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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CN201180059188.1A
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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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION 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
    • A01N47/00—Biocides, 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
    • A01N47/08—Biocides, 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
    • A01N47/28—Ureas or thioureas containing the groups >N—CO—N< or >N—CS—N<
    • A01N47/36—Ureas 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
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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
    • C07D491/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic 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
    • C07D513/02—Heterocyclic 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
    • C07D513/04—Ortho-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)
  • Public Health (AREA)
  • Oncology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Communicable Diseases (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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 (enExample)
EP (1) EP2625178A4 (enExample)
JP (1) JP5864589B2 (enExample)
CN (1) CN103249732B (enExample)
AU (1) AU2011313820A1 (enExample)
WO (1) WO2012045124A1 (enExample)

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JP6085829B2 (ja) 2011-01-14 2017-03-01 スペロ トリネム， インコーポレイテッド ピリミジンジャイレースおよびトポイソメラーゼｉｖ阻害剤
MX341342B (es) 2011-01-14 2016-08-17 Vertex Pharma Formas solidas del inhibidor de girasa (r)-1-etil-3-[6-fluoro-5-[2 -(1-hidroxi-1-metil-etil) pirimidin-5-il]-7-(tetrahidrofuran-2-il) -1h-benzimidazol-2-il]urea.
US8481552B2 (en) 2011-01-14 2013-07-09 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
KR101882172B1 (ko) 2011-01-14 2018-07-26 스페로 트리넴, 인코포레이티드 자이라제 및 토포이소머라제 ⅳ 억제제의 제조방법
ES2576298T3 (es) 2011-06-20 2016-07-06 Vertex Pharmaceuticals Incorporated Ésteres de fosfato de inhibidores de girasa y topoisomerasa
HK1206031A1 (en) 2012-03-22 2015-12-31 生物区欧洲有限公司 Antibacterial compounds
US9572809B2 (en) 2012-07-18 2017-02-21 Spero Trinem, Inc. Combination therapy to treat Mycobacterium diseases
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
SG11201606332PA (en) 2014-02-03 2016-09-29 Spero Gyrase Inc Antibacterial combinations comprising polymyxin
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
WO2016119700A1 (en) * 2015-01-28 2016-08-04 Jn Therapeutics Substituted imidazo [1, 2-a] pyridin-2-ylamine compounds, and pharmaceutical compositions and methods of use thereof
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
TWI828027B (zh) 2016-03-28 2024-01-01 美商英塞特公司 作為tam抑制劑之吡咯并三嗪化合物
JP6888101B2 (ja) * 2017-01-18 2021-06-16 アレイ バイオファーマ インコーポレイテッド ＲＥＴキナーゼ阻害剤としての置換ピラゾロ［１，５−ａ］ピラジン化合物
RU2019133662A (ru) 2017-03-24 2021-04-26 Тайсо Фармасьютикал Ко., Лтд. Производное 2(1h)-хинолинона
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
BR112022002815A2 (pt) * 2019-08-15 2022-05-10 Bayer Ag Método para preparar 2-(fenilimino)-3-alquil-1,3-tiazolidin- 4-onas
CN115315425B (zh) * 2020-08-14 2025-03-28 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
CN118955404B (zh) * 2024-07-30 2026-06-12 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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PT100905A (pt) * 1991-09-30 1994-02-28 Eisai Co Ltd Compostos heterociclicos azotados biciclicos contendo aneis de benzeno, ciclo-hexano ou piridina e de pirimidina, piridina ou imidazol substituidos e composicoes farmaceuticas que os contem
PL362691A1 (en) * 2000-12-15 2004-11-02 Vertex Pharmaceuticals Incorporated Bacterial gyrase inhibitors and uses thereof
US8404852B2 (en) * 2003-01-31 2013-03-26 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
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
US20090281097A1 (en) * 2006-04-14 2009-11-12 Takeda Pharmaceutical Company Limited Nitrogen-containing heterocyclic compound
GB0724342D0 (en) * 2007-12-13 2008-01-30 Prolysis Ltd Anitbacterial compositions
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
US9181234B2 (en) 2015-11-10
EP2625178A4 (en) 2014-04-30
AU2011313820A1 (en) 2013-04-11
WO2012045124A1 (en) 2012-04-12
JP5864589B2 (ja) 2016-02-17
US20120088750A1 (en) 2012-04-12
CN103249732A (zh) 2013-08-14
JP2013542204A (ja) 2013-11-21
EP2625178A1 (en) 2013-08-14

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