FI872951A - ACYLDERIVAT. - Google Patents

ACYLDERIVAT. Download PDF

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Publication number
FI872951A
FI872951A FI872951A FI872951A FI872951A FI 872951 A FI872951 A FI 872951A FI 872951 A FI872951 A FI 872951A FI 872951 A FI872951 A FI 872951A FI 872951 A FI872951 A FI 872951A
Authority
FI
Finland
Prior art keywords
represents hydrogen
halogen
group
lower alkyl
salts
Prior art date
Application number
FI872951A
Other languages
Finnish (fi)
Other versions
FI88392B (en
FI872951A0 (en
FI88392C (en
Inventor
Harry Allen Albrecht
Ka Kong Chan
Dennis Dalton Keith
Rudolf Ludwig Then
Manfred Weigele
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 FI872951A0 publication Critical patent/FI872951A0/en
Publication of FI872951A publication Critical patent/FI872951A/en
Publication of FI88392B publication Critical patent/FI88392B/en
Application granted granted Critical
Publication of FI88392C publication Critical patent/FI88392C/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D501/00—Heterocyclic 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
    • C07D501/14—Compounds having a nitrogen atom directly attached in position 7
    • C07D501/16—Compounds having a nitrogen atom directly attached in position 7 with a double bond between positions 2 and 3
    • C07D501/20—7-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids
    • C07D501/24—7-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
    • C07D501/26—Methylene radicals, substituted by oxygen atoms; Lactones thereof with the 2-carboxyl group
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B82—NANOTECHNOLOGY
    • B82Y—SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
    • B82Y5/00—Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
    • A61K47/552—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds one of the codrug's components being an antibiotic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/555—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound pre-targeting systems involving an organic compound, other than a peptide, protein or antibody, for targeting specific cells
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6891—Pre-targeting systems involving an antibody for targeting specific cells
    • A61K47/6899—Antibody-Directed Enzyme Prodrug Therapy [ADEPT]
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Nanotechnology (AREA)
  • General Engineering & Computer Science (AREA)
  • Medical Informatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biophysics (AREA)
  • Biotechnology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Communicable Diseases (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Cephalosporin Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Cephalosporin derivatives of the formula <IMAGE> in which m represents 0, 1 or 2, R<1> represents hydrogen or an acyl group, R<2> represents hydrogen, lower alkoxy, amino, lower alkylthio or lower alkanoylamino, R<3><1> represents hydrogen, lower alkyl, lower alkenyl, C3-C7-cycloalkyl, halogen-lower alkyl or halophenyl; Z represents R<3><0>-C or nitrogen, R<3><0> represents hydrogen or halogen, or R<3><0> and R<3><1> together represent a C3-C5-alkylene group, a C2-C4-alkylene- monooxy group or a C1-C2-alkylenedioxy group, R<3><2> represents hydrogen, halogen, lower alkyl or an optionally substituted 5- or 6-membered heterocyclic ring having one, two or three oxygen, nitrogen and/or sulphur atoms and R<3><3> represents hydrogen or halogen or R<3><2> and R<3><3> together represent a C1-C4-alkylenedioxy group, and easily hydrolysable esters and salts of these compounds and hydrates of the compounds of the formula I or of their esters and salts are described. The products have antimicrobial activity.
FI872951A 1986-07-03 1987-07-03 Process for the preparation of therapeutically active acyl cephalosporin derivatives FI88392C (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US88155586A 1986-07-03 1986-07-03
US88155586 1986-07-03

Publications (4)

Publication Number Publication Date
FI872951A0 FI872951A0 (en) 1987-07-03
FI872951A true FI872951A (en) 1988-01-04
FI88392B FI88392B (en) 1993-01-29
FI88392C FI88392C (en) 1993-05-10

Family

ID=25378717

Family Applications (1)

Application Number Title Priority Date Filing Date
FI872951A FI88392C (en) 1986-07-03 1987-07-03 Process for the preparation of therapeutically active acyl cephalosporin derivatives

Country Status (22)

