CN103717582B - 用作抗菌剂的异*唑衍生物 - Google Patents
用作抗菌剂的异*唑衍生物 Download PDFInfo
- Publication number
- CN103717582B CN103717582B CN201280016114.4A CN201280016114A CN103717582B CN 103717582 B CN103717582 B CN 103717582B CN 201280016114 A CN201280016114 A CN 201280016114A CN 103717582 B CN103717582 B CN 103717582B
- Authority
- CN
- China
- Prior art keywords
- methyl
- base
- azoles
- different
- butyramide
- 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 CCCC(*)(*)C(NO)=O Chemical compound CCCC(*)(*)C(NO)=O 0.000 description 1
Classifications
-
- 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
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
- C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
- C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members 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 to ring carbon atoms
- C07D261/14—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
- C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
- C07D261/08—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic 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
- A61K31/42—Oxazoles
-
- 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
- A61P31/10—Antimycotics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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)
- Oncology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Communicable Diseases (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161473540P | 2011-04-08 | 2011-04-08 | |
| US61/473,540 | 2011-04-08 | ||
| PCT/IB2012/051406 WO2012137094A1 (en) | 2011-04-08 | 2012-03-23 | Isoxazole derivatives useful as antibacterial agents |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103717582A CN103717582A (zh) | 2014-04-09 |
| CN103717582B true CN103717582B (zh) | 2015-09-30 |
Family
ID=45999906
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201280016114.4A Expired - Fee Related CN103717582B (zh) | 2011-04-08 | 2012-03-23 | 用作抗菌剂的异*唑衍生物 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US8748466B2 (2) |
| EP (1) | EP2694488B1 (2) |
| JP (1) | JP2014510132A (2) |
| KR (1) | KR20130140868A (2) |
| CN (1) | CN103717582B (2) |
| AU (1) | AU2012238374B2 (2) |
| CA (1) | CA2830920C (2) |
| DK (1) | DK2694488T3 (2) |
| ES (1) | ES2526687T3 (2) |
| IL (2) | IL228799A (2) |
| MX (1) | MX2013011526A (2) |
| SG (1) | SG193367A1 (2) |
| WO (1) | WO2012137094A1 (2) |
| ZA (1) | ZA201306736B (2) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5524215B2 (ja) | 2008-09-19 | 2014-06-18 | ファイザー・インク | 抗菌剤として有用なヒドロキサム酸誘導体 |
| WO2011073845A1 (en) | 2009-12-16 | 2011-06-23 | Pfizer Inc. | N-linked hydroxamic acid derivatives useful as antibacterial agents |
| ES2626457T3 (es) | 2011-03-07 | 2017-07-25 | Pfizer Inc. | Derivados de fluoro-piridinona útiles como agentes antibacterianos |
| ES2526687T3 (es) | 2011-04-08 | 2015-01-14 | Pfizer Inc. | Derivados de isoxazol útiles como agentes antibacterianos |
