CN105367547B (zh) * 2014-08-19 2019-04-23 北京桦冠生物技术有限公司 一种噁唑啉酮抗生素的新合成工艺
AR102215A1 (es) * 2014-10-10 2017-02-15 Glaxosmithkline Ip Dev Ltd Compuesto de pirazol-4-carboxamida, composición farmacéutica que lo comprende y su uso para la fabricación de un medicamento
HK1249758A1 (zh) 2015-03-11 2018-11-09 Melinta Therapeutics, Inc. 抗微生物化合物及其制备和使用方法
US10513528B2 (en) 2016-02-25 2019-12-24 Taxis Pharmaceuticals, Inc. Synthetic processes and intermediates
EP3439655B1 (en) 2016-04-08 2021-03-03 Quretech Bio AB Ring-fused thiazolino 2-pyridones, methods for preparation thereof and their use in the treatment and/or prevention of tuberculosis
US11098047B2 (en) 2016-05-06 2021-08-24 BioVersys AG Antimicrobials and methods of making and using same
CA3057431A1 (en) 2017-03-24 2018-09-27 Taisho Pharmaceutical Co., Ltd. 2(1h)-quinolinone derivative
WO2018183917A1 (en) 2017-03-30 2018-10-04 Taxis Pharmaceuticals, Inc. Synthetic processes and synthetic intermediates
CN107325093B (zh) * 2017-07-09 2020-06-05 西南科技大学 具抗菌活性的硫脲类化合物合成及应用
WO2019162458A1 (en) 2018-02-23 2019-08-29 Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung e.V. Novel inhibitors of bacterial glutaminyl cyclases for use in the treatment of periodontal and related diseases
CN114945366B (zh) 2019-09-13 2025-01-07 林伯士萨顿公司 Hpk1拮抗剂和其用途
CN117120090A (zh) 2021-02-12 2023-11-24 林伯士萨顿公司 Hpk1拮抗剂和其用途
EP4301756A4 (en) 2021-03-05 2025-02-26 Nimbus Saturn, Inc. Hpk1 antagonists and uses thereof
WO2022213062A1 (en) 2021-03-29 2022-10-06 Nimbus Saturn, Inc. Hpk1 antagonists and uses thereof
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US3725428A (en) * 1968-11-01 1973-04-03 Ciba Geigy Ag N-benzothiazol-2-yl-n{40 -propylureas
CN1481368A (zh) * 2000-12-15 2004-03-10 ��̩��˹ҩ��ɷ����޹�˾ 促旋酶抑制剂和其用途
EP1790640A1 (en) * 2004-09-09 2007-05-30 Chugai Seiyaku Kabushiki Kaisha Novel imidazolidine derivative and use thereof

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CN1481368A (zh) * 2000-12-15 2004-03-10 ��̩��˹ҩ��ɷ����޹�˾ 促旋酶抑制剂和其用途
EP1790640A1 (en) * 2004-09-09 2007-05-30 Chugai Seiyaku Kabushiki Kaisha Novel imidazolidine derivative and use thereof

Also Published As

Publication number Publication date
EA018104B1 (ru) 2013-05-30
JP5539898B2 (ja) 2014-07-02
EA201000993A1 (ru) 2011-02-28
ES2416059T3 (es) 2013-07-30
EP2231653A1 (en) 2010-09-29
WO2009074812A1 (en) 2009-06-18
KR20100105847A (ko) 2010-09-30
AU2008334427A1 (en) 2009-06-18
CN102015700A (zh) 2011-04-13
US20100305067A1 (en) 2010-12-02
NZ586508A (en) 2012-05-25
EP2231653B1 (en) 2013-04-03
BRPI0820656A2 (pt) 2015-06-16
JP2011506417A (ja) 2011-03-03
MX2010006428A (es) 2010-09-30
GB0724342D0 (en) 2008-01-30
CA2709021A1 (en) 2009-06-18
AU2008334427B2 (en) 2014-06-19
US8299065B2 (en) 2012-10-30

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Granted publication date: 20141203

Termination date: 20171212

CF01 Termination of patent right due to non-payment of annual fee