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HUP0401596A2 - Összekapcsolt glikopeptid-kefalosporin antibiotikumok és ezeket tartalmazó gyógyszerkészítmények - Google Patents

Összekapcsolt glikopeptid-kefalosporin antibiotikumok és ezeket tartalmazó gyógyszerkészítmények

Info

Publication number
HUP0401596A2
HUP0401596A2 HU0401596A HUP0401596A HUP0401596A2 HU P0401596 A2 HUP0401596 A2 HU P0401596A2 HU 0401596 A HU0401596 A HU 0401596A HU P0401596 A HUP0401596 A HU P0401596A HU P0401596 A2 HUP0401596 A2 HU P0401596A2
Authority
HU
Hungary
Prior art keywords
group
independently
hydrogen atom
nrdre
formula
Prior art date
Application number
HU0401596A
Other languages
English (en)
Inventor
Paul Fatheree
Martin S. Linsell
Daniel D. Long
Daniel Marquess
Edmund J. Moran
Matthew B. Nodwell
S. Derek Turner
James Aggen
Original Assignee
Theravance, Inc.
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 Theravance, Inc. filed Critical Theravance, Inc.
Publication of HUP0401596A2 publication Critical patent/HUP0401596A2/hu
Publication of HUP0401596A3 publication Critical patent/HUP0401596A3/hu
Publication of HU230158B1 publication Critical patent/HU230158B1/hu

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D501/00Heterocyclic compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
    • C07D501/14Compounds having a nitrogen atom directly attached in position 7
    • C07D501/16Compounds having a nitrogen atom directly attached in position 7 with a double bond between positions 2 and 3
    • C07D501/207-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/545Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/38Nitrogen atoms
    • C07D277/40Unsubstituted amino or imino radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/38Nitrogen atoms
    • C07D277/42Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D407/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/12Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D407/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D501/00Heterocyclic compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D501/00Heterocyclic compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
    • C07D501/14Compounds having a nitrogen atom directly attached in position 7
    • C07D501/16Compounds having a nitrogen atom directly attached in position 7 with a double bond between positions 2 and 3
    • C07D501/207-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids
    • C07D501/247-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids with hydrocarbon radicals, substituted by hetero atoms or hetero rings, attached in position 3
    • C07D501/38Methylene radicals, substituted by nitrogen atoms; Lactams thereof with the 2-carboxyl group; Methylene radicals substituted by nitrogen-containing hetero rings attached by the ring nitrogen atom; Quaternary compounds thereof
    • C07D501/46Methylene radicals, substituted by nitrogen atoms; Lactams thereof with the 2-carboxyl group; Methylene radicals substituted by nitrogen-containing hetero rings attached by the ring nitrogen atom; Quaternary compounds thereof with the 7-amino radical acylated by carboxylic acids containing hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K9/00Peptides having up to 20 amino acids, containing saccharide radicals and having a fully defined sequence; Derivatives thereof
    • C07K9/006Peptides having up to 20 amino acids, containing saccharide radicals and having a fully defined sequence; Derivatives thereof the peptide sequence being part of a ring structure
    • C07K9/008Peptides having up to 20 amino acids, containing saccharide radicals and having a fully defined sequence; Derivatives thereof the peptide sequence being part of a ring structure directly attached to a hetero atom of the saccharide radical, e.g. actaplanin, avoparcin, ristomycin, vancomycin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biophysics (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Communicable Diseases (AREA)
  • Biochemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Cephalosporin Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)

Abstract

A jelen találmány tárgya (I) általános képletű összekapcsoltglikopeptid-kefalosporin származékok és azok gyógyászatilagelfogadható sói, amelyek hatásos antibiotikumok. A jelen találmánytárgya továbbá ilyen vegyületeket tartalmazó gyógyszerkészítmények;ilyen vegyületek alkalmazása emlősök bakteriális fertőzéseinekkezelésénél; valamint ilyen vegyületek előállítására alkalmazhatóeljárások és közbenső termékek. Az (I) általános képetben X1 és X2jelentése egymástól függetlenül hidrogénatom vagy klóratom; R1jelentése -Ya-(W)n-Yb- általános képletű csoport; W jelentése -O-, -N(Rd)-, -S-, -S(O)-, -S(O)2- képletű csoport, 3-6 szénatomoscikloalkilén-, 6-10 szénatomos arilén- vagy 2-9 szénatomosheteroarilén-csoport; ahol az arilén-, cikloalkilén- és heteroarilén-csoportok adott esetben, egyaránt egy és három közötti számú Rbképletű csoporttal helyettesítettek; Ya és Yb jelentése egymástólfüggetlenül 1-5 szénatomos alkiléncsoport, vagy ha W jelentésecikloalkilén-, arilén- vagy heteroarilén-csoport, akkor Ya és Ybjelentése egymástól függetlenül kovalens kötés vagy 1-5 szénatomosalkiléncsoport; R2 jelentése hidrogénatom vagy 1-6 szénatomosalkilcsoport; mindegyik R3 jelentése egymástól függetlenül 1-6szénatomos alkil-, 2-6 szénatomos alkenil-, 2-6 szénatomos alkinil-,3-6 szénatomos cikloalkil-, 6-10 szénatomos aril-, 2-9 szénatomosheteroarilcsoport, 3-6 szénatomos heterogyűrűs csoport vagy Ra képletűcsoport; R4 és R5 közül az egyik hidroxilcsoport, a másik pedighidrogénatom; R6 és R7 jelentése egymástól függetlenül hidrogénatomvagy metilcsoport; R8 jelentése hidrogénatom vagy (i) képletű csoport;mindegyik Ra jelentése egymástól függetlenül -ORd képletű csoport,halogénatom, -SRd, -S(O)Rd, -S(O)2Rd, -S(O)2NRdRe, -NRdRe, -CO2Rd, -OC(O)Rd, -C(O)NRdRe, -NRdC(O)Re, -OC(O)NRdRe, -NRdC(O)ORe, -NRdC(O)NRdRe, -CF3 vagy -OCF3 képletű csoport; Ó
HU0401596A 2001-10-12 2002-10-11 Összekapcsolt glikopeptid-kefalosporin antibiotikumok HU230158B1 (hu)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US32888901P 2001-10-12 2001-10-12
US60/328,889 2001-10-12
PCT/US2002/032534 WO2003031449A2 (en) 2001-10-12 2002-10-11 Cross-linked glycopeptide-cephalosporin antibiotics