| CA2830866A1 (en) * | 2011-04-08 | 2012-10-11 | Pfizer Inc. | Imidazole, pyrazole, and triazole derivatives useful as antibacterial agents |
| AR097617A1 (es) | 2013-09-13 | 2016-04-06 | Actelion Pharmaceuticals Ltd | Derivados antibacterianos del 2h-indazol |
| WO2015057964A2 (en) * | 2013-10-16 | 2015-04-23 | The Board Of Regents Of The University Of Texas System | Modulation of mrtf-a activity in pathologic fibrosis and wound healing |
| EA030730B1 (ru) | 2013-12-19 | 2018-09-28 | Идорсиа Фармасьютиклз Лтд | Антибактериальные производные 1h-индазола и 1h-индола |
| AR099612A1 (es) | 2014-03-04 | 2016-08-03 | Actelion Pharmaceuticals Ltd | Derivados antibacterianos de 1,2-dihidro-3h-pirrolo[1,2-c]imidazol-3-ona |
| EP3134401B1 (en) | 2014-04-22 | 2018-06-13 | Novartis AG | Isoxazoline hydroxamic acid derivatives as lpxc inhibitors |
| CA2948077A1 (en) | 2014-05-16 | 2015-11-19 | Actelion Pharmaceuticals Ltd | Antibacterial quinazoline-4(3h)-one derivatives |
| KR20170086079A (ko) | 2014-11-19 | 2017-07-25 | 액테리온 파마슈티칼 리미티드 | 항균성 벤조티아졸 유도체 |
| DK3233843T3 (da) * | 2014-12-16 | 2019-11-18 | Novartis Ag | Isoxazol-hydraxamsyreforbindelser som LPXC-hæmmere |
| AR105646A1 (es) | 2015-08-11 | 2017-10-25 | Actelion Pharmaceuticals Ltd | Agentes antibacterianos de 1,2-dihidro-3h-pirrolo[1,2-c]imidazol-3-ona sustituida |
| AR105848A1 (es) * | 2015-08-31 | 2017-11-15 | Actelion Pharmaceuticals Ltd | Derivados heterocíclicos antibacterianos |
| AR105889A1 (es) | 2015-09-03 | 2017-11-22 | Actelion Pharmaceuticals Ltd | Compuestos antibacterianos 1,2-dihidro-3h-pirrolo[1,2-c]imidazol-3-ona sustituidos |
| US10590498B2 (en) * | 2016-05-17 | 2020-03-17 | Lawrence Livermore National Security, Llc | Compounds for reactivation of acetylcholinesterase and related compositions methods and systems |
| JP6941630B2 (ja) | 2016-06-14 | 2021-09-29 | ノバルティス アーゲー | 抗菌剤としての(r)−4(5−(シクロプロピルエチニル)イソオキサゾール−3−イル)−n−ヒドロキシ−2−メチル−2−(メチルスルホニル)ブタンアミドの結晶形 |
| DE102016113269A1 (de) | 2016-07-19 | 2018-01-25 | Osram Opto Semiconductors Gmbh | Leuchtvorrichtung für ein mobiles endgerät |
| TWI604678B (zh) * | 2016-09-07 | 2017-11-01 | 國立暨南國際大學 | Radio transmission system |
| JP6812542B2 (ja) * | 2016-09-28 | 2021-01-13 | ドン−ア エスティ カンパニー リミテッド | テトラヒドロピリジン誘導体および抗菌剤としてのその使用 |
| US11186548B2 (en) | 2017-11-23 | 2021-11-30 | Lawrence Livermore National Security, Llc | Compounds for central reactivation of organophosphorus-based compound-inhibited acetylcholinesterase and/or inactivation of organophosphorus-based acetylcholinesterase inhibitors and related compositions methods and systems for making and using them |
| KR20210093884A (ko) * | 2018-11-21 | 2021-07-28 | 다이쇼 세이야꾸 가부시끼가이샤 | 신규 이미다졸 유도체 |
| CN111944719B (zh) * | 2020-08-14 | 2022-04-29 | 暨南大学 | 一株二恶烷降解菌is20及其制备方法和应用 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1437349A1 (en) * | 2001-07-20 | 2004-07-14 | Laboratorios S.A.L.V.A.T., S.A. | Substituted isoxazoles and the use thereof as antibiotics |
| CN101016270A (zh) * | 2006-12-30 | 2007-08-15 | 天津药物研究院 | 取代的哌嗪基苯基异噁唑啉衍生物及其用途 |
