WO2000063224A3 - Macrolide antiinfective agents - Google Patents

Macrolide antiinfective agents Download PDF

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Publication number
WO2000063224A3
WO2000063224A3 PCT/US2000/009914 US0009914W WO0063224A3 WO 2000063224 A3 WO2000063224 A3 WO 2000063224A3 US 0009914 W US0009914 W US 0009914W WO 0063224 A3 WO0063224 A3 WO 0063224A3
Authority
WO
WIPO (PCT)
Prior art keywords
substituted
unsubstituted
alkyl
amino
methylene
Prior art date
Application number
PCT/US2000/009914
Other languages
French (fr)
Other versions
WO2000063224A2 (en
Inventor
Daniel T W Chu
Gary W Ashley
Original Assignee
Kosan Biosciences Inc
Daniel T W Chu
Gary W Ashley
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
Priority to NZ515027A priority Critical patent/NZ515027A/en
Priority to BR0010680-1A priority patent/BR0010680A/en
Priority to DE60030847T priority patent/DE60030847T2/en
Priority to JP2000612314A priority patent/JP2003523938A/en
Priority to EP00922149A priority patent/EP1171446B1/en
Priority to CA002369816A priority patent/CA2369816A1/en
Application filed by Kosan Biosciences Inc, Daniel T W Chu, Gary W Ashley filed Critical Kosan Biosciences Inc
Priority to IL14577700A priority patent/IL145777A0/en
Priority to MXPA01010524A priority patent/MXPA01010524A/en
Priority to AU42379/00A priority patent/AU773678B2/en
Publication of WO2000063224A2 publication Critical patent/WO2000063224A2/en
Publication of WO2000063224A3 publication Critical patent/WO2000063224A3/en
Priority to IL145777A priority patent/IL145777A/en

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
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L3/00—Preservation of foods or foodstuffs, in general, e.g. pasteurising, sterilising, specially adapted for foods or foodstuffs
    • A23L3/34—Preservation of foods or foodstuffs, in general, e.g. pasteurising, sterilising, specially adapted for foods or foodstuffs by treatment with chemicals
    • 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
    • A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
    • 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Epidemiology (AREA)
  • Nutrition Science (AREA)
  • Food Science & Technology (AREA)
  • Polymers & Plastics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Compounds of formula (1), (2) or (3), wherein Ra is H; substituted or unsubstituted alkyl (1-10C); substituted or unsubstituted alkenyl (2-10C); substituted or unsubstituted alkynyl (2-10C); substituted or unsubstituted aryl (4-14C); substituted or unsubstituted arylalkyl (5-20C); or ORa is replaced by H; Rb is H or halogen; Rc is H or a protecting group; Rd is methyl, unsubstituted alkyl (3-10C); substituted alkyl (1-10C); substituted or unsubstituted alkynyl (2-10C); substituted or unsubstituted aryl (4-14C); substituted or unsubstituted arylalkyl (5-20C); substituted or unsubstituted arylalkenyl (5-20C); substituted or unsubstituted arylalkynyl (5-20C); substituted or unsubstituted amidoarylalkyl (5-20C); substituted or unsubstituted amidoarylalkenyl (5-20C); or substituted or unsubstituted amidoarylalkynyl (5-20C); Re is H or a protecting group; L is methylene or carbonyl; T is -O-, -N(R)-, -N(OR)-, -N(NHCOR)-, -N(N=CHR)-, or -N(NHR)- wherein R is H or Ra as defined above, with the proviso that when L is methylene, T is -O-; one of Z and Y is H and the other is OH, protected OH, or amino, mono- or dialkylamino, protected amino, or an amino heterocycle or Z and Y together are =O, =NOH or a derivatized oxime; including any pharmaceutically acceptable salts thereof and any stereoisomeric forms and mixtures of stereoisomeric forms thereof, are antimicrobial agents.
PCT/US2000/009914 1999-04-16 2000-04-14 Macrolide antiinfective agents WO2000063224A2 (en)

