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

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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
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Chinese (zh)
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A.G.迈尔斯
I.B.塞普尔
Z.张
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Harvard University
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Harvard University
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Priority to CN202010566628.3A priority Critical patent/CN111825733A/zh
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/42Oxazoles
    • A61K31/424Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/7056Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00Preparation of carboxylic acid amides
    • C07C231/12Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34Heterocyclic 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
    • C07D307/38Heterocyclic 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
    • C07D307/54Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D317/00Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/10Heterocyclic 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
    • C07D317/14Heterocyclic 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
    • C07D317/30Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/18Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804Compounds having Si-O-C linkages
    • C07F7/1872Preparation; Treatments not provided for in C07F7/20
    • C07F7/1892Preparation; Treatments not provided for in C07F7/20 by reactions not provided for in C07F7/1876 - C07F7/1888
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/04Heterocyclic radicals containing only oxygen as ring hetero atoms
    • C07H17/08Hetero rings containing eight or more ring members, e.g. erythromycins
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/08Bridged systems

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  • 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)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Epidemiology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pain & Pain Management (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

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Family Applications (2)

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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

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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 (https=)
EP (2) EP2988597B1 (https=)
JP (3) JP6437523B2 (https=)
KR (2) KR102363621B1 (https=)
CN (2) CN105246334A (https=)
AU (3) AU2014248014B2 (https=)
BR (1) BR112015025159A2 (https=)
CA (2) CA2908575C (https=)
IL (1) IL241878B (https=)
MX (2) MX377459B (https=)
WO (1) WO2014165792A2 (https=)

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

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CN105732745A (zh) 2007-10-25 2016-07-06 森普拉制药公司 大环内酯类抗菌剂的制备方法
AU2009308182B2 (en) 2008-10-24 2016-05-19 Cempra Pharmaceuticals, Inc. Biodefenses using triazole-containing macrolides
US9937194B1 (en) 2009-06-12 2018-04-10 Cempra Pharmaceuticals, Inc. Compounds and methods for treating inflammatory diseases
US9480679B2 (en) 2009-09-10 2016-11-01 Cempra Pharmaceuticals, Inc. Methods for treating malaria, tuberculosis and MAC diseases
EP2613630A4 (en) 2010-09-10 2014-01-15 Cempra Pharmaceuticals Inc HYDROGEN BOND FOR THE PREPARATION OF FLUOROCHETOLIDES FOR THE TREATMENT OF DISEASES
MX2014011537A (es) 2012-03-27 2015-02-10 Cempra Pharmaceuticals Inc Formulaciones parenterales para la administracion de antibioticos macrolidos.
HK1217665A1 (zh) 2013-03-14 2017-01-20 森普拉制药公司 用於治療呼吸道疾病的方法及其製劑
RU2015138797A (ru) 2013-03-15 2017-04-24 Семпра Фармасьютикалс, Инк. Конвергентные способы получения макролидных антибактериальных агентов
US9982005B2 (en) 2013-04-04 2018-05-29 President And Fellows Of Harvard College Macrolides and methods of their preparation and use
JP6564369B2 (ja) 2013-12-09 2019-08-21 デュレクト コーポレイション 薬学的活性剤複合体、ポリマー複合体、ならびにこれらを伴う組成物及び方法
US10633407B2 (en) 2014-10-08 2020-04-28 President And Fellows Of Harvard College 14-membered ketolides and methods of their preparation and use
RU2017131253A (ru) * 2015-03-06 2019-04-08 Семпра Фармасьютикалз, Инк. Способы получения фторкетолидов
JP2018509452A (ja) * 2015-03-25 2018-04-05 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 修飾デソサミン糖をもつマクロライドおよびその使用
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WO2018152424A1 (en) * 2017-02-17 2018-08-23 Cempra Pharmaceuticals, Inc. Triazole-containing macrolides and ophthalmic uses therefor
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ES3063764T3 (en) 2018-11-19 2026-04-20 Zikani Therapeutics Inc C10-alkylene substituted 13-membered macrolides and uses thereof
KR20210123288A (ko) * 2018-11-19 2021-10-13 지카니 테라퓨틱스, 인크. C11-환식 치환된 13-원 마크롤라이드 및 이의 용도

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