CN105246334A - 大环内酯及其制备和使用方法 - Google Patents

大环内酯及其制备和使用方法 Download PDF

Info

Publication number
CN105246334A
CN105246334A CN201480031522.6A CN201480031522A CN105246334A CN 105246334 A CN105246334 A CN 105246334A CN 201480031522 A CN201480031522 A CN 201480031522A CN 105246334 A CN105246334 A CN 105246334A
Authority
CN
China
Prior art keywords
optional
replaced
alkyl
optionally substituted
compound
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.)
Pending
Application number
CN201480031522.6A
Other languages
English (en)
Chinese (zh)
Inventor
A.G.迈尔斯
I.B.塞普尔
Z.张
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Harvard University
Original Assignee
Harvard University
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Harvard University filed Critical Harvard University
Priority to CN202010566628.3A priority Critical patent/CN111825733A/zh
Publication of CN105246334A publication Critical patent/CN105246334A/zh
Pending legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • 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
    • A61K31/424—Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/7056—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00—Preparation of carboxylic acid amides
    • C07C231/12—Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D307/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/10—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings
    • C07D317/14—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D317/30—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic 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
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages
    • C07F7/1872—Preparation; Treatments not provided for in C07F7/20
    • C07F7/1892—Preparation; Treatments not provided for in C07F7/20 by reactions not provided for in C07F7/1876 - C07F7/1888
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/04—Heterocyclic radicals containing only oxygen as ring hetero atoms
    • C07H17/08—Hetero rings containing eight or more ring members, e.g. erythromycins
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic 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
    • C07D498/08—Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Rheumatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN201480031522.6A 2013-04-04 2014-04-04 大环内酯及其制备和使用方法 Pending CN105246334A (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202010566628.3A CN111825733A (zh) 2013-04-04 2014-04-04 大环内酯及其制备和使用方法

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201361808441P 2013-04-04 2013-04-04
US61/808,441 2013-04-04
US201361832639P 2013-06-07 2013-06-07
US61/832,639 2013-06-07
US201461946604P 2014-02-28 2014-02-28
US61/946,604 2014-02-28
PCT/US2014/033025 WO2014165792A2 (en) 2013-04-04 2014-04-04 Macrolides and methods of their preparation and use

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN202010566628.3A Division CN111825733A (zh) 2013-04-04 2014-04-04 大环内酯及其制备和使用方法

Publications (1)

Publication Number Publication Date
CN105246334A true CN105246334A (zh) 2016-01-13

Family

ID=51659360

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201480031522.6A Pending CN105246334A (zh) 2013-04-04 2014-04-04 大环内酯及其制备和使用方法
CN202010566628.3A Pending CN111825733A (zh) 2013-04-04 2014-04-04 大环内酯及其制备和使用方法

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN202010566628.3A Pending CN111825733A (zh) 2013-04-04 2014-04-04 大环内酯及其制备和使用方法

Country Status (11)

Country Link
US (3) US9982005B2 (cg-RX-API-DMAC7.html)
EP (2) EP2988597B1 (cg-RX-API-DMAC7.html)
JP (3) JP6437523B2 (cg-RX-API-DMAC7.html)
KR (2) KR102363621B1 (cg-RX-API-DMAC7.html)
CN (2) CN105246334A (cg-RX-API-DMAC7.html)
AU (3) AU2014248014B2 (cg-RX-API-DMAC7.html)
BR (1) BR112015025159A2 (cg-RX-API-DMAC7.html)
CA (2) CA2908575C (cg-RX-API-DMAC7.html)
IL (1) IL241878B (cg-RX-API-DMAC7.html)
MX (2) MX2020011518A (cg-RX-API-DMAC7.html)
WO (1) WO2014165792A2 (cg-RX-API-DMAC7.html)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109311929A (zh) * 2016-05-11 2019-02-05 菲德尔塔公司 Seco大环内酯化合物
CN114591286A (zh) * 2021-04-12 2022-06-07 南京大学 新型大环内酯化合物acautalides A-C及其制备方法和应用