Priority Applications (10)

Application Number Priority Date Filing Date Title
BR0010680-1A BR0010680A (en) 1999-04-16 2000-04-14 Anti-infectious macrolide agents
DE60030847T DE60030847T2 (en) 1999-04-16 2000-04-14 ANTI-INFECTIOUS MAKROLIDE DERIVATIVES
JP2000612314A JP2003523938A (en) 1999-04-16 2000-04-14 Macrolide anti-infectives
EP00922149A EP1171446B1 (en) 1999-04-16 2000-04-14 Macrolide antiinfective agents
CA002369816A CA2369816A1 (en) 1999-04-16 2000-04-14 Macrolide antiinfective agents
NZ515027A NZ515027A (en) 1999-04-16 2000-04-14 Erythromycin derivatives as antibiotics
IL14577700A IL145777A0 (en) 1999-04-16 2000-04-14 Macrolide antiinfective agents
MXPA01010524A MXPA01010524A (en) 1999-04-16 2000-04-14 Macrolide antiinfective agents.
AU42379/00A AU773678B2 (en) 1999-04-16 2000-04-14 Macrolide antiinfective agents
IL145777A IL145777A (en) 1999-04-16 2001-10-04 3 - descladinosyl - 3 - oxo - erythromycin a 11,12 - cyclic carbamate derivatives and antiinfective pharmaceutical compositions containing them

Applications Claiming Priority (14)

Application Number Priority Date Filing Date Title
US12972999P 1999-04-16 1999-04-16
US60/129,729 1999-04-16
US14017599P 1999-06-18 1999-06-18
US60/140,175 1999-06-18
US17215999P 1999-12-17 1999-12-17
US17215499P 1999-12-17 1999-12-17
US60/172,159 1999-12-17
US60/172,154 1999-12-17
US17380599P 1999-12-30 1999-12-30
US17380499P 1999-12-30 1999-12-30
US60/173,805 1999-12-30
US60/173,804 1999-12-30
US09/550,045 2000-04-14
US09/550,045 US6395710B1 (en) 1999-04-16 2000-04-14 Macrolide antiinfective agents

Publications (2)

Publication Number Publication Date
WO2000063224A2 WO2000063224A2 (en) 2000-10-26
WO2000063224A3 true WO2000063224A3 (en) 2001-01-18

Family

ID=27568857

Family Applications (2)

Application Number Title Priority Date Filing Date
PCT/US2000/009914 WO2000063224A2 (en) 1999-04-16 2000-04-14 Macrolide antiinfective agents
PCT/US2000/009915 WO2000063225A2 (en) 1999-04-16 2000-04-14 Macrolide antiinfective agents

Family Applications After (1)

Application Number Title Priority Date Filing Date
PCT/US2000/009915 WO2000063225A2 (en) 1999-04-16 2000-04-14 Macrolide antiinfective agents

Country Status (16)

Country Link
US (3) US6395710B1 (en)
EP (1) EP1171446B1 (en)
JP (1) JP2003523938A (en)
KR (2) KR100710605B1 (en)
CN (1) CN1241931C (en)
AT (1) ATE340183T1 (en)
AU (2) AU775637B2 (en)
BR (1) BR0010680A (en)
CA (1) CA2369816A1 (en)
DE (1) DE60030847T2 (en)
ES (1) ES2272273T3 (en)
ID (1) ID30547A (en)
IL (2) IL145777A0 (en)
MX (1) MXPA01010524A (en)
NZ (1) NZ515027A (en)
WO (2) WO2000063224A2 (en)

