CN102548552B - 作为抗结核剂的大观霉素酰胺 - Google Patents

作为抗结核剂的大观霉素酰胺 Download PDF

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Publication number
CN102548552B
CN102548552B CN201080042448.XA CN201080042448A CN102548552B CN 102548552 B CN102548552 B CN 102548552B CN 201080042448 A CN201080042448 A CN 201080042448A CN 102548552 B CN102548552 B CN 102548552B
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dihydro
deoxidation
spectinomycin
phenyl
base
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CN102548552A (zh
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R·E·李
J·齐
J·G·胡德勒
B·迈博姆
P·K·瓦戴迪
拉凯什
J·刘
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University of Tennessee Research Foundation
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University of Tennessee Research Foundation
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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
    • A61K31/13—Amines
    • A61K31/133—Amines having hydroxy groups, e.g. sphingosine
    • 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
    • A61K31/395—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
    • A61K31/423—Oxazoles 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
    • A61K31/41—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
    • A61K31/435—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
    • A61K31/4409—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/495—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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines 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
    • A61K31/495—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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A61P31/06—Antibacterial agents for tuberculosis
    • 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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pulmonology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201080042448.XA 2009-07-24 2010-07-26 作为抗结核剂的大观霉素酰胺 Active CN102548552B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US22826609P 2009-07-24 2009-07-24
US61/228,266 2009-07-24
PCT/US2010/043244 WO2011011783A1 (en) 2009-07-24 2010-07-26 Spectinamides as anti-tuberculosis agents

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CN102548552A CN102548552A (zh) 2012-07-04
CN102548552B true CN102548552B (zh) 2016-06-01

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US (2) US8685978B2 (enExample)
EP (1) EP2461805B1 (enExample)
JP (1) JP5770181B2 (enExample)
CN (1) CN102548552B (enExample)
AU (1) AU2010275375B2 (enExample)
CA (1) CA2768582C (enExample)
WO (1) WO2011011783A1 (enExample)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103319496B (zh) * 2012-03-23 2015-06-17 中国科学院微生物研究所 来源于海洋疣孢菌的多环聚酮类化合物及其制备方法与应用
EP3049154B1 (en) * 2013-09-29 2019-11-13 St. Jude Children's Research Hospital, Inc. Aryl substituted aminomethyl spectinomycin analogs as antibacterial agents
CN104725392B (zh) * 2013-12-24 2017-01-11 中国农业大学 半抗原spe-ede及其相应的人工抗原与应用
CN104886160A (zh) * 2015-07-08 2015-09-09 孟宪胜 一种眼科诊断室用杀菌剂
CN108218886B (zh) * 2018-02-11 2020-06-12 中国医药集团总公司四川抗菌素工业研究所 一种大观霉素衍生物及其制备方法和应用
CN108148072A (zh) * 2018-02-11 2018-06-12 中国医药集团总公司四川抗菌素工业研究所 一种大观霉素衍生物及其制备方法和应用
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

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4173647A (en) * 1977-12-21 1979-11-06 Boehringer Ingelheim Gmbh 4-Spectinomycylamine and salts thereof
US4465848A (en) * 1981-10-23 1984-08-14 The Upjohn Company Spectinomycin compounds
US4730059A (en) * 1986-03-10 1988-03-08 The Upjohn Company 6'-thiomethylsubstituted spectinomycins
WO1996026945A1 (en) * 1995-03-01 1996-09-06 Merial Aqueous spectinomycin borate solutions

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2851953A1 (de) * 1978-12-01 1980-06-19 Thomae Gmbh Dr K Neue spectinomycylamine, verfahren zu ihrer herstellung und diese enthaltenden arzneimittel
EP0079125B1 (en) 1981-10-23 1989-04-05 The Upjohn Company 3-substituted spectinomycin analogues and their preparation
US5399558A (en) * 1993-11-24 1995-03-21 Pathogenesis Corporation Isoflavonoid antibacterial compounds, compositions and use
US5628984A (en) * 1995-07-31 1997-05-13 University Of North Carolina At Chapel Hill Method of detecting lung disease
ES2482700T3 (es) * 2005-02-14 2014-08-04 Venus Remedies Limited Terapia de combinación parenteral para enfermedades infecciosas causadas por una bacteria resistente a los medicamentos

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4173647A (en) * 1977-12-21 1979-11-06 Boehringer Ingelheim Gmbh 4-Spectinomycylamine and salts thereof
US4465848A (en) * 1981-10-23 1984-08-14 The Upjohn Company Spectinomycin compounds
US4730059A (en) * 1986-03-10 1988-03-08 The Upjohn Company 6'-thiomethylsubstituted spectinomycins
WO1996026945A1 (en) * 1995-03-01 1996-09-06 Merial Aqueous spectinomycin borate solutions

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Publication number Publication date
CA2768582C (en) 2017-02-14
EP2461805A1 (en) 2012-06-13
US20110118272A1 (en) 2011-05-19
US8685978B2 (en) 2014-04-01
US20140249155A1 (en) 2014-09-04
CN102548552A (zh) 2012-07-04
JP5770181B2 (ja) 2015-08-26
EP2461805A4 (en) 2014-05-07
JP2013500270A (ja) 2013-01-07
AU2010275375B2 (en) 2016-01-21
WO2011011783A1 (en) 2011-01-27
EP2461805B1 (en) 2017-11-01
US9284325B2 (en) 2016-03-15
CA2768582A1 (en) 2011-01-27
AU2010275375A1 (en) 2012-02-09

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