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2703475A1 (en) 2007-10-25 2009-04-30 Cempra Pharmaceuticals, Inc. Process for the preparation of macrolide antibacterial agents
CN102223794B (zh) 2008-10-24 2017-12-22 森普拉制药公司 使用含三唑的大环内酯治疗抗性疾病的方法
US9937194B1 (en) 2009-06-12 2018-04-10 Cempra Pharmaceuticals, Inc. Compounds and methods for treating inflammatory diseases
CN108310000A (zh) 2009-09-10 2018-07-24 森普拉制药公司 治疗疟疾、结核病和mac疾病的方法
EP2613630A4 (en) 2010-09-10 2014-01-15 Cempra Pharmaceuticals Inc HYDROGEN BOND FOR THE PREPARATION OF FLUOROCHETOLIDES FOR THE TREATMENT OF DISEASES
NZ700182A (en) 2012-03-27 2017-02-24 Cempra Pharmaceuticals Inc Parenteral formulations for administering macrolide antibiotics
WO2014152326A1 (en) 2013-03-14 2014-09-25 Cempra Pharmaceuticals, Inc. Methods for treating respiratory diseases and formulations therefor
WO2014145210A1 (en) 2013-03-15 2014-09-18 Cempra Pharmaceuticals, Inc. Convergent processes for preparing macrolide antibacterial agents
CN105246334A (zh) 2013-04-04 2016-01-13 哈佛大学的校长及成员们 大环内酯及其制备和使用方法
US20160303242A1 (en) 2013-12-09 2016-10-20 Durect Corporation Pharmaceutically Active Agent Complexes, Polymer Complexes, and Compositions and Methods Involving the Same
JP2017531663A (ja) 2014-10-08 2017-10-26 プレジデント アンド フェローズ オブ ハーバード カレッジ １４員ケトライドならびにそれらの調製および使用の方法
PE20180219A1 (es) * 2015-03-06 2018-01-31 Cempra Pharmaceuticals Inc Procesos para preparar fluorocetolidos
CA2980315A1 (en) 2015-03-25 2016-09-29 President And Fellows Of Harvard College Macrolides with modified desosamine sugars and uses thereof
US10544182B2 (en) * 2015-03-25 2020-01-28 Presidents and Fellow of Harvard College Synthesis of desosamines
BR112019017223A2 (pt) * 2017-02-17 2020-04-14 Cempra Pharmaceuticals Inc macrolídeos contendo triazol e seus usos oftálmicos
US11673910B2 (en) 2017-04-28 2023-06-13 Zikani Therapeutics, Inc. Macrolides with modified desosamine sugars and uses thereof
CN113573779A (zh) 2018-11-19 2021-10-29 齐卡尼治疗股份有限公司 C10-亚烷基取代的13元大环内酯及其用途
EP3883945A1 (en) * 2018-11-19 2021-09-29 Zikani Therapeutics, Inc. C11-cyclic substituted 13-membered macrolides and uses thereof

Citations (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999000125A1 (en) * 1997-06-27 1999-01-07 Merck & Co., Inc. 9a-aza-3-ketolides, compositions containing such compounds and methods of treatment
WO1999021866A1 (en) * 1997-10-29 1999-05-06 Pfizer Products Inc. 9-amino-3-keto erythromycin derivatives
CN1259955A (zh) * 1997-06-11 2000-07-12 辉瑞产品公司 C－4"－取代的大环内酯衍生物
JP2001247595A (ja) * 2000-03-09 2001-09-11 Shionogi & Co Ltd ８ａ−オキサホモエリスロマイシン誘導体、製造方法、合成中間体および医薬組成物
CN1333782A (zh) * 1998-11-10 2002-01-30 艾文蒂斯药品公司 新的红霉素衍生物、其制备方法和作为药物的用途
US20060100164A1 (en) * 2003-03-10 2006-05-11 Chang-Hsing Liang Novel antibacterial agents
CN1984918A (zh) * 2000-10-18 2007-06-20 奥索-麦克尼尔药品公司 酮基内酯抗菌剂
CN101103039A (zh) * 2005-01-12 2008-01-09 阿尔法马股份公司 作为抗菌剂的红霉素衍生物
CN101142225A (zh) * 2005-01-13 2008-03-12 葛兰素伊斯特拉齐瓦基森塔萨格勒布公司 具有抗炎活性的大环内酯
CN101631795A (zh) * 2007-03-13 2010-01-20 辉瑞产品公司 基于红霉素的大环内酯
CN102245022A (zh) * 2008-10-24 2011-11-16 森普拉制药公司 治疗胃肠病的方法

