ZA874696B - Acyl derivatives - Google Patents

Acyl derivatives

Info

Publication number
ZA874696B
ZA874696B ZA874696A ZA874696A ZA874696B ZA 874696 B ZA874696 B ZA 874696B ZA 874696 A ZA874696 A ZA 874696A ZA 874696 A ZA874696 A ZA 874696A ZA 874696 B ZA874696 B ZA 874696B
Authority
ZA
South Africa
Prior art keywords
represents hydrogen
halogen
group
lower alkyl
salts
Prior art date
Application number
ZA874696A
Inventor
Allen Albrecht Harry
Chan Ka-Kong
Dalton Keith Dennis
Ludwig Then Rudolf
Weigele Manfred
Original Assignee
F. Hoffmann-La Roche & Co. Aktiengesellschaft
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 F. Hoffmann-La Roche & Co. Aktiengesellschaft filed Critical F. Hoffmann-La Roche & Co. Aktiengesellschaft
Publication of ZA874696B publication Critical patent/ZA874696B/en

Links

Classifications

    • 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
    • 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
    • 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

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.
ZA874696A 1986-07-03 1987-06-29 Acyl derivatives ZA874696B (en)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
ZA874696B true ZA874696B (en) 1988-01-04

Family

ID=25378717

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA874696A ZA874696B (en) 1986-07-03 1987-06-29 Acyl 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
EP0997466A1 (en) * 1988-10-24 2000-05-03 PROCTER &amp; GAMBLE PHARMACEUTICALS, INC. Novel antimicrobial lactam-quinolones
DE68928925T2 (en) * 1988-10-24 1999-08-26 Procter & Gamble Pharma Antimicrobial fluoroquinolonylcephem 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
DE68929227T2 (en) * 1988-10-24 2001-05-31 Procter & Gamble Pharma Quinolonyl lactam antimicrobial esters
EP0366193A3 (en) * 1988-10-24 1992-01-08 Norwich Eaton Pharmaceuticals, Inc. Novel antimicrobial quinolonyl lactams
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
KR100204987B1 (en) * 1990-04-18 1999-06-15 제이코버스 코넬리스 레이서 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.
EP3698793A1 (en) 2014-01-29 2020-08-26 Vyome Therapeutics Limited Besifloxacin for the 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
HU168497B (en) * 1972-12-18 1976-05-28
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
US4808711A (en) * 1985-01-21 1989-02-28 Sankei Pharmaceutical Co., Ltd. Cephalosporin derivatives
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
IE871765L (en) 1988-01-03
DK340387A (en) 1988-01-04
DK340387D0 (en) 1987-07-02
NZ220914A (en) 1990-09-26
FI88392B (en) 1993-01-29
DE3788306D1 (en) 1994-01-13
KR880001675A (en) 1988-04-26
ZW12787A1 (en) 1988-02-03
FI88392C (en) 1993-05-10
AU603364B2 (en) 1990-11-15
EP0251330B1 (en) 1993-12-01
JPS6322586A (en) 1988-01-30
HUT44258A (en) 1988-02-29
PT85246B (en) 1990-03-30
EP0251330A3 (en) 1989-06-28
IE61434B1 (en) 1994-11-02
HU200185B (en) 1990-04-28
ATA264587A (en) 1990-02-15
NO872770L (en) 1988-01-04
CN87105204A (en) 1988-06-29
CS496787A2 (en) 1989-10-13
FI872951A0 (en) 1987-07-03
ATE97901T1 (en) 1993-12-15
PH23940A (en) 1990-01-23
IL83046A (en) 1992-07-15
CN1021226C (en) 1993-06-16
MC1833A1 (en) 1988-06-03
IL83046A0 (en) 1987-12-31
AT391137B (en) 1990-08-27
MX7189A (en) 1993-08-01
AU7500987A (en) 1988-01-07
CS395091A3 (en) 1992-12-16
EP0251330A2 (en) 1988-01-07
NO168890B (en) 1992-01-06
PT85246A (en) 1987-08-01
FI872951A (en) 1988-01-04
CS270227B2 (en) 1990-06-13
JPH0730083B2 (en) 1995-04-05
NO168890C (en) 1992-04-15
NO872770D0 (en) 1987-07-02
ES2060583T3 (en) 1994-12-01

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