Publications (3)

Publication Number Publication Date
HUP0401596A2 true HUP0401596A2 (hu) 2004-12-28
HUP0401596A3 HUP0401596A3 (en) 2013-06-28
HU230158B1 HU230158B1 (hu) 2015-09-28

Family

ID=23282891

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0401596A HU230158B1 (hu) 2001-10-12 2002-10-11 Összekapcsolt glikopeptid-kefalosporin antibiotikumok

Country Status (30)

Country Link
US (11) US6974797B2 (hu)
EP (1) EP1434779B1 (hu)
JP (3) JP4249023B2 (hu)
KR (1) KR100888660B1 (hu)
CN (2) CN100358901C (hu)
AT (1) ATE314376T1 (hu)
AU (1) AU2002332111B2 (hu)
BR (2) BR0213154A (hu)
CA (1) CA2463544C (hu)
CO (1) CO5580782A2 (hu)
DE (1) DE60208404T2 (hu)
DK (1) DK1434779T3 (hu)
EA (1) EA007001B1 (hu)
ES (1) ES2254738T3 (hu)
HK (1) HK1066007A1 (hu)
HR (1) HRP20040243B1 (hu)
HU (1) HU230158B1 (hu)
IL (2) IL160846A0 (hu)
IS (1) IS2422B (hu)
MX (1) MXPA04003273A (hu)
NO (1) NO334092B1 (hu)
NZ (1) NZ531576A (hu)
PL (1) PL209757B1 (hu)
RS (1) RS50888B (hu)
SI (1) SI1434779T1 (hu)
SK (1) SK2052004A3 (hu)
TW (1) TWI335332B (hu)
UA (1) UA80098C2 (hu)
WO (1) WO2003031449A2 (hu)
ZA (1) ZA200402732B (hu)

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Also Published As

Publication number Publication date
HRP20040243A2 (en) 2004-08-31
HUP0401596A3 (en) 2013-06-28
US20050239691A1 (en) 2005-10-27
DE60208404D1 (de) 2006-02-02
US7728127B2 (en) 2010-06-01
US20080039611A1 (en) 2008-02-14
IS2422B (is) 2008-10-15
US7649080B2 (en) 2010-01-19
ES2254738T3 (es) 2006-06-16
KR20050035122A (ko) 2005-04-15
US8044195B2 (en) 2011-10-25
CN1568325A (zh) 2005-01-19
US20080051577A1 (en) 2008-02-28
CA2463544A1 (en) 2003-04-17
US20100197569A1 (en) 2010-08-05
IS7172A (is) 2004-03-04
DE60208404T2 (de) 2006-07-27
US20080194465A1 (en) 2008-08-14
SI1434779T1 (sl) 2006-06-30
NO20041912L (no) 2004-05-10
CA2463544C (en) 2011-03-29
US7601690B2 (en) 2009-10-13
SK2052004A3 (en) 2004-10-05
US7553962B2 (en) 2009-06-30
DK1434779T3 (da) 2006-01-30
US8557978B2 (en) 2013-10-15
US7341993B2 (en) 2008-03-11
EA007001B1 (ru) 2006-06-30
IL160846A (en) 2010-05-17
CN1329397C (zh) 2007-08-01
US20080194464A1 (en) 2008-08-14
EP1434779B1 (en) 2005-12-28
US20080045721A1 (en) 2008-02-21
US20030130173A1 (en) 2003-07-10
WO2003031449A2 (en) 2003-04-17
MXPA04003273A (es) 2004-07-08
PL209757B1 (pl) 2011-10-31
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ZA200402732B (en) 2005-05-25
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US7713931B2 (en) 2010-05-11
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US7612037B2 (en) 2009-11-03
CN1781916A (zh) 2006-06-07
KR100888660B1 (ko) 2009-03-13
BR0213154A (pt) 2004-08-10
JP2009143962A (ja) 2009-07-02
ATE314376T1 (de) 2006-01-15
HK1066007A1 (en) 2005-03-11
JP2009040795A (ja) 2009-02-26
YU29504A (sh) 2006-08-17
US20080039374A1 (en) 2008-02-14
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US7655621B2 (en) 2010-02-02
PL368451A1 (en) 2005-03-21
HRP20040243B1 (en) 2008-07-31
BRPI0213154B1 (pt) 2018-01-16
US6974797B2 (en) 2005-12-13
RS50888B (sr) 2010-08-31
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US20120214967A1 (en) 2012-08-23
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