Family Cites Families (86)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4270537A (en) 1979-11-19 1981-06-02 Romaine Richard A Automatic hypodermic syringe
ZA859575B (en) * 1984-12-21 1986-08-27 Hoffmann La Roche Oxetanones
US4596556A (en) 1985-03-25 1986-06-24 Bioject, Inc. Hypodermic injection apparatus
US4886499A (en) 1986-12-18 1989-12-12 Hoffmann-La Roche Inc. Portable injection appliance
GB8704027D0 (en) 1987-02-20 1987-03-25 Owen Mumford Ltd Syringe needle combination
US4941880A (en) 1987-06-19 1990-07-17 Bioject, Inc. Pre-filled ampule and non-invasive hypodermic injection device assembly
US4940460A (en) 1987-06-19 1990-07-10 Bioject, Inc. Patient-fillable and non-invasive hypodermic injection device assembly
US4790824A (en) 1987-06-19 1988-12-13 Bioject, Inc. Non-invasive hypodermic injection device
US5339163A (en) 1988-03-16 1994-08-16 Canon Kabushiki Kaisha Automatic exposure control device using plural image plane detection areas
FR2638359A1 (fr) 1988-11-03 1990-05-04 Tino Dalto Guide de seringue avec reglage de la profondeur de penetration de l'aiguille dans la peau
US5312335A (en) 1989-11-09 1994-05-17 Bioject Inc. Needleless hypodermic injection device
US5064413A (en) 1989-11-09 1991-11-12 Bioject, Inc. Needleless hypodermic injection device
US5190521A (en) 1990-08-22 1993-03-02 Tecnol Medical Products, Inc. Apparatus and method for raising a skin wheal and anesthetizing skin
US5527288A (en) 1990-12-13 1996-06-18 Elan Medical Technologies Limited Intradermal drug delivery device and method for intradermal delivery of drugs
GB9118204D0 (en) 1991-08-23 1991-10-09 Weston Terence E Needle-less injector
SE9102652D0 (sv) 1991-09-13 1991-09-13 Kabi Pharmacia Ab Injection needle arrangement
US5328483A (en) 1992-02-27 1994-07-12 Jacoby Richard M Intradermal injection device with medication and needle guard
FR2692579B1 (fr) * 1992-06-19 1995-06-02 Roussel Uclaf Nouveaux dérivés de la picromycine, leur procédé de préparation et leur application comme médicaments.
US5383851A (en) 1992-07-24 1995-01-24 Bioject Inc. Needleless hypodermic injection device
US5569189A (en) 1992-09-28 1996-10-29 Equidyne Systems, Inc. hypodermic jet injector
US5334144A (en) 1992-10-30 1994-08-02 Becton, Dickinson And Company Single use disposable needleless injector
WO1994015617A1 (en) 1993-01-11 1994-07-21 Merck & Co., Inc. 8a-aza and 9a-aza macrolide antibiotics, and a process for producing same and methods of use
WO1995024176A1 (en) 1994-03-07 1995-09-14 Bioject, Inc. Ampule filling device
US5466220A (en) 1994-03-08 1995-11-14 Bioject, Inc. Drug vial mixing and transfer device
FR2718450B1 (fr) 1994-04-08 1997-01-10 Roussel Uclaf Nouveaux dérivés de l'érythromycine, leur procédé de préparation et leur application comme médicaments.
US5599302A (en) 1995-01-09 1997-02-04 Medi-Ject Corporation Medical injection system and method, gas spring thereof and launching device using gas spring
JP3652394B2 (ja) * 1995-01-27 2005-05-25 高砂香料工業株式会社 Ｎ−置換−７−アミノ−５−ヒドロキシ−３−オキソヘプタン酸誘導体およびその製造法
US5730723A (en) 1995-10-10 1998-03-24 Visionary Medical Products Corporation, Inc. Gas pressured needle-less injection device and method
US5893397A (en) 1996-01-12 1999-04-13 Bioject Inc. Medication vial/syringe liquid-transfer apparatus
GB9607549D0 (en) 1996-04-11 1996-06-12 Weston Medical Ltd Spring-powered dispensing device
US5993412A (en) 1997-05-19 1999-11-30 Bioject, Inc. Injection apparatus
IT1298087B1 (it) 1998-01-08 1999-12-20 Fiderm S R L Dispositivo per il controllo della profondita' di penetrazione di un ago, in particolare applicabile ad una siringa per iniezioni
GB9814006D0 (en) 1998-06-29 1998-08-26 Biotica Tech Ltd Polyketides and their synthesis
US6262030B1 (en) 1998-11-03 2001-07-17 Pfizer Inc. Erythromycin derivatives
CA2370743A1 (en) 1999-04-16 2000-10-26 Dennis Hlasta Ketolide antibacterials
US6939861B2 (en) 1999-04-16 2005-09-06 Kosan Biosciences, Inc. Amido macrolides
HRP990116B1 (en) 1999-04-20 2007-10-31 GlaxoSmithKline istra�iva�ki centar Zagreb d.o.o. NOVEL 8a AND 9a- 15-MEMBERED LACTAMES
EP1180110A1 (en) 1999-05-24 2002-02-20 Pfizer Products Inc. 13-methyl-erythromycin derivatives
WO2001010879A1 (fr) 1999-08-06 2001-02-15 Taisho Pharmaceutical Co., Ltd. Derives d'erythromycine a
WO2001014397A1 (en) 1999-08-24 2001-03-01 Abbott Laboratories 9a-azalides with antibacterial activity
BRPI0017013B8 (pt) 2000-01-27 2022-11-16 Pfizer Prod Inc composição de antibiótico azalídeo e método para sua obtenção
US6440942B1 (en) 2000-12-22 2002-08-27 Enanta Pharmaceuticals, Inc. 14-membered macrolides derived from leucomycins
IL162292A0 (en) 2001-12-05 2005-11-20 Ortho Mcneil Pharm Inc 6-O-acyl ketolide derivatives of erythromycine useful as antibacterials
US8063021B2 (en) 2002-01-17 2011-11-22 Kosan Biosciences Incorporated Ketolide anti-infective compounds
