CN103249732B - 抑制2-乙基氨甲酰氨基-1,3-苯并噻唑-5-基的细菌拓扑异构酶ii - Google Patents

抑制2-乙基氨甲酰氨基-1,3-苯并噻唑-5-基的细菌拓扑异构酶ii Download PDF

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Publication number
CN103249732B
CN103249732B CN201180059188.1A CN201180059188A CN103249732B CN 103249732 B CN103249732 B CN 103249732B CN 201180059188 A CN201180059188 A CN 201180059188A CN 103249732 B CN103249732 B CN 103249732B
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China
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alkyl
methyl
piperidine
mmol
benzothiazol
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Expired - Fee Related
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Chinese (zh)
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CN103249732A (zh
Inventor
J·T·帕尔默
C·J·鲁尼斯
D·A·奥夫曼
L·C·阿克斯福德
M·布莱尔
D·R·米歇尔
N·J·帕尔默
C·斯蒂尔
J·阿瑟奥
D·沃森
D·J·海顿
L·G·洽普勒斯基
D·戴维斯
I·克林斯
E·M·泰恩戴尔
L·安德罗
G·R·W·皮特
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Biota Europe Ltd
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Biota Europe Ltd
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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
    • C07D417/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N47/00Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid
    • A01N47/08Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid the carbon atom having one or more single bonds to nitrogen atoms
    • A01N47/28Ureas or thioureas containing the groups >N—CO—N< or >N—CS—N<
    • A01N47/36Ureas or thioureas containing the groups >N—CO—N< or >N—CS—N< containing the group >N—CO—N< directly attached to at least one heterocyclic ring; Thio analogues thereof
    • 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
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-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

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Zoology (AREA)
  • Environmental Sciences (AREA)
  • Wood Science & Technology (AREA)
  • Dentistry (AREA)
  • Plant Pathology (AREA)
  • Pest Control & Pesticides (AREA)
  • Agronomy & Crop Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Oncology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Communicable Diseases (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN201180059188.1A 2010-10-08 2011-10-07 抑制2-乙基氨甲酰氨基-1,3-苯并噻唑-5-基的细菌拓扑异构酶ii Expired - Fee Related CN103249732B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US39116310P 2010-10-08 2010-10-08
US61/391,163 2010-10-08
PCT/AU2011/001284 WO2012045124A1 (en) 2010-10-08 2011-10-07 Bacteria topoisomerase ii inhibiting 2-ethylcarbamoylamino-1, 3-benzothiazol-5-yls

Publications (2)

Publication Number Publication Date
CN103249732A CN103249732A (zh) 2013-08-14
CN103249732B true CN103249732B (zh) 2016-08-10

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CN201180059188.1A Expired - Fee Related CN103249732B (zh) 2010-10-08 2011-10-07 抑制2-乙基氨甲酰氨基-1,3-苯并噻唑-5-基的细菌拓扑异构酶ii

Country Status (6)

Country Link
US (1) US9181234B2 (https=)
EP (1) EP2625178A4 (https=)
JP (1) JP5864589B2 (https=)
CN (1) CN103249732B (https=)
AU (1) AU2011313820A1 (https=)
WO (1) WO2012045124A1 (https=)

