AU2014248014B2 - Macrolides and methods of their preparation and use - Google Patents

Macrolides and methods of their preparation and use Download PDF

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Publication number
AU2014248014B2
AU2014248014B2 AU2014248014A AU2014248014A AU2014248014B2 AU 2014248014 B2 AU2014248014 B2 AU 2014248014B2 AU 2014248014 A AU2014248014 A AU 2014248014A AU 2014248014 A AU2014248014 A AU 2014248014A AU 2014248014 B2 AU2014248014 B2 AU 2014248014B2
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optionally substituted
alkyl
hydrogen
certain embodiments
group
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AU2014248014A1 (en
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Andrew G. Myers
Ian Bass SEIPLE
Ziyang Zhang
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Harvard University
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Harvard University
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Priority to AU2019200494A priority Critical patent/AU2019200494B2/en
Priority to AU2020281043A priority patent/AU2020281043C1/en
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    • 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

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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)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Tropical Medicine & Parasitology (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)
AU2014248014A 2013-04-04 2014-04-04 Macrolides and methods of their preparation and use Active AU2014248014B2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
AU2019200494A AU2019200494B2 (en) 2013-04-04 2019-01-24 Macrolides and methods of their preparation and use
AU2020281043A AU2020281043C1 (en) 2013-04-04 2020-12-02 Macrolides and methods of their preparation and use

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
AU2019200494A Division AU2019200494B2 (en) 2013-04-04 2019-01-24 Macrolides and methods of their preparation and use

Publications (2)

Publication Number Publication Date
AU2014248014A1 AU2014248014A1 (en) 2015-10-22
AU2014248014B2 true AU2014248014B2 (en) 2018-11-08

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AU2014248014A Active AU2014248014B2 (en) 2013-04-04 2014-04-04 Macrolides and methods of their preparation and use
AU2019200494A Active AU2019200494B2 (en) 2013-04-04 2019-01-24 Macrolides and methods of their preparation and use
AU2020281043A Active AU2020281043C1 (en) 2013-04-04 2020-12-02 Macrolides and methods of their preparation and use

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AU2019200494A Active AU2019200494B2 (en) 2013-04-04 2019-01-24 Macrolides and methods of their preparation and use
AU2020281043A Active AU2020281043C1 (en) 2013-04-04 2020-12-02 Macrolides and methods of their preparation and use

Country Status (11)

Country Link
US (3) US9982005B2 (enExample)
EP (2) EP4095146A1 (enExample)
JP (3) JP6437523B2 (enExample)
KR (2) KR102363621B1 (enExample)
CN (2) CN105246334A (enExample)
AU (3) AU2014248014B2 (enExample)
BR (1) BR112015025159A2 (enExample)
CA (2) CA3130061C (enExample)
IL (1) IL241878B (enExample)
MX (2) MX2020011518A (enExample)
WO (1) WO2014165792A2 (enExample)

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AU2008316830B2 (en) 2007-10-25 2016-03-17 Cempra Pharmaceuticals, Inc. Process for the preparation of macrolide antibacterial agents
CN107854477A (zh) 2008-10-24 2018-03-30 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
US9480679B2 (en) 2009-09-10 2016-11-01 Cempra Pharmaceuticals, Inc. Methods for treating malaria, tuberculosis and MAC diseases
KR20130120458A (ko) 2010-09-10 2013-11-04 셈프라 파마슈티컬스, 인크. 질환을 치료하기 위한 수소결합 형성 플루오로 케토라이드
WO2013148891A1 (en) 2012-03-27 2013-10-03 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
AU2014233240B2 (en) 2013-03-15 2018-08-09 Cempra Pharmaceuticals, Inc. Convergent processes for preparing macrolide antibacterial agents
EP4095146A1 (en) 2013-04-04 2022-11-30 President And Fellows Of Harvard College Macrolides and methods of their preparation and use
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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
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WO2016154591A1 (en) * 2015-03-25 2016-09-29 President And Fellows Of Harvard College Macrolides with modified desosamine sugars and uses thereof
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AU2019385333B2 (en) 2018-11-19 2025-04-17 President And Fellows Of Harvard College C10-alkylene substituted 13-membered macrolides and uses thereof
IL283185B2 (en) * 2018-11-19 2024-06-01 Zikani Therapeutics Inc Macrolides with 13 members converted to C10-cyclic and their uses
CN114591286B (zh) * 2021-04-12 2023-05-23 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
TW202313065A (zh) * 2021-05-28 2023-04-01 美商季卡尼醫療公司 用於治療遺傳疾病之化合物

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