RU2330069C2 (ru) * 2002-11-29 2008-07-27 Мершан Корпорейшн Способ получения макролидного соединения и штаммы streptomyces sp., mortierella sp. и micromonosporaceae
WO2004065346A1 (ja) 2003-01-21 2004-08-05 Sumitomo Chemical Company, Limited （－）－テトラヒドロリプスタチンおよびその中間体の製造方法
CN1530079A (zh) 2003-03-13 2004-09-22 钱本文 中空分叉髓内钉
HRP20030381B1 (en) 2003-05-14 2007-05-31 GlaxoSmithKline istra�iva�ki centar Zagreb d.o.o. 3-DECLADINOZYL 9a-N-CARBAMOYL AND 9a-N-THIOCARBAMOYL DERIVATIVES 9-DEOXO-9-DIHYDRO-9a-AZA-9a-HOMOERYTHROMICYNE A
WO2005030227A1 (en) 2003-09-23 2005-04-07 Enanta Pharmaceuticals, Inc. 9a, 11-3C-BICYCLIC 9a-AZALIDE DERIVATIVES
JP2008508322A (ja) 2004-07-28 2008-03-21 ランバクシー ラボラトリーズ リミテッド 抗菌剤としてのケトライド誘導体
US7767797B1 (en) 2004-09-30 2010-08-03 Synovo Gmbh Macrocyclic compounds and methods of use thereof
WO2006046112A2 (en) 2004-10-25 2006-05-04 Ranbaxy Laboratories Limited Ketolide derivatives as antibacterial agents
US20060096158A1 (en) * 2004-11-08 2006-05-11 Robinson J M Lactones as new oxygenate fuel additives, fuels based thereon and methods for using same
EP1841775A2 (en) * 2005-01-12 2007-10-10 Alpharma APS Erythromycin derivatives as antibacterial agents
WO2006120541A1 (en) 2005-05-10 2006-11-16 Glaxosmithkline Istrazivacki Centar Zagreb D.O.O. Ether linked macrolides useful for the treatment of microbial infections
AU2006274197A1 (en) 2005-07-26 2007-02-01 Merckle Gmbh Macrolide conjugates of pyrrolizine and indolizine compounds as inhibitors of 5-lipooxygenase and cyclooxygenase
WO2007034909A1 (ja) * 2005-09-22 2007-03-29 Kaneka Corporation （３ｒ，５ｒ）－７－アミノ－３，５－ジヒドロキシヘプタン酸誘導体の製造法
CN102010403A (zh) * 2005-10-13 2011-04-13 卫材R&D管理有限公司 普拉二烯内酯b和普拉二烯内酯d的全合成
EP1985620A4 (en) 2006-02-07 2012-08-15 Taisho Pharmaceutical Co Ltd COMPOUND 10a-AZALIDE
DE102007046388A1 (de) * 2007-09-21 2009-09-10 Universität Hamburg Entwicklung eines Bindungsassays und Darstellung neuartiger Inhibitoren des Myelin Assoziierten Glycoproteins
CA2703475A1 (en) 2007-10-25 2009-04-30 Cempra Pharmaceuticals, Inc. Process for the preparation of macrolide antibacterial agents
US20090209547A1 (en) 2008-02-15 2009-08-20 In Jong Kim C-8 halogenated macrolides
KR100980379B1 (ko) * 2008-04-02 2010-09-06 주식회사 파마코스텍 광학활성을 갖는 5-히드록시-3-옥소헵타노에이트 유도체의제조방법
WO2010015703A2 (en) 2008-08-07 2010-02-11 Glaxosmithkline Istrazivacki Centar Zagreb D.O.O. Novel 6-o-substituted 15-membered 8a- and 9a-lactams
EP2464651B1 (en) 2009-08-13 2016-04-20 Basilea Pharmaceutica AG New macrolides and their use
CN108310000A (zh) 2009-09-10 2018-07-24 森普拉制药公司 治疗疟疾、结核病和mac疾病的方法
DK2544537T3 (en) 2010-03-10 2017-08-28 Cempra Pharmaceuticals Inc PARENTERAL FORMULATIONS OF MACROLIDE ANTIBIOTICS
PL2550286T3 (pl) 2010-03-22 2016-07-29 Cempra Pharmaceuticals Inc Krystaliczne postaci makrolidu i ich zastosowanie
WO2011131749A1 (en) 2010-04-23 2011-10-27 Glaxo Group Limited New 14 and 15 membered macrolides for the treatment of neutrophil dominated inflammatory diseases
CN105198944B (zh) 2010-05-20 2018-06-01 森普拉制药公司 制备大环内酯和酮内酯及其中间体的方法
EP4324524A2 (en) 2010-07-01 2024-02-21 Elanco Tiergesundheit AG Antibiotic compositions
US8975232B2 (en) 2010-07-29 2015-03-10 President And Fellows Of Harvard College Macrocyclic kinase inhibitors and uses thereof
US8796474B1 (en) 2010-08-23 2014-08-05 Rutgers, The State University Of New Jersey Macrolide compounds and methods and intermediates useful for their preparation
EP2613630A4 (en) 2010-09-10 2014-01-15 Cempra Pharmaceuticals Inc HYDROGEN BOND FOR THE PREPARATION OF FLUOROCHETOLIDES FOR THE TREATMENT OF DISEASES
MX2013004013A (es) 2010-10-10 2013-09-26 Synovo Gmbh Macrolidos antiinflamatorios.
WO2012068202A1 (en) * 2010-11-16 2012-05-24 Merial Limited Novel monensin derivatives for the treatment and prevention of protozoal infections
WO2012127351A1 (en) 2011-03-22 2012-09-27 Wockhardt Limited Process for preparation of ketolide compounds
CN102690297A (zh) 2011-03-22 2012-09-26 连云港海康生物科技有限公司 一种壳寡糖季铵盐及其合成方法
AU2012279202A1 (en) 2011-07-01 2014-02-20 President And Fellows Of Harvard College Macrocyclic insulin-degrading enzyme (IDE) inhibitors and uses thereof
NZ700182A (en) 2012-03-27 2017-02-24 Cempra Pharmaceuticals Inc Parenteral formulations for administering macrolide antibiotics
WO2014152326A1 (en) 2013-03-14 2014-09-25 Cempra Pharmaceuticals, Inc. Methods for treating respiratory diseases and formulations therefor
WO2014145210A1 (en) 2013-03-15 2014-09-18 Cempra Pharmaceuticals, Inc. Convergent processes for preparing macrolide antibacterial agents
CN105246334A (zh) 2013-04-04 2016-01-13 哈佛大学的校长及成员们 大环内酯及其制备和使用方法
JP2017531663A (ja) 2014-10-08 2017-10-26 プレジデント アンド フェローズ オブ ハーバード カレッジ １４員ケトライドならびにそれらの調製および使用の方法
US10544182B2 (en) 2015-03-25 2020-01-28 Presidents and Fellow of Harvard College Synthesis of desosamines
CA2980315A1 (en) 2015-03-25 2016-09-29 President And Fellows Of Harvard College Macrolides with modified desosamine sugars and uses thereof