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US6451768B1 (en) 1999-04-16 2002-09-17 Kosan Biosciences, Inc. Macrolide antiinfective agents
US6590083B1 (en) * 1999-04-16 2003-07-08 Ortho-Mcneil Pharmaceutical, Inc. Ketolide antibacterials
ATE271062T1 (en) 2000-06-30 2004-07-15 Pfizer Prod Inc MACROLIDE ANTIBIOTICS
US6472372B1 (en) 2000-12-06 2002-10-29 Ortho-Mcneil Pharmaceuticals, Inc. 6-O-Carbamoyl ketolide antibacterials
DK1373290T3 (en) * 2001-03-21 2014-12-01 Dow Agrosciences Llc Pesticidal spinosyn derivatives
EP1430068A1 (en) 2001-09-17 2004-06-23 Ortho-Mcneil Pharmaceutical, Inc. 6-o-carbamate-11,12-lacto-ketolide antimicrobials
MXPA04005424A (en) 2001-12-05 2005-06-20 Johnson & Johnson 6-o-acyl ketolide derivatives of erythromycine useful as antibacterials.
US8063021B2 (en) * 2002-01-17 2011-11-22 Kosan Biosciences Incorporated Ketolide anti-infective compounds
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US7595300B2 (en) 2005-12-13 2009-09-29 Kosan Biosciences Incorporated 7-quinolyl ketolide antibacterial agents
AU2008316830B2 (en) * 2007-10-25 2016-03-17 Cempra Pharmaceuticals, Inc. Process for the preparation of macrolide antibacterial agents
CN101939012B (en) * 2008-02-08 2015-04-22 巴斯利尔药物股份公司 Macrolides for treating diseases mediated through PDE inhibition
DK2358379T3 (en) * 2008-10-24 2016-03-07 Cempra Pharmaceuticals Inc BIOFORSVAR USING TRIAZOLHOLDIGE macrolides
US9937194B1 (en) 2009-06-12 2018-04-10 Cempra Pharmaceuticals, Inc. Compounds and methods for treating inflammatory diseases
AU2010292010B2 (en) 2009-09-10 2016-01-07 Cempra Pharmaceuticals, Inc. Methods for treating malaria, tuberculosis and MAC diseases
CA2793884C (en) 2010-03-22 2019-09-10 Cempra Pharmaceuticals, Inc. Crystalline forms of a macrolide, and uses therefor
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US8796474B1 (en) 2010-08-23 2014-08-05 Rutgers, The State University Of New Jersey Macrolide compounds and methods and intermediates useful for their preparation
EP2613630A4 (en) 2010-09-10 2014-01-15 Cempra Pharmaceuticals Inc Hydrogen bond forming fluoro ketolides for treating diseases
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Also Published As

Publication number Publication date
AU775637B2 (en) 2004-08-12
IL145777A0 (en) 2002-07-25
WO2000063225A3 (en) 2001-01-18
MXPA01010524A (en) 2002-03-14
CN1384838A (en) 2002-12-11
KR20020007374A (en) 2002-01-26
WO2000063225A2 (en) 2000-10-26
ES2272273T3 (en) 2007-05-01
US20020119938A1 (en) 2002-08-29
CA2369816A1 (en) 2000-10-26
ATE340183T1 (en) 2006-10-15
EP1171446B1 (en) 2006-09-20
IL145777A (en) 2007-02-11
BR0010680A (en) 2002-02-19
US6593302B2 (en) 2003-07-15
AU773678B2 (en) 2004-06-03
WO2000063224A2 (en) 2000-10-26
US6395710B1 (en) 2002-05-28
KR100710605B1 (en) 2007-04-24
AU4457800A (en) 2000-11-02
CN1241931C (en) 2006-02-15
EP1171446A2 (en) 2002-01-16
JP2003523938A (en) 2003-08-12
KR20020007372A (en) 2002-01-26
DE60030847D1 (en) 2006-11-02
USRE39836E1 (en) 2007-09-11
DE60030847T2 (en) 2007-04-19
NZ515027A (en) 2004-01-30
AU4237900A (en) 2000-11-02
ID30547A (en) 2001-12-20

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