Country Link
EP (1) EP0251330B1 (en)
JP (1) JPH0730083B2 (en)
KR (1) KR880001675A (en)
CN (1) CN1021226C (en)
AT (2) ATE97901T1 (en)
AU (1) AU603364B2 (en)
CS (2) CS270227B2 (en)
DE (1) DE3788306D1 (en)
DK (1) DK340387A (en)
ES (1) ES2060583T3 (en)
FI (1) FI88392C (en)
HU (1) HU200185B (en)
IE (1) IE61434B1 (en)
IL (1) IL83046A (en)
MC (1) MC1833A1 (en)
MX (1) MX7189A (en)
NO (1) NO168890C (en)
NZ (1) NZ220914A (en)
PH (1) PH23940A (en)
PT (1) PT85246B (en)
ZA (1) ZA874696B (en)
ZW (1) ZW12787A1 (en)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ227470A (en) * 1987-12-28 1991-06-25 Hoffmann La Roche Acyl derivatives of substituted cephem compounds; pharmaceutical compositions and methods for preparation and treatment
HUT49889A (en) * 1988-03-31 1989-11-28 Hoffmann La Roche Process for producing acyl derivatives
ES2129388T3 (en) * 1988-10-24 1999-06-16 Procter & Gamble Pharma FLUOROQUINOLONIL-CEFEMS ANTIMICROBIALS.
EP0366193A3 (en) * 1988-10-24 1992-01-08 Norwich Eaton Pharmaceuticals, Inc. Novel antimicrobial quinolonyl lactams
EP0366189A3 (en) * 1988-10-24 1992-01-02 Norwich Eaton Pharmaceuticals, Inc. Novel antimicrobial lactam-quinolones
CA2001203C (en) * 1988-10-24 2001-02-13 Thomas P. Demuth, Jr. Novel antimicrobial dithiocarbamoyl quinolones
ATE194353T1 (en) * 1988-10-24 2000-07-15 Norwich Eaton Pharma ANTIMICROBIAL QUINOLONYLLACTAMESTERS
US5328908A (en) * 1988-10-24 1994-07-12 Procter & Gamble Pharmaceuticals, Inc. Antimicrobial quinolone thioureas
AU633867B2 (en) * 1989-02-02 1993-02-11 Eli Lilly And Company Delivery of cytotoxic agents
GB8907617D0 (en) * 1989-04-05 1989-05-17 Celltech Ltd Drug delivery system
CA2078444A1 (en) * 1990-04-18 1991-10-19 Thomas P. Demuth, Jr. Antimicrobial quinolonyl lactams
US5066800A (en) * 1990-04-27 1991-11-19 Hoffmann-La Roche Inc. Qunoline intermediates useful therein for synthesizing antibacterial compounds
US5244892A (en) * 1990-10-16 1993-09-14 Kyorin Pharmaceutical Co., Ltd. Cephem compounds, and antibacterial agents
GB9216759D0 (en) * 1992-08-07 1992-09-23 Finpael Spa Process for the production of 7-amino thiazolyl cephalosporins
DE4234330A1 (en) * 1992-10-12 1994-04-14 Bayer Ag Quinolonecarboxylic acids
EP0746561B1 (en) * 1994-02-25 1999-04-28 Laboratorios Aranda, S.A. De C.V. (Mx/Mx) Quinolonylcarboxamidocephalosporin derivatives and pharmaceutical compositions containing them
MX9505113A (en) * 1995-12-07 1997-06-28 Aranda Lab Sa De Cv Cephalosporine-fluoroquinolonates derivatives and pharmaceutical compositions containing them.
MX2016009898A (en) * 2014-01-29 2017-01-23 Vyome Biosciences Pvt Ltd Treatments for resistant acne.