Patent Citations (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1259955A (zh) * 1997-06-11 2000-07-12 辉瑞产品公司 C－4"－取代的大环内酯衍生物
WO1999000125A1 (en) * 1997-06-27 1999-01-07 Merck & Co., Inc. 9a-aza-3-ketolides, compositions containing such compounds and methods of treatment
WO1999021866A1 (en) * 1997-10-29 1999-05-06 Pfizer Products Inc. 9-amino-3-keto erythromycin derivatives
CN1333782A (zh) * 1998-11-10 2002-01-30 艾文蒂斯药品公司 新的红霉素衍生物、其制备方法和作为药物的用途
JP2001247595A (ja) * 2000-03-09 2001-09-11 Shionogi & Co Ltd ８ａ−オキサホモエリスロマイシン誘導体、製造方法、合成中間体および医薬組成物
CN1984918A (zh) * 2000-10-18 2007-06-20 奥索-麦克尼尔药品公司 酮基内酯抗菌剂
US20060100164A1 (en) * 2003-03-10 2006-05-11 Chang-Hsing Liang Novel antibacterial agents
CN101103039A (zh) * 2005-01-12 2008-01-09 阿尔法马股份公司 作为抗菌剂的红霉素衍生物
CN101142225A (zh) * 2005-01-13 2008-03-12 葛兰素伊斯特拉齐瓦基森塔萨格勒布公司 具有抗炎活性的大环内酯
CN101631795A (zh) * 2007-03-13 2010-01-20 辉瑞产品公司 基于红霉素的大环内酯
CN102245022A (zh) * 2008-10-24 2011-11-16 森普拉制药公司 治疗胃肠病的方法

