CS496787A2 - Method of new acyl derivatives production - Google Patents

Method of new acyl derivatives production

Info

Publication number
CS496787A2
CS496787A2 CS874967A CS496787A CS496787A2 CS 496787 A2 CS496787 A2 CS 496787A2 CS 874967 A CS874967 A CS 874967A CS 496787 A CS496787 A CS 496787A CS 496787 A2 CS496787 A2 CS 496787A2
Authority
CS
Czechoslovakia
Prior art keywords
represents hydrogen
halogen
group
lower alkyl
salts
Prior art date
Application number
CS874967A
Other languages
Czech (cs)
Other versions
CS270227B2 (en
Inventor
Harry A Albrecht
Ka-Kong Chan
Dennis D Keith
Rudolf L 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
Priority to CS884246A priority Critical patent/CS270247B2/en
Priority to CS884245A priority patent/CS270246B2/en
Priority to CS884243A priority patent/CS270244B2/en
Priority to CS884244A priority patent/CS270245B2/en
Publication of CS496787A2 publication Critical patent/CS496787A2/en
Publication of CS270227B2 publication Critical patent/CS270227B2/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
    • 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 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)
  • Communicable Diseases (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biophysics (AREA)
  • Biotechnology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (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.
CS874967A 1986-07-03 1987-07-01 Method of new acyl derivatives production CS270227B2 (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
CS884246A CS270247B2 (en) 1986-07-03 1988-06-20 Method of cephalosporin's new salts production
CS884245A CS270246B2 (en) 1986-07-03 1988-06-20 Method of new acyl derivatives production
CS884243A CS270244B2 (en) 1986-07-03 1988-06-20 Method of new acyl derivatives production
CS884244A CS270245B2 (en) 1986-07-03 1988-06-20 Method of new acyl derivatives production

Applications Claiming Priority (1)

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

Publications (2)

Publication Number Publication Date
CS496787A2 true CS496787A2 (en) 1989-10-13
CS270227B2 CS270227B2 (en) 1990-06-13

Family

ID=25378717

Family Applications (2)

Application Number Title Priority Date Filing Date
CS874967A CS270227B2 (en) 1986-07-03 1987-07-01 Method of new acyl derivatives production
CS913950A CS395091A3 (en) 1986-07-03 1991-12-20 Acyl derivatives of cephalosporin and pharmaceutical preparations basedthereon

Family Applications After (1)

Application Number Title Priority Date Filing Date
CS913950A CS395091A3 (en) 1986-07-03 1991-12-20 Acyl derivatives of cephalosporin and pharmaceutical preparations basedthereon

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
CA2001203C (en) * 1988-10-24 2001-02-13 Thomas P. Demuth, Jr. Novel antimicrobial dithiocarbamoyl quinolones
US5328908A (en) * 1988-10-24 1994-07-12 Procter & Gamble Pharmaceuticals, Inc. Antimicrobial quinolone thioureas
ES2148135T3 (en) * 1988-10-24 2000-10-16 Norwich Eaton Pharma NEW ANTIMICROBIAL ESTERS OF QUINOLONYL LACTAMS.
EP0366193A3 (en) * 1988-10-24 1992-01-08 Norwich Eaton Pharmaceuticals, Inc. Novel antimicrobial quinolonyl lactams
ES2129388T3 (en) * 1988-10-24 1999-06-16 Procter & Gamble Pharma FLUOROQUINOLONIL-CEFEMS ANTIMICROBIALS.
EP0366189A3 (en) * 1988-10-24 1992-01-02 Norwich Eaton Pharmaceuticals, Inc. Novel antimicrobial lactam-quinolones
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
WO1991016327A1 (en) * 1990-04-18 1991-10-31 Norwich Eaton Pharmaceuticals, Inc. 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
AU7706394A (en) * 1994-02-25 1995-09-11 Arrieta Munguia, Judith Marcia 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.
CN113559105B (en) 2014-01-29 2026-06-23 维奥姆治疗有限公司 Treatment of 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
DE2362553A1 (en) * 1972-12-18 1974-06-20 Dainippon Pharmaceutical Co NEW PIPERAZINE DERIVATIVES
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
IE61434B1 (en) 1994-11-02
FI88392B (en) 1993-01-29
ATE97901T1 (en) 1993-12-15
CN87105204A (en) 1988-06-29
EP0251330B1 (en) 1993-12-01
IL83046A0 (en) 1987-12-31
CN1021226C (en) 1993-06-16
HUT44258A (en) 1988-02-29
EP0251330A2 (en) 1988-01-07
NZ220914A (en) 1990-09-26
PT85246B (en) 1990-03-30
CS270227B2 (en) 1990-06-13
HU200185B (en) 1990-04-28
NO168890B (en) 1992-01-06
JPH0730083B2 (en) 1995-04-05
FI872951A0 (en) 1987-07-03
JPS6322586A (en) 1988-01-30
NO168890C (en) 1992-04-15
AU7500987A (en) 1988-01-07
NO872770L (en) 1988-01-04
IE871765L (en) 1988-01-03
PH23940A (en) 1990-01-23
IL83046A (en) 1992-07-15
DE3788306D1 (en) 1994-01-13
DK340387D0 (en) 1987-07-02
AT391137B (en) 1990-08-27
DK340387A (en) 1988-01-04
EP0251330A3 (en) 1989-06-28
NO872770D0 (en) 1987-07-02
KR880001675A (en) 1988-04-26
ZA874696B (en) 1988-01-04
MX7189A (en) 1993-08-01
MC1833A1 (en) 1988-06-03
AU603364B2 (en) 1990-11-15
CS395091A3 (en) 1992-12-16
ATA264587A (en) 1990-02-15
FI88392C (en) 1993-05-10
PT85246A (en) 1987-08-01
ES2060583T3 (en) 1994-12-01
FI872951A7 (en) 1988-01-04
ZW12787A1 (en) 1988-02-03

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