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WO2001010879A1 - Derives d'erythromycine a - Google Patents

Derives d'erythromycine a Download PDF

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Publication number
WO2001010879A1
WO2001010879A1 PCT/JP2000/005145 JP0005145W WO0110879A1 WO 2001010879 A1 WO2001010879 A1 WO 2001010879A1 JP 0005145 W JP0005145 W JP 0005145W WO 0110879 A1 WO0110879 A1 WO 0110879A1
Authority
WO
WIPO (PCT)
Prior art keywords
group
acetyl
carbon atoms
pyridine
pyridyl
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.)
Ceased
Application number
PCT/JP2000/005145
Other languages
English (en)
Japanese (ja)
Inventor
Toshifumi Asaka
Masato Kashimura
Akira Manaka
Tetsuya Tanikawa
Tomohiro Sugimoto
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.)
Taisho Pharmaceutical Co Ltd
Original Assignee
Taisho Pharmaceutical Co Ltd
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 Taisho Pharmaceutical Co Ltd filed Critical Taisho Pharmaceutical Co Ltd
Priority to AU63164/00A priority Critical patent/AU6316400A/en
Publication of WO2001010879A1 publication Critical patent/WO2001010879A1/fr
Anticipated expiration legal-status Critical
Ceased 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
    • C07H17/04—Heterocyclic radicals containing only oxygen as ring hetero atoms
    • C07H17/08—Hetero rings containing eight or more ring members, e.g. erythromycins
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents

Definitions

  • Example 5 10,11-Hydro_2'_0-acetyl—12—0_imidazolylcarbonyl—3—O_ (2-virazyl) acetyl—5—0—desosa miniru 6 obtained in (1) — O-Methylerythronolide A prepared with 0.35 g (0.43 mmol) of 4- [3 — (pyridine-3-yl) — 1 H—1,2,4—triazolyl-1—yl] The same operation as in Example 5 (2) was performed using 0.37 g (1.70 mmol) of butylamine to obtain 305 mg of the title compound.
  • Example 6 10,11-Hydro-2'_0-acetyl- 12- ⁇ -imidazolylcarbonyl 2'_3_0_ (thiazol-4-yl) acetyl-5-0—desosaminyl-1 6— obtained in (1) Performed using 0.44 g (1.93 mmol) of 4- [4 _ (thiazoyl 5-yl) thiazol-2-yl] butylamine prepared with 0.54 g (0.65 mmol) of O-methylerythronolide A The same operation as in Example 6 (2) gave 419 mg of the title compound.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Molecular Biology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Communicable Diseases (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La présente invention concerne de nouveaux dérivés d'érythromycine représentés par la formule générale (1), caractérisés par un groupe acyle introduit à la position 3, une structure de carbamate cyclique condensée aux positions 11 et 12, et un hétérocycle à cinq chaînons substitué par aryle, dont un des atomes de carbone ou d'azote est lié à l'atome d'azote carbamate par un groupe alkyle C2-C6; ces nouveaux dérivés présentant des effets antimicrobiens puissants sur les bactéries résistant à l'érythromycine et sur l'Haemophilus influenzae.
PCT/JP2000/005145 1999-08-06 2000-07-31 Derives d'erythromycine a Ceased WO2001010879A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU63164/00A AU6316400A (en) 1999-08-06 2000-07-31 Erythromycin a derivatives

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP11/223555 1999-08-06
JP22355599 1999-08-06

Publications (1)

Publication Number Publication Date
WO2001010879A1 true WO2001010879A1 (fr) 2001-02-15

Family

ID=16800004

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2000/005145 Ceased WO2001010879A1 (fr) 1999-08-06 2000-07-31 Derives d'erythromycine a

Country Status (2)

Country Link
AU (1) AU6316400A (fr)
WO (1) WO2001010879A1 (fr)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006035301A3 (fr) * 2004-09-27 2007-04-19 Ranbaxy Lab Ltd Agents antibactériens
US20190062342A1 (en) * 2003-03-10 2019-02-28 Merck Sharp Dohme Corp. Novel antibacterial agents
US10633407B2 (en) * 2014-10-08 2020-04-28 President And Fellows Of Harvard College 14-membered ketolides and methods of their preparation and use
US10640528B2 (en) 2015-03-25 2020-05-05 President And Fellows Of Havard College Macrolides with modified desosamine sugars and uses thereof
US10913764B2 (en) 2013-04-04 2021-02-09 President And Fellows Of Harvard College Macrolides and methods of their preparation and use

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997031929A1 (fr) * 1996-02-28 1997-09-04 Hoechst Marion Roussel Nouveaux derives de l'erythromycine, leur procede de preparation et leur application comme medicaments
US5786339A (en) * 1994-12-09 1998-07-28 Roussel Uclaf Erythromycins
AU6421398A (en) * 1997-03-24 1998-10-20 Taisho Pharmaceutical Co., Ltd. Erythromycin a derivatives

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5786339A (en) * 1994-12-09 1998-07-28 Roussel Uclaf Erythromycins
WO1997031929A1 (fr) * 1996-02-28 1997-09-04 Hoechst Marion Roussel Nouveaux derives de l'erythromycine, leur procede de preparation et leur application comme medicaments
AU6421398A (en) * 1997-03-24 1998-10-20 Taisho Pharmaceutical Co., Ltd. Erythromycin a derivatives

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20190062342A1 (en) * 2003-03-10 2019-02-28 Merck Sharp Dohme Corp. Novel antibacterial agents
WO2006035301A3 (fr) * 2004-09-27 2007-04-19 Ranbaxy Lab Ltd Agents antibactériens
US10913764B2 (en) 2013-04-04 2021-02-09 President And Fellows Of Harvard College Macrolides and methods of their preparation and use
US11634449B2 (en) 2013-04-04 2023-04-25 President And Fellows Of Harvard College Macrolides and methods of their preparation and use
US10633407B2 (en) * 2014-10-08 2020-04-28 President And Fellows Of Harvard College 14-membered ketolides and methods of their preparation and use
US11466046B2 (en) 2014-10-08 2022-10-11 President And Fellows Of Harvard College 14-membered ketolides and methods of their preparation and use
US10640528B2 (en) 2015-03-25 2020-05-05 President And Fellows Of Havard College Macrolides with modified desosamine sugars and uses thereof
US11535643B2 (en) 2015-03-25 2022-12-27 President And Fellows Of Harvard College Macrolides with modified desosamine sugars and uses thereof

Also Published As

Publication number Publication date
AU6316400A (en) 2001-03-05

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