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
MASATAKA HIKOTA ET AL: "Stereoselective Synthesis of Erythronolide A via an Extremely Efficient Macrolactonization by the Modified Yamaguchi Method", 《J. ORG. CHEM.》 *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109311929A (zh) * 2016-05-11 2019-02-05 菲德尔塔公司 Seco大环内酯化合物
CN109311929B (zh) * 2016-05-11 2022-10-04 塞尔维塔公司 Seco大环内酯化合物
CN114591286A (zh) * 2021-04-12 2022-06-07 南京大学 新型大环内酯化合物acautalides A-C及其制备方法和应用

Also Published As

Publication number Publication date
JP2016520551A (ja) 2016-07-14
KR20150140735A (ko) 2015-12-16
AU2014248014B2 (en) 2018-11-08
EP2988597B1 (en) 2022-06-08
CA2908575C (en) 2021-11-16
WO2014165792A3 (en) 2014-12-24
KR102528984B1 (ko) 2023-05-08
MX377459B (es) 2025-03-10
US11634449B2 (en) 2023-04-25
CA3130061A1 (en) 2014-10-09
KR102363621B1 (ko) 2022-02-25
US20220332747A1 (en) 2022-10-20
EP4095146A1 (en) 2022-11-30
AU2014248014A1 (en) 2015-10-22
MX2015014026A (es) 2016-08-03
US9982005B2 (en) 2018-05-29
KR20220025901A (ko) 2022-03-03
MX2020011518A (es) 2022-10-17
CA3130061C (en) 2024-05-28
CN111825733A (zh) 2020-10-27
US10913764B2 (en) 2021-02-09
US20160052951A1 (en) 2016-02-25
AU2019200494A1 (en) 2019-02-14
EP2988597A4 (en) 2017-03-08
JP7111381B2 (ja) 2022-08-02
JP6437523B2 (ja) 2018-12-12
JP6850783B2 (ja) 2021-03-31
AU2019200494B2 (en) 2020-09-17
AU2020281043B9 (en) 2023-02-09
BR112015025159A2 (pt) 2017-07-18
US20180298048A1 (en) 2018-10-18
WO2014165792A2 (en) 2014-10-09
AU2020281043B2 (en) 2023-02-02
CA2908575A1 (en) 2014-10-09
IL241878B (en) 2021-09-30
AU2020281043A1 (en) 2021-01-07
JP2019055968A (ja) 2019-04-11
JP2020169174A (ja) 2020-10-15
AU2020281043C1 (en) 2023-06-01
EP2988597A2 (en) 2016-03-02

Similar Documents

Publication Publication Date Title
JP7111381B2 (ja) マクロライドならびにそれらの調製および使用の方法
CN106998685A (zh) 14‑元酮内酯及其制备和使用方法
EP2691396B1 (en) Enopeptins, uses thereof, and methods of synthesis thereto
WO2017059411A9 (en) Inhibitors of menaquinone biosynthesis
CN107530365A (zh) 具有修饰的脱氧糖胺糖的大环内酯及其用途
HK40085225A (en) Macrolides and methods of their preparation and use
HK1225228B (en) Macrolides and methods of their preparation and use
HK1225228A1 (en) Macrolides and methods of their preparation and use
CN119403559A (zh) 林可酰胺及其用途

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
RJ01 Rejection of invention patent application after publication

Application publication date: 20160113

RJ01 Rejection of invention patent application after publication