CA2924733C - Aryl substituted aminomethyl spectinomycin analogs as antibacterial agents - Google Patents

Aryl substituted aminomethyl spectinomycin analogs as antibacterial agents Download PDF

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Publication number
CA2924733C
CA2924733C CA2924733A CA2924733A CA2924733C CA 2924733 C CA2924733 C CA 2924733C CA 2924733 A CA2924733 A CA 2924733A CA 2924733 A CA2924733 A CA 2924733A CA 2924733 C CA2924733 C CA 2924733C
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Canada
Prior art keywords
hydrogen
hydroxyl
cyano
alkoxy
further aspect
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CA2924733A
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English (en)
French (fr)
Other versions
CA2924733A1 (en
Inventor
Richard E. Lee
Samanthi L. Waidyarachchi
David F. Bruhn
Jiuyu Liu
Zhong Zheng
Jason W. Rosch
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St. Jude Children's Research Hospital
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St. Jude Children's Research Hospital
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
    • 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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/425—Thiazoles
    • A61K31/428—Thiazoles condensed with carbocyclic rings
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4433—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Dermatology (AREA)
  • Communicable Diseases (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Farming Of Fish And Shellfish (AREA)
  • Fodder In General (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
CA2924733A 2013-09-29 2014-09-29 Aryl substituted aminomethyl spectinomycin analogs as antibacterial agents Active CA2924733C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361884085P 2013-09-29 2013-09-29
US61/884,085 2013-09-29
PCT/US2014/058137 WO2015048692A1 (en) 2013-09-29 2014-09-29 Aryl substituted aminomethyl spectinomycin analogs as antibacterial agents

Publications (2)

Publication Number Publication Date
CA2924733A1 CA2924733A1 (en) 2015-04-02
CA2924733C true CA2924733C (en) 2018-02-27

Family

ID=52744583

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2924733A Active CA2924733C (en) 2013-09-29 2014-09-29 Aryl substituted aminomethyl spectinomycin analogs as antibacterial agents

Country Status (6)

Country Link
US (1) US10266544B2 (enExample)
EP (1) EP3049154B1 (enExample)
JP (1) JP6545177B2 (enExample)
AU (1) AU2014324535B2 (enExample)
CA (1) CA2924733C (enExample)
WO (1) WO2015048692A1 (enExample)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20180141897A1 (en) 2014-12-08 2018-05-24 The Research Foundation For The State University Of New York Anti-fungals targeting the synthesis of fungal shingolipids
EP3638649A4 (en) 2017-06-16 2021-03-17 The Research Foundation for The State University of New York FUNGUSKID AGENTS AGAINST THE SYNTHESIS OF FUNGAL SHINGOLIPIDS
US20210388012A1 (en) * 2018-11-05 2021-12-16 St. Jude Children's Research Hospital, Inc. Methods and compositions for prodrug forms of spectinomycin and spectinamide analogs
CN111239265B (zh) * 2018-11-28 2022-07-26 江苏先声药业有限公司 一种测定阿莫西林克拉维酸钾药物组合物中克拉维酸有关物质的液相色谱方法
GB201905721D0 (en) 2019-04-24 2019-06-05 Univ Dundee Compounds

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3207764A (en) * 1962-01-22 1965-09-21 Upjohn Co Actinospectacin acylates
DE2756914A1 (de) 1977-12-21 1979-07-05 Thomae Gmbh Dr K 4-spectinomycylamin und seine physiologisch vertraegliche salze, verfahren zur herstellung und diese stoffe enthaltende arzneimittel
US4465848A (en) 1981-10-23 1984-08-14 The Upjohn Company Spectinomycin compounds
EP0079125B1 (en) * 1981-10-23 1989-04-05 The Upjohn Company 3-substituted spectinomycin analogues and their preparation
US5543158A (en) 1993-07-23 1996-08-06 Massachusetts Institute Of Technology Biodegradable injectable nanoparticles
EP1278542A2 (en) 2000-05-05 2003-01-29 Cytos Biotechnology AG Molecular antigen arrays and vaccines
GB0025414D0 (en) 2000-10-16 2000-11-29 Consejo Superior Investigacion Nanoparticles
CN101675993A (zh) 2003-03-26 2010-03-24 赛托斯生物技术公司 Melan-a肽类似物-病毒样颗粒偶联物
WO2005101466A2 (en) 2003-12-19 2005-10-27 The University Of North Carolina At Chapel Hill Methods for fabricating isolated micro- and nano- structures using soft or imprint lithography
WO2006080951A2 (en) 2004-07-01 2006-08-03 Yale University Targeted and high density drug loaded polymeric materials
US20090226525A1 (en) 2007-04-09 2009-09-10 Chimeros Inc. Self-assembling nanoparticle drug delivery system
MX2010003642A (es) 2007-10-12 2010-08-09 Massachusetts Inst Technology Nanotecnologia de vacuna.
WO2009106999A2 (en) 2008-02-28 2009-09-03 Deutsches Krebsforschungszentrum, Stiftung Des Öffentlichen Rechts Hollow nanoparticles and uses thereof
WO2010047839A1 (en) 2008-10-25 2010-04-29 Aura Biosciences Modified plant virus particles and uses therefor
CA2768582C (en) * 2009-07-24 2017-02-14 University Of Tennessee Research Foundation Spectinamides as anti-tuberculosis agents
CN101671336B (zh) 2009-09-23 2013-11-13 辽宁利锋科技开发有限公司 芳杂环并嘧啶衍生物和类似物及其制备方法和用途

Also Published As

Publication number Publication date
WO2015048692A1 (en) 2015-04-02
EP3049154A1 (en) 2016-08-03
JP6545177B2 (ja) 2019-07-17
EP3049154B1 (en) 2019-11-13
CA2924733A1 (en) 2015-04-02
AU2014324535A1 (en) 2016-04-07
EP3049154A4 (en) 2017-03-01
US10266544B2 (en) 2019-04-23
AU2014324535B2 (en) 2017-03-30
US20160347762A1 (en) 2016-12-01
JP2016535075A (ja) 2016-11-10

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