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NO885221L - ESTERS OF PHARMACOLOGICALLY ACTIVE CARBOXYLIC ACIDS. - Google Patents

ESTERS OF PHARMACOLOGICALLY ACTIVE CARBOXYLIC ACIDS.

Info

Publication number
NO885221L
NO885221L NO88885221A NO885221A NO885221L NO 885221 L NO885221 L NO 885221L NO 88885221 A NO88885221 A NO 88885221A NO 885221 A NO885221 A NO 885221A NO 885221 L NO885221 L NO 885221L
Authority
NO
Norway
Prior art keywords
lower alkyl
group
aryl
carboxylic acids
esters
Prior art date
Application number
NO88885221A
Other languages
Norwegian (no)
Other versions
NO885221D0 (en
Inventor
Andre Furlenmeier
Marc Montavon
Christian Hubschwerlen
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of NO885221D0 publication Critical patent/NO885221D0/en
Publication of NO885221L publication Critical patent/NO885221L/en
Priority to NO921057A priority Critical patent/NO921057D0/en

Links

Classifications

    • 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
    • C07D501/227-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids with radicals containing only hydrogen and carbon atoms, attached in position 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems
    • 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
    • A61K31/40Heterocyclic 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
    • 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
    • C07D463/00Heterocyclic compounds containing 1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbacephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
    • C07D463/10Heterocyclic compounds containing 1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbacephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring with a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2
    • C07D463/14Heterocyclic compounds containing 1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbacephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring with a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2 with hetero atoms directly attached in position 7
    • C07D463/16Nitrogen atoms
    • C07D463/18Nitrogen atoms further acylated by radicals derived from carboxylic acids or by nitrogen or sulfur analogues thereof
    • C07D463/20Nitrogen atoms further acylated by radicals derived from carboxylic acids or by nitrogen or sulfur analogues thereof with the acylating radicals further substituted by hetero atoms or by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D463/22Nitrogen atoms further acylated by radicals derived from carboxylic acids or by nitrogen or sulfur analogues thereof with the acylating radicals further substituted by hetero atoms or by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen further substituted by nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D477/00Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring
    • C07D477/02Preparation
    • C07D477/06Preparation from compounds already containing the ring or condensed ring systems, e.g. by dehydrogenation of the ring, by introduction, elimination or modification of substituents
    • C07D477/08Modification of a carboxyl group directly attached in position 2, e.g. esterification
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D499/00Heterocyclic compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. penicillins, penems; 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
    • C07D501/36Methylene radicals, substituted by sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D505/00Heterocyclic compounds containing 5-oxa-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. oxacephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Cephalosporin Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Det er beskrevet nye, under fysiologiske betingelser spaltbare estere av farmakologisk virksomme karbonsyrer, spesielt antiblotisk aktive karbonsyrer av gruppen 0-laktam antibiotika, hvilke er særpreget ved at alkoholdelen av esteren er en gruppe av formel. 1 2. hvor R er H eller lavere alkyl, R er H, lavere alkyl, lavere halogenalkyl, lavere alkenyl, lavere alkoksy-k ar bo ny 1, aryi eller heteroaryl, eller sammen med Rlavere alkylen. Rer H, lavere alkyl eller lavere alkoksykarbonyl, R 4 er gruppen -COOR 5 , -COR £ , -SOj-R 6,. -CONReller -PO(OR), hvor Rer en substituert eller usubstituert hydrokarbonrest med opp til 12 karbonatomer, hvori opp til to metylengrupper kan være utbyttet med oksygenatomer, aryl eller aryl-lavere alkyl, R 6 er lavere alkyl eller aryl, R 7 og R 8 er hver H eller lavere alkyl eller sammen lavere alkylen, hvori en metylengruppe kan vatre erstattet med et oksygen-. eiler svovelatom eller med en imino- eller lavere alkyl-iminogruppe, og R q er lavere alkyl. Slike estere kan, såfremt det foreligger en basisk substituent,også eksistere i form av farmasøytisk fordragellge syreaddlsjonssalter.New physiologically cleavable esters of pharmacologically active carboxylic acids have been described, in particular antiblotically active carboxylic acids of the group O-lactam antibiotics, which are characterized in that the alcohol moiety of the ester is a group of formula. 1 wherein R is H or lower alkyl, R is H, lower alkyl, lower haloalkyl, lower alkenyl, lower alkoxy-carbonyl 1, aryl or heteroaryl, or together with R lower alkylene. R 1 is H, lower alkyl or lower alkoxycarbonyl, R 4 is the group -COOR 5, -COR -CONR or -PO (OR), wherein R 1 is a substituted or unsubstituted hydrocarbon radical having up to 12 carbon atoms, in which up to two methylene groups may be exchanged with oxygen atoms, aryl or aryl-lower alkyl, R 6 is lower alkyl or aryl, R 7 and R 8 is each H or lower alkyl or together lower alkylene, wherein a methylene group may be replaced with an oxygen-. or sulfur atom or with an imino or lower alkyl imino group, and R q is lower alkyl. Such esters, if a basic substituent is present, may also exist in the form of pharmaceutically acceptable acid addition salts.