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RU2609259C2 (ru) 2011-01-14 2017-01-31 Сперо Тринем, Инк. Пиримидиновые ингибиторы гиразы и топоизомеразы iv
KR101882172B1 (ko) 2011-01-14 2018-07-26 스페로 트리넴, 인코포레이티드 자이라제 및 토포이소머라제 ⅳ 억제제의 제조방법
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
BR112013017977A2 (pt) 2011-01-14 2019-09-24 Vertex Pharma formas sólidas de inibidor de girase (r) 1-etil-3-[5-[2-{1-hidroxi-1-metil-etil}pirimidin-5-il]-7-(tetrai-drofuran-2-il)-1h-benzimidazol-2-il]ureia
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
WO2013138860A1 (en) 2012-03-22 2013-09-26 Biota Europe Limited Antibacterial compounds
US9018216B2 (en) 2012-07-18 2015-04-28 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
WO2014014845A1 (en) 2012-07-18 2014-01-23 Vertex Pharmaceuticals Incorporated Combination therapy comprising|1 -ethyl-3-[5-[2-{1 -hydroxy-1 -methyl-ethyl}pyrimidin-5-yl]-7-(tetra hydrofuran-2-|yl}-1 h-benzimidazol-2-yl]urea and derivatives thereof to treat mycobacterium|diseases
US20170007615A1 (en) 2014-02-03 2017-01-12 Biota Europe Ltd Antibacterial Compounds
CN104230991A (zh) * 2014-08-25 2014-12-24 亿腾药业(泰州)有限公司 一种控制福沙吡坦二甲葡胺中钯残留的方法
KR101987994B1 (ko) 2015-01-28 2019-06-11 제이엔 테라퓨틱스 치환된 이미다조[1,2-a]피리딘-2-일아민 화합물, 및 약학 조성물 및 이의 사용 방법
CN106167486B (zh) * 2015-05-22 2019-06-14 北京四环制药有限公司 单环类回旋酶和拓扑异构酶iv抑制剂
KR102483020B1 (ko) 2016-03-28 2023-01-04 인사이트 코포레이션 Tam 저해제로서의 피롤로트리아진 화합물
WO2018136661A1 (en) * 2017-01-18 2018-07-26 Andrews Steven W SUBSTITUTED PYRAZOLO[1,5-a]PYRAZINE COMPOUNDS AS RET KINASE INHIBITORS
CA3057431A1 (en) 2017-03-24 2018-09-27 Taisho Pharmaceutical Co., Ltd. 2(1h)-quinolinone derivative
WO2019057946A1 (en) 2017-09-25 2019-03-28 F. Hoffmann-La Roche Ag MULTI-CYCLIC AROMATIC COMPOUNDS AS D-FACTOR INHIBITORS
WO2019126731A1 (en) 2017-12-22 2019-06-27 Petra Pharma Corporation Aminopyridine derivatives as phosphatidylinositol phosphate kinase inhibitors
TW202112767A (zh) 2019-06-17 2021-04-01 美商佩特拉製藥公司 作為磷脂酸肌醇磷酸激酶抑制劑之胺基吡啶衍生物
JP2022544389A (ja) * 2019-08-15 2022-10-18 バイエル・アクチエンゲゼルシヤフト 2-(フェニルイミノ)-3-アルキル-1,3-チアゾリジン-4-オンの製造方法
WO2022032644A1 (zh) * 2020-08-14 2022-02-17 上海复旦张江生物医药股份有限公司 一种取代的咪唑并[1,2-a]吡啶-2-基酰胺化合物的制备方法及其中间体
CN115073358B (zh) * 2022-07-21 2023-09-26 安徽德诺医药股份有限公司 一种n-苄基-4-哌啶甲酸乙酯的制备方法
CN118955404A (zh) * 2024-07-30 2024-11-15 凯美克(上海)医药科技有限公司 一种化合物3,5-二溴哒嗪的合成方法

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DE60131015T2 (de) * 2000-12-15 2008-07-10 Vertex Pharmaceuticals Inc., Cambridge Bakterielle gyrase-hemmer und deren verwendung
US7569591B2 (en) * 2003-01-31 2009-08-04 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
US7618974B2 (en) * 2003-01-31 2009-11-17 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
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EP2321309A1 (en) * 2008-06-25 2011-05-18 Ranbaxy Laboratories Limited Benzothiazoles and aza-analogues thereof use as antibacterial agents
WO2010100144A1 (en) * 2009-03-04 2010-09-10 Merck Serono S.A. Fused bicyclic compounds as inhibitors for pi3 kinase

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Publication number Publication date
WO2012045124A1 (en) 2012-04-12
US20120088750A1 (en) 2012-04-12
AU2011313820A1 (en) 2013-04-11
CN103249732A (zh) 2013-08-14
US9181234B2 (en) 2015-11-10
EP2625178A4 (en) 2014-04-30
JP5864589B2 (ja) 2016-02-17
EP2625178A1 (en) 2013-08-14
JP2013542204A (ja) 2013-11-21

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