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3971778A (en) 1972-05-12 1976-07-27 Glaxo Laboratories Limited Cephalosporins having (α-etherified oximino)acylamido groups at the 7-position
CA1006521A (en) * 1972-12-18 1977-03-08 Minoru Sugita Piperazine derivatives and process for preparing them
US4173199A (en) 1974-12-02 1979-11-06 Codama Holding S.A. Apparatus for reinforcing a fabric by applying a fluid reinforcing material thereto
DE2760123C2 (en) 1976-01-23 1986-04-30 Roussel-Uclaf, Paris 7-Aminothiazolyl-syn-oxyiminoacetamidocephalosporanic acids, their preparation and pharmaceutical compositions containing them
DE2716677C2 (en) 1977-04-15 1985-10-10 Hoechst Ag, 6230 Frankfurt Cephem derivatives and processes for their preparation
JPS5854157B2 (en) 1977-06-10 1983-12-02 山之内製薬株式会社 New derivatives of cephalosporin compounds and their production method
JPS5630964A (en) * 1979-08-22 1981-03-28 Kyorin Pharmaceut Co Ltd Novel substituted quinolinecarboxylic acid and its preparation
US4266049A (en) 1980-02-20 1981-05-05 Eli Lilly And Company Process for 3-iodomethyl cephalosporins
FR2501209B1 (en) * 1981-03-03 1986-07-04 Sanofi Sa NOVEL CEPHALOSPORIN DERIVATIVES AND ANTIBIOTIC DRUGS CONTAINING THE SAME
SE440354B (en) * 1981-02-19 1985-07-29 Kyorin Seiyaku Kk quinolinecarboxylic
FR2570702B1 (en) * 1984-09-27 1987-01-09 Sanofi Sa CEPHALOSPORIN DERIVATIVES, PROCESSES FOR OBTAINING THEM AND THEIR APPLICATION AS ANTIBIOTICS
DE3687279T2 (en) * 1985-01-21 1993-05-13 Nippon Pharma Dev Inst BETA LACTAM ANTIBIOTICS.
NZ227470A (en) * 1987-12-28 1991-06-25 Hoffmann La Roche Acyl derivatives of substituted cephem compounds; pharmaceutical compositions and methods for preparation and treatment

Also Published As

Publication number Publication date
DE3788306D1 (en) 1994-01-13
ZW12787A1 (en) 1988-02-03
ATE97901T1 (en) 1993-12-15
JPH0730083B2 (en) 1995-04-05
AU7500987A (en) 1988-01-07
IL83046A (en) 1992-07-15
EP0251330B1 (en) 1993-12-01
CS270227B2 (en) 1990-06-13
HU200185B (en) 1990-04-28
DK340387D0 (en) 1987-07-02
CN87105204A (en) 1988-06-29
KR880001675A (en) 1988-04-26
NZ220914A (en) 1990-09-26
EP0251330A3 (en) 1989-06-28
PT85246A (en) 1987-08-01
HUT44258A (en) 1988-02-29
MX7189A (en) 1993-08-01
PH23940A (en) 1990-01-23
NO168890C (en) 1992-04-15
AU603364B2 (en) 1990-11-15
IE871765L (en) 1988-01-03
FI88392B (en) 1993-01-29
FI872951A0 (en) 1987-07-03
CS496787A2 (en) 1989-10-13
NO872770L (en) 1988-01-04
DK340387A (en) 1988-01-04
NO168890B (en) 1992-01-06
EP0251330A2 (en) 1988-01-07
MC1833A1 (en) 1988-06-03
FI88392C (en) 1993-05-10
JPS6322586A (en) 1988-01-30
CN1021226C (en) 1993-06-16
CS395091A3 (en) 1992-12-16
PT85246B (en) 1990-03-30
ZA874696B (en) 1988-01-04
AT391137B (en) 1990-08-27
NO872770D0 (en) 1987-07-02
ES2060583T3 (en) 1994-12-01
ATA264587A (en) 1990-02-15
IL83046A0 (en) 1987-12-31
IE61434B1 (en) 1994-11-02

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Legal Events

Date Code Title Description
BB Publication of examined application
PC Transfer of assignment of patent

Owner name: KEKSINT!SÄÄTI!

MM Patent lapsed
MM Patent lapsed

Owner name: F. HOFFMANN-LA ROCHE AG