| WO2007093904A1 (en) * | 2006-02-14 | 2007-08-23 | Pfizer Products Inc. | Benzoxazinone and benzoxazepinone oxazolidinones as antibacterial agents |
| WO2010032147A2 (en) * | 2008-09-19 | 2010-03-25 | Pfizer Inc. | Hydroxamic acid derivatives useful as antibacterial agents |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4769461A (en) | 1986-09-16 | 1988-09-06 | American Home Products Corporation | Quinolinyl benzene hydroxamic acids as anti-inflammatory/antiallergic agents |
| US5110831A (en) | 1990-11-30 | 1992-05-05 | Du Pont Merck Pharmaceutical Company | Vinylogous hydroxamic acids and derivatives thereof as 5-lipoxygenase inhibitors |
| DK1052984T3 (da) | 1998-02-07 | 2004-09-20 | Vernalis Oxford Ltd | Antibakterielle midler |
| GB9925470D0 (en) | 1999-10-27 | 1999-12-29 | Smithkline Beecham Plc | Novel compounds |
| JPWO2002074298A1 (ja) | 2001-03-21 | 2004-07-08 | 小野薬品工業株式会社 | Il−6産生阻害剤 |
| KR101076018B1 (ko) | 2003-01-08 | 2011-10-21 | 유니버시티 오브 워싱톤 | 항균제 |
| GB0302431D0 (en) | 2003-01-30 | 2003-03-05 | Glaxo Group Ltd | Novel compounds |
| MX2007006961A (es) | 2004-12-10 | 2007-10-04 | Univ Emory | Analogos nucleosidos de ciclobutilo 2' y 3'-sustituidos para el tratamiento de infeccciones virales y proliferacion celular anormal. |
| WO2006118155A1 (ja) | 2005-04-27 | 2006-11-09 | Ishihara Sangyo Kaisha, Ltd. | ビフェニル誘導体又はその塩、並びにそれらを有効成分として含有する農園芸用殺菌剤 |
| US20060258691A1 (en) | 2005-05-13 | 2006-11-16 | Joseph Barbosa | Methods and compositions for improving cognition |
| JP2009520695A (ja) | 2005-12-15 | 2009-05-28 | ヴィキュロン ファーマシューティカルズ インコーポレイテッド | 抗菌活性を有するn−ヒドロキシアミド誘導体 |
| WO2008045671A1 (en) | 2006-10-06 | 2008-04-17 | Janssen Pharmaceutica, N.V. | Matrix metalloprotease inhibitors |
| US7879911B2 (en) | 2007-02-01 | 2011-02-01 | Johnson Alan T | Hydroxamic acid derivatives of phenoxy-acetic acids and analogs useful as therapeutic agents for treating anthrax poisoning |
| JP5227304B2 (ja) | 2007-02-28 | 2013-07-03 | 大正製薬株式会社 | 新規なヒドロキサム酸誘導体 |
| WO2008115262A2 (en) | 2007-03-20 | 2008-09-25 | Curis, Inc. | Hsp90 inhibitors containing a zinc binding moiety |
| WO2010017060A1 (en) | 2008-08-04 | 2010-02-11 | Schering Corporation | Urea derivatives as antibacterial agents |
| JP5455913B2 (ja) | 2008-08-27 | 2014-03-26 | 大正製薬株式会社 | ナフチリジン−n−オキシドを有する新規ヒドロキサム酸誘導体 |
| US8372885B2 (en) | 2008-09-17 | 2013-02-12 | Novartis Ag | Organic compounds and their uses |
| WO2010100475A1 (en) | 2009-03-02 | 2010-09-10 | Astrazeneca Ab | Hydroxamic acid derivatives as gram-negative antibacterial agents |
| WO2011073845A1 (en) | 2009-12-16 | 2011-06-23 | Pfizer Inc. | N-linked hydroxamic acid derivatives useful as antibacterial agents |
| ES2626457T3 (es) | 2011-03-07 | 2017-07-25 | Pfizer Inc. | Derivados de fluoro-piridinona útiles como agentes antibacterianos |
| CA2830866A1 (en) | 2011-04-08 | 2012-10-11 | Pfizer Inc. | Imidazole, pyrazole, and triazole derivatives useful as antibacterial agents |