NO88885221A 1987-11-24 1988-11-23 ESTERS OF PHARMACOLOGICALLY ACTIVE CARBOXYLIC ACIDS. NO885221L (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
NO921057A NO921057D0 (en) 1987-11-24 1992-03-18 7-AMINOCEFALOSPORINDERIVATER

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CH457087 1987-11-24
CH316588 1988-08-25

Publications (2)

Publication Number Publication Date
NO885221D0 NO885221D0 (en) 1988-11-23
NO885221L true NO885221L (en) 1989-05-25

Family

ID=25692354

Family Applications (1)

Application Number Title Priority Date Filing Date
NO88885221A NO885221L (en) 1987-11-24 1988-11-23 ESTERS OF PHARMACOLOGICALLY ACTIVE CARBOXYLIC ACIDS.

Country Status (14)

Country Link
EP (1) EP0318767A3 (en)
JP (1) JPH01165585A (en)
KR (1) KR890008082A (en)
AU (1) AU614793B2 (en)
DK (1) DK637888A (en)
FI (1) FI885330A7 (en)
HU (1) HU207522B (en)
IL (1) IL88403A0 (en)
MC (1) MC1991A1 (en)
NO (1) NO885221L (en)
NZ (1) NZ226989A (en)
PT (1) PT89080B (en)
SU (1) SU1598880A3 (en)
YU (2) YU216188A (en)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL99898A (en) * 1990-11-09 1996-10-31 Eisai Co Ltd 7-Acyl-3-substituted carbamoyloxy cephem compounds their preparation and antibacterial compositions containing them
WO1996034869A1 (en) * 1995-05-03 1996-11-07 Smithkline Beecham Plc Esters of carbapenems
BR112014004716A2 (en) * 2011-08-31 2017-03-28 Mallinckrodt Llc remote assembly of targeted nanoparticles using h-phosphonate-en / y-hydrophosphonylation reactions
WO2013036783A2 (en) 2011-09-09 2013-03-14 Cubist Pharmaceuticals, Inc. Methods for treating intrapulmonary infections
US8809314B1 (en) 2012-09-07 2014-08-19 Cubist Pharmacueticals, Inc. Cephalosporin compound
US8476425B1 (en) 2012-09-27 2013-07-02 Cubist Pharmaceuticals, Inc. Tazobactam arginine compositions
UA121298C2 (en) 2013-03-15 2020-05-12 Мерк Шарп І Доум Корп. ANTIBIOTIC COMPOSITION BASED ON CEFTOLOSAN AND TAZOBACTAM
US20140274997A1 (en) 2013-03-15 2014-09-18 Cubist Pharmaceuticals, Inc. Cephalosporin pharmaceutical compositions
US9872906B2 (en) 2013-03-15 2018-01-23 Merck Sharp & Dohme Corp. Ceftolozane antibiotic compositions
EP3043797B1 (en) 2013-09-09 2020-04-08 Merck Sharp & Dohme Corp. Treating infections with ceftolozane/tazobactam in subjects having impaired renal function
US8906898B1 (en) 2013-09-27 2014-12-09 Calixa Therapeutics, Inc. Solid forms of ceftolozane

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2476087A1 (en) * 1980-02-18 1981-08-21 Roussel Uclaf NOVEL OXIMES DERIVED FROM 3-ALKYLOXY OR 3-ALKYL-THIOMETHYL 7-AMINO THIAZOLYL ACETAMIDO CEPHALOSPORANIC ACID, PROCESS FOR PREPARING THEM AND THEIR APPLICATION AS MEDICAMENTS
JPS5984889A (en) * 1982-11-05 1984-05-16 Sumitomo Chem Co Ltd Cephalosporin derivative and its preparation

Also Published As

Publication number Publication date
PT89080B (en) 1993-04-30
EP0318767A2 (en) 1989-06-07
AU2578588A (en) 1989-05-25
PT89080A (en) 1988-12-01
IL88403A0 (en) 1989-06-30
NZ226989A (en) 1992-05-26
DK637888A (en) 1989-05-25
FI885330A0 (en) 1988-11-17
HU207522B (en) 1993-04-28
HUT48895A (en) 1989-07-28
NO885221D0 (en) 1988-11-23
EP0318767A3 (en) 1991-03-20
AU614793B2 (en) 1991-09-12
DK637888D0 (en) 1988-11-15
YU191589A (en) 1991-02-28
FI885330A7 (en) 1989-05-25
YU216188A (en) 1990-04-30
MC1991A1 (en) 1989-11-30
KR890008082A (en) 1989-07-08
SU1598880A3 (en) 1990-10-07
JPH01165585A (en) 1989-06-29

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