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 PDFInfo
- 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
- Authority
- CN
- China
- Prior art keywords
- alkyl
- methyl
- piperidine
- mmol
- benzothiazol
- 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
Links
- 0 CCNC(NC(SC1C(C)=C)=N[C@]1*=C(C)C(C=I)=C*=C(*)N(CC1)CCC1(*)C(O)=O)=O Chemical compound CCNC(NC(SC1C(C)=C)=N[C@]1*=C(C)C(C=I)=C*=C(*)N(CC1)CCC1(*)C(O)=O)=O 0.000 description 17
- USXWLLACBRLNTL-UHFFFAOYSA-N CCCCCN(CCCC(O)=O)c1nc(-c(cc2-c3ccccn3)cc3c2[s]c(CNCC(NCC)=O)n3)c[s]1 Chemical compound CCCCCN(CCCC(O)=O)c1nc(-c(cc2-c3ccccn3)cc3c2[s]c(CNCC(NCC)=O)n3)c[s]1 USXWLLACBRLNTL-UHFFFAOYSA-N 0.000 description 1
- DMJPWVYCRXWSKJ-UHFFFAOYSA-N CCOC(C1(CCNCC1)SC)=C Chemical compound CCOC(C1(CCNCC1)SC)=C DMJPWVYCRXWSKJ-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Environmental Sciences (AREA)
- Plant Pathology (AREA)
- Engineering & Computer Science (AREA)
- Dentistry (AREA)
- Pest Control & Pesticides (AREA)
- Wood Science & Technology (AREA)
- Zoology (AREA)
- Agronomy & Crop Science (AREA)
- General Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Communicable Diseases (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Oncology (AREA)
- Public Health (AREA)
- Veterinary Medicine (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)
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 |
Family
ID=45925612
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2824519C (en) | 2011-01-14 | 2020-06-16 | Vertex Pharmaceuticals Incorporated | Process of making gyrase and topoisomerase inhibitors |
| TW201309676A (zh) | 2011-01-14 | 2013-03-01 | Vertex Pharma | 旋轉酶抑制劑(r)-1-乙基-3-[5-[2-(1-羥基-1-甲基-乙基)嘧啶-5-基]-7-(四氫呋喃-2-基]-1h-苯并咪唑-2-基]脲之固體形式 |
| EP2663562B1 (en) | 2011-01-14 | 2018-11-07 | Spero Trinem, Inc. | 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 |
| 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 |
| TWI554515B (zh) | 2011-06-20 | 2016-10-21 | 維泰克斯製藥公司 | 旋轉酶(gyrase)及拓樸異構酶抑制劑之磷酸酯 |
| WO2013138860A1 (en) | 2012-03-22 | 2013-09-26 | Biota Europe Limited | Antibacterial compounds |
| 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 |
| JP2017504662A (ja) | 2014-02-03 | 2017-02-09 | スペロ ジャイレース インク | ポリミキシンを含む抗菌剤の組合せ |
| 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 |
| EP3436461B1 (en) | 2016-03-28 | 2023-11-01 | Incyte Corporation | Pyrrolotriazine compounds as tam inhibitors |
| CN110267960B (zh) * | 2017-01-18 | 2022-04-26 | 阿雷生物药品公司 | 作为RET激酶抑制剂的取代的吡唑并[1,5-a]吡嗪化合物 |
| KR20190133667A (ko) | 2017-03-24 | 2019-12-03 | 다이쇼 세이야꾸 가부시끼가이샤 | 2(1h)-퀴놀리논 유도체 |
| WO2019057946A1 (en) | 2017-09-25 | 2019-03-28 | F. Hoffmann-La Roche Ag | MULTI-CYCLIC AROMATIC COMPOUNDS AS D-FACTOR INHIBITORS |
| JP7569688B2 (ja) | 2017-12-22 | 2024-10-18 | ハイバーセル,インコーポレイテッド | ホスファチジルイノシトールリン酸キナーゼ阻害剤としてのアミノピリジン誘導体 |
| 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 |
| MX2022001861A (es) * | 2019-08-15 | 2022-03-11 | Bayer Ag | Procedimiento para la preparacion de 2-(fenilimino)-3-alquil-1,3-t iazolidin-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 |
| 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 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| ES2331250T3 (es) * | 2000-12-15 | 2009-12-28 | Vertex Pharmaceuticals Incorporated | Inhibidores de la girasa bacteriana y usos de los mismos. |
| US7618974B2 (en) * | 2003-01-31 | 2009-11-17 | Vertex Pharmaceuticals Incorporated | 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 |
| CA2648748A1 (en) * | 2006-04-14 | 2007-10-25 | 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 |
-
2011
- 2011-10-07 JP JP2013532015A patent/JP5864589B2/ja not_active Expired - Fee Related
- 2011-10-07 CN CN201180059188.1A patent/CN103249732B/zh not_active Expired - Fee Related
- 2011-10-07 AU AU2011313820A patent/AU2011313820A1/en not_active Abandoned
- 2011-10-07 EP EP11830125.8A patent/EP2625178A4/en not_active Withdrawn
- 2011-10-07 WO PCT/AU2011/001284 patent/WO2012045124A1/en not_active Ceased
- 2011-10-07 US US13/268,154 patent/US9181234B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| JP5864589B2 (ja) | 2016-02-17 |
| EP2625178A4 (en) | 2014-04-30 |
| US9181234B2 (en) | 2015-11-10 |
| US20120088750A1 (en) | 2012-04-12 |
| JP2013542204A (ja) | 2013-11-21 |
| CN103249732A (zh) | 2013-08-14 |
| WO2012045124A1 (en) | 2012-04-12 |
| AU2011313820A1 (en) | 2013-04-11 |
| EP2625178A1 (en) | 2013-08-14 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20160810 Termination date: 20171007 |
|
| CF01 | Termination of patent right due to non-payment of annual fee |