| ES2526687T3 (es) | 2011-04-08 | 2015-01-14 | Pfizer Inc. | Derivados de isoxazol útiles como agentes antibacterianos |
-
2012
- 2012-03-23 ES ES12716624.7T patent/ES2526687T3/es active Active
- 2012-03-23 MX MX2013011526A patent/MX2013011526A/es not_active Application Discontinuation
- 2012-03-23 AU AU2012238374A patent/AU2012238374B2/en not_active Ceased
- 2012-03-23 KR KR1020137029552A patent/KR20130140868A/ko not_active Abandoned
- 2012-03-23 SG SG2013067616A patent/SG193367A1/en unknown
- 2012-03-23 JP JP2014503238A patent/JP2014510132A/ja active Pending
- 2012-03-23 DK DK12716624.7T patent/DK2694488T3/en active
- 2012-03-23 CA CA2830920A patent/CA2830920C/en not_active Expired - Fee Related
- 2012-03-23 CN CN201280016114.4A patent/CN103717582B/zh not_active Expired - Fee Related
- 2012-03-23 US US14/110,157 patent/US8748466B2/en not_active Expired - Fee Related
- 2012-03-23 EP EP12716624.7A patent/EP2694488B1/en not_active Not-in-force
- 2012-03-23 WO PCT/IB2012/051406 patent/WO2012137094A1/en not_active Ceased
-
2013
- 2013-09-09 ZA ZA2013/06736A patent/ZA201306736B/en unknown
- 2013-10-08 IL IL228799A patent/IL228799A/en not_active IP Right Cessation
-
2015
- 2015-07-21 IL IL240078A patent/IL240078A0/en unknown
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1437349A1 (en) * | 2001-07-20 | 2004-07-14 | Laboratorios S.A.L.V.A.T., S.A. | Substituted isoxazoles and the use thereof as antibiotics |
| WO2007093904A1 (en) * | 2006-02-14 | 2007-08-23 | Pfizer Products Inc. | Benzoxazinone and benzoxazepinone oxazolidinones as antibacterial agents |
| CN101016270A (zh) * | 2006-12-30 | 2007-08-15 | 天津药物研究院 | 取代的哌嗪基苯基异噁唑啉衍生物及其用途 |
| WO2010032147A2 (en) * | 2008-09-19 | 2010-03-25 | Pfizer Inc. | Hydroxamic acid derivatives useful as antibacterial agents |
Non-Patent Citations (3)
| Title |
|---|
| 3-(吗啉吡啶基)-5-取代异噁唑类化合物的合成及抗菌活性研究;杜光剑,等;《有机化学》;20091231;第29卷(第10期);第1575-1581页 * |
| Hydroxamic Acid Derivatives as Potent Peptide Deformylase Inhibitors and Antibacterial Agents;Christian Apfel,等;《J.Med.Chem.》;20000520;第43卷(第12期);第2324-2331页 * |
| Potent Inhibitors of LpxC for the Treatment of Gram-Negative Infections;Matthew F.Brown,等;《Journal of Medicinal Chemistry》;20111218;第55卷(第18期);第914-923页 * |
Also Published As
| Publication number | Publication date |
|---|---|
| SG193367A1 (en) | 2013-10-30 |
| DK2694488T3 (en) | 2014-12-15 |
| WO2012137094A1 (en) | 2012-10-11 |
| US8748466B2 (en) | 2014-06-10 |
| CN103717582A (zh) | 2014-04-09 |
| EP2694488B1 (en) | 2014-11-12 |
| IL240078A0 (en) | 2015-08-31 |
| US20140024690A1 (en) | 2014-01-23 |
| AU2012238374A1 (en) | 2013-09-26 |
| CA2830920A1 (en) | 2012-10-11 |
| AU2012238374B2 (en) | 2015-04-02 |
| MX2013011526A (es) | 2013-12-06 |
| EP2694488A1 (en) | 2014-02-12 |
| IL228799A (en) | 2015-08-31 |
| ZA201306736B (en) | 2014-11-26 |
| ES2526687T3 (es) | 2015-01-14 |
| CA2830920C (en) | 2015-07-14 |
| IL228799A0 (en) | 2013-12-31 |
| KR20130140868A (ko) | 2013-12-24 |
| JP2014510132A (ja) | 2